ALDOSE REDUCTASE INHIBITORS AND USES THEREOF (Fri, 25 Jul 2014)
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, hut 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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ANTIOXIDANT FLAVONOID DERIVATIVES (Fri, 18 Jul 2014)
The present invention relates to antioxidant flavonoids, compositions containing such antioxidant flavonoids and methods for using such antioxidant flavonoids to treat, e.g., AMD.
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LIPID BILAYERS FOR DNA MOLECULE ORGANIZATION AND USES THEREOF (Fri, 27 Jun 2014)
The invention is related to nucleic acid arrays involving fluid lipid bilayers disposed on the support and methods of using the nucleic acid arrays.
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METHOD FOR CULTURE OF HUMAN AND MOUSE PROSTATE ORGANOIDS AND USES THEREOF (Sat, 31 May 2014)
The invention discloses a methodology for the culture of prostate tissue (organoids) from and human prostate, both benign as well as cancer tissue.
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UNDERCARBOXYLATED/UNCARBOXYLATED OSTEOCALCIN INCREASES BETA-CELL PROLIFERATION, INSULIN SECRETION, INSULIN SENSITIVITY, GLUCOSE TOLERANCE AND DECREASES FAT MASS (Fri, 09 May 2014)
<p id="p-0001" num="0000">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.</p>
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METHODS FOR IDENTIFYING CANDIDATES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES (Fri, 09 May 2014)
The present invention provides, inter alia, methods for identifying a candidate agent that may be effective to treat or ameliorate an effect of a neurodegenerative disease in a subject. These methods include: (a) contacting a wildtype neuron and a mutant neuron with a stressor which is effective to accelerate the degeneration of the mutant neuron; (b) further contacting the wildtype neuron and the mutant neuron from step (a) with a candidate agent; and (c) determining whether the candidate agent lowers a wildtype to mutant survival ratio or increases both wildtype and mutant neuron survival.
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Two Pore Channels as a Therapeutic Target to Protect Against Myocardial Ischemia and as an Adjuvant in Cardiac Surgery (Fri, 25 Apr 2014)
<p id="p-0001" num="0000">The present invention relates to methods and compositions for modulating the activity of two-pore domain K+ channels (“K<b>2</b>P channels”) as a means for inducing preconditioning protection. Such preconditioning can be used to reduce the effect of ischemia associated with ischemic heart disease, myocardial infarction or cardiac surgery. The invention is based on the discovery that the myoprotective current induced by short periods of ischemia is carried by a non-classical two-pore domain K+ channel.</p>
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DESIGN AND SYNTHESIS OF CLEAVABLE FLUORESCENT NUCLEOTIDES AS REVERSIBLE TERMINATORS FOR DNA SEQUENCING BY SYNTHESIS (Fri, 04 Apr 2014)
<p id="p-0001" num="0000">This invention provides novel azido linkers for deoxynucleotide analogues having a detectable marker attached thereto.</p>
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NOVEL GABAA AGONISTS AND METHODS OF USING TO CONTROL AIRWAY HYPERRESPONSIVENESS AND INFLAMMATION IN ASTHMA (Fri, 28 Mar 2014)
Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzodiazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAA receptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.
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Methods for Treating Hair Loss Disorders (Fri, 07 Mar 2014)
<p id="p-0001" num="0000">The invention provides for methods for treating a hair loss disorder in a subject by administering a JAK/STAT inhibitor.</p>
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METHODS FOR REGULATING HAIR GROWTH DISORDERS (Fri, 07 Feb 2014)
The presently disclosed subject matter provides methods for treating a hair loss disorder in a subject by administering a FGF5 inhibitor. The presently disclosed subject matter further provides methods for treating a hair growth disorder in a subject by administering a FGF5 activator.
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CYCLOPROPENIUM POLYMERS AND METHODS FOR MAKING THE SAME (Fri, 07 Feb 2014)
The present invention provides, inter alia, a process for incorporating a cyclopropenium ion into a polymeric system. Processes for making cross-linked polymers, linear polymers, and dendritic polymers, as well as for incorporating a cyclopropenium ion onto a preformed polymer are also provided. Further provided are stable, polycationic compounds, various polymers that contain stable cyclopropenium cations, and substrates containing such polymers. The use of these polymers in water purification systems, antimicrobial coatings, ion-transport membranes, cell supports, drug delivery vehicles, and gene therapeutic vectors are also provided.
