Columbia university - organic-reaction.com

METHODS FOR ASSESSING THE IMMUNE SYSTEM IN A PATIENT (Fri, 24 May 2013)
Methods of determining the onset or susceptibility of an immunological disease are provided herein. Also provided are immunoassay techniques for carrying out such methods.
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HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF (Fri, 17 May 2013)
The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
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CYCLOPROPENIMINE CATALYST COMPOSITIONS AND PROCESSES (Fri, 26 Apr 2013)
The present invention provides, inter alia, a cyclopropenimine Brønsted base catalyst and a cyclopropenimine scaffold for use as a Brønsted base catalyst. This cyclopropenimine has the structure (100). Methods for making such a cyclopropenimine are also provided. Further provided are processes for carrying out an organic synthetic reaction and processes for catalyzing a proton transfer reaction enantioselectively using such a cyclopropenimine Brønsted base catalyst.
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NOVEL MOLECULES THAT SELECTIVELY INHIBIT HISTONE DEACETYLASE 6 RELATIVE TO HISTONE DEACETYLASE 1 (Fri, 12 Apr 2013)
The compounds of the present invention are HDAC6 selective inhibitors which are identified on the basis of accumulation of acetylated tubulin without accumulation of acetylated histones. Histone deacetylase or "HDAC" refers to enzymes capable of cleaving an acetyl group (-C(=0)CH3) from proteins, including histone and microtubulins. Compositions comprising the molecules and methods for their use to inhibit the activity of histone deacetylase, including for treatment, are also disclosed.
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RESVERATROL-BASED COMPOUNDS (Fri, 05 Apr 2013)
The invention provides a compound having the structure compound having the structure: Formula wherein bond a is present or absent, wherein when bond a is absent, then bond β is: Sign (I) and R1 is: Formula and when bond a is present, then R1 is OR10, wherein the phenyl is substituted or unsubstituted; wherein R10 is H, methyl, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, phosphate, sulfate, sulfonic ester, or ester; and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently H or OR11 wherein each occurrence of Rn is independently H, methyl, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, phosphate, sulfate, sulfonic ester, or ester; or a salt thereof.
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COMPOSITIONS AND METHODS FOR TREATING HYPERPROLINEMIA-ASSOCIATED MENTAL DISORDERS (Fri, 22 Mar 2013)
The present invention provides methods for treating or ameliorating the effects of schizophrenia, which include administering to a patient in need thereof a therapeutically effective amount of a proline modulator. Further provided are methods of selecting a patient at risk for or suffering from schizophrenia that is likely to benefit from proline modulation. Methods for identifying an agent that modulates proline levels in a patient and methods for identifying a patient at risk for developing a DTNBP1-related psychiatric illness, as well as other methods and compositions for treating or ameliorating the effects of schizophrenia are also provided.
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SMALL MOLECULE INDUCERS OF GDNF AS POTENTIAL NEW THERAPEUTICS FOR NEUROPSYCHIATRIC DISORDERS (Fri, 01 Mar 2013)
The invention provides a compound having the structure (I), wherein A is a substituted or unsubstituted ring; Z is present or absent and when present is (II), wherein n is 0, 1, 2, 3, or 4; Y is -(CR11R12)-, -NH(CR11R12)- or -O(CR11R12)- wherein R11 and R12 are each hydrogen or combine to form a carbonyl; and wherein R1 to R10 are herein as described.
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RBAP48 TRANSGENIC MICE FOR DRUG DISCOVERY IN AGE-RELATED MEMORY DECLINE (Fri, 15 Feb 2013)
Described is a transgenic mouse with two transgenes, each of which transgene comprises a DNA sequence encoding a dominant negative form of RbAp48 protein, wherein the expression of the dominant negative form of RbAp48 is spatially restricted to the forebrain by a CaM Kinase Ila promoter and wherein the expression of the dominant negative form of RbAp48 is controlled by tetracycline-controlled transcriptional activation. Also provided are methods for evaluating in the transgenic mouse the potential therapeutic effect of an agent for slowing, inhibiting or preventing age-related memory decline in a mammalian subject.
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METHOD OF COLLECTING AND PROCESSING ELECTRON DIFFRACTION DATA (Fri, 25 Jan 2013)
One aspect of the present disclosure is a method for determining an atomic pair distribution function of a sample using electron diffraction. According to this method, the sample is exposed to a beam of electrons. The sample causes electrons to scatter from the beam, the scattered electrons are detected, and a diffraction pattern of the sample is produced. Either the sample or the electron beam can be manipulated to limit the exposure of the sample to the electron beam. Limiting the sample's exposure to the electron beam can reduce damage to the sample. Finally, the signal is analyzed to determine the atomic pair distribution function of the sample.
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USES OF HISTONE ACETYLTRANSFERASE ACTIVATORS (Fri, 14 Dec 2012)
The invention provides methods for enhancing histone acylation, learning, memory and/or cognition in subjects with compound (I) or compositions comprising compound (I), or a pharmaceutically acceptable salt thereof.
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DNA SEQUENCING BY SYNTHESIS USING RAMAN AND INFRARED SPECTROSCOPY DETECTION (Fri, 30 Nov 2012)
This invention provides nucleoside triphosphate analogues having the structure: formula (I), wherein B is a base and is adenine, guanine, cytosine, uracil or thymine, wherein R'' is an OH or an H, and wherein R' is azidomethyl, a hydrocarbyl, or a substituted hydrocarbyl, and which has a Raman spectroscopy peak with wavenumber from 2000 cm-1 to 2300 cm-1 or a Fourier transform-infrared spectroscopy spectroscopy peak with wavenumber from 2000 cm-1 to 2300 cm-1, and also to methods of DNA sequencing and SNP detection.
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OSTEOBLAST-EXPRESSED LIPOCALIN 2 REGULATES GLUCOSE METABOLISM (Fri, 19 Oct 2012)
Diseases including diabetes, metabolic syndrome, and obesity or obesity-related diseases are due to impairment in glucose metabolism. The skeleton has been shown to regulate energy metabolism and play a role in glucose metabolism. The present invention relates to methods for treating or preventing diseases such as diabetes, metabolic syndrome, and obesity or obesity-related by administering a therapeutically effective amount of osteoblast-expressed Lcn-2 or a biologically active fragment.
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CHLORIDE CHANNEL AND CHLORIDE TRANSPORTER MODULATORS FOR THERAPY IN SMOOTH MUSCLE DISEASES (Fri, 05 Oct 2012)
The present invention provides, inter alia, methods and pharmaceutical compositions for treating or ameliorating the effects of a disease characterized by altered smooth muscle contractility, such as e.g., asthma and chronic obstructive pulmonary disease. It has been found that depolarization of the plasma membrane and intracellular concentrations of chloride are decreased by simultaneous blockade of CaCCs and the NKCCs.
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THE RECEPTOR FOR ADVANCED GLYCATION ENDPRODUCTS (RAGE) IS A RECEPTOR FOR LYSOPHOSPHATIDIC ACID (LPA) (Fri, 17 Aug 2012)
Provided herein are methods for treating a lysophosatidic acid (LPA) mediated disorder in a subject comprising administering antagonists of receptor for advanced glycation endproducts (RAGE). Also provided are methods of treating RAGE related disorders comprising administering LPA antagonists. Still further, provided are methods for treating ovarian cancer, inhibiting metastasis of ovarian cancer and treating atherosclerosis comprising administering an agent that inhibits the binding of RAGE with LPA. Also described are methods for inhibiting LPA induced phsophorylation of Akt in a cell comprising administering an antagonist of RAGE. Finally, described herein are methods for determining whether a compound inhibits the interaction of RAGE with LPA.
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HISTONE ACETYLTRANSFERASE MODULATORS AND USESE THEREOF (Fri, 29 Jun 2012)
The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.
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METHODS FOR TREATING HAIR LOSS DISORDERS (Fri, 11 May 2012)
The invention provides for methods for treating a hair loss disorder in a subject by administering a JAK/STAT inhibitor.
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METHODS FOR TREATING HAIR LOSS DISORDERS (Fri, 11 May 2012)
The invention provides for methods for treating a hair loss disorder in a subject by administering a NKG2D inhibitor, IL-15 inhibitor, or a combination thereof.
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UNIQUE HALOGEN-INDUCED CYCLIZATIONS, REAGENTS THEREFOR, AND COMPOUNDS PRODUCED THEREBY (Fri, 23 Mar 2012)
This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed. A representative halonium compound of the disclosure is: Formula (I).
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METHODS OF PREVENTING AND TREATING SARCOPENIA (Fri, 10 Feb 2012)
The present invention provides methods and compositions useful for the treatment and/or prevention of sarcopenia. The compositions include one or more of the following benzothiazepine, benzoxazepine, benzodiazepine or benzazepine compounds (The formula should be inserted here) as disclosed herein while the methods include administering to a subject a therapeutically or prophylactically effective amount of the compounds or compositions to a subject in need thereof.
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Four-color DNA sequencing by synthesis using cleavable fluorescent nucleotide reversible terminators (Fri, 27 Jan 2012)
This invention provides a process for sequencing single-stranded DNA employing modified nucleotides.
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SYNTHESIS OF RESVERATROL-BASED COMPOUNDS (Fri, 27 Jan 2012)
A compound having the structure: bond α is present or absent, wherein when bond α is absent, then R1 is =0 or S(CH2)1-3-phenyl and when bond α is present, then R1 is H, wherein the phenyl is substituted or unsubstituted; R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently H or OR11 wherein each occurrence of R11 is independently H, methyl, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, phosphate, sulfate, sulfonic ester, or ester; when α is absent and R1 is =0, then R10 is other than OH; and when α is absent and R1 is S(CH2)1-3-phenyl, then R10 is other thanOCH3, or a salt thereof.
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ALDOSE REDUCTASE INHIBITORS AND USES THEREOF (Fri, 20 Jan 2012)
The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like.
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FORCE-CLAMP SPECTROMETER AND METHODS OF USE (Fri, 20 Jan 2012)
The disclosed subject matter relates to a force-clamp spectrometer that enables operation in constant force mode and allows for automated data acquisition and analysis, using feedback electronics and software. The disclosed subject matter also relates to methods of using the force-clamp spectrometer for the measurement of the dynamics of chemical reactions. The methods may include, but are not limited to, the measurement of the dynamics of substrate folding and unfolding, as well as bond cleavage and bond formation.
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ANCESTRAL PROTEINS (Fri, 20 Jan 2012)
The invention provides a method for increasing the stability and/or activity of a polypeptide at low pH and/or elevated temperatures. The invention further provides a method for increasing the melting termperature of a polypeptide. Also provided are paleoenzymologically reconstructed thioredoxin polypeptides having activity at higher temperatures and/or lower pH than extant thioredoxin polypepetides, as well as paleoenzymologically reconstructed thioredoxin polypeptides having higher melting temperatures than extant thioredoxin polypepetides.
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METHOD FOR INDUCING FAT LOSS IN MAMMALS (Fri, 30 Dec 2011)
The present invention is a method of increasing lipolysis in an adipose tissue of a mammal comprising delivering to macrophages at the adipose tissue of the mammal an effective amount of an agent which reduces the concentration of macrophages at the adipose tissue of the mammal, thereby increasing lipolysis in the adipose tissue of the mammal.
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E3 BINDING POCKETS AND IDENTIFICATION AND USE OF E3 LIGASE INHIBITORS (Fri, 23 Dec 2011)
The present invention provides, inter alia, an isolated protein fragment that includes a binding pocket or active site on an E3 ligase that modulates the E2-E3 interface, wherein the binding pocket is defined by the capacity of residue F63 of E2 to fit within the pocket. The present invention also provides an agent that interacts with such a binding pocket on a E3 ligase. Methods for identifying an agent that may inhibit a RING-domain E3 ubiquitin ligase, methods for treating a condition in a mammal using such an agent, and methods for selectively inhibiting the ubiquitination function of an E3 ligase, are further provided.
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HYPOGLYCEMIC DIHYDROPYRIDONES (Fri, 02 Dec 2011)
The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.12mm" wi="59.61mm" file="US20110294800A1-20111201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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SELECTIVE HDAC INHIBITORS (Fri, 25 Nov 2011)
This disclosure is related to compounds having the structure (I) wherein Ar1, Ar2, R1 - R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
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METHODS OF PREVENTING AND TREATING LOW BONE MASS DISEASES (Fri, 18 Nov 2011)
The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.
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RADIOLABELED COMPOUNDS AND USES THEREOF (Fri, 11 Nov 2011)
The present invention relates to Radiolabeled Compounds labeled with fluorine, bromine, iodine, carbon, or tritium isotopes and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
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DETERGENT COMPOSITIONS UTILIZING HYDROPHOBICALLY MODIFIED POLYMER (Fri, 28 Oct 2011)
Embodiments of the invention relate to a detergent composition including a poly(maleic acid/vinyl octyl ether) (PMAOVE) hydrophobically modified polymer; and a heavy duty liquid detergent. In addition, embodiments relate to a method of cleaning a substrate, including contacting a substrate with a poly(maleic acid/vinyl octyl ether) (PMAOVE) hydrophobically modified polymer solution.
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SYNTHESIS OF THE POTENT IMMUNOSUPPRESSANT AGENTS DALESCONOL A AND B (Fri, 26 Aug 2011)
This invention relates to compounds having the structure: wherein bonds α, β, γ, δ, ω, η, χ, ε, κ, and μ are each present or absent, and R1-R18 are various substituents described herein.
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METHODS FOR ALTERING POLYPEPTIDE EXPRESSION AND SOLUBILITY (Fri, 19 Aug 2011)
The invention is directed to methods and metric suitable for use in determining the solubility, expression and usability of a polypeptide encoded by a nucleic acid sequence. In certain aspects, the invention also relates to methods for introducing modifications in a polypeptide, for example through substitution of one or more codons in the nucleic acid sequence encoding the polypeptide, to increase or decrease the solubility, expression or usability of the polypeptide.
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PH RESPONSIVE FLUORESCENT FALSE NEUROTRANSMITTERS AND THEIR USE (Fri, 05 Aug 2011)
This invention relates to compounds having the following structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or atom Z is a nitrogen and bonds χ, δ and γ are absent, or atom Z is a nitrogen and bonds χ and δ are present and γ is absent. R1, R2, R3, R4, R5, and R6 are various substituents as described in the specification.
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OSTEOCALCIN AS A TREATMENT FOR MALE REPRODUCTIVE DISORDERS (Fri, 29 Jul 2011)
Methods and compositions for treating, preventing, or diagnosing disorders related to reproduction in male mammals, preferably humans, are provided. The methods generally involve modulation of the OST-PTP signaling pathway or the PTP-IB signaling pathway involving gamma-carboxylase and osteocalcin. Disorders amenable to treatment by the methods include, but are not limited to, male infertility, low sperm count, impaired sperm motility, impaired sperm viability, low testosterone levels, reduced libido, erectile dysfunction, underdevelopment of testes, and excess apoptosis in testes.
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METHODS FOR DETECTING AND REGULATING ALOPECIA AREATA AND GENE COHORTS THEREOF (Fri, 08 Jul 2011)
The invention provides for methods for controlling hair growth by administering a HLDGC modulating compound to a subject. The invention further provides for a method for screening compounds that bind to and modulate polypeptides encoded by HLDGC genes. The invention also provides methods of detecting the presence of or a predisposition to a hair-loss disorder in a human subject as well as methods of treating such disorders.
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VOXEL-BASED METHODS FOR ASSESSING SUBJECTS USING POSITRON EMISSION TOMOGRAPHY (Fri, 01 Jul 2011)
The subject matter disclosed herein relates to methods for diagnosing a neurological disorder in a subject. In certain aspects, the methods described herein involve determining one or more critical areas in the brain from PET data where two groups differ and measuring PET signal within determined critical areas in a new subject in order to assign risk or diagnosis.
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METHODS, DEVICES, AND SYSTEMS FOR ON-DEMAND ULTRASOUND-TRIGGERED DRUG DELIVERY (Fri, 24 Jun 2011)
Injectable or implantable drug delivery systems providing on-demand ultrasound- triggered drug release and methods for controlling the release of drug in a patient are provided herein. The on-demand drug delivery systems contain a drug depot and a drug encapsulated in an encapsulating material, where the encapsulating material is different from the depot. In the preferred embodiment, the depot also contains microbubbles that encapsulate one or more gases. The microbubbles enhance the drug release when ultrasound is applied compared to the same system in the absence of microbubbles. In a preferred embodiment, the drug delivery system, contains an encapsulating material, preferably liposomes, a drug to be delivered, microbubbles, and at least two hydrogel- forming precursor components. Following injection or implantation, the patient can control the time, location and dosage released by administering ultrasound.
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HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF (Fri, 17 Jun 2011)
The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
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METHODS FOR ASSESSING THE IMMUNE SYSTEM IN A PATIENT (Fri, 20 May 2011)
Methods of determining the onset or susceptibility of an immunological disease are provided herein. Also provided are immunoassay techniques for carrying out such methods.
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CONTROL OF SPORE GERMINATION (Fri, 15 Apr 2011)
Provided are compositions and methods for treating bacterial infections. It is demonstrated herein that bacteria cell wall materials stimulate germination of spores of Gram-positive bacteria, and that such activity requires Ser/Thr kinase PrkC. By modulating one or both, spores (which can be antibiotic resistant) can be stimulated or inhibited from germination, which can be exploited in various methods of therapeutic treatment. Also provided is a method of modulating germination of a spore of a Gram-positive bacterium. Also provided is a method of decontaminating an environment.
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SYNERGISTIC TRANSCRIPTION MODULES AND USES THEREOF (Fri, 11 Mar 2011)
The invention provides for methods for treating nervous system cancers in a subject. The invention further provides methods for treating nervous system tumor cell invasion, migration, proliferation, and angiogenesis associated with nervous system tumors.
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COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING HEART TISSUE DEGENERATION AND USES THEREOF (Fri, 07 Jan 2011)
The present invention provides compositions useful for cardiac therapy comprising a cyclin-associated agent. The present invention also provides kits for use in delivering a cyclin-associated agent to cardiac cells in a subject, comprising the composition of the present invention and a catheter. The present invention additionally provides a methods for enhancing cardiac function; promoting regeneration of cardiac tissue; inducing endogenous myocardial regeneration; and preventing or treating heart failure in a subject in need thereof by augmenting cyclin in cells.
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PHOTOLABILE COMPOUNDS (Thu, 30 Dec 2010)
The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.
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AUTISM-ASSOCIATED BIOMARKERS AND USES THEREOF (Fri, 24 Dec 2010)
Biomarkers for human autism are disclosed. Methods for treating, preventing, and diagnosing human autism and autism-related disorders are also disclosed.
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ENZYMATIC DEGRADATION OF A2E AND OTHER BISRETINOID COMPOUNDS OF RPE LIPOFUSCIN (Fri, 26 Nov 2010)
The present invention provides methods for reducing the amount of lipofuscin compounds present in a cell which comprises contacting the cell with an amount of an enzyme sufficient to directly or indirectly degrade the amount of lipofuscin compounds, so as to reduce the amount of lipofuscin compounds, wherein the enzyme is a carotenoid cleaving dioxygenase or an oxo-iron heme-based enzyme. The invention also provides methods for. treating a subject suffering from a lipofuscin- associated disorder which comprises administering to the subject a composition comprising an amount of an enzyme sufficient to directly or indirectly degrade lipofuscin compounds associated with the disorder in cells of the subject, so as to thereby treat subject's the lipofuscin- associated disorder, wherein the enzyme is a carotenoid cleaving dioxygenase or an oxo-iron heme-based enzyme.
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SELECTIVE PROTEASOME INHIBITORS FOR TREATING DIABETES (Fri, 24 Sep 2010)
Methods of modulating chronic low-grade inflammation are provided. More particularly, methods of treating diabetes, such as for example, type-2 diabetes mellitus, in a mammal by administering an effective amount of a selective proteasome inhibitor are provided. Also provided are unit dosage forms of such inhibitors.
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E3 LIGASE INHIBITORS (Fri, 24 Sep 2010)
The present invention provides, e.g., compounds having the structure of formula (I): The present invention also provides pharmaceutical compositions that include such compounds, and methods for modulating murine double minute 2 protein (Mdm2) E3 ligase activity, particularly the Mdm2-MdmX hetero-complex E3 ligase activity, using such compounds.
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SYNTHESIS OF OLIGOMERIC NEOLIGNANS AND THEIR USE (Fri, 02 Jul 2010)
Compounds having the structure formule (I) and their uses are described herein.
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PHOSPHODIESTERASE INHIBITORS AND USES THEREOF (Fri, 02 Jul 2010)
The invention provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention further provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
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METAL OXIDE NANOCRYSTALS: PREPARATION AND USES (Fri, 04 Jun 2010)
Nanocrystalline forms of metal oxides, including binary metal oxide, perovskite type metal oxides, and complex metal oxides, including doped metal oxides, are provided. Methods of preparation of the nanocrystals are also provided. The nanocrystals, including uncapped and uncoated metal oxide nanocrystals, can be dispersed in a liquid to provide dispersions that are stable and do not precipitate over a period of time ranging from hours to months. Methods of preparation of the dispersions, and methods of use of the dispersions in forming films, are likewise provided. The films can include an organic, inorganic, or mixed organic/inorganic matrix. The films can be substantially free of all organic materials. The films can be used as coatings, or can be used as dielectric layers in a variety of electronics applications, for example as a dielectric material for an ultracapacitor, which can include a mesoporous material. Or the films can be used as a high-K dielectric in organic field-effect transistors. In various embodiments, a layered gate dielectric can include spin-cast (e.g., 8 nm-diameter) high-K BaTiO3 nanocrystals and parylene-C for pentacene OFETs.
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METHODS OF PREVENTING AND TREATING LOW BONE MASS DISEASES (Fri, 21 May 2010)
The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1inhibitors or serotonin receptor antagonists.
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NEURAMINIDASE INHIBITORS AND USES THEREOF (Fri, 21 May 2010)
The invention is related to various methods for inhibiting or reducing biofilm formation, treating a biofilm production-related disorder, preventing biofilm formation, and screening for neuraminidase inhibitors.
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HETEROBIFUNCTIONAL POLYMERS AND METHODS FOR LAYER-BY-LAYER CONSTRUCTION OF MULTILAYER FILMS (Sat, 15 May 2010)
In one aspect, the present invention is directed to methods for modification of functionalized substrates. In another aspect, the invention relates to systems and methods for fabricating multilayer polymer compositions. In certain embodiments, the multilayer polymer compositions described herein can comprise heterobifunctional polymers and heterotrifunctional molecules.
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METHOD FOR APCDD1 MEDIATED REGULATION OF HAIR GROWTH AND PIGMENTATION AND MUTANTS THEREOF (Fri, 07 May 2010)
The invention provides for methods for controlling hair growth by administering an APCDDl modulating compound to a subject. The invention further provides for a method for screening compounds that bind to and modulate APCDDl.
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COMPOUNDS THAT INHIBIT NFκB ACTIVITY (Fri, 07 May 2010)
The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
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Photochemical methods and photoactive compounds for modifying surfaces (Fri, 23 Apr 2010)
Compounds and methods for controlling the surface properties are described. Compounds of the invention can form radicals upon exposure to irradiation, which can then react with nearby molecules to alter the surface properties of various substrates. The invention can provide surfaces that are resistant to dewetting, surfaces that have immobilized molecules such as carbohydrates and polymers immobilized, and surfaces that have metals deposited on the surface. The invention can be utilized in a wide range of application, such as sensors, microreactors, microarrays, electroless deposition of metals, and the like.
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Four-color DNA sequencing by synthesis using cleavable fluorescent nucleotide reversible terminators (Fri, 16 Apr 2010)
This invention provides a process for sequencing single-stranded DNA by employing a nanopore and modified nucleotides.
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NGAL-BINDING SIDEROPHORES AND USE THEREOF TO TREAT IRON DEFICIENCY AND IRON OVERLOAD (Fri, 26 Mar 2010)
The invention provides compositions comprising a lipocalin, such as NGAL, and a mammalian siderophore that are useful as iron chelators and iron donors. The invention also provides mammalian siderophore compounds of Formula (I): The invention further provides, methods of treatment and methods of diagnosis.
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COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND TREATING OR PREVENTING DISEASES (Fri, 05 Mar 2010)
The present invention provides compounds of Formula (I), compositions comprising an effective amount of a Compound of Formula (I), optionally with chemotherapeutic drug, such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, for example chemotherapy agents, treating or preventing cancer or a neurotrophic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making Compounds of Formula (I).
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Synthesis of four color 3′O-allyl, modified photocleavable fluorescent nucleotides and related methods (Fri, 19 Feb 2010)
This invention provides a process for making 3′-O-allyl-dGTP-PC-Biodopy-FL-510, 3′-O-allyl-dATP-PC-ROX, 3′-O-allyl-dCTP-PC-Bodipy-650 and 3′-O-allyl-dUTP-PC-R6G, and related methods.
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Fluorescent substrates for monoamine transporters as optical false neurotransmitters (Fri, 12 Feb 2010)
The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.52mm" wi="69.85mm" file="US08337941-20121225-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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HYPOGLYCEMIC DIHYDROPYRIDONES (Fri, 12 Feb 2010)
The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
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UNIVERSAL METHYLATION PROFILING METHODS (Fri, 29 Jan 2010)
This invention provides methods of derivatizing a double-stranded DNA comprising contacting double-stranded DNA with a CpG methyltransf erase and an s-adenosylmethionine analog. This invention also provides methods of sequencing DNA to determine methylation patterns. This invention also provides neobases and methods of sequencing for methylation patterns using neobases.
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Pentacyclic Alkaloid Compounds and Methods of Use Thereof (Fri, 01 Jan 2010)
The present invention relates to Pentacyclic Alkaloid Compounds, compositions comprising an effective amount of a Pentacyclic Alkaloid Compound and methods for treating or preventing cancer, a bacterial infection, a fungal infection, or a yeast infection, comprising administering to a subject in need thereof an effective amount of a Pentacyclic Alkaloid Compound. The present invention also relates to compounds and methods that are useful for making Cribrostatin IV.
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METHODS TO TREAT OR PREVENT HORMONE-RESISTANT PROSTATE CANCER USING siRNA SPECIFIC FOR PROTOCADHERIN-PC, OR OTHER INHIBITORS OF PROTOCADHERIN-PC EXPRESSION OR ACTIVITY (Fri, 18 Dec 2009)
The invention is directed to compounds and methods for treating or preventing hormone-resistant prostate cancer using siRNA specific for protocadherin-PC, or other inhibitors of protocadherin-PC expression or activity, including antisense oligonucleotides and antibodies. The invention also provides for the use of protocadherin-PC as an in vivo prostate cancer biomarker, and includes a kit for detecting prostate cancer in biological samples. Also covered by the invention is a transgenic non-human mammal engineered to overexpress protocadherin-PC specifically in the prostate.
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VOXEL-BASED METHODS FOR ASSESSING SUBJECTS USING POSITRON EMISSION TOMOGRAPHY (Fri, 04 Dec 2009)
The subject matter disclosed herein relates to methods for diagnosing a neurological disorder in a subject. In certain aspects, the methods described herein involve determining one or more critical areas in the brain from PET data where two groups differ and measuring PET signal within determined critical areas in a new subject in order to assign risk or diagnosis.
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METHODS FOR SYNTHESIZING BENZOTHIAZEPINE COMPOUNDS (Fri, 27 Nov 2009)
The present invention provides improved methods for synthesizing novel benzothiazepine compounds. In particular, the invention relates to a new method that generally is used to make the substituted 2,3,4,5-tetrahydro-1,4-benzothiazepine compounds of a general formula <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="13.80mm" wi="27.01mm" file="us20090292119a1-20091126-c00001.tif" img-content="chem" img-format="tif"/> </chemistry> which then may be used to make many other benzothiazepine compounds.
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Method of preparing a star polymer macromonomer (Fri, 16 Oct 2009)
The present invention relates to methods for preparing degradable model networks from any monomer functionality with any degradation methodology. It is based on the use of Atom-Transfer Radical Polymerization CLICK chemistry and a tetrafunctional initiator having terminal halogen groups to form the desired product.
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PHOSPHODIESTERASE INHIBITORS AND USES THEREOF (Fri, 09 Oct 2009)
The invention provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention further provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
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Biomolecular coupling methods using 1,3-dipolar cycloaddition chemistry (Fri, 25 Sep 2009)
This invention provides methods for covalently affixing a biomolecule to either a second molecule or a solid surface using 1,3-dipolar cycloaddition chemistry. This invention also provides related methods and compositions.
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COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING DISEASES (Fri, 28 Aug 2009)
The present invention provides compounds of Formula (I), compositions comprising an effective amount of a Compound of Formula (I), optionally with a tubulin-binding drug, methods of their use for treating or preventing cancer or a neurotrophic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, and methods for making Compounds of the invention.
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R-SPONDIN COMPOSITIONS AND METHODS OF USE THEREOF (Fri, 21 Aug 2009)
The invention provides for a method for screening compounds that bind to and modulate a regulator of Wnt signaling, R-spondin 4. The invention further provides for methods for diagnosing a keratin-related abnormality, such as anonychia congenital, in a subject. The invention also provides for isolated RSPO4 mutant molecules.
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METHODS FOR TESTING ANTI-THROMBOTIC AGENTS (Fri, 14 Aug 2009)
The invention provides a transgenic non-human animal expressing von Willebrand Factor A1 protein containing at least one mutation selected from the group consisting of: 1263P>;S, 1269N>;D, 1274K>;R, 1287M>;R, 1302G>;D, 1308H>;R, 1313R>;W, 1314I>;V, 1326R>;H, 1329L>;I, 1330E>;G, 1333A>;D, 1344T>;A, 1347I>;V, 1350T>;A, 1370G>;S, 1379H>;R, 1381T>;A, 1385T>;M 1391P>;Q, 1394A>;S, 1397L>;F, 1421S>;N, 1439L>;V, 1442G>;S, 1449R>;Q, 1466A>;P, 1469Q>;L, 1472Q>;H, 1473V>;M, 1475H>;Q, 1479S>;G, and any combination thereof.
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ANALOGUES OF (-)-PICROPODOPHYLLIN, SYNTHESIS AND USES THEREOF (Fri, 14 Aug 2009)
Compounds, compositions, methods of making, and methods of using analogues of (-)-picropodophyllin, as well as a transgenic animal model and its use for identifying anticancer agents.
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MOLECULAR PROBES FOR PET-IMAGING OF DOPAMINE NEUROTRANSMISSION AND NEUROENDOCRINE PROCESSES IN VIVO (Fri, 07 Aug 2009)
The present invention relates to compounds of the general structure (I), wherein Y is O, X is O, bond alpha is absent and bond beta is present, or, Y is H, X is CH, bond alpha is present, and bond beta is is absent, atom Z is a carbon and bonds X, delta and gamma are present, or atom Z is a nitrogen and bonds X, delta and gamma are absent, or atom Z is a nitrogen and bonds X and delta are present and gamma is absent R1, R2, R3, R4, R5 and R6 are various subtitutents as described in the specification.
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METHODS FOR P2RY5 MEDIATED REGULATION OF HAIR GROWTH AND MUTANTS THEREOF (Fri, 17 Jul 2009)
The invention provides for a method for screening compounds that bind to and modulate the hair-specific G-protein coupled receptor, P2RY5. The invention further provides for methods for controlling hair growth by administering a P2RY5 modulating compound to a subject.
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Ginkgolide Compounds, Compositions, And Extracts, And Uses Thereof (Fri, 19 Jun 2009)
The present invention relates to Ginkgolide derivatives, compositions and extracts comprising one or more Ginkgolides and/or derivatives thereof and methods of use of the compositions to treat neurological disorders and as imaging agents.
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METHODS FOR IDENTIFYING COMPOUNDS THAT MODULATE LISCH-LIKE PROTEIN OR C1ORF32 PROTEIN ACTIVITY AND METHODS OF USE (Fri, 19 Jun 2009)
The invention provides methods for reducing diabetes susceptibility in a subject and methods for increasing the expression of LL or CLORF32 in a subject. The invention further provides a method for identifying an agent which modulates expression of an Ll RNA or Clorf32 RNA comprising contacting a cell with an agent; determining expression of the Ll RNA or Clorf32 RNA in the presence and the absence of the agent; and comparing expression of the Ll RNA or Clorf32 RNA in the presence and the absence of the agent, wherein a change in the expression of the Ll RNA or Clorf32 RNA in the presence of the agent is indicative of an agent which modulates the level of expression of the RNA.
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COMPOUND FOR ACTIVATING 5-HT2C RECEPTORS IN COMBINATION WITH AN AMPHETAMINE COMPOUND (Fri, 15 May 2009)
A method of treating or preventing obesity in a subject comprising administering to the subject identified as in need thereof a combination of a PAT compound and an amphetamine compound, wherein the PAT compound is capable of selectively activating 5- HT2c relative to 5-HT2a or 5HT2b.
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Processes of making sesquiterpenoid tashironin, its analogs and their uses (Fri, 24 Apr 2009)
A compound having the structure of the formula (genus of compound 1 excluding Tashironin or Debenzoyltashironin) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.21mm" wi="55.29mm" file="US08067462-20111129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and methods of the same. 
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DESIGN AND SYNTHESIS OF CLEAVABLE FLUORESCENT NUCLEOTIDES AS REVERSIBLE TERMINATORS FOR DNA SEQUENCING BY SYNTHESIS (Fri, 24 Apr 2009)
This invention provides novel azido linkers for deoxynucleotide analogues having a detectable marker attached thereto.
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CONTROL OF SPORE GERMINATION (Fri, 03 Apr 2009)
Provided is a method of stimulating germination of a spore of a Gram-positive bacterium. Also provided is a method of inhibiting germination of a spore of a Gram-positive bacterium. Additionally provided is a composition comprising (i) a preparation of cell walls from a Gram-positive bacterium or (ii) a compound that stimulates activity of a serine/threonine protein kinase of the Gram-positive bacterium or (iii) a compound that inhibits activity of a PPM-like phosphatase of the Gram-positive bacterium. Also provided is a composition comprising an antibiotic and a compound that inhibits activity of a serine/threonine protein kinase of a Gram-positive bacterium. A method of treating a mammal infected with a spore-forming Gram-positive bacterium is additionally provided. A method of decontaminating an environment, a method of determining whether a compound inhibits germination of a spore, and a method of determining whether a compound stimulates germination of a spore of a Gram-positive bacterium are also provided.
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SYNTHESIS OF RESVERATROL-BASED NATURAL PRODUCTS (Fri, 27 Mar 2009)
Processes for synthesizing reveratrol-based oligomers are provided. In addition, reservatrol-based oligomer compounds free of plant extract are provided.
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METHODS AND SYSTEMS OF CALCULATING DIFFERENCES OF BINDING AFFINITIES BETWEEN CONGENERIC PAIRS OF LIGANDS (Fri, 13 Feb 2009)
Described is a technique to exhaustively enumerate the thermodynamic properties of the water molecules solvating the active site of a protein in its apostate and calculate the relative binding affinities of congeneric compounds that bind to this protein. The subject matter includes sampling the configurations of the solvating water in the active site; extracting the thermodynamic information about the solvating water from these configurations by clustering the observed water configurations into regions of high water occupancy (e.g., 'hydration sites'), computing the average system interaction energies of water molecules occupying the various hydrations sites, computing excess entropies of water molecules occupying the hydration sites; constructing a 3 dimensional hydration thermodynamics map of the protein active site; and computing relative binding affinities of congeneric ligands based on the principle that tighter binding ligands can displace more entropically structured and energetically depleted hydration sites from the active site into the bulk fluid.
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SENSING DEVICES FROM MOLECULAR ELECTRONIC DEVICES UTILIZING HEXABENZOCORONENES (Fri, 30 Jan 2009)
The present invention generally relates to the fabrication of molecular electronics devices from molecular wires and Single Wall Nanotubes (SWNT). In one embodiment, the cutting of a SWNT is achieved by opening a window of small width by lithography patterning of a protective layer on top of the SWNT, followed by applying an oxygen plasma to the exposed SWNT portion. In another embodiment, the gap of a cut SWNT is reconnected by one or more difunctional molecules having appropriate lengths reacting to the functional groups on the cut SWNT ends to form covalent bonds. In another embodiment, the gap of a cut SWNT gap is filled with a self-assembled monolayer from derivatives of novel contorted hexabenzocoranenes. In yet another embodiment, a device based on molecular wire reconnecting a cut SWNT is used as a sensor to detect a biological binding event.
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Methods of inhibiting binding of beta-sheet fibril to rage and consequences thereof (Fri, 30 Jan 2009)
This invention provides a method of inhibiting the binding of beta-sheet fibril to RAGE on the surface of a cell which comprises contacting the cell with a binding-inhibiting amount of a compound capable of inhibiting binding of beta-sheet fibril to RAGE so as to thereby inhibit binding of beta-sheet fibril to RAGE. In one embodiment, the beta-sheet fibril is amyloid fibril. In one embodiment, the compound is sRAGE or a fragment thereof. In another embodiment, the compound is an anti-RAGE antibody or portion thereof. This invention provides the above method wherein the inhibition of binding of the beta-sheet fibril to RAGE has the consequences of decreasing the load of beta-sheet fibril in the tissue, inhibiting fibril-induced programmed cell death, and inhibiting fibril-induced cell stress. This invention also provides methods of determining whether a compound inhibits binding of a beta-sheet fibril to RAGE on the surface of a cell.
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Sensing devices from molecular electronic devices (Fri, 16 Jan 2009)
The present invention generally relates to the fabrication of molecular electronics devices from molecular wires and Single Wall Nanotubes (SWNT). In one embodiment, the cutting of a SWNT is achieved by opening a window of small width by lithography patterning of a protective layer on top of the SWNT, followed by applying an oxygen plasma to the exposed SWNT portion. In another embodiment, the gap of a cut SWNT is reconnected by one or more difunctional molecules having appropriate lengths reacting to the functional groups on the cut SWNT ends to form covalent bonds. In another embodiment, the gap of a cut SWNT gap is filled with a self-assembled monolayer from derivatives of novel contorted hexabenzocoranenes. In yet another embodiment, a device based on molecular wire reconnecting a cut SWNT is used as a sensor to detect a biological binding event.
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RADIOLABELED COMPOUNDS AND USES THEREOF (Fri, 09 Jan 2009)
The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as an imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
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Removal of contaminants from water using sugar based surfactant enhanced ultrafiltration (Fri, 19 Dec 2008)
Embodiments of the present invention relate to the removal of contaminants from water using sugar based surfactant enhanced ultrafiltration. Embodiments of the present invention are directed to a process for removal of an at least slightly water-soluble organic compound from an organic-contaminated water solution to provide a purified water solution, including: adding a surfactant to the organic-contaminated water solution in sufficient quantity to achieve at least a critical micellar concentration of the surfactant in the organic-contaminated water solution, wherein the surfactant comprises an alkylglycoside, to provide a micellar water solution comprising micelles comprising the surfactant and the organic compound; contacting an ultrafiltration membrane with the micellar water solution under pressure and temperature conditions sufficient for liquid flow through the ultrafiltration membrane to take place; and collecting liquid permeating the ultrafiltration membrane to provide the purified water solution.
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Preparation Of Ginkgolide And F-Seco-Ginkgolide Lactols (Fri, 12 Dec 2008)
The present invention relates to synthesis of C11 natural ginkgolide derivatives and C11 f-seco-gingkolide derivatives from the corresponding lactols which are selectively obtained using NaBH4.