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ORGANOCATALYTIC CARBONYL-OLEFIN AND OLEFIN-OLEFIN METATHESIS (Fri, 07 Feb 2014)
The present invention provides, inter alia, organocatalytic carbonyl-olefin metathesis process. This process involves contacting a carbonyl-containing moiety with an olefin-containing moiety in the presence of a catalyst and under conditions sufficient to form a metathesis product with the proviso that the process takes place in the absence of photochemical promotion, stoichiometric amounts of transition metals, and Brnsted and Lewis acid catalysts. The present invention also provides an organocatalytic olefin-olefin metathesis process. This process involves contacting a first olefin-containing moiety with a second olefin-containing moiety in the presence of a catalyst and under conditions sufficient to form a metathesis product with the proviso that the process takes place in the absence of stoichiometric amounts of transition metals. Products made by the processes disclosed herein are also provided.
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SELECTIVE HDAC INHIBITORS (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">This disclosure is related to compounds having the structure</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="12.19mm" wi="61.98mm" file="US20140031368A1-20140130-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">wherein Ar<sub>1</sub>, Ar<sub>2</sub>, R<sub>1</sub>-R<sub>6</sub>, 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.</p>
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QUINAZOLINONE-BASED ONCOGENIC-RAS-SELECTIVE LETHAL COMPOUNDS AND THEIR USE (Fri, 17 Jan 2014)
The present invention provides, inter alia, compounds having the structure (1) compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided.
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NUCLEIC ACID SEQUENCING BY NANOPORE DETECTION OF TAG MOLECULES (Sat, 28 Dec 2013)
This disclosure provides systems and methods for sequencing nucleic acids using nucleotide analogues and translocation of tags from incorporated nucleotide analogues through a nanopore. In aspects, this disclosure is related to composition, method, and system for sequencing a nucleic acid using tag molecules and detection of translocation through a nanopore of tags released from incorporation of the molecule.
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METHODS TO TREAT ALZHEIMER'S DISEASE USING APOE INHIBITORS (Fri, 06 Dec 2013)
Non-familial late-onset Alzheimer's disease (LOAD), a condition associated with the accumulation of the amyloid precursor protein- derived (APP) Abeta fragment in the brain, can be the consequence of combined genetic and environmental risk factors. One of these risk factors is the presence of the apolipoprotein E4 (APOE4) allele. This invention provides for a neuron model that can be used to screen and identify compounds that can prevent the APOE4-induced pre-LOAD state. This invention provides for methods for the treatment and/or prevention of a neurodegenerative disorder by using an inhibitor of APOE4, such as an antibody inhibitor, or by using an excess of APOE3 protein.
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FOUR-COLOR DNA SEQUENCING BY SYNTHESIS USING CLEAVABLE FLUORESCENT NUCLEOTIDE REVERSIBLE TERMINATORS (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">This invention provides a process for sequencing single-stranded DNA employing modified nucleotides.</p>
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METHOD OF PREPARATION OF NANOPORE AND USES THEREOF (Fri, 18 Oct 2013)
This disclosure provides systems and methods for sequencing nucleic acids using nucleotide analogues and translocation of tags from incorporated nucleotide analogues through a nanopore. In aspects, this disclosure is related to composition, method, and system for sequencing a nucleic acid using tag molecules and detection of translocation through a nanopore of tags released from incorporation of the molecule.
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COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS (Fri, 11 Oct 2013)
The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
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METHODS FOR TREATING HAIR LOSS DISORDERS (Fri, 04 Oct 2013)
The invention provides for methods for treating a hair loss disorder in a subject by administering; a JAK3 inhibitor.
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METHODS FOR REGULATING HAIR GROWTH DISORDERS (Fri, 04 Oct 2013)
The invention provides for methods for treating a hair loss disorder in a subject by administering a FGF13 inhibitor. In one embodiment, the hair loss disorder comprises androgenetic alopecia, telogen effluvium, alopecia areata, tinea capitis, alopecia totalis, hypotrichosis, hereditary hypotrichosis simplex, or alopecia universalis. In one embodiment, the method further comprises the step (b) determining whether the inhibitor administered induced hair growth in the subject afflicted with a hair loss disorder as compared to the subject's hair growth prior to treatment with the inhibitor.