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METHODS FOR CONTROLLING SURFACE FUNCTIONALITY OF METAL OXIDE NANOPARTICLES, METAL OXIDE NANOPARTICLES HAVING CONTROLLED FUNCTIONALITY, AND USES THEREOF (Fri, 05 Dec 2008)
Methods for controlling surface functionality of metal oxide nanoparticles, nanoparticles having controlled surface functionality, and uses thereof are described herein. Methods for controlling the surface functionality of a metal oxide nanoparticle are can include attaching a ligand to a metal oxide nanoparticle, where the ligand can include a functional portion that is capable of forming an irreversible bond with an object at a site that is complementary to the functional portion without reacting with other reactive sites that may be present. Moreover, metal oxide nanoparticles having versatile ligands can include an anchoring portion that binds to the surface of the metal oxide nanoparticle and a functional portion that is capable of forming an irreversible bond with an object at a site that is complementary to the functional portion without reacting with other reactive sites that may be present. Uses thereof can include cancer detection, electronics, cosmetics, cellular delivery carriers, magnetic storage media, drug delivery carriers, nanocomposite formation for improved mechanical properties, and the like.
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SUBSTITUTED ( 5, 6 ) -DIHYDRONAPHRAALENYL COMPOUNDS AS REVERSIBLE MALE CONTRACEPTIVES (Fri, 14 Nov 2008)
The invention provides a method for inhibiting spermatogenesis in a mammal, as well as a reversible contraceptive for use in a mammal.
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MICROFLUIDIC CELLS WITH PARALLEL ARRAYS OF INDIVIDUAL DNA MOLECULES (Fri, 07 Nov 2008)
Nucleic acid arrays and methods of using nucleic acid arrays are disclosed.
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Polymeric Nanoparticles and Nanogels for Extraction and Release of Compounds (Fri, 24 Oct 2008)
The invention relates to polymeric nanoparticles and nanogels, which can contain, deliver, and/or release one or more active agents, such as biologically active molecules or fragrance molecules, and methods of preparing the polymeric nanoparticles and nanogels. The nanoparticles are crosslinked utilizing radiation (g-radiation) as the catalyst for free radical polymerization (see FIG. 1) rather than by toxic chemical means. The nanoparticles and nanogels can be modified, without limitation, with hydrophobic, hydrophilic, or ionic groups or moieties. or with enzymes. Methods of preparing nanoparticles and nanogels containing or encapsulating a variety of molecules, including biologically active molecules and fragrance molecules, are provided.
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METAL OXIDE NANOCRYSTALS: PREPARATION AND USES (Fri, 03 Oct 2008)
Nanocrystalline forms of metal oxides, including binary metal oxide, perovskite type metal oxides, and complex metal oxides, including doped metal oxides, are provided. Methods of preparation of the nanocrystals are also provided. The nanocrystals, including uncapped and uncoated metal oxide nanocrystals, can be dispersed in a liquid to provide dispersions that are stable and do not precipitate over a period of time ranging from hours to months. Methods of preparation of the dispersions, and methods of use of the dispersions in forming films, are likewise provided. The films can include an organic, inorganic, or mixed organic/inorganic matrix. The films can be substantially free of all organic materials. The films can be used as coatings, or can be used as dielectric layers in a variety of electronics applications, for example as a dielectric material for an ultracapacitor, which can include a mesoporous material.
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NOVEL ANTI-ARRYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RYR2) (Thu, 31 Jul 2008)
• same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or ; prevent a decrease in the level of RyR -bound FKBPI2.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; I and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention : further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these ! methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, i atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided i are agents identified by such methods. O o
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Photolabile compounds (Fri, 25 Jul 2008)
The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect.
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METHODS FOR IDENTIFYING, OR ASSAYING FOR AGENTS THAT INCREASE BETA-CELL PROLIFERATION, INSULIN SECRETION, INSULIN SENSITIVITY, GLUCOSE TOLERANCE AND DECREASES FAT MASS (Fri, 25 Jul 2008)
The present invention is directed to cell-based and non-cell based methods of drug screening to identify agents, or assay agents, that reduce OST-PTP or gamma-carboxylase activity or expression, or increase the level of undercarboxylated osteocalcin or adiponectin activity or expression. Such agents find use in treating or preventing a disorder related to the OST-PTP signaling pathway. Such disorders include, metabolic syndrome, glucose intolerance, type 1 or type 2 diabetes, atherosclerosis, or obesity. Such agents may be used to treat disorders characterized by decreased insulin production, deceased insulin sensitivity, and decreased glucose tolerance or increased fat mass.
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Silacycle compounds and methods of use thereof (Fri, 11 Jul 2008)
The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.
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Radiolabeled compounds and uses thereof (Fri, 13 Jun 2008)
The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
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Radiolabeled Arylsulfonyl Compounds and Uses Thereof (Fri, 13 Jun 2008)
The present invention relates to Radiolabeled Arylsulfonyl Compounds and methods of use thereof as imaging agents for the COX-2 enzyme using positronemission tomograpy (PET). Methods of making the Radiolabeled Arylsulfonyl Compounds and pharmaceutical compositions comprising an effective amount of a Radiolabeled Arylsulfonyl Compound are also disclosed.
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FOUR-COLOR DNA SEQUENCING BY SYNTHESIS USING CLEAVABLE FLUORESCENT NUCLEOTIDE REVERSIBLE TERMINATORS (Fri, 13 Jun 2008)
This invention provides a process for sequencing single- stranded DNA by employing a nanopore and modified nucleotides.
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USES OF A MURINE MODEL OF HIV-1 INFECTION (Fri, 13 Jun 2008)
The invention provides for a chimeric HIV-1 construct, EcoHIV, capable of replication in a rodent cell. The invention also provides a convenient and safe rodent model of HIV-1 infection and AIDS. A rodent model of HIV-1 infection is also provided which is useful for screening of candidate anti-viral drugs. Additionally, the invention provides for a method to test immunogenic compositions or pharmaceutical interventions effective in preventing infection, reducing viral load, or reducing disease symptoms in a subject.
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PHOTOCHEMICAL METHODS AND PHOTOACTIVE COMPOUNDS FOR MODIFYING SURFACES (Fri, 09 May 2008)
Compounds and methods for controlling the surface properties are described. Compounds of the invention can form radicals upon exposure to irradiation, which can then react with nearby molecules to alter the surface properties of various substrates. The invention can provide surfaces that are resistant to dewetting, surfaces that have immobilized molecules such as carbohydrates and polymers immobilized, and surfaces that have metals deposited on the surface. The invention can be utilized in a wide range of application, such as sensors, microreactors, microarrays, electroless deposition of metals, and the like.
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UNDERCARBOXYLATED/UNCARBOXYLATED OSTEOCALCIN INCREASES BETA-CELL PROLIFERATION, INSULIN SECRETION, INSULIN SENSITIVITY, GLUCOSE TOLERANCE AND DECREASES FAT MASS (Fri, 21 Mar 2008)
The present invention relates to methods and compositions for treating and diagnosing disorders related to energy metabolism and the OST-PTP signaling pathway involving gamma-carboxylase, osteocalcin and adiponectin. Such disorders include, but are not limited to, metabolic syndrome, glucose intolerance, diabetes types 1 and 2, atherosclerosis and obesity.
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SYSTEMS AND METHODS FOR HIGH-THROUGHPUT, MINIMALLY-INVASIVE RADIATION BIODOSIMETRY (Fri, 29 Feb 2008)
A method for obtaining a sample, determining the sample's metabolomic signature, comparing that signature to at least one known metabolomic signature, and quantifying the radiation exposure of the sample Sample sources may include blood, blood plasma, sweat, urine, sebum, saliva, or cells, or a combination thereof The method may utilize samples obtained noninvasively The method may be capable of high throughput, 50, 100, 1000, 10,000, 100,000, or more samples per hour The method may utilize samples from mice, humans, or other mammals The method may utilize chromatography, mass spectroscopy, or radiofrequency differential ion mobility spectrometry analysis, or a combination thereof The method may employ software for comparing the metabolomic signature of the sample with at least one known radiation exposure metabolomics signature
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IMAGING CORRELATES OF NEUROGENESIS WITH MRI (Fri, 22 Feb 2008)
This invention provides a method for treating a mammalian subject afflicted with a disorder associated with reduced neurogenesis in the subject's hippocampal dentate gyrus which comprises administering to the subject a therapeutically effective amount of a compound which increases cerebral blood volume in the subject's hippocampal dentate gyrus by a percentage greater than that by which it increases the cerebral blood volume in the subject's hippocampal CAl region, thereby treating the subject.
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R-SPONDIN COMPOSITIONS AND METHODS OF USE THEREOF (Fri, 22 Feb 2008)
The invention provides for a method for screening compounds that bind to and modulate a regulator of Wnt signaling, R-spondin 4. The invention further provides for methods for diagnosing a keratin-related abnormality, such as anonychia congenital, in a subject. The invention also provides for isolated RSPO4 mutant molecules.
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Human chorionic gonadotropin antagonists and methods to prevent ovarian hyperstimulation (Fri, 15 Feb 2008)
The present invention is directed to a human chorionic gonadotropin (hCG) antagonist comprising deglycosylated hCG. Methods of recombinantly producing the hCG antagonist in a glycosylation-deficient host cell are also provided. Methods of treating hCG related conditions including ovarian hyperstimulation syndrome, gestational trophoblastic disease, and hCG related tumors by administering an effective amount of the hCG antagonist are also provided herein. 
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FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS (Fri, 01 Feb 2008)
The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is -H, -OH, -O-R7, -N(H) -R8, -N (H) - (CH2) n-NH2, -N(R9) (R10), or a piperazine cation; R2 is either covalently bound to R9, or is -H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R3 is =O; R4 is, inter alia, -H, -OH, or -R11NH2; R5 is, inter alia, -H, -OH, or -R12NH2, and R6 is either is covalently bound to R10 or is -H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
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Methods of inhibiting binding of beta-sheet fibril to rage and consequences thereof (Fri, 25 Jan 2008)
This invention provides a method of inhibiting the binding of a β-sheet fibril to RAGE on the surface of a cell which comprises contacting the cell with a binding inhibiting amount of a compound capable of inhibiting binding of the β-sheet fibril to RAGE so as to thereby inhibit binding of the β-sheet fibril to RAGE. In one embodiment the β-sheet fibril is amyloid fibril. In one embodiment, the compound is sRAGE or a fragment thereof. In another embodiment, the compound is an anti-RAGE antibody or portion thereof. This invention provides the above method wherein the inhibition of binding of the β-sheet fibril to RAGE has the consequences of decreasing the load of β-sheet fibril in the tissue, inhibiting fibril-induced programmed cell death, inhibiting fibril-induced cell stress. This invention also provides methods of determining whether a compound inhibits binding of a β-sheet fibril to RAGE on the surface of a cell. 
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METHODS FOR TESTING ANTI-THROMBOTIC AGENTS (Fri, 11 Jan 2008)
The invention provides a transgenic non-human animal expressing von Willebrand Factor Al protein containing at least one mutation selected from the group consisting of: 1263P>S, 1269N>D, 1274K>R, 1287M>R, 1302G>D, 1308H>R, 1313R>W, 1314I>V, 1326R>H, 1329L>I, 1330E>G, 1333A>D, 1344T>A, 1347I>V, 1350T>A, 1370G>S, 1379H>R, 1381T>A, 1385T>M 1391P>Q, 1394A>S, 1397L>F, 1421S>N, 1439L>V, 1442G>S, 1449R>Q, 1466A>P, 1469Q>L, 1472Q>H, 1473V>M, 1475H>Q, 1479S>G, and any combination thereof.
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Complex amplitude modulation in blood flow and perfusion measurement for measuring a distribution of transit times on a voxel by voxel basis (Fri, 07 Dec 2007)
Systems and methods for blood flow and perfusion measurement using complex amplitude modulation of MRI pulses are presented. In exemplary embodiments of the disclosed subject matter, inflowing arterial spins can be modulated using a complex modulation function having certain mathematical properties in the frequency domain, such as, for example, a pseudo-random sequence. In exemplary embodiments of the disclosed subject matter the mathematical properties of such complex modulation functions can be used to measure individual transit times by deconvolving them from a series of acquired images. In exemplary embodiments of the disclosed subject matter images can be acquired at the same rapid rate as arterial modulation, and transit time distribution in the imaged tissue can be determined as part of a single integrated acquisition.
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Photocleavable fluorescent nucleotides for DNA sequencing on chip constructed by site-specific coupling chemistry (Fri, 30 Nov 2007)
This invention provides a method for determining the sequence of a DNA or an RNA, wherein (i) about 1000 or fewer copies of the DNA or RNA are bound to a solid substrate via 1,3-dipolar azide-alkyne cycloaddition chemistry and (ii) each copy of the DNA or RNA comprises a self-priming moiety.
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SENSING DEVICES FROM MOLECULAR ELECTRONIC DEVICES UTILIZING HEXABENZOCORONENES (Fri, 23 Nov 2007)
The present invention generally relates to the fabrication of molecular electronics devices from molecular wires and Single Wall Nanotubes (SWNT). In one embodiment, the cutting of a SWNT is achieved by opening a window of small width by lithography patterning of a protective layer on top of the SWNT, followed by applying an oxygen plasma to the exposed SWNT portion. In another embodiment, the gap of a cut SWNT is reconnected by one or more difunctional molecules having appropriate lengths reacting to the functional groups on the cut SWNT ends to form covalent bonds. In another embodiment, the gap of a cut SWNT gap is filled with a self-assembled monolayer from derivatives of novel contorted hexabenzocoranenes. In yet another embodiment, a device based on molecular wire reconnecting a cut SWNT is used as a sensor to detect a biological binding event.
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Methods to treat or prevent hormone-resistant prostate cancer using siRNA specific for protocadherin-PC, or other inhibitors of protocadherin-PC expression or activity (Fri, 26 Oct 2007)
The invention is directed to compounds and methods for treating or preventing hormone-resistant prostate cancer using siRNA specific for protocadherin-PC, or other inhibitors of protocadherin-PC expression or activity, including antisense oligonucleotides and antibodies. The invention also provides for the use of protocadherin-PC as an in vivo prostate cancer biomarker, and includes a kit for detecting prostate cancer in biological samples. Also covered by the invention is a transgenic non-human mammal engineered to overexpress protocadherin-PC specifically in the prostate. 
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SENSING DEVICES FROM MOLECULAR ELECTRONIC DEVICES (Fri, 26 Oct 2007)
The present invention generally relates to the fabrication of molecular electronics devices from molecular wires and Single Wall Nano tubes (SWNT). In one embodiment, the cutting of a SWNT is achieved by opening a window of small width by lithography patterning of a protective layer on top of the SWNT, followed by applying an oxygen plasma to the exposed SWNT portion. In another embodiment, the gap of a cut SWNT is reconnected by one or more difunctional molecules having appropriate lengths reacting to the functional groups on the cut SWNT ends to form covalent bonds. In another embodiment, the gap of a cut SWNT gap is filled with a self-assembled monolayer from derivatives of novel contorted hexabenzocoranenes. In yet another embodiment, a device based on molecular wire reconnecting a cut SWNT is used as a sensor to detect a biological binding event.
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Side population cells in cardiac repair (Fri, 03 Aug 2007)
It has been discovered that side-population cells induce cardiac tissue repair of infarcted myocardium. Provided herein are methods directed to treatment of cardiac injury using side-population cells.
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THE TOTAL SYNTHESIS OF ECTEINASCIDIN 743 AND DERIVATIVES THEREOF (Fri, 03 Aug 2007)
This invention provides a method of synthesizing ecteinascidin 743 and derivatives. This invention also provides intermediate compounds and methods of treating tumors.
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Agents for preventing and treating disorders involving modulation of the RyR receptors (Fri, 27 Jul 2007)
The present invention provides compounds of Formula I <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.25mm" wi="36.91mm" file="US07879840-20110201-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. 
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CRYSTAL STRUCTURE OF A BACTERIAL HOMOLOGUE OF NA(+) CL(-)-DEPENDENT NEUROTRANSMITTER TRANSPORTERS (Fri, 27 Jul 2007)
The present invention relates to three dimensional structural models of the LeuTAa transporter, and, in particular, the modeled sites of these proteins. The structural information of the present invention may be used for the rational design of compounds which act as modulators of the LeuTAa transporter and its eukaryotic counterparts. The present invention further provides for actual or virtual screening assays which may be used to identify compounds having such modulator activities, or to confirm the activity of designed compounds.
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Hydroxamic acid compounds and methods of use thereof (Fri, 06 Jul 2007)
The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
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CHEMICALLY DERIVATIZED CD4 AND USES THEREOF (Fri, 06 Jul 2007)
This invention provides two soluble polypeptides which comprise a portion of CD4 comprising all HIV gpl20-binding epitopes present on intact CD4, wherein the polypeptide has a cysteine substitution at a residue which, in intact CD4, interfaces with HIV gpl20. This invention provides also provides a method for making a derivatized soluble polypeptide and a method for obtaining a structural model useful in the design of an agent for inhibiting CD4 binding to HIV gpl20.
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Methods for modifying surfaces (Fri, 15 Jun 2007)
The invention is directed to methods for coating monolayer films of surface-active polymers onto substrates of arbitrary shape, and molecular-based methods and processes to control the chemical and physical nature of surfaces and interfaces. The invention is also directed to methods for modifying a surface of a monolayer comprising a) coating a monolayer on a substrate, wherein the monolayer is formed by self-assembly of end-surfactant molecules, thereby positioning a photoactive functional group at the air-monolayer interface; and b) exposing the monolayer to radiation, wherein each organic group of the monolayer contains a first functionality that is not converted to a second functionality upon exposure to acid.
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THE USE OF HUMAN STEM CELLS AND/OR FACTORS THEY PRODUCE TO PROMOTE ADULT MAMMALIAN CARDIAC REPAIR THROUGH CARDIOMYOCYTE CELL DIVISION (Fri, 15 Jun 2007)
The present invention relates to methods and compositions for stimulating the proliferation of cardiomyocytes for enhancement of cardiac repair. The invention is based on. the discovery that upon contact with stem cells, or conditioned media derived from said stem cells, terminally differentiated cardiomyocytes can be stimulated to enter the cell cycle. Additionally, scaffolds capable of attracting stem cells to the area of implantation have been shown to induce cardiomyocyte proliferation. The present invention further relates to the discovery that the Wnt-5 A ligand, which binds to the frizzled receptor (fz), functions to stimulate cardiomyocyte proliferation. The methods and compositions of the invention may be used in the treatment of cardiac disorders including, but not limited to, myocardial dysfunction or infarction. The invention further relates to screening assays designed to identify compounds that modulate the proliferative activity of cardiomyocytes and the use of such compounds in the treatment of cardiac disorders.
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SYNTHESIS OF FOUR COLOR 3'-O-ALLYL MODIFIED PHOTOCLEAVABLE FLUORESCENT NUCLEOTIDES AND RELATED METHODS (Fri, 11 May 2007)
This invention provides a process for making 3'-O- allyl-dGTP-PC-Biodopy-FL-51O, 3' -0-allyl-dATP-PC-ROX, 3'-O-allyl-dCTP-PC-Bodipy-650 and 3' -O-allyl-dUTP-PC- R6G, and related methods.
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CHEMICALLY CLEAVABLE 3'-O-ALLYL-DNTP-ALLYL-FLUOROPHORE FLUORESCENT NUCLEOTIDE ANALOGUES AND RELATED METHODS (Fri, 11 May 2007)
This invention provides a nucleotide analogue comprising (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine and uracil, (ii) a deoxyribose, (iii) an allyl moiety bound to the 3' -oxygen of the deoxyribose and (iv) a fluorophore bound to the base via an allyl linker, and methods of nucleic acid sequencing employing the nucleotide analogue.