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Systems And Methods For Predicting Protein-Protein Interactions (Fri, 27 Sep 2013)
<p id="p-0001" num="0000">The present subject matter relates to systems and methods for predicting molecular interactions within biological networks based on structural and non-structural indicators. Such molecules include but are not limited to proteins, nucleic acids and small molecules. In some embodiments, the present subject matter is directed to methods for predicting protein-protein interactions comprising obtaining a pair of query proteins, using sequence alignment to identify structural representatives for each of the pair of query proteins, and using structural alignment to determine sets of close and remote structural neighbors for each of the structural representatives. The method can include analyzing the close and remote structural neighbors to identify a reported complex, and using the reported complex to define a template for creating a model for interaction of the pair of query proteins. In another embodiment, the method includes determining sets of non-structural and structural-based scores to measure properties of the modeled interaction and the query proteins.</p>
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SYSTEM, ARRANGEMENT AND METHOD FOR DECOUPLING RF COILS USING ONE OR MORE NON-STANDARDLY-MATCHED COIL ELEMENTS (Fri, 30 Aug 2013)
Arrangement, magnetic resonance imaging system and method can be provided, according to certain exemplary embodiments of the present disclosure. For example, a plurality of radio frequency (RF) coil elements can be utilized which can include at least one coil element that is coupled to and non-standard impedance matched with at least one preamplifier.
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NOVEL CYSTEINE PROTEASE INHIBITORS AND USES THEREOF (Fri, 09 Aug 2013)
The invention provides for novel cysteine protease inh ibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
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MACROMONOMERS FOR PREPARATION OF DEGRADABLE POLYMERS AND MODEL NETWORKS (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">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 and CLICK chemistry to form the desired product.</p>
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FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">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; R<sub>1 </sub>is —H, —OH, —O—R<sub>7</sub>, —N(H)—R<sub>8</sub>, —N(H)—(CH<sub>2</sub>)<sub>n</sub>—NH<sub>2</sub>, —N(R<sub>9</sub>)(R<sub>10</sub>), or a piperazine cation; R<sub>2 </sub>is either covalently bound to R<sub>9</sub>, or is —H, or is covalently bound to R<sub>3 </sub>so as to form a substituted or unsubstituted pyrrole or R<sub>2 </sub>is covalently bound to R<sub>9 </sub>or R<sub>8 </sub>or R<sub>7</sub>; or R<sub>1 </sub>and R<sub>2 </sub>are covalently joined to form an aromatic ring; R<sub>3 </sub>is either covalently bound to R<sub>2 </sub>so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R<sub>3 </sub>is ═O; R<sub>4 </sub>is, inter alia, —H, —OH, or —R<sub>11</sub>NH<sub>2</sub>; R<sub>5 </sub>is, inter alia, —H, —OH, or —R<sub>12</sub>NH<sub>2</sub>, and R<sub>6 </sub>is either is covalently bound to R<sub>10 </sub>or is —H, or R<sub>6 </sub>is covalently bound to R<sub>10 </sub>or R<sub>8 </sub>or R<sub>7</sub>. 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.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="69.85mm" file="US20130190497A1-20130725-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NOVEL PHOSPHODIESTERASE INHIBITORS AND USES THEREOF (Fri, 26 Jul 2013)
The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5.
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METHODS FOR SYNTHESIS OF POLYMACROMOLECULES AND POLYMACROMOLECULAR BRUSHES (Fri, 05 Jul 2013)
<p id="p-0001" num="0000">In one aspect, the present invention is directed to methods for fabricating multilayer polymacromer compositions. In some embodiments, the multilayer polymacromer compositions described herein can comprise heterobifunctional macromolecules and heterotrifunctional molecules.</p>
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PHOTOLABILE COMPOUNDS (Fri, 28 Jun 2013)
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 photoreieased 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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RADIOLABELED COMPOUNDS AND USES THEREOF (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">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.</p>
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METHODS FOR IDENTIFYING COMPOUNDS THAT MODULATE LISCH-LIKE PROTEIN OR C1ORF32 PROTEIN ACTIVITY AND METHODS OF USE (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">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.</p>
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CD4-MIMETIC INHIBITORS OF HIV-1 ENTRY AND METHODS OF USE THEREOF (Fri, 21 Jun 2013)
Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gpl20, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD- 556.