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Analogs of terpene trilactones from Ginkgo biloba and related compounds and uses thereof (Fri, 04 May 2007)
The subject invention provides compounds having the structure: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="80.52mm" wi="41.57mm" file="US07473788-20090106-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1-C5) alkyl group, (C2-C5) alkenyl, or a (C2-C5) alkynyl, (C1-C5) alkoxy, (C2-C5) alkenyloxy, or (C2-C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1-C5) alkyl, (C2-C5) alkenyl, or (C2-C5) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1-C10) alkyl, (C1-C10) alkenyl, (C1-C10) alkynyl, -A-Ar, -A-Z-Ar, —SO2—Ar, or -A-NR5, or —R7, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject. 
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MICROFLUIDIC CELLS WITH PARALLEL ARRAYS OF INDIVIDUAL DNA MOLECULES (Fri, 13 Apr 2007)
Nucleic acid arrays and methods of using nucleic acid arrays are disclosed The nucleic acids are bound on one or both nucleic acid ends to a flow cell containing a lipid layer to prevent nonspecific binding The length and conformation of the nucleic acid is then visualized by evanescent illumination of fluorescent labels associated with the nucleic acid microscopic observation The methods can be used to visualize nucleic acid-protein interactions, and other interactions that affect the length or conformation of the nucleic acid.
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COMPOSITIONS AND METHODS FOR DETECTING LIGAND-RECEPTOR INTERACTIONS (Fri, 13 Apr 2007)
The present invention relates to methods and compositions for labeling receptors in vivo or in vitro, whereby a fluorescent molecular rotor is conjugated to a ligand or receptor which exhibits substantially increased fluorescence when the ligand binds to the receptor.
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SIDE POPULATION CELLS IN CARDIAC REPAIR (Fri, 06 Apr 2007)
It has been discovered that side-population cells induce cardiac tissue repair of infarcted myocardium. Provided herein are methods directed to treatment of cardiac injury using side-population cells.
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Covalent methods for immobilization of thiolated biomolecules on siliceous and metallic surfaces (Fri, 30 Mar 2007)
The present invention is directed to methods for immobilizing molecules on siliceous and metallic surfaces. Molecules are immobilized on siliceous or metallic surfaces by stable covalent linkages that are capable of withstanding prolonged use and elevated temperatures. Further, the methods of the present invention describe less-complicated chemistries for the immobilization of molecules that will benefit the reproducibility, efficiency and effectiveness of applications in sensing, chromatography, medical diagnostics and related areas where specific recognition between immobilized and free molecules provides diagnostic information or serves as part of a purification or separations process. 
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Agents for preventing and treating disorders involving modulation of the RyR receptors (Fri, 02 Mar 2007)
The present invention provides novel compounds of Formula I <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="26.25mm" wi="34.04mm" file="US07704990-20100427-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss. 
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AGENTS FOR PREVENTING AND TREATING DISORDERS INVOLVING MODULATION OF THE RYR RECEPTORS (Fri, 02 Mar 2007)
The present invention provides compounds of Formula I, (I) and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
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FLUOROGENIC PROBES FOR MEDIUM CHAIN ACYL-COA DEHYDROGENASE ( MCAD ) (Fri, 23 Feb 2007)
The present invention relates to compounds useful for detecting the activity of human MCAD, compounds useful for competitively inhibiting human MCAD, as well as methods of manufacture thereof .
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SYNTHESIS OF SCABRONINES AND ANALOGUES THEREOF (Fri, 02 Feb 2007)
A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
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Compositions and methods for treating and preventing heart tissue degeneration, and uses thereof (Fri, 19 Jan 2007)
The present invention provides methods for promoting generation of heart tissue, and for treating and preventing heart tissue degeneration. Additionally, the present invention provides a therapeutic composition comprising a cyclin-associated agent, and a kit comprising the composition. The present invention further provides a heart tissue cell, a sidepopulation progenitor cell, and a stem cell in which cyclin is augmented. Also provided are cell lines comprising these cells, screening methods using the cell lines, and drugs identified by these methods. The present invention further provides in vitro systems for use in screening candidate drugs for at least one cardiotoxic effect and/or for synergy with cyclin in the treatment and prevention of heart tissue degeneration. Finally, the present invention provides use of a cyclin-associated agent in the generation of heart tissue, and use of a cyclin associated agent in the treatment or prevention of heart tissue degeneration.
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Method and system of tracking an intracorporeal device with MR imaging (Fri, 12 Jan 2007)
A system and method for tracking or otherwise determining positioning of an intracorporeal device is provided. The invention includes a device that may be inserted into a subject and tracked based on an imageable tag included with the device. The imageable tag is at least partially formed of a substance whose nuclei precess at a Larmor frequency different than the Larmor frequency of hydrogen when subjected to a polarizing magnetic field. MR data may be acquired from the imageable tag using an RF receiver tuned to the Larmor frequency of the substance and used to track movement of the device within the subject.
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CORE-MODIFIED TERPENE TRILACTONES FROM GINKGO BILOBA EXTRACT AND BIOLOGICAL EVALUATION THEREOF (Fri, 05 Jan 2007)
Lactone-rings of ginkgolides are converted into the corresponding tetrahydrofuran moieties via DIBAL-H reduction followed by deoxygenation of the formed lactols with Et3SiH/BF3 Et2O producing a series of lactol-free ginkgolides. The present invention also relates to synthesis of hydroxyl-free, or hydroxyl-free and lactone- free, ginkgolides and bilobalides .
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Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof (Fri, 27 Oct 2006)
The present invention provides the compound having the formula: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="19.47mm" wi="45.72mm" file="US07345174-20080318-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above. 
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SYSTEM AND METHOD FOR STORAGE AND ACCESS OF DATA FILES OVER A NETWORK (Fri, 13 Oct 2006)
A system for storage and access of data files on a network comprising one or more workstation servers and apparatuses for generating data files. A data storage array (element 122) comprises data partitions corresponding to the at least one workstation server. A metadata server may be provided which permits the at least one workstation (elements 134 a and b) server to access data on the data storage array. The data storage array is accessed via a switch connected to the at least one workstation server, the data storage array, and the metadata server. An internet router may be provided to remotely access the data storage array.
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Peptides and methods for deactivation of organophosphorus-based nerve agents and insecticides (Fri, 29 Sep 2006)
This invention provides methods and peptides for the inactivation of organophosphorus-based insecticides and chemical warfare agents. The instant methods include peptide screening methods, peptides and peptide libraries, related compositions of matter, articles of manufacture, and methods for prophylaxis, treatment, decontamination and detection.
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NOVEL ANTI-ARRYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RYR2) (Fri, 29 Sep 2006)
The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exerciseinduced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.
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NOVEL ANTI-ARRYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RYR2) (Fri, 29 Sep 2006)
The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.
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Cross reactive arrays of three-way junction sensors for steroid determination (Fri, 15 Sep 2006)
This invention provides analyte sensitive oligonucleotide compositions for detecting and analyzing analytes in solution, including complex solutions using cross reactive arrays of analyte sensitive oligonucleotide compositions.
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PENTACYCLIC ALKALOID COMPOUNDS AND METHODS OF USE THEREOF (Sat, 09 Sep 2006)
The present invention relates to Pentacyclic Alkaloid Compounds, compositions comprising an effective amount of a Pentacyclic Alkaloid Compound and methods for treating or preventing cancer, a bacterial infection, a fungal infection, or a yeast infection, comprising administering to a subject in need thereof an effective amount of a Pentacyclic Alkaloid Compound. The present invention also relates to compounds and methods that are useful for making Cribrostatin IV.
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Agents for preventing and treating disorders involving modulation of the RyR receptors (Fri, 01 Sep 2006)
The present invention provides novel compounds of Formula I <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.99mm" wi="34.04mm" file="US08022058-20110920-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells. Such disorders and diseases include, by way of example only, cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases, malignant hyperthermia, diabetes, and sudden infant death syndrome. Cardiac disorder and diseases include, but are not limited to, irregular heartbeat disorders and diseases; exercise-induced irregular heartbeat disorders and diseases; sudden cardiac death; exercise-induced sudden cardiac death; congestive heart failure; chronic obstructive pulmonary disease; and high blood pressure. Irregular heartbeat disorders and diseases include and exercise-induced irregular heartbeat disorders and diseases include, but are not limited to, atrial and ventricular arrhythmia; atrial and ventricular fibrillation; atrial and ventricular tachyarrhythmia; atrial and ventricular tachycardia; catecholaminergic polymorphic ventricular tachycardia (CPVT); and exercise-induced variants thereof. Skeletal muscular disorder and diseases include, but are not limited to, skeletal muscle fatigue, exercise-induced skeletal muscle fatigue, muscular dystrophy, bladder disorders, and incontinence. Cognitive disorders and diseases include, but are not limited to, Alzheimer's Disease, forms of memory loss, and age-dependent memory loss. 
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METHODS TO TREAT OR PREVENT HORMONE-RESISTANT PROSTATE CANCER USING SIRNA SPECIFIC FOR PROTOCADHERIN-PC, OR OTHER INHIBITORS OF PROTOCADHERIN-PC EXPRESSION OR ACTIVITY (Fri, 18 Aug 2006)
The invention is directed to compounds and methods for treating or preventing hormone-resistant prostate cancer using siRNA specific for protocadherin-PC, or other inhibitors of protocadherin-PC expression or activity, including antisense oligonucleotides and antibodies. The invention also provides for the use of protocadherin-PC as an in vivo prostate cancer biomarker, and includes a kit for detecting prostate cancer in biological samples. Also covered by the invention is a transgenic non-human mammal engineered to overexpress protocadherin-PC specifically in the prostate.
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RADIOLABELED COMPOUNDS AND USES THEREOF (Fri, 11 Aug 2006)
The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
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PROCESSES OF MAKING SESQUITERPENOID TASHIRONIN, ITS ANALOGS AND THEIR USES (Fri, 11 Aug 2006)
The compound having the structure of the formula (genus of compound 1 excluding Tashironin or Debenzoyltashironin) wherein, R1 is H or Bz when no more than three of R8, R9, R10 and R11 are H, or R1 is Bn, (C1-C4) alkyl, or CF3; R2 is H, (C1-C4) aldyl, halide, OC(O) (C1-C4) alkyl, OC(O) Ph, or OCF3; R3 is p-toluene sulfonyloxy, methane sulfonyloxy, C(O) (C1-C4)alkyl, or OC(O) (C1-C4)alkyl, bond α is a single bond, and bond β is a double bond or R3 is O, bond α is a double bond and bond β is a single bond; R4 is H, I, Br, Cl, Si(CH3)3, (C1-C4)alkyl, or OCF3; R5 is OH, OSi (CH3)3, O(C1-C4)alkyl, or OCF3, and bond Ϝ is a single bond, or R5 is O and bond Ϝ is a double bond; R6 is H, (C1-C4) alkyl, or CF3.
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PREPARATION OF GINKGOLIDE AND F-SECO-GINKGOLIDE LACTOLS (Fri, 11 Aug 2006)
The present invention relates to synthesis of C11 natural ginkgolide derivatives and C11 f-seco-gingkolide derivatives from the corresponding lactols which are selectively obtained using NaBH4.
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QUINOXALINE DERIVATIVES AS ANTITUMOR AGENTS (Fri, 04 Aug 2006)
The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also provides reagents and methods for effective killing of cancer cells with erastin and related compounds or derivatives, such like the compounds (1).
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ERASTIN ANALOGUES AND THEIR USES FOR KILLING CANCER CELLS (Fri, 04 Aug 2006)
The invention provides methods for effective killing of cancer cells with erastin and related compounds or derivatives.
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ENANTIOSELECTIVE SYNTHESIS OF MERRILACTONE A AND ITS ANALOGS (Fri, 28 Jul 2006)
This invention provides a method of synthesizing enantioenriched merrilactone A and enantiopure merrilactone A, as well as an improved method of synthesizing racemic merrilactone. This invention also provides intermediate compounds and methods of treating peripheral neuropathies.
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Compositions and methods for treating and preventing heart tissue degeneration and uses thereof (Fri, 21 Jul 2006)
The present invention provides compositions useful for cardiac therapy comprising a cyclin-associated agent. The present invention also provides kits for use in delivering a cyclin-associated agent to cardiac cells in a subject, comprising the composition of the present invention and a catheter. The present invention additionally provides a methods for enhancing cardiac function; promoting regeneration of cardiac tissue; inducing endogenous myocardial regeneration; and preventing or treating heart failure in a subject in need thereof by augmenting cyclin in cells.
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SILACYCLE COMPOUNDS AND METHODS OF USE THEREOF (Fri, 16 Jun 2006)
The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.
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Transgenic mice over-expressing ABAD and mutant APP in brain as model of Alzheimer's disease and uses thereof (Wed, 14 Jun 2006)
The present invention provides for a transgenic non-human animal whose cells contain a DNA sequence comprising: (a) a nerve tissue specific promoter operatively linked to a DNA sequence which encodes amyloid-beta peptide alcohol dehydrogenase (ABAD), and (b) a nerve tissue specific promoter operatively linked to a DNA sequence encoding a mutant human amyloid precursor protein hAPP695, hAPP751 and hAPP770 bearing mutations linked to familial Alzheimer's disease in humans, wherein the non-human animal exhibits at least one phenotype from the group consisting of: reduced basal synaptic transmission; inhibited synaptic plasticity; increased neuronal stress; elevated 4-hydroxynonenal in cerebral cortex; increased heme oxygenase type I in cerebral cortex; decreased synaptophysin in cerebral cortex; decreased micortubule-associated protein 2 in cerebral cortex; and increased levels of activated caspase 3 antigen in cortical neurons.
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POLYMERIC NANOPARTICLES AND NANOGELS FOR EXTRACTION AND RELEASE OF COMPOUNDS (Fri, 19 May 2006)
The invention relates to polymeric nanoparticles and nanogels, which can contain, deliver, and/or release one or more active agents, such as biologically active molecules or fragrance molecules, and methods of preparing the polymeric nanoparticles and nanogels. The nanoparticles are crosslinked utilizing radiation (g-radiation) as the catalyst for free radical polymerization ( see Figure 1) rather than by toxic chemical means. The nanoparticles and nanogels can be modified, without limitation, with hydrophobic, hydrophilic, or ionic groups or moieties. or with enzymes. Methods of preparing nanoparticles and nanogels containing or encapsulating a variety of molecules, including biologically active molecules and fragrance molecules, are provided.
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Crystallization reagent matrices and related methods and kits (Fri, 12 May 2006)
This invention provides methods, kits and automated systems for identifying a reagent in which a compound crystallizes, and methods for crystallizing a compound.
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METHODS AND COMPOSITIONS TO TREAT MOTOR NEURON DISEASE (Fri, 12 May 2006)
The invention features compositions and methods for treating motor neuron diseases, such as spinal muscular atrophy and amyotrophic lateral sclerosis. The compositions and methods include derivatives of indoprofen.
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CROSS REACTIVE ARRAYS OF THREE-WAY JUNCTION SENSORS FOR STEROID DETERMINATION (Fri, 10 Mar 2006)
This invention provides analyte sensitive oligonucleotide compositions for detecting and analyzing analytes in solution, including complex solutions using cross reactive arrays of analyte sensitive oligonucleotide compositions.
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LIGANDS FOR ALDOKETOREDUCTASES (Fri, 03 Mar 2006)
The present invention relates to compounds useful for detecting the activity of human aldoketoreductase 1Cs, compounds useful for competitively inhibiting human aldoketoreductase 1Cs and compounds useful for treating human aldoketoreductase 1C-related cancers, as well as pharmaceutical compositions and methods of manufacture thereof.
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PROCESSES FOR PRODUCING AND CRYSTALLIZING G-PROTEIN COUPLED RECEPTORS (Fri, 03 Mar 2006)
This invention provides methods for producing a membrane-bound protein in mammalian cells. This invention also provides nucleic acids for making novel fusion proteins (e.g., GPCR fusion proteins). This invention further provides related bacterial expression vectors; expression methods; fusion proteins; bacterial cells; GPCR vector screens; bacterial spheroplasts; methods for making antiGPCR antibodies; and GPCR binding screens. This invention also provides a method for identifying a reagent in which a membrane protein is likely to crystallize. Finally, this invention provides methods for producing crystals of a protein which, in a cell, is a membrane-bound protein.
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COMPOUNDS AND THEIR PREPARATION FOR THE TREATMENT OF ALZHEIMER'S DISEASE BY INHIBITING BETA-AMYLOID PEPTIDE PRODUCTION (Fri, 24 Feb 2006)
The present invention provides novel ginsenoside compounds, compositions (e.g. pharmaceutical compositions) comprising the ginsenoside compounds, and methods for the synthesis of these ginsenoside compounds. Additionally, the present invention provides methods for inhibiting beta-amyloid peptide production and methods for treating or preventing a pathological condition, particularly, neurodegeneration diseases (e.g. Alzheimer's disease), using these ginsenoside compounds.
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SYSTEMS AND METHODS FOR DETECTING LIVING ORGANISMS IN SEDIMENTS AND ROCKS (Fri, 17 Feb 2006)
The embodiments are directed to systems and methods for determining in-situ microorganisms in a solid matrix including sediments and rocks. The methods include collecting data such as, effective measured complex dielectric constant, propagation and attenuation time of an electromagnetic wave and porosity, using a multi-frequency impedance spectrometer, an electromagnetic propagation device and a density device. The method further includes calculating and comparing an effective complex dielectric constant with the measured complex dielectric constant and determining a cell concentration of the micro-organisms.
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Reagents for asymmetric allylation, aldol, and tandem aldol and allyation reactions (Fri, 30 Dec 2005)
A new class of reagents and method of use of the reagents in the reaction of the reagents with electrophilic compounds. The invention in one embodiment is directed to a method for the formation of an alcohol of the formula (I). The method includes reacting a reagent of the formula (II) with an aldehyde of the formula R10CHO to form the alcohol. X3 is one of O and C(R4)(R5). Each of X1 and X2 is independently O or N—R. Each of Ca and Cb is independently an achiral center, an (S) chiral center or an (R) chiral center. Ra and Rb are (i) each independently C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl, or (ii) taken together to form a C3—C4 alkylene chain which together with Ca and Cb forms a 5-membered or 6-membered aliphatic ring. Rc and Rd are each independently hydrogen, C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl. R is C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl. Each of R1, R2, R3, R4, R5 is independently hydrogen, C1—C10 alkyl, C6-10 aryl, C3-9 heteroaryl, C1-10 alkoxy, C6-10 aryloxy, C1-10 dialkylamino, C1-10 alkyl-C6-10 arylamino, C1-10 diarylamino, or halogen. R6 is halogen, hydrogen, C1-10 alkyl, C6-10 aryl, C3-9 heteroaryl, C1-10 alkoxy, C6-10 aryloxy, C1-10 alkyl-C6-10 arylamino, C1-10 diarylamino, OSO2CF3 or SR. R10 may be C1-10 alkyl, C6-10 aryl, or C3-9 heteroaryl. <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="41.15mm" wi="62.74mm" file="US07534905-20090519-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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RADIOLABELED ARYLSULFONYL COMPOUNDS AND USES THEREOF (Fri, 23 Dec 2005)
The present invention relates to Radiolabeled Arylsulfonyl Compounds and methods of use thereof as imaging agents for the COX-2 enzyme using positronemission tomograpy (PET). Methods of making the Radiolabeled Arylsulfonyl Compounds and pharmaceutical compositions comprising an effective amount of a Radiolabeled Arylsulfonyl Compound are also disclosed.
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ENHANCING IMAGES SUPERIMPOSED ON UNEVEN OR PARTIALLY OBSCURED BACKGROUND (Fri, 04 Nov 2005)
This invention provides a method of leveling an image of a non-uniform background. The method uses all or a portion of the image data from the original image and mathematical algorithms to construct a model image that reflects the non-uniform background of the original image and subtract the model image from the original image to generate an image with a more uniform background (figure 7). This invention also provides computer software for performing the methods of the invention.
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Enhancing images superimposed on uneven or partially obscured background (Fri, 21 Oct 2005)
This invention provides a method of leveling an image of a non-uniform background. The method uses all or a portion of the image data from the original image and mathematical algorithms to construct a model image that reflects the non-uniform background of the original image and subtract the model image from the original image to generate an image with a more uniform background. This invention also provides computer software for performing the methods of the invention.
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NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RYR2) AND USES THEREOF (Fri, 14 Oct 2005)
The present invention provides methods for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject. The present invention further provides methods for treating and preventing atrial and ventricular cardiac arrhythmias, heart failure, and exercise-induced sudden cardiac death in a subject. Additionally, the present invention provides use of JTV-519 in a method for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject who has, or is a candidate for, atrial fibrillation. Also provided are uses of 1,4-benzothiazepine derivatives in methods for treating and preventing atrial and ventricular cardiac arrhythmias and heart failure in a subject, and for preventing exercise-induced sudden cardiac death. The present invention also provides methods for identifying agents for use in treating and preventing atrial fibrillation and heart failure, and agents identified by these methods.
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GINKGOLIDE COMPOUNDS, COMPOSITIONS, EXTRACTS, AND USES THEREOF (Fri, 07 Oct 2005)
The present invention relates to Ginkgolide derivatives, compositions and extracts comprising one or more Ginkgolides and/or derivatives thereof and methods of use of the compositions to treat neurological disorders and as imaging agents.
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Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof (Fri, 30 Sep 2005)
The present invention provides methods for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject. The present invention further provides methods for treating and preventing atrial and ventricular cardiac arrhythmias, heart failure, and exercise-induced sudden cardiac death in a subject. Additionally, the present invention provides use of JTV-519 in a method for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject who has, or is a candidate for, atrial fibrillation. Also provided are uses of 1,4-benzothiazepine derivatives in methods for treating and preventing atrial and ventricular cardiac arrhythmias and heart failure in a subject, and for preventing exercise-induced sudden cardiac death. The present invention also provides methods for identifying agents for use in treating and preventing atrial fibrillation and heart failure, and agents identified by these methods.
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PHOTOCLEAVABLE FLUORESCENT NUCLEOTIDES FOR DNA SEQUENCING ON CHIP CONSTRUCTED BY SITE-SPECIFIC COUPLING CHEMISTRY (Fri, 16 Sep 2005)
This invention provides a method for determining the sequence of a DNA or an RNA, wherein (i) about 1000 or fewer copies of the DNA or RNA are bound to a solid substrate via 1,3-dipolar azide-alkyne cycloaddition chemistry and (ii) each copy of the DNA or RNA comprises a self-priming moiety.
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COMPUTER-IMPLEMENTED METHODS AND SYSTEMS FOR GENERATING ELASTIC BLOCK CIPHERS FOR ENCRYPTION AND DECRYPTION (Sat, 10 Sep 2005)
In accordance with the present invention, computer implemented methods and systems are provided for converting an elastic block cipher from an original block cipher. The elastic block cipher accepts variable length inputs where the computation workload increases in proportion to the block size. To generate the elastic block cipher, the number of rounds in the block cipher is increased such that the round function is applied to each bit position at least the same number of times as the original block cipher. In addition, bits that are beyond the normal block size are left out of the round function and XORed and swapped with bits output from the round function to become part of the input to the next round.
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Methods for identifying a chemical compound that directly enhances binding of FKBP12.6 to PKA-phosphorylated type 2 ryanodine receptor (RyR2) (Fri, 26 Aug 2005)
The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.
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Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) (Fri, 26 Aug 2005)
The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.
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ANTHOCYANIN COMPOUNDS AND METHODS OF USE THEREOF (Fri, 26 Aug 2005)
The present invention is directed to methods for treating or preventing eye diseases or disorders, such as macular degeneration, by administering one or more anthocyanins and/or Anthocyanin Derivatives. These methods are based in part on the present findings that anthocyanins can prevent and/or reduce cell death and damage induced by a byproduct of the visual cycle, A2E. Thus, the present invention provides methods for identifying particular anthocyanins and Anthocyanin Derivatives that are effective for treating or preventing eye diseases or disorders, and compositions comprising Anthocyanin Derivatives and specific mixtures of anthocyanins. The present invention also provides anthocyanin and/or anthocyanin derivative-based therapeutic compositions and methods that involve specific effects against A2E-mediated cellular damage. Methods are also provided which identify the anthocyanins and Anthocyanin Derivatives that can prevent or reduce A2E-mediated cellular damage, and the dose amount and formulations that provide such therapeutic effects.
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PHOTOLABILE COMPOUNDS (Fri, 22 Jul 2005)
The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect.
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Synthesis of derivatives of ginkgolide C (Fri, 03 Jun 2005)
The subject invention provides ginkgolide C derivatives compounds having the structure: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="38.61mm" wi="43.60mm" file="US07429670-20080930-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001-en" list-style="none"> <li>wherein R is H or -A-Ar, <ul id="ul0002-en" list-style="none"><li>where A is an alkyl group; and</li><li>Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6; <ul id="ul0003-en" list-style="none"><li>where R4 is an alkyl group; and</li><li>R5 and R6 are each, independently, hydrogen or a branched or unbranched alkyl group;</li></ul></li></ul></li> <li>wherein R1 is H or —COR7, <ul id="ul0004-en" list-style="none"><li>where R7 is alkyl, aryl or amino;</li></ul></li> <li>wherein R2 is present or absent, and when present is H, —COR8 or —CO—Z—R8; <ul id="ul0005-en" list-style="none"><li>where R8 is alkyl, aryl or amino; and</li><li>Z is oxygen;</li></ul></li> <li>wherein R3 is present or absent, and when present is —COR9; <ul id="ul0006-en" list-style="none"><li>where R9 is alkyl or aryl;</li></ul></li> <li>wherein only one of R2 or R3 is present in the compound;</li> <li>wherein only two of R, R1, R2 and R3 are H; and</li> <li>wherein each of a and b designates a single covalent bond which is present or absent, <ul id="ul0007-en" list-style="none"><li>where bond a is present when R3 is absent and bond b is present when R2 is absent; or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds. </li></ul></li> </ul> 
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SEPARATION OF GINKGOLIDES AND BILOBALIDE FROM G. BILOBA (Fri, 27 May 2005)
The subject invention provides a method for separating a terpene trilactone from Ginkgo biloba plant material or from an extract of Ginkgo biloba comprising a mixture of terpene trilactones, the process comprising the steps of: a) subjecting the Ginkgo biloba plant material or the extract to column chromatography with an appropriate solvent system to produce at least a first fraction containing the terpene trilactone bilobalide, a second fraction eluted after the first fraction containing the terpene trilactones GA and GB, and a third fraction eluted after the second fraction containing at least a preponderance of the terpene trilactones GC and GJ; and b) alkylating the terpene trilactone GB of the second fraction so as to produce a first mixture including terpene trilactone GA and alkylated terpene trilactone GB; or alkylating the terpene trilactone GC of the third fraction so as produce a second mixture including terpene trilactone GJ and alkylated terpene trilactone GC, so as to thereby isolate a terpene trilactone.
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HIGH RESOLUTION METABOLIC BRAIN (Fri, 20 May 2005)
This invention provides a method for determining whether a subject is afflicted with Alzheimer's disease by comparing the metabolic activity of the subject's hippocampal entorhinal cortex with that of a second region of the subject's brain. This invention further provides a method for determining whether a subject is afflicted with Alzheimer's disease by comparing the metabolic activity of the subject's hippocampal entorhinal cortex determined at a first and second time point. Finally, this invention provides a method for determining the amount of blood in a volume of cerebral tissue in vivo, wherein the volume of tissue is 1mm3 or less.
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Transgenic mice over-expressing amyloid-beta alcohol dehydrogenase (ABAD) in brain as model of alzheimer's disease and uses thereof (Wed, 11 May 2005)
The present invention provides for a transgenic non-human animal whose cells contain a recombinant DNA sequence comprising a nerve tissue specific promoter operatively linked to a DNA sequence which encodes amyloid-beta peptide alcohol dehydrogenase (ABAD), and exhibits at least one phenotype from the group consisting of: overexpression of ABAD, elevated levels of basal ATP; protection from metabolic or ischemic stress.
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COMPOSITIONS AND METHODS FOR TREATING HEART FAILURE (Fri, 29 Apr 2005)
The present invention provides compositions and methods for the following : preventing and treating heart failure; preventing heart failure in a patient with a pre-heart failure condition; treating and preventing heart failure with ischemic and non-ischemic causes;. treating and preventing heart failure in a subject status post myocardial infarction; reversing damage to the heart following myocardial infarction;by administering to a subject an effective amount of an adrenergic beta-agonist either alone or in combination with an effective amount of an adrenergic beta-1 antagonist. Figure 1 is a bar graph representing relative infarct sizes, as expressed as a percentage of left ventricular circumference.
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METALLORADICALS AS CHAIN TRANSFER CATALYSTS (Fri, 25 Mar 2005)
The present invention is directed to polymerization methods, comprising contacting a monomer with at least one mononuclear metal hydride, wherein the metal is selected from the group consisting of Cr, Mo, W, V, and Fe, or a combination thereof; provided that the metal hydride is not (ŋ5-C5Ph5)Cr(CO)3H. The invention is also directed to polymerization methods, comprising admixing a polymerization intermediate with a chain transfer catalyst, wherein the chain transfer catalyst comprises at least one mononuclear metalloradical, wherein the metal is selected from the group consisting of Cr, Mo, W, V, and Fe, or a combination thereof; provided that the chain transfer catalyst is not (ŋ5-C5Ph5)Cr(CO)3•, thereby forming a polymerization product.
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SYNTHESIS OF DERIVATIVES OF GINKGOLIDE C (Fri, 11 Mar 2005)
The subject invention provides ginkgolide C derivatives or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.
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Protein/solubility folding assessed by structural complementation (Fri, 28 Jan 2005)
Many proteins, when produced recombinantly, suffer from improper processing, folding and lack normal solubility. Modified proteins, including those indicative of disease states, also can have such defects. The present invention is directed to methods of identifying proper and improper protein folding, aberrant processing and/or insolubility. The method relies on the use of two components: a specialized fusion protein and structural complementation. The fusion protein contains sequences from the protein of interest and one portion of a marker protein that, by itself, is not active. A host cell then provides the remainder of the marker protein that serves to “complement” the function of the fused marker protein such that their association restores activity, permitting detection.
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EGR GENES AS TARGETS FOR THE DIAGNOSIS AND TREATMENT OF SCHIZOPHRENIA (Fri, 21 Jan 2005)
The present invention provides targets, methods, and reagents for the diagnosis and treatment of schizophrenia and related conditions. The invention provides methods for the diagnosis of schizophrenia and susceptibility to schizophrenia by detection of polymorphisms, mutations, variations, alterations in expression, etc., in genes encoding an EGR molecule or an EGR interacting molecule, or polymorphisms linked to such genes. The invention provides oligonucleotides, arrays, and antibodies for detection of polymorphisms and variants. The invention provides transgenic mice having alterations in such genes. The invention also provides methods of treating schizophrenia by administering compounds that target these genes. The invention further provides screening methods for identifying such compounds and compounds obtained by performing the screens.
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Carboxyltransferase domain of acetyl-CoA carboxylase (Fri, 14 Jan 2005)
The present invention provides compositions and crystals of the carboxyltransferase (CT) domain (the C-terminal ˜90 kDa fragment) of various acetyl-CoA carboxylase (ACC) proteins, including yeast, mouse and human ACCs. Further, the present invention provides methods for identifying and designing compounds that can modulate ACC activity. These methods are based, in part, on the X-ray crystallographic structures of the CT domain of yeast ACC, either alone or bound to acetyl-CoA or a CT inhibitor, such as haloxyfop or diclofop or CP-640186. Thus, the present invention relates to the crystal structures of the carboxyltransferase (“CT”) domain of acetyl-CoA carboxylase (“ACC”), and to the use of these structures in the design of anti-obesity compounds, anti-diabetes compounds, antibiotic compounds, herbicide compounds, and in the design of herbicide resistant plants.
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COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING HEART TISSUE DEGENERATION, AND USES THEREOF (Fri, 07 Jan 2005)
The present invention provides methods for promoting generation of heart tissue, and for treating and preventing heurt tissue degeneration. Additionally, the present invention provides a therapeutic composition comprising a cyclin-associated agent, and a kit comprising the composition. The present invention further provides a heart tissue tell, a sidepopulation progenitor tell, and a stem tell in which cyclin is augmented. Also provided are tell lins comprising these tells, screening methods using the tell lins, and drugs identified by these methods. The present invention further provides in vitro systems for use in screening candidate drugs for at least one cardiotoxic effect and/or for synergy with cyclin in the treatment and prevention of heart tissue degeneration. Finally, the present invention provides use of a cyclin-associated agent in the generation of heart tissue, and use of a cyclin associated agent in the treatment or prevention of heart tissue degeneration.
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Hydroxamic acid compounds and methods of use thereof (Fri, 31 Dec 2004)
The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
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COVALENT METHODS FOR IMMOBILIZATION OF THIOLATED BIOMOLECULES ON SILICEOUS AND METALLIC SURFACES (Thu, 30 Dec 2004)
The present invention is directed to methods for immobilizing molecules on siliceous and metallic surfaces. Molecules are immobilized on siliceous or metallic surfaces by stable covalent linkages that are capable of withstanding prolonged use and elevated temperatures. Further, the methods of the present invention describe less-complicated chemistries for the immobilization of molecules that will benefit the reproducibility, efficiency and effectiveness of applications in sensing, chromatography, medical diagnostics and related areas where specific recognition between immobilized and free molecules provides diagnostic information or serves as part of a purification or separations process.
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HYDROXAMIC ACID COMPOUNDS AND METHODS OF USE THEREOF (Fri, 22 Oct 2004)
The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
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Synthetic receptors (Wed, 29 Sep 2004)
The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain, cyclic or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In a preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier. In addition, the invention includes methods of preparing synthetic receptors and synthetic receptor libraries. The synthetic library may be linked with identifiers such that the library comprises a plurality of different synthetic receptor members. The invention also provides methods for assaying a synthetic receptor library to determine suitable synthetic receptor(s) which (a) bind an acceptor molecule; (b) exhibit biological activity; (c) which catalyze a reaction or inhibit a catalyzed reaction; and (d) separate compounds in chromatography.
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Method of re-sensitizing vancomycin resistant bacteria which selectively cleave a cell wall depsipeptide (Fri, 17 Sep 2004)
The present invention relates to pyrrolidine compounds of the general structure: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="19.39mm" wi="28.28mm" file="US06953861-20051011-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> where n is an integer 1-6 and R is hydrogen or a C1 to C6 straight chain or branched alkyl group, and wherein when n=1, R=CH3 or H, useful for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond on the cell wall peptide precursors of the bacteria. 
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STRUCTURAL MODELS OF CARNITINE ACYLTRANSFERASES AND USES THEREOF (Fri, 30 Jul 2004)
The present invention relates to structural models of carnitine acyltransferases, and, in particular, to models of the reactive sites of these enzymes. It is based, at least in part, on the X-ray crystallographic structures of murine carnitine acetyltransferase ('mCRAT'), both in pure form and in complex with its substrates carnitine and coenzyme A ('CoA'). The structural information provides a basis for designing modulators of the activity of CRAT and related enzymes.
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METHODS OF USING CRYSTAL STRUCTURE OF CARBOXYLTRANSFERASE DOMAIN OF ACETYL-COA CARBOXYLASE, MODULATORS THEREOF, AND COMPUTER METHODS (Fri, 30 Jul 2004)
The present invention provides compositions and crystals of the carboxyltransferase (CT) domain (the C-terminal ~90 kDa fragment) of various acetyl-CoA carboxylase (ACC) proteins, including yeast, mouse and human ACCs. Further, the present invention provides methods for identifying and designing compounds that can modulate ACC activity. These methods are based, in part, on the X-ray crystallographic structures of the CT domain of yeast ACC, either alone or bound to acetyl-CoA or a CT inhibitor, such as haloxyfop or diclofop or CP-640186. Thus, the present invention relates to the crystal structures of the carboxyltransferase ('CT') domain of acetyl-CoA carboxylase ('ACC'), and to the use of these structures in the design of anti-obesity compounds, anti-diabetes compounds, antibiotic compounds, herbicide compounds, and in the design of herbicide resistant plants.
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METHOD OF PREPARATION OF BIOMAGNETIC NANOPARTICLES COATED WITH A NOBLE METAL LAYER (Fri, 23 Jul 2004)
A method for the preparation of magnetic nanoparticles coated with a noble metal is described. The method includes providing a first mixture containing a first non-polar organic solvent and uncoated magnetic nanoparticles (103). The first mixture is mixed with a second mixture containing a second non-polar organic solvent and ions comprising the noble metal to form a third mixture. The third mixture is mixed with an organic ligand or a fourth mixture containing an organic ligand to form a fifth mixture. The fifth mixture is reacted with a sixth mixture containing a reducing agent to form a seventh mixture containing the monodispersed magnetic nanoparticles coated with the noble metal. The monodispersed magnetic coated nanoparticles may be separated from the seventh mixture by adding a polar organic solvent or a mixture of polar organic solvents in which the nanoparticles are insoluble.
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Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof (Fri, 02 Jul 2004)
Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="39.20mm" wi="52.41mm" file="US06936714-20050830-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry><ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group;</li><li>wherein R2 is an ether, ester, amide, or a phthalimide group;</li><li>wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group;</li><li>wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.</li></ul></li></ul>
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BIOMOLECULAR COUPLING METHODS USING 1,3-DIPOLAR CYCLOADDITION CHEMISTRY (Fri, 02 Jul 2004)
This invention provides methods for covalently affixing a biomolecule to either a second molecule or a solid surface using 1,3-dipolar cycloaddition chemistry. This invention also provides related methods and compositions.
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PEPTIDES AND METHODS FOR DEACTIVATION OF ORGANOPHOSPHORUS-BASED NERVE AGENTS AND INSECTICIDES (Fri, 25 Jun 2004)
This invention provides methods and peptides for the inactivation of organophosphorus-based insecticides and chemical warfare agents. The instant methods include peptide screening methods, peptides and peptide libraries, related compositions of matter, articles of manufacture, and methods for prophylaxis, treatment, decontamination and detection.
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BACTERIAL SMALL-MOLECULE THREE-HYBRID SYSTEM (Sat, 22 May 2004)
A transgenic bacterial cell comprising (a) a dimeric small molecule which comprises a first moiety known to bind a first receptor domain covalently linked to a second moiety known to bind a second receptor domain; (b) nucleotide sequences which upon transcription encode i) a first fusion protein comprising the first receptor domain, and ii) a second fusion protein comprising the second receptor domain; and (c) a reporter gene wherein expression of the reporter gene is conditioned on the proximity of the first fusion protein to the second fusion protein. The cell is also adapted for use in a method for identifying a molecule that binds to a known target in a bacterial cell from a pool of candidate molecules, and a method for identifying an unknown target receptor to which a molecule is capable of binding in a bacterial cell. Also described are compounds and kits for carrying out the methods.
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Method for isolating terpene trilactones (ginkgolides, bilobalide) from leaves and pharmaceutical powders of Ginkgo biloba (Fri, 23 Apr 2004)
A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
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A COMPUTATIONAL METHOD FOR PREDICTING INTRAMOLECULAR AND INTERMOLECULAR BIOPOLYMER INTERACTIONS (Fri, 02 Apr 2004)
Disclosed is a computational method for predicting intramolecular and intermolecular biopolymer interactions which provides an improved way of determining structure and function information, including intramolecular and intermolecular interactions using an ab initio-type approach, i.e. using only sequence information. The method is a widely applicable sequence-mining tool capable of detecting both intramolecular and intermolecular interactions for all biopolymers, including, but not limited to, DNA, RNA and protein. It possesses an adaptive screening process that allows for high accuracy. It can be an entirely rule-free, unbiased methodology, and thus can detect novel interactions for all biopolymers. Due to the incorporation of a misalignment process, it can be used iteratively and is capable of refining its own predictions and detecting and managing errors. Therefore, the disclosed method also provides a technique for more accurately determining (and refining) sequence alignments.
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METHOD OF RECORDING A REACTION HISTORY OF A SOLID SUPPORT (Mon, 09 Feb 2004)

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Sodium magnetic reasonance imaging used in diagnosing tumors and assessing response to treatment (Wed, 21 Jan 2004)
The present invention provides a method for measuring the magnetic resonance signal of an intracellular population of predetermined nuclei in a cell-containing sample by: a) applying to the sample a first radio frequency pulse, in a magnetic field, b) after a set time interval (TI), applying to the sample a second radio frequency pulse sufficient to cause a measurable signal, and c) measuring the measurable signal for the sample so produced, which method is utilized in methods of (i) determining the effectiveness of chemotherapy, (ii) detecting and characterizing tumors, and (iii) determining cell death in a cell-containing sample.
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Total synthesis of merrilactone A (Fri, 09 Jan 2004)
This invention provides a total synthesis of Merrillactone and Merrilactone analogues for use as neurotrophic agents in the treatment of neurodegenerative diseases. The invention also provides intermediates for use in the synthesis of Merrilactone and its analogues.
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Protein/solubility folding assessed by structural complementation (Fri, 02 Jan 2004)
Many proteins, when produced recombinantly, suffer from improper processing, folding and lack normal solubility. Modified proteins, including those indicative of disease states, also can have such defects. The present invention is directed to methods of identifying proper and improper protein folding, aberrant processing and/or insolubility. The method relies on the use of two components: a specialized fusion protein and structural complementation. The fusion protein contains sequences from the protein of interest and one portion of a marker protein that, by itself, is not active. A host cell then provides the remainder of the marker protein that serves to “complement” the function of the fused marker protein such that their association restores activity, permitting detection.
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Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof (Fri, 02 Jan 2004)
The present invention provides the compound having the formula: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="19.47mm" wi="42.42mm" file="US07126001-20061024-C00001.TIF" alt="embedded image" img-content="photograph" img-format="png"/> </chemistry> wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above. 
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α,φ-ALLYL TERMINATED LINEAR POLY(METHACRYLIC ACID) MACROMONOMERS FOR END-LINKED HYDROGELS AND METHOD OF PREPARATION (Fri, 12 Dec 2003)
Disclosed is a method for making α,φ-allyl terminated macromonomers comprising a plurality of units of an α,β-unsaturated carboxylic acid. The method comprises forming a first mixture containing an ester of an α,β-unsaturated carboxylic acid, a radical initiator comprising an allyl group and a halogen, and a catalyst comprising a transition metal complex. The ester of the α,β-unsaturated carboxylic acid is an ester capable of reacting with a mixture comprising trifluoroacetic acid (TFA) to form the α,β-unsaturated carboxylic acid. The mixture is stirred to form a second mixture containing an α-allyl,φ-halogen-terminated macromonomer comprising a plurality of units of the ester of the α,β-unsaturated carboxylic acid. A third mixture comprising a compound containing at least one transferable allyl group is then added to the second mixture to form a fourth mixture containing a first α,φ-allyl terminated macromonomer comprising a plurality of units of the ester of the α,β-unsaturated carboxylic acid. The first α,φ-allyl terminated macromonomer is separated from the fourth mixture and is mixed with a mixture containing TFA to form a fifth mixture containing the α,φ-allyl terminated macromonomer comprising a plurality of units of the α,β-unsaturated carboxylic acid. The α,φ-allyl terminated macromonomer comprising a plurality of units of the α,β-unsaturated carboxylic acid is then separated from the fifth mixture. Also enclosed is a related method for making end-linked hydrogels comprising a plurality of units of an α,β-unsaturated carboxylic acid. The method comprises forming a first mixture containing an α,φ-allyl terminated macromonomer comprising a plurality of units of the α,β-unsaturated carboxylic acid and a radical initiator. The first mixture is treated with UV-radiation, visible light, or heat to form a second mixture comprising an end-linked hydrogel comprising a plurality of units of the α,β-unsaturated carboxylic acid.
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Analogs of terpene trilactones from Ginkgo biloba and related compounds and uses thereof (Fri, 05 Dec 2003)
The subject invention provides compounds having the structure: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="71.29mm" wi="41.49mm" file="US07145021-20061205-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1–C10) alkyl, (C1–C10) alkenyl, (C1–C10) alkynyl, -A-Ar, -A-Z-Ar, —SO2—Ar, or -A-NR5, or —R7, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject. 
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CARBON-11 AND FLUORINE-18 LABELED RADIOLIGANDS FOR POSITRON EMISSION TOMOGRAPHY (PET) IMAGING FOR THE BRAIN SEROTONIN TRANSPORTERS (Fri, 28 Nov 2003)
This invention provides a compound having the structure: (I) This invention also provides for related compounds and pharmaceutical compositions. This invention further provides for a compound that can be used for non-invasive method for positron emission tomography (PET) imaging of serotonin transporter sites in mammals comprising labeling serotonin transporter sites (SERT) with an image-generating amount of the radiolabeled compound disclosed herein and measuring spatial distribution of the compound in the mammal by PET so as to thereby image the serotonin transporter sites.
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SYSTEM AND METHOD FOR MRI TAGGING USING SPATIAL MODULATION OF MAGNETIZATION (Fri, 14 Nov 2003)
A method of inducing tag lines in an MRI image is provided which allows adjustment of tag line width and spacing. The method includes determining a desired tag line width (505) and then selecting a parameter of a SINC modulating function, such as main lobe bandwidth, in accordance with the desired tag line width. The method also includes determining a desired tag line separation (51) and selecting a parameter of an ARF pulse train based upon the desired tag line separation. A gradiant field is applied to the specimen being imaged. The RF pulse train is modulated in accordance with the SINC modulating function (520) and the modulated RF pulse train is applied to the specimen being imaged prior to an image acquisition operation. In one embodiment of the invention, the gradiant is activated between pulses of the RF pulses.
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System and method for MRI tagging using spatial modulation of magnetization (Fri, 07 Nov 2003)
A method of inducing tag lines in an MRI image is provided which allows adjustment of tag line width and spacing. The method includes determining a desired tag line width and then selecting a parameter of a SINC modulating function, such as main lobe bandwidth, in accordance with the desired tag line width. The method also includes determining a desired tag line separation and selecting a parameter of an RF pulse train based upon the desired tag line separation. A gradient field is applied to the specimen being imaged. The RF pulse train is modulated in accordance with the SINC modulating function and the modulated RF pulse train is applied to the specimen being imaged prior to an image acquisition operation. In one embodiment of the invention, the gradient is activated between pulses of the RF pulse train and is deactivated during the RF pulses.
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Bacterial small-molecule three-hybrid system (Fri, 31 Oct 2003)
A transgenic bacterial cell comprising <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>(a) a dimeric small molecule which comprises a first moiety known to bind a first receptor domain covalently linked to a second moiety known to bind a second receptor domain;</li><li>(b) nucleotide sequences which upon transcription encode <ul id="ul0003-en" list-style="none"><li>i) a first fusion protein comprising the first receptor domain, and</li><li>ii) a second fusion protein comprising the second receptor domain; and</li></ul></li><li>(c) a reporter gene wherein expression of the reporter gene is conditioned on the proximity of the first fusion protein to the second fusion protein. The cell is also adapted for use in a method for identifying a molecule that binds to a known target in a bacterial cell from a pool of candidate molecules, and a method for identifying an unknown target receptor to which a molecule is capable of binding in a bacterial cell. Also described are compounds and kits for carrying out the methods.</li></ul></li></ul>
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Analogs of terpene trilactones from Ginkgo biloba for bioorganic and imaging studies (Fri, 17 Oct 2003)
A compound having the structure:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06693091-20040217-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein R1is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3is H or OH; wherein R4is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.
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ANALOGS OF TERPENE TRILACTONES FROM GINKGO BILOBA AND RELATED COMPOUNDS AND USES THEREOF (Fri, 10 Oct 2003)
The subject invention provides compounds having the structure Formula (I): wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1-C5) alkyl group, (C2-C5) alkenyl, or a (C2-C5) alkynyl, (C1-C5) alkoxy, (C2-C5) alkenyloxy, or (C2-C5) alkynyloxy, -N3, -COR5, -CONR5R6, -CO2R5, -OCOR5, -NH(OH), -NR5R6, -NHCOR5, .N(OH)COR5, -CH2OR5, -OCH2CO2R5, -CH2SR5, -CH2NR5R6, -SR5, -OSR5, or -NR5SO2R6, where R5 and R6 are each independently hydrogen substituted or unsubstituted (C1-C5) alkyl, (C2-C5) alkenyl, or (C2-C5) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1-C10) alkyl, (C1-C10) alkenyl, (C1-C10) alkynyl, -A-Ar, -A-Z-Ar, -SO2-Ar, or -A-NR5, or -R7, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject.
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METHOD OF PREPARING A PROTEIN ARRAY BASED ON BIOCHEMICAL PROTEIN-PROTEIN INTERACTION (Fri, 19 Sep 2003)
A method of preparing a protein array based on biochemical protein-protein interaction is provided. An array of a first protein which includes a PDZ domain is deposited on a substrate. A second protein, which includes an amino acid sequence (S/T)-X-(V/I/L)-COOH (each hyphen represents a peptide bond, each parenthesis encloses amino acids which are alternatives to one other, each slash within such parentheses separates the alternative amino acids, and the X represents any amino acid which is selected from the group comprising the twenty naturally occurring amino acids), is applied to the first protein array. The amino acid sequence (S/T)-X-(V/I/L)-COOH of the second protein is bound to the PDZ domain of the first protein.
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REAGENTS FOR ASYMMETRIC ALLYLATION, ALDOL, AND TANDEM ALDOL AND ALLYLATION REACTIONS (Sat, 13 Sep 2003)
A new class of reagents and method of use of the reagents in the reaction of the reagents with electrophilic compounds. The invention in one embodiment is directed to a method for the formation of an alcohol of the formula (I). The method includes reacting a reagent of the formula (II). with an aldehyde of the formula R10CHO to form the alcohol. X3 is one of O and C(R4)(R5). Each of X1 and X2 is independently O or N-R. Each of Ca and Cb is independently an achiral center, an (S) chiral center or an (R) chiral center. Ra and Rb are (i) each independently C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl, or (ii) taken together to form a C3-C4 alkylene chain which together with Ca and Cb forms a 5-membered or 6-membered aliphatic ring. Rc and Rd are each independently hydrogen, C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl. R is C1-10 alkyl, C6-10 aryl or C3-9 heteroaryl. Each of R1, R2, R3, R4, R5 is independently hydrogen, C1-C10 alkyl, C6-10 aryl, C3-9 heteroaryl, C1-10 alkoxy, C6-10 aryloxy, C1-10 dialkylamino, C1-10 alkyl-C6-10 arylamino, C1-10 diarylamino, or halogen. R6 is halogen, hydrogen, C1-10 alkyl, C6-10 aryl, C3-9 heteroaryl, C1-10 alkoxy, C6-10 aryloxy, C1-10 alkyl-C6-10 arylamino, C1-10 diarylamino, OSO2CF3 or SR. R10 may be C1-10 alkyl, C6-10 aryl, or C3-9 heteroaryl.
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AN IN VIVO PROTEIN SCREEN BASED ON ENZYME-ASSISTED CHEMICALLY INDUCED DIMERIZATION ('CID') (Fri, 25 Jul 2003)
A method for identifying which protein from a pool of candidate proteins catalyzes in a cell a bond forming reaction between a first substrate and a second substrate, comprising: (a) providing a dimeric small molecule which comprises a known moiety' that binds a known receptor domain covalently linked with a moiety that contains the first substrate; (b) introducing the dimeric molecule into a cell which comprises i) a first fusion protein comprising the known receptor domain, ii) a second fusion protein comprising the second substrate, iii) a protein from the pool of candidate proteins, and iv) a reporter gene wherein expression of the reporter gene is conditioned on the proximity of the first fusion protein to the second fusion protein; (c) permitting the dimeric molecule to bind to the first fusion protein and to enzymatically form a bond with the second fusion protein so as to activate the expression of the reporter gene; (d) selecting which cell expresses the reporter gene; and (e) identifying the protein that catalyzes the bond formation reaction in the cell between the first substrate and the second substrate. The method is also adapted to identify which substrate from a pool of candidate substrates is selected in a cell by a known enzyme for a bond forming reaction between the substrate and a known amino acid. Also, cells, compounds and kits for carrying out the methods.
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Antibodies specific for fullerenes (Wed, 16 Jul 2003)
This invention provides a hybridoma produced by the fusion of a mouse antibody-producing cell and a mouse myeloma which is designated 1-10F-8A and deposited with the ATCC under Accession Number PTA-279, said hybridoma producing a monoclonal antibody which binds to fullerene C60. This invention provides a mouse monoclonal antibody specific for a fullerene-C60 and produced by the mouse monoclonal antibody-producing hybridoma designated 1-10F-8A. The invention provides the amino acid and encoding nucleic acid sequences of the heavy and light chains of the 1-10F-8A monoclonal antibody. This invention also provides methods of determining a serum concentration of a fullerene in a subject and of purifying a fullerene from a sample.
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Method for re-sensitizing vancomycin resistant bacteria which selectively cleave a cell wall depsipeptide (Fri, 04 Jul 2003)
The present invention relates a method for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond in the cell wall peptide precursors of the bacteria which comprises using an antibacterial amount of vancomycin or a homolog of vancomycin and an amount of an agent effective to selectively cleave the ester bond so as to thereby re-sensitize vancomycin resistant bacteria.
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Complex combinatorial chemical libraries encoded with tags (Fri, 27 Jun 2003)
Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detachable from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
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THE TOTAL SYNTHESIS OF MERRILACTONE A (Fri, 27 Jun 2003)
This invention provides a total synthesis of Merrillactone and Merrilactone analogues having the structure formula (I), wherein Z is 0 or >N-X, where X is H, straight or branched substituted or unsubstituted alkyl, alkenyl or alkynyl, or acyl, carbamoyl, cycloalkyl, aryl, heterocycloalkyl, heteroaryl, aralkyl, amino, alkyl amino, or dialkyl amino; and all the R’s groups are described in the specification.
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BETA-CYCLODEXTRIN DIMERS AND PHTHALOCYANINES AND USES THEREOF (Fri, 27 Jun 2003)
The invention provides β-cyclodextrin dimers and phthalocyanines which can be used in photodynamic therapy of cancer.
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Synthetic receptors, libraries and uses thereof (Fri, 06 Jun 2003)
Libraries of synthetic receptors are disclosed. The receptors include a polyfunctional organic template which is covalently linked to two or more oligomers. The oligomers may be the same or different and may be straight chain, cyclic or branched. The template may be linked to an identifier which is unique to each synthetic receptor. Although the identifier may be directly attached to the template, it is more common and preferable that the template be covalently linked to a solid support which is itself linked to the identifier. Methods of preparing synthetic receptors and libraries of synthetic receptors are also disclosed as are methods for assaying the libraries to determine which receptors have various desirable characteristics. Among the desirable characteristics are (a) the ability to bind an acceptor molecule; (b) biological activity; (c) the ability to catalyze or inhibit a reaction and (d) potential utility for separating compounds in chromatography.
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Catalytic antibodies against cocaine and methods of using and producing same (Wed, 21 May 2003)
This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further provides pharmaceutical composition for decreasing cocaine concentration in a subject using the antibodies produced.
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Anti-cocaine catalytic antibody (Fri, 25 Apr 2003)
Disclosed are catalytic antibodies and polypeptides capable of degrading cocaine. Said catalytic antibodies and polypeptides are characterized by the amino acid sequence of their complementary determining regions and framework regions. The present invention also discloses a pharmaceutical composition and a method for decreasing the concentration and a method for decreasing the concentration of cocaine of a subject. Finally, the invention discloses pharmaceutical compositions and methods for treating cocaine overdose and addiction in subjects.
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Method for isolating terpene trilactones (ginkgolides, bilobalide) from leaves and pharmaceutical powders of ginkgo biloba (Fri, 14 Feb 2003)
A method of isolating terpene trilactones fromGinkgo bilobaplant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
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Process for pan-genomic determination of macromolecular atomic structures (Fri, 31 Jan 2003)
A process for determination of three-dimensional macromolecular atomic structures of proteins is provided. A plurality of gene products are clustered into at least one family of homologous sequences. At least one protein encoded by a sequence selected from each of the families is prepared, purified and characterized. The purified proteins are crystallized in parallel against crystallization screens. Diffraction data produced by the crystallized proteins is measured using a multi-wavelength anomalous diffraction method. The diffraction data is analyzed by using a multi-wavelength anomalous diffraction phasing method, an atomic model is built, and the model is refined based on the diffraction data to determine a three-dimensional macromolecular atomic structure for each of the crystallized proteins. 
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ANTIBODIES SPECIFIC FOR NANOTUBES AND RELATED METHODS AND COMPOSITIONS (Fri, 31 Jan 2003)
This invention provides two compositions. The first composition comprises a nanotube and at least one anti-nanotube antibody, wherein the anti-nanotube antibody is bound to the nanotube. The second composition comprises a fullerene and at least one anti-fullerene antibody, wherein the anti-fullerene antibody is bound to the fullerene. Finally, this invention provides methods and kits relating to the antibody and compositions of matter.
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Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof (Wed, 29 Jan 2003)
The present invention provides the compound having the formula:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06511990-20030128-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein each of R1and R2is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
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Oligonucleotide inhibitors of bcl-xL (Fri, 24 Jan 2003)
This invention provides an antisense oligonucleotide or analog thereof comprising 10 or more contiguous bases or base analogs from the sequence of bases of sequence A, B, C, D, E, F, G, H, I, J, K, L, or M of FIG. 1. This invention also provides the above-described antisense oligonucleotides, wherein the nucleotide sequence comprises nucleotide sequence A, A′, B, C, C′, D, E, E, E′, F, G, G′, H, H′, I, I′, J, K, K′, L, L′, M, or M′ of FIGS. 2A and 2B. This invention also provides the above-described antisense oligonucleotides, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention also provides the above-described antisense oligonucleotides, wherein the phosphate backbone comprises phosphorothioate bonds. In addition, this invention provides a method of treating cancer, comprising introducing into a tumor cell an effective amount of the the above-described antisense oligonucleotide, thereby reducing the levels of bcl-xL protein produced and treating cancer. This invention also provides the above-described methods, wherein the introducing comprises using porphyrin or lipofectin as a delivery agent. This invention also provides the above-described pharmaceutical compositions, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention further provides the above-described pharmaceutical compositions, wherein the pharmaceutical composition comprises tetra meso-(4-methylpyridyl)porphine or tetra meso-(anilinium)porphine or a combination thereof.
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METHOD FOR ISOLATING TERPENE TRILACTONES (GINKGOLIDES, BILOBALIDE) FROM LEAVES AND PHARMACEUTICAL POWDERS OF GINKGO BILOBA (Fri, 24 Jan 2003)
A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
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Complex combinatorial chemical libraries encoded with tags (Wed, 08 Jan 2003)
Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
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Synthesis of dysidiolide and uses thereof (Wed, 20 Nov 2002)
This invention provides a process for the preparation of a racemic mixture of dysidiolide a method for inhibiting growth of cancerous cells comprising contracting an amount of the racemic mixture of dysidiolide effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the racemic mixture of dysidiolide.
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Oligonucleotide inhibitors of bcl-xL (Fri, 26 Jul 2002)
This invention provides an antisense oligonucleotide or analog thereof comprising 10 or more contiguous bases or base analogs from the sequence of bases of sequence A, B, C, D, E, F, G, H, I, J, K, L, or M of FIG. 1. This invention also provides the above-described antisense oligonucleotides, wherein the nucleotide sequence comprises nucleotide sequence A, A′, B, C, C′, D, E, E′, F, G, G′, H, H′, I, I′, J, K, K′, L, L′, M, or M′ of FIGS. 2A and 2B. This invention also provides the above-described antisense oligonucleotides, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention also provides the above-described antisense oligonucleotides, wherein the phosphate backbone comprises phosphorothioate bonds. In addition, this invention provides a method of treating cancer, comprising introducing into a tumor cell an effective amount of the the above-described antisense oligonucleotide, thereby reducing the levels of bcl-xL protein produced and treating cancer. This invention also provides the above-described methods, wherein the introducing comprises using porphyrin or lipofectin as a delivery agent. This invention also provides the above-described pharmaceutical compositions, wherein the oligonucleotide is encapsulated in a liposome or nanoparticle. This invention further provides the above-described pharmaceutical compositions, wherein the pharmaceutical composition comprises tetra meso-(4-methylpyridyl)porphine or tetra meso-(anilinium)porphine or a combination thereof. 
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Intermediates for the synthesis of vitamin D and steroid derivatives and process for preparation thereof (Wed, 05 Jun 2002)
A process for preparing a compound having structure (I) wherein n is an integer from 1-5; each of R1and R2independently is optionally substituted C1-C6alkyl; each of W and X is independently hydrogen or C1-C6alkyl; Y is O, S or NR3where R3is hydrogen, C1-C6alkyl or a protective group; and Z is a CD ring structure, a steroid structure, or a vitamin D structure, each of which optionally having structure (IV) wherein W, X, Y and Z are defined above, in the presence of a base, with a compound having structure (V) or (v′) wherein n, R1and R2are as defined above, and E is an eliminating group.
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Method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal circulation (Wed, 22 May 2002)
This invention provides a method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal blood circulation which comprises contacting the extracorporeal circulating blood with a Factor IXa compound in an amount effective to inhibit thrombosis in the blood of a patient and under conditions such that the Factor IXa compound circulates in the patient. The Factor IXa compound may include an active site-blocked Factor IXa compound or Glu-Gly-Arg chloromethyl ketone-inactivated human factor IXa compound. This invention also provides that the effective amount may be from about 0.1 μg/ml plasma to about 250 μg/ml plasma or from about 0.5 μg/ml plasma to about 25 μg/ml plasma. The patient may be subjected to extracorporeal blood circulation during transplant surgery or cardiopulmonary bypass surgery. This invention further provides for a method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal blood circulation, which comprises contacting the extracorporeal circulating blood with an agent capable of inhibiting a step of the intrinsic pathway of coagulation in an amount effective to inhibit thrombosis in the blood of a patient and under conditions such that the Factor IXa compound circulates in the patient. The agent may be an active site-blocked Factor XII compound or an active site-blocked Factor XI compound.
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Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof (Fri, 01 Mar 2002)
Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06686470-20040203-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein R1and R4is H, a C1to C4alkyl group, or an acyl group; wherein R2is an ether, ester, amide, or a phthalimide group; wherein R3is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8and R9are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8and R9are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10and R11are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12is H, a C1to C4alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
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Helical discotic switch (Wed, 06 Feb 2002)
The present invention provides liquid crystal having a spiral coil structure and a dipole moment along its axis and a helical discotic switch using the same, wherein the helicene compound has the structure:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06344153-20020205-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein X is O, or S and Y is —O—C(═O)CH2—O—R5, wherein R5is H, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, wherein R1, R2, R3and R4are independently the same or different and are substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.
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Hydrophilic carrier for photosensitizers that cleaves when they catalyze the formation of singlet oxygen (Wed, 19 Dec 2001)
The invention provides a composition of matter comprising two β-cyclodextrin molecules and a cleavable linker attached to and joining each such β-cyclodextrin. This invention further provides a composition which comprises a hydrophilic matrix comprising the above-described composition of matter and a photosensitizer encapsulated within the matrix, wherein the cleavable linker is cleaved upon exposure to light of a wavelength appropriate for the light to be absorbed by the photosensltlzer. This invention also provides a method of killing a tumor cell which comprises bringing into proximity with the tumor cell the above-described composition and exposing the composition to light so as to cleave the cleavable linker and release the photosensitizer.
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Anti-cocaine catalytic antibody (Wed, 29 Aug 2001)
This invention provides a polypeptide comprising a light chain domain which comprises a complementarity determining region 1 having the amino acid sequence RSSXGTITXXNYAN (Seq ID No: 73), a complementarity determining region 2 having the amino acid sequence XNNYRPP (Seq ID No: 74) and a complementarity determining region 3 having the amino acid sequence ALWYSNHWV (Seq ID No: 75), interposed between appropriate framework regions, and linked to said light chain domain a heavy chain domain which comprises a complementarity determining region 1 having the amino acid sequence DYNMY (Seq ID No: 76), a complementarity determining region 2 having the amino acid sequence YIDPXNGXIFYNQKFXG (Seq ID No: 77) and a complementarity determining region 3 having the amino acid sequence GGGLFAX (Seq ID No: 78) interposed between appropriate framework regions, said polypeptide having a conformation suitable for degrading cocaine.
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COMPLEMENTATION ASSAY ASSESSING PROTEIN SOLUBILITY AND FOLDING (Fri, 24 Aug 2001)
Many proteins, when produced recombinantly, suffer from improper processing, folding and lack normal solubility. Modified proteins, including those indicative of disease states, also can have such defects. The present invention is directed to methods of identifying proper and improper protein folding, aberrant processing and/or insolubility. The method relies on the use of two components: a specialized fusion protein and structural complementation. The fusion protein contains sequences from the protein of interest and one portion of a marker protein that, by itself, is not active. A host cell then provides the remainder of the marker protein that serves to 'complement' the function of the fused marker protein such that their association restores activity, permitting detection.
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Intermediates for the synthesis of debromohymenialdisine and process thereof (Fri, 10 Aug 2001)
The synthesis of C11N5marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]lazepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.
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ASSAYS FOR EVALUATING THE FUNCTION OF RNA HELICASES (Fri, 03 Aug 2001)
The present invention provides a method for detecting the release of a single-stranded RNA from an RNA duplex which comprises admixing an RNA helicase with the RNA duplex under conditions permitting the RNA helicase to unwind the RNA duplex and release single-stranded RNA, wherein the RNA duplex comprises a first RNA having a first label attached thereto and a second RNA, such first label being capable of producing a luminescent energy pattern when the first RNA is present in the RNA duplex which differs from the luminescent energy pattern produced when the first RNA is not present in the RNA duplex, subjecting the admixture to conditions which permit (i) the RNA helicase to unwind the RNA duplex and release single-stranded RNA, and (ii) the first label to produce luminescent energy, and detecting a change in the luminescent energy pattern produced by the first label so as to thereby detect release of single-stranded RNA from the RNA duplex.
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COMPOUNDS OF THE SAFRAMYCIN-ECTEINASCIDIN SERIES, USES, AND SYNTHESIS THEREOF (Fri, 27 Jul 2001)
Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the general formula (1), their uses and synthesis, are disclosed. In said formula, R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; R2 is an ether, ester, amide, or a phthalimide group; R3 is =O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; R6 is =O, OH, OCH3, CN, or an acyfoxy group; wherein R7 is =0, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3 OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; R12 is H, a C1 to C4 alkyl group, or an acyl group; and the chiral center marked * has the R or the S configuration.
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Bicyclic aminoimidazoles (Wed, 18 Apr 2001)
The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds.
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NOVEL CLASS OF CYTODIFFERENTIATING AGENTS AND HISTONE DEACETYLASE INHIBITORS, AND METHODS OF USE THEREOF (Fri, 16 Mar 2001)
The present invention provides the compound having formula (I), wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, -O-, -S-, -NH-, or -CH2-; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
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ANTIBODIES SPECIFIC FOR FULLERENES (Fri, 09 Mar 2001)
This invention provides antibodies specific for a fullerene or derivative thereof, a single-walled fullerene nanotube, and a multi-walled fullerene nanotube, wherein the fullerene is selected from the group consisting of a fullerene carbon compound having from 20 to 540 carbon atoms. The antibodies may be monoclonal or polyclonal antibodies. This invention provides a hybridoma produced by the fusion of a mouse antibody-producing cell and a mouse myeloma which is designated 1-10F-8A and deposited with the ATCC under Accession Number PTA-279, said hybridoma producing a monoclonal antibody which binds to fullerene C60. This invention provides a mouse monoclonal antibody specific for a fullerene-C60 and produced by the mouse monoclonal antibody-producing hybridoma designated 1-10F-8A. This invention also provides methods of determining a serum concentration of a fullerene in a subject and of purifying a fullerene from a sample. This invention provides methods of preparing nonascale devices which comprise manipulating a single-walled or a multi-walled fullerene nanotube(s) with the above-described antibodies specific for single-walled or multi-walled fullerene nanotubes to assemble electronic or chemical components of the nanoscale device.
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A HELICAL DISCOTIC SWITCH (Fri, 09 Mar 2001)
The present invention provides liquid crystal having a spiral coil structure and a dipole moment along its axis and a helical discotic switch using the same, wherein the helicene compound has structure (I) wherein X is O, or S and Y is -O-C(=O)CH2-O-R5, wherein R5 is H, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, wherein R1, R2, R3 and R4 are independently the same or different and are substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.
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Intermediates for the synthesis of debromohymenialdisine and processes thereof (Wed, 07 Mar 2001)
The synthesis of C11N5marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]azepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in3and4,which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.
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METHODS OF INHIBITING BINDING OF β-SHEET FIBRIL TO RAGE AND CONSEQUENCES THEREOF (Fri, 23 Feb 2001)
This invention provides a method of inhibiting the binding of a β-sheet fibril to RAGE on the surface of a cell which comprises contacting the cell with a binding inhibiting amount of a compound capable of inhibiting binding of the β-sheet fibril to RAGE so as to thereby inhibit binding of the β-sheet fibril to RAGE. In one embodiment the β-sheet fibril is amyloid fibril. In one embodiment, the compound is sRAGE or a fragment thereof. In another embodiment, the compound is an anti-RAGE antibody or portion thereof. This invention provides the above method wherein the inhibition of binding of the β-sheet fibril to RAGE has the consequences of decreasing the load of β-sheet fibril in the tissue, inhibiting fibril-induced programmed cell death, inhibiting fibril-induced cell stress. This invention also provides methods of determining whether a compound inhibits binding of a β-sheet fibril to RAGE on the surface of a cell.
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Catalytic antibodies against cocaine and methods of using and producing same (Wed, 07 Feb 2001)
This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further provides pharmaceutical composition for decreasing concentration in a subject using the antibodies produced.
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Screening methods for the identification of anti-HIV compounds employing a cyclosporine-specific monoclonal antibody that cross-reacts with HIV-1 p24 (Wed, 24 Jan 2001)
The subject invention provides new uses for novel derivatives of cyclosporine A and antibodies directed thereto. Specifically, the derivatives and antibodies are useful in methods of treating AIDS, methods of purifying the Gag protein of HIV, methods of screening for anti-HIV compounds, and methods for detecting HIV in a subject. The derivatives and antibodies can also be incorporated into a kit useful for screening for anti-HIV compounds.
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Method and apparatus for selecting a molecule based on conformational free energy (Wed, 24 Jan 2001)
A method of using a computer processor to analyze electrical signals and data representative of a first molecule to determine conformational free energy of the first molecule so as to determine whether the first molecule is more stable than a second molecule, wherein both molecules have a predefined connectivity and exist in a predefined environment, includes generating a set of data representative of low-energy minimum conformations of the first molecule derived from connectivity of the first molecule, a potential energy function, and a conformational search method. Conformational free energy of the first molecule is determined by calculating a configuration integral in all degrees of freedom based upon a contribution of each conformation of the set of conformations of the first molecule, and the configuration integral is calculated by performing importance sampling multidimensional Monte Carlo integration over a multidimensional volume enclosing a current conformation of the first molecule in a conformational space, repeating the integration for each conformation in the set of data, and summing the conformational contributions so as to determine a total configuration integral for the first molecule and thereby determine the conformational free energy of the first molecule.
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A HYDROPHILIC CARRIER FOR PHOTOSENSITIZERS THAT CLEAVES WHEN THEY CATALYZE THE FORMATION OF SINGLET OXYGEN (Fri, 19 Jan 2001)
The invention provides a composition of matter comprising two β-cyclodextrin molecules and a cleavable linker attached to and joining each such β-cyclodextrin. This invention further provides a composition which comprises a hydrophilic matrix comprising the above-described composition of matter and a photosensitizer encapsulated within the matrix, wherein the cleavable linker is cleaved upon exposure to light of a wavelength appropriate for the light to be absorbed by the photosensitizer. This invention also provides a method of killing a tumor cell which comprises bringing into proximity with the tumor cell the above-described composition and exposing the composition to light so as to cleave the cleavable linker and release the photosensitizer.
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GENE ENCODING NADE, P75NTR-ASSOCIATED CELL DEATH EXECUTOR AND USES THEREOF (Fri, 15 Dec 2000)
This invention provides an isolated nucleic molecule encoding a polypeptide capable of binding a p75NTR receptor, and a purified version of said polypeptide capable of binding a p75NTR receptor. This invention provides a method of producing a purified polypeptide capable of binding a p75NTR receptor. This invention provides an antisense oligonucleotide having a nucleic acid sequence capable of specifically hybridizing to an mRNA molecule encoding the above described polypeptide. This invention provides a method producing a polypeptide capable of binding p75NT receptor into a suitable vector. This invention provides a method of inducing apoptosis, a method of determinig physiological effects, a method for identifying an apoptosis inducing or inhibiting compound, a method for screening cDNA libraries of said polypeptide, a method to induce caspase-2 and caspase-3 activity to cleave poly (ADP-ribose) polymerase and fragment nuclear DNA in a cell, a method to inhibit NF-kB activation in a cell, a method to detect a neurodegenerative disease, a method of producing the isolated human HGR74 protein into a suitable vector, a pharmaceutical composition comprising a purified polypeptide capable of binding a p75NTR receptor and a phamaceutically acceptable carrier and a method of identifying a compound which is an apoptosis inhibitor.
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SODIUM MAGNETIC RESONANCE IMAGING USED IN DIAGNOSING TUMORS AND ASSESSING RESPONSE TO TREATMENT (Fri, 24 Nov 2000)
The present invention provides a method for acquiring magnetic resonance data from a sample by: a) applying a radio frequency pulse to a sample in a magnetic field, thereby causing alignment of nuclei populations within the sample, b) applying a radio frequency pulse at a set time interval (TI), thereby causing a measurable signal in the transverse plane, c) suppressing a nuclei population in the sample by suitably selecting TI or by applying a multiple quantum filter, d) applying image encoding or multiple quantum filters to the sample in (a), e) detecting and analyzing the output signal to obtain a weighted image, f) applying the magnetic field to the sample in (a), g) detecting and analyzing the output signal to obtain an unweighted image, and h) comparing the weighted and unweighted images. The present invention also provides a method of determining the effectiveness of chemotherapy, detecting and characterizing tumors or determining cell death or cellular dysfunction by administering a dose of antineoplastic agent to a subject prior to surgical removal of a cancerous tumor and applying the method for acquiring magnetic resonance data to determine if the antineoplastic agent has altered the nuclei populations in a subject.
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Analogues of N-acetylardeemin, method of preparation and uses thereof (Wed, 15 Nov 2000)
The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 R.sub.6 and R.sub.7 are independently hydrogen, OH, NH.sub.2, SH, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, alkylmercapto, alkylamino, dialkylamino, alkoxy, phenyl, etc.; wherein R.sub.0 and R.sub.2 are independently hydrogen, OH, linear or branched chain alkyl, --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4 ; wherein R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; and wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain acyl, benzoyl, etc.; with the proviso that (a) when R.sub.2 is --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, then R.sub.2 is hydrogen; (b) when R.sub.0 is --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, then R.sub.2 is OH; and (c) when (i) R.sub.0 or R.sub.2 is --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4, (ii) R.sub.3 and R.sub.5 are CH.sub.3 and (iii) R.sub.4 is hydrogen, then R.sub.1, R.sub.6 and R.sub.7 are not all hydrogen. Also provided are related compounds and compositions, and methods of inhibiting the growth of multidrug resistant cells by means of MDR reversal, collateral sensitivity and quantitative synergism. -GOVT PAR This invention was made with government support under grants HL25848, CA28824, CA18856 and HL09187 from the National Institutes of Health. Accordingly, the U.S. Government has certain rights in the invention.
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COMPLEX COMBINATORIAL CHEMICAL LIBRARIES ENCODED WITH TAGS (Wed, 01 Nov 2000)
A method of determining the structure of a compound, which comprises: (a) providing a solid support on which a compound was synthesized by a reaction series comprising at least a first stage reagent and first stage reaction condition and a second stage reagent and second stage reaction condition, wherein the first stage precedes the second stage in the reaction series, which solid support has attached thereto: (i) a first tag, which tag comprises a code that records the first stage reagent or the first stage reaction condition; and (ii) a second tag, which tag comprises a code that records the second stage reagent or the second stage reaction condition; (b) detaching the tags from the solid support such that a mixture of soluble tags is formed; (c) separating the mixed first and second tags, each from the other; and (d) detecting the separated tags, whereby the identities of the reagents and reaction conditions of the first and the second stage of the reaction series are determine
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Bicyclic aminoimidazoles (Wed, 16 Aug 2000)
The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds.
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Catalyst that oxidizes steroids and other substrates with catalytic turnover (Wed, 16 Aug 2000)
The present invention provides a metalloporphyrin catalyst represented by the structure: ##STR1## -GOVT PAR The invention disclosed herein was made with Government support under NIH Grant No. GM-18754 and NSF Grant No. CHF-94-14855. Accordingly, the U.S. Government has certain rights in this invention.
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PROCESS FOR PAN-GENOMIC DETERMINATION OF MACROMOLECULAR ATOMIC STRUCTURES (Fri, 28 Jul 2000)
A process pan-genomic determination of three-dimensional macromolecular atomic structures uses a unique combination of components. All known structural information, sequence information and functional information are systematically organized into a genomics database.
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Potent inducers of terminal differentiation and methods of use thereof (Wed, 12 Jul 2000)
The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. PAL The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
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Production of 3-alkoxyalkanals by hydroformylation of enol ether substrates (Wed, 03 May 2000)
The present invention provides a process for producing an optically active aldehyde which comprises hydroformylating a terminal olefin substrate represented by the formula: EQU Q.sub.1 Q.sub.2 C.dbd.CH.sub.2 PAL wherein Q.sub.1 is an atom or group other than carbon or hydrogen and Q.sub.2 is an atom or group other than hydrogen, in the presence of CO, H.sub.2 and a catalyst, which catalyst comprises a transition metal based compound and a ligand.
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ANTIMALARIAL AGENTS (Fri, 31 Mar 2000)
Composition and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The substituents are detailed in the specification, desferrithiocin and derivatives thereof are comprised within the compounds of formula (I).
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CARDENOLIDE COMPLEXES USEFUL AS CARDIOACTIVE AGENTS (Fri, 03 Mar 2000)
The invention relates to synthetic Na+/K+-ATPase inhibitory factors, compositions and dosage forms comprising them, and methods of their preparation and use. Specific inhibitory factors of the invention include borate and phosphate complexes of ouabain.
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Substituted [6]helicene compounds that show enhanced nonlinear optical rotatory power and uses thereof (Wed, 26 Jan 2000)
This invention provides a compound having the structure: ##STR1## wherein rings A and B represent independent electron accepting ring systems and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are the same or different and are H, substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, --SR, --NRR', --OR, --OC(O)R, SC(O)R, --SCR, wherein R and R' are independently substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl. PAL This invention also provides thin films comprising a compound having the above structure or suitable derivatives thereof. PAL This invention further provides liquid crystal display devices and non-linear optical devises comprising a compound having the above structure or a suitable derivative thereof. PAL Finally, this invention provides a method for achieving a high order non-linear electrooptical response comprising contacting a suitable sample of the inventive compound or a derivative thereof with an appropriate light source.
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OLIGONUCLEOTIDE INHIBITORS OF bcl-xL (Fri, 14 Jan 2000)

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Aggregrates of substituted (6)helicene compounds that show enhanced optical rotatory power and nonlinear optical response and uses thereof (Wed, 01 Dec 1999)
This invention provides an aggregate of a compound capable of forming helical structures such that the aggregate is capable of achieving a specific rotation of at least 100,000.degree. for plane polarized light having a wavelength of 589 nm. -GOVT PAR The invention described herein was made in the course of work under Grant No. CHE92-24634 from the National Science Foundation. The United States Government has certain rights in this invention.
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Simple allylic amination procedure (Wed, 10 Nov 1999)
The subject invention provides a method of preparing an allylic amine having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, cyano, nitro, linear or branched chain alkyl, aryl, etc.; wherein each alkyl or arylalkyl if present is independently unsubstituted or substituted by fluoro, cyano, nitro, linear or branched chain acyl, dialkylamino, etc.; wherein each aryl if present is independently unsubstituted or substituted by fluoro, cyano, nitro, linear or branched chain alkyl, arylmercapto, etc.; and wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 optionally is covalently bonded linking pairwise a suitable atom from each to form from 0 to about 10 rings, wherein each ring contains between about four and about twelve atoms, using disubstituted sulfur diimides prepared in situ. Also provided are methods of preparing cyclic allylic amines in which allylic double bonds are endocyclic and exocyclic. -GOVT PAR This invention was made with government support under Grant No. CHE 92-24634 from the National Science Foundation. Accordingly, the U.S. Government has certain rights in the invention.
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Catalytic antibodies against cocaine (Wed, 03 Nov 1999)
This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further provides pharmaceutical composition for decreasing concentration in a subject using the antibodies produced.
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A CATALYST THAT OXIDIZES STEROIDS AND OTHER SUBSTRATES WITH CATALYTIC TURNOVER (Fri, 15 Oct 1999)
The present invention provides a metalloporphyrin catalyst represented by structure (8) wherein (a) = beta-cyclodextrin.
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Anti-cocaine catalytic antibody (Wed, 08 Sep 1999)
Disclosed are catalytic antibodies and polypeptides capable of degrading cocaine. Said catalytic antibodies and polypeptides are characterized by the amino acid sequence of their complementarity determining regions and framework regions. The present invention also discloses a pharmaceutical composition and a method for decreasing the concentration of cocaine in a subject. Finally, the invention discloses pharmaceutical compositions and methods for treating cocaine overdose and addiction in subjects.
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SYNTHESIS OF DYSIDIOLIDE AND USES THEREOF (Fri, 13 Aug 1999)
This invention provides a process for the preparation of a racemic mixture of dysidiolide a method for inhibiting growth of cancerous cells comprising contracting an amount of the racemic mixture of dysidiolide effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the racemic mixture of dysidiolide.
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A SYNTHETIC PROCESS TOWARD TOTAL SYNTHESIS OF ELEUTHERUBIN AND ITS ANALOGUES AND USES THEREOF (Fri, 18 Jun 1999)
This invention provides a process for the preparation of a Eleutherobin derivative of formula wherein R1 is a hydrogen, ester, nitrile or CH2-R4 (I), wherein R4 is a carbohydrate, an alcohol, an amine, an amide, an alkyne; or R2 is a linear or branched alkyl moiety; R3 is an ester, an amide, a carbamate, an acetal compound, an ether or a urethane; R4 is a hydrogen or CH2; position C2 and C3 is cis or trans; position C8 is α or β and a compound is produced having the structures (II) and (III). Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.
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PRODUCTION OF AN OPTICALLY ACTIVE ALDEHYDE BY HYDROFORMYLATION OF A TERMINAL OLEFIN SUBSTRATE (Fri, 21 May 1999)
The present invention provides a process for producing an optically active aldehyde which comprises hydroformylating a terminal olefin substrate represented by the formula: Q1Q2C=CH2, wherein Q1 is an atom or group other than carbon or hydrogen and Q2 is an atom or group other than hydrogen, in the presence of CO, H2 and a catalyst, which catalyst comprises a transition metal based compound and a ligand.
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A METHOD FOR SELECTING A MOLECULE BASED ON CONFORMATIONAL FREE ENERGY OF ONE MOLECULE FOR ANOTHER MOLECULE (Fri, 09 Apr 1999)
The invention is directed to a method of using a computer processor to analyze electrical signals and data representative of a first molecule (1) to determine conformational free energy of the first molecule so as to determine whether the first molecule is more stable than a second molecule (2), wherein both molecules have a predefined connectivity and exist in a predefined environment, comprising: (a) generating a set of data representative of low-energy minimum conformations of the first molecule (1) derived from connectivity of the first molecule, a potential energy function, and a conformational search method and determining conformational free energy of the first molecule (1) by calculating a configuration integral in all degrees of freedom based upon a contribution of each conformation of the set of conformations of the first molecule (1) and by using Monte Carlo integration.
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Potent inducers of terminal differentiation and method of use thereof (Wed, 25 Nov 1998)
The invention provides compounds, several of which belong to a class having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound. The invention also concents a method of selectively inducing termini differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effective to selectively induce terminal differentiation. Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.
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Method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal circulation (Wed, 25 Nov 1998)
This invention provides an assay to monitor antithrombic activity of a Factor IXa compound infused into circulation of a patient which includes: (a) obtaining Factor IXa-deficient plasma; (b) mixing the plasma from step (a) with diatomaceous and with plasma from the patient; (c) incubating the mixture with a source of lipid and calcium chloride under conditions suitable for clot formation; and (d) measuring time necessary for clot formation in the incubate, thereby monitoring the antithrombic activity of the Factor IXa compound infused into the circulation of the patient.
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Bicyclic aminoimidazoles (Wed, 11 Nov 1998)
The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds. The bicyclic aminoimidazole compounds of the invention have anti-tumor and anti-microbial activity.
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Synthesis of optically active helical ladder polymers with unbroken double-bond conjugation (Wed, 04 Nov 1998)
Optically active ladder polymers that are chiral and have an unbroken network of conjugated double bonds along a helical path are synthesized. -GOVT PAR The invention described herein was made in the course of work under Grant No. NSFCHE92-24634 from the National Science Foundation. The U.S. Government has certain rights in this invention.
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Synthetic receptors, libraries and uses thereof (Wed, 09 Sep 1998)
The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier. -GOVT PAR The invention was made in part with government funds under Grant CHE92-08254 from the National Science Foundation. Therefore, the U.S. Government has certain rights in the invention.
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Regulating gene expression using retinoids with Ch.sub.2 OH or related groups at the side chain terminal position (Wed, 29 Jul 1998)
For the first time, certain retinoids with a side chain terminal CH.sub.2 OH group or ester or ether thereof or aldehyde rather than a side chain terminal COOH group and substitution at the 4-position have been indicated to bind to nuclear receptors and to be biologically active in inducing cell differentiation of normal and tumor cells. These compounds activate gene expression through binding to nuclear receptor proteins. These compounds induce differentiation in normal and cancer cells and are useful for treating leukemias, and lymphomas, squamous cell carcinomas, deep (cystic) acne, psoriasis and photodamaged or aging skin. These compounds have stability and in vitro half-life advantages over and solubility differences from all-trans-retinoic acid and activity advantages over 13-cis retinoic acid. -GOVT PAR The invention described herein was made in the course of work under grant number R01 CA43796 from the National Institutes of Health, in the United States Government. The United States Government has certain rights in this invention.
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Screening method for the identification of compounds capable of abrogation HIV-1 gag-cyclophilin complex formation (Wed, 01 Jul 1998)
The human immunodeficiency virus type 1 (HIV-1) gag gene product is capable of directing the assembly of virion particles independent of other viral elements. The Gag protein also plays an important role during the early stages of viral replication. Employing the yeast two-hybrid system, a cDNA expression library was screened and two host proteins identified. These proteins, designated cyclophilins A and B (CyPsA and B), interacted specifically with the HIV-1 Gag polyprotein Pr55.sup.gag. Glutathione S-transferase-CyP fusion proteins bind tightly to Pr55.sup.gag in vitro. Cyclosporin A (CsA) efficiently disrupts the Gag-CyPA binding interaction. The identification of novel compounds capable of abrogating this protein-protein interaction employing the disclosed screening assay will facilitate the development of HIV-1 antiviral agents. -GOVT PAR The invention disclosed herein was made with Government support under Grant Nos. Al24845 and Al00988 from the National Institute of Allergy and Infectious Disease. Accordingly, the U.S. Government has certain rights in this invention.
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Potent inducers of terminal differentiation and method of use thereof (Wed, 01 Jul 1998)
The invention provides a class of compounds and compositions thereof having the structure: ##STR1## wherein A is: ##STR2## The invention also concerns a method of selectively inducing terminal differentiation of neoplastic cells thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable conditions with an amount of the compound to selectively induce terminal differentiation. It also provides a method of treating a patient having a tumor characterized by proliferatoin of neoplastic cells comprising administration of an amount of the compound effective to inhibit proliferation and suppress oncogenicity of neoplastic cells.
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Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same (Wed, 24 Jun 1998)
The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is hydrogen or a branched or unbranched, substituted or unsubstituted aminoalkyl having from two to twenty atoms in the chain, R.sub.2 is hydrogen, methyl, or a branched or unbranched, substituted or unsubstituted alkyl having from two to twenty atoms in the chain; when R.sub.2 is methyl, R.sub.3 is either hydrogen or a substituted or unsubstituted aryl; and R.sub.4 is methyl, a branched or unbranched, substituted or unsubstituted alkyl, alkenyl, alkynyl, alkenynyl, or cycloalkyl having from two to twenty atoms in the chain, or a substituted or unsubstituted aryl group. PAL The invention also concerns a method of preparing the compound from the venom, venom sacs or venom glands of the wasp Philanthus triangulun F. Additionally, the invention provides a method of chemically synthesizing the compound. PAL Another aspect of the invention concerns a method of treating a subject afflicted by a disorder associated with binding of an etiological agent to a glutamate receptor. Lastly, the invention provides an insecticidal composition which comprises an effective amount of the compound and a suitable carrier and a method of combatting insects which comprises administering to the insects the insecticidal composition. -GOVT PAC BUTYRYL-TYROSINYL SPERMINE, ANALOGS THEREOF AND METHODS OF PREPARING AND USING SAME PAR The invention described herein was made in the course of work under Grant No. INT-8610138 from the National Science Foundation, and Grant Nos. AI 10187, ES 02594, and E504977 from the National Institute of Health, U.S. Department of Health and Human Services. Accordingly, the U.S. Government has certain rights in the invention.
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INTERMEDIATES FOR THE SYNTHESIS OF VITAMIN D AND STEROID DERIVATIVES AND PROCESSES FOR PREPARATION THEREOF (Fri, 13 Mar 1998)
A process for preparing a compound having structure (I) wherein n is an integer from 1-5; each of R1 and R2 independently is optionally substituted C1-C6 alkyl; each of W and X is independently hydrogen or C1-C6 alkyl; Y is O, S or NR3 where R3 is hydrogen, C1-C6 alkyl or a protective group; and Z is a CD ring structure, a steroid structure, or a vitamin D structure, each of which optionally has one or more protected or unprotected substituents and/or one or more protective groups. This process comprises reacting a compound having structure (IV) wherein W, X, Y and Z are as defined above, in the presence of a base, with a compound having structure (V) or (V') wherein n, R1 and R2 are as defined above, and E is an eliminating group.
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COMPOUNDS THAT INHIBIT INTERACTION BETWEEN SIGNAL-TRANSDUCING PROTEINS AND THE GLGF (PDZ/DHR) DOMAIN AND USES THEREOF (Fri, 13 Feb 1998)
This invention provides for a composition capable of inhibiting specific binding between a signal-transducing protein and a cytoplasmic protein. This invention also provides a method of identifying a compound capable of inhibiting specific binding between a signal-transducing protein and a cytoplasmic protein. This invention also provides a method of inhibiting the proliferation of cancer cells. This invention also provides a method of treating cancer with a composition in an amount effective to result in an amount in apoptosis of the cells. This invention also provides a method of inhibiting the proliferation of virally infected cells. This invention also provides for a method of treating a virally-infected subject with a composition in an amount effective to result in apoptosis of the cells. This invention also provides for pharmaceutical compositions.
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ANTI-COCAINE CATALYTIC ANTIBODY (Thu, 01 Jan 1998)
Disclosed are catalytic antibodies and polypeptides capable of degrading cocaine. Said catalytic antibodies and polypeptides are characterized by the amino acid sequence of their complementarity determining regions and framework regions. The present invention also discloses a pharmaceutical composition and a method for decreasing the concentration of cocaine in a subject. Finally, the invention discloses pharmaceutical compositions and methods for treating cocaine overdose and addiction in subjects.
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PHOSPHOROTHIOATE OLIGONUCLEOTIDES THAT BIND TO THE V3-LOOP AND USES THEREOF (Fri, 12 Dec 1997)
The present invention provides phosphorothioate oligonucleotide moieties comprising a phosphorothioate oligonucleotide comprising the sequence GmXnGp, wherein G is guanosine; X is thymidine, adenosine or cytidine, or a combination thereof; each of m, n and p is independently an integer greater than 2; the phosphorothioate oligonucleotide moiety being capable of binding to a V3 loop of HIV envelope glycoprotein. The invention further provides for a method of inhibiting HIV activity. The invention also provides for a method of inhibiting HIV activity in a subject. The invention further provides for a method of treating an HIV related disorder in a subject. Finally, the invention provides a pharmaceutical composition comprising a phosphorothioate oligonucleotide moiety and a pharmaceutically acceptable carrier.
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METHOD FOR INHIBITING THROMBOSIS IN A PATIENT WHOSE BLOOD IS SUBJECTED TO EXTRACORPOREAL CIRCULATION (Fri, 21 Nov 1997)
This invention provides a method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal blood circulation which comprises contacting the extracorporeal circulating blood with a Factor IXa compound in an amount effective to inhibit thrombosis in the patient. The Factor IXa compound may include an active site-blocked Factor IXa compound or Glu-Gly-Arg chloromethyl ketone-inactivated human factor IXa compound. This invention also provides that the effective amount may be from about 0.1 νg/ml plasma to about 250 νg/ml plasma or from about 0.5 νg/ml plasma to about 25 νg/ml plasma. The patient may be subjected to extracorporeal blood circulation during transplant surgery or cardiopulmonary bypass surgery. This invention further provides for a pharmaceutical composition which includes an effective amount of a Factor IXa compound and a pharmaceutically acceptable carrier.
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Potent inducers of terminal differentiation and method of use thereof (Wed, 17 Sep 1997)
##STR1## wherein each of R, R.sub.1, and R.sub.4 is a hydrogen atom or a methyl, ethyl or propyl group, R and R.sub.1 are the same and R and R.sub.4 are the same or different; and wherein y is 4, 5, 6 or 7. PAL The invention also concerns a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effect to selectively induce terminal differentiation. PAL Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity. PAL Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound in an amount effective less than an amount which would cause toxicity in the patient.
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Retro-alpha-retinol derivative and uses of retro-alpha-retinol (Wed, 16 Jul 1997)
This invention provides a homogeneous retro-retinoid compound, a method of enhancing the growth of a cell in a vitamin A reduced environment, a method for enhancing transcription of a gene regulated by retinoid in a cell, and a method for enhancing an immune response in a subject, wherein the compound has the structure: ##STR1##
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AGGREGRATES OF SUBSTITUTED [6]HELICENE COMPOUNDS THAT SHOW ENHANCED OPTICAL ROTATORY POWER AND NONLINEAR OPTICAL RESPONSE AND USES THEREOF (Fri, 07 Mar 1997)
This invention provides an aggregate of a compound capable of forming helical structures such that the aggregate is capable of achieving a specific rotation of at least 100,000° for plane polarized light having a wavelength of 589 nm.
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Method for the detection of HIV-1 using a cyclosporine-specific monoclonal antibody that reacts with the P24 Gag protein (Wed, 19 Feb 1997)
Monoclonal antibodies to cyclosporine A (CsA), a potent immunosuppressant, were generated in Balb/c mice using a novel antigen prepared by linking CsA to a protein carrier via a photoactive cross-linking reagent, 4-benzoylbenzoic acid (BBa). Twenty-two monoclonal anti-CsA antibodies were generated, using CsA-BBa-bovine serum albumin (CsA-BBa-BSA) as the immunogen. Epitope mapping studies were performed using a series of singly substituted CsA derivatives and an antibody was identified that recognizes N-methyl leucine residues 9 and 10 of CsA. This antibody also cross-reacts with the HIV-1 Gag protein. A method for the detection of HIV-1 in patient samples employing this monoclonal antibody is disclosed. -GOVT PAR This invention was made with government support under Grant Numbers RO1 NS-15581, RO1 H1-36581 and PO1 HL-36581 and training grants 2-T32-AI-07161-11 and T32-CA-09503 from the National Institute of Health, U.S. Department of Health and Human Resources. Accordingly, the U.S. Government has certain rights in the invention.
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A.sub.4 B.sub.6 macrotricyclic enantioselective receptors for amino acid derivatives, and other compounds (Wed, 05 Feb 1997)
The subject invention provides chiral receptor molecules having the structure: ##STR1## wherein A has the structure: ##STR2## and R.sub.1 and R.sub.2 are independently the same or different and are H, F, alkyl, aryl, etc.; X is CH.sub.2 or NH; Y is C.dbd.O or SO.sub.2 ; and n is 0 to about 3; which are useful for the purification of enantiomers of amino acid derivatives and other compounds. The subject invention also provides methods of preparing said receptor molecules. -GOVT PAR This invention was made with government support under grant #GM-44525 from the National Institutes of Health and grants #CHE89-11008 and #CHE92-08245 from the National Science Foundation. Accordingly, the U.S. Government has certain rights in the invention.
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Method for determining protein tertiary structure (Wed, 05 Feb 1997)
The subject invention provides a method for determining the most stable tertiary structure of a protein having a known primary structure which comprises the steps of (a) producing a reduced representation of the protein by assigning to the protein (i) all secondary structural motifs present therein and (ii) all .phi. and .PHI. dihedral angles for the amino acid residues present therein; (b) determining which conformations of the reduced representation are physically permissible, so as to determine which conformations of the protein are physically permissible; and (c) determining which of the physically permissible conformations of the protein possesses the lowest free energy, so as to thereby determine the most stable tertiary structure of the protein. -GOVT PAR This invention was made with support under Grant No. P41-RR06892 from the National Institutes of Health. Accordingly, the U.S. government has certain rights in the invention.
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Method of purifying organic compounds using an enantioselective receptor (Wed, 06 Nov 1996)
The present invention relates to a composition having the general formula: ##STR1## wherein each of A, B, C, X, Y, and Z is independently O, NH, N(CH.sub.2).sub.m CH.sub.3, N(C.dbd.O) (CH.sub.2).sub.m CH.sub.3, CH.sub.2, S, or Se; each of R.sub.1, R.sub.2, and R.sub.3 is independently phenyl, 4-hydroxyphenyl, pyridyl, pyrrolyl, indolyl, naphthyl, thiophenyl, (C.dbd.O) (CH.sub.2).sub.p CH.sub.3, NH(C.dbd.O) (CH.sub.2).sub.p CH.sub.3, OH, COOH, NH.sub.2, or SH; and m, n, and p are integers between 0 and 5. The composition is a chiral receptor molecule useful for the purification of enantiomers of derivatives of amino acids and of compounds able to form hydrogen bonds. The preparation of the composition involves coupling a trifunctional aromatic molecule with three protected chiral molecules at the three aromatic groups, cleaving protecting groups, and joining adjacent chiral groups by multiple lactamizations. The receptor may be used in a form either bound to a solid support or dissolved in an immiscible phase to effect convenient purification of enantiomers or other compounds of interest. -GOVT PAR This invention was made with government support under grants #GM-44525 and #CHE89-11008 from the National Institutes of Health and the National Science Foundation, respectively. Accordingly, the U.S. Government has certain rights in the invention.
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