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Force-Clamp Spectrometer And Methods Of Use (Fri, 07 Jun 2013)
<p id="p-0001" num="0000">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.</p>
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METHODS FOR ASSESSING THE IMMUNE SYSTEM IN A PATIENT (Fri, 24 May 2013)
<p id="p-0001" num="0000">Methods of determining the onset or susceptibility of an immunological disease are provided herein. Also provided are immunoassay techniques for carrying out such methods.</p>
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HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF (Fri, 17 May 2013)
<p id="p-0001" num="0000">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.</p>
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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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Compositions and methods for stereoselective aldehyde allylation and crotylation (Fri, 27 Jul 2012)
<p id="p-0001" num="0000">Compositions and methods for practical, stereoselective allylation and crotylation for aldehyde substrates are described. The compositions and methods comprise reagents for allylation and/or crotylation and acids. In some embodiments, the reagents and acids are pre-mixed.</p>
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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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Phosphodiesterase inhibitors and uses thereof (Fri, 30 Mar 2012)
<p id="p-0001" num="0000">The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.</p>
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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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Compounds that inhibit NFκB and BACE1 activity (Fri, 16 Mar 2012)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">This invention provides a process for sequencing single-stranded DNA employing modified nucleotides.</p>
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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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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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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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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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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.</p>
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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)
<p id="p-0001" num="0000">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.</p> <p id="p-0002" num="0000"><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> </p>
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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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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.</p>
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Methods of preventing and treating low bone mass diseases (Fri, 18 Nov 2011)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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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 a is absent and bond ß is present, or Y is H, X is CH, bond a is present, and bond ß is absent; atom Z is a carbon and bonds ?, d and ? are present, or atom Z is a nitrogen and bonds ?, d and ? are absent, or atom Z is a nitrogen and bonds ? and d are present and ? is absent. R1, R2, R3, R4, R5, and R6 are various substituents as described in the specification.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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Functionalization of organic surfaces (Fri, 31 Dec 2010)
<p id="p-0001" num="0000">The present invention relates to functionalizing a surface of an organic material. For example, surfaces of materials having C—H bonds, such as polymers having C—H bonds, can be functionalized. In certain embodiments, a heterobifunctional molecule having a photoactive anchor, a spacer, and a terminal functional group is applied to the surface of an organic material that contains one or more C—H bonds. The heterobifunctional molecule can be bound to any surface having C—H bonds as the photoactive anchor can react with C—H bonds upon irradiation. The terminal functional group has a “click” functionality which can be utilized to functionalize the surface of the organic material with any desired functionalizing moiety having the orthogonal click functionality.</p>
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Photo-generated carbohydrate arrays and the rapid identification of pathogen-specific antigens and antibodies (Fri, 31 Dec 2010)
<p id="p-0001" num="0000">The invention relates to novel photo-generated carbohydrate arrays and methods of their use to detect the presence of one or more agents in a sample. The invention also relates to a high-throughput strategy to facilitate the identification and immunological characterization of pathogen-specific carbohydrates, including those of <i>Bacillus anthracis</i>. The invention can be used to determine the presence of a pathogen and whether a subject has been exposed to a pathogen, such as by screening for pathogen-specific antibodies.</p>
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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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System, method and computer-accessible medium for providing breath-hold multi-echo fast spin-echo pulse sequence for accurate R<sub>2 </sub>measurement (Fri, 03 Dec 2010)
<p id="p-0001" num="0000">Exemplary embodiments of system, method and computer-accessible medium can be provided in accordance with the present disclosure can be provided for generating a plurality of images associated with at least one anatomical structure using magnetic resonance imaging (MRI) data. For example, using such exemplary embodiments, it is possible to obtain at least one multi-echo fast spin-echo (FSE) pulse sequence based on the MRI data, which can include, e.g., hardware specifications of the MRI system. Further, it is possible to generate each of the images based on a particular arrangement of multiple echoes produced by the multi-echo FSE pulse sequence(s).</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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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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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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METAL OXIDE NANOCRYSTALS: PREPARATION AND USES (Fri, 04 Jun 2010)
<p id="p-0001-en" num="0000">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 BaTiO<sub>3 </sub>nanocrystals and parylene-C for pentacene OFETs.</p>
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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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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.
>> read more

DETERGENT COMPOSITIONS UTILIZING HYDROPHOBICALLY MODIFIED POLYMER (Fri, 21 May 2010)
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. </p>
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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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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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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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Photochemical methods and photoactive compounds for modifying surfaces (Fri, 23 Apr 2010)
<p id="p-0001" num="0000">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.</p>
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Four-color DNA sequencing by synthesis using cleavable fluorescent nucleotide reversible terminators (Fri, 16 Apr 2010)
<p id="p-0001" num="0000">This invention provides a process for sequencing single-stranded DNA by employing a nanopore and modified nucleotides.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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Fluorescent substrates for monoamine transporters as optical false neurotransmitters (Fri, 12 Feb 2010)
<p id="p-0001" num="0000">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; R<sub>1 </sub>is —H, —OH, —O—R<sub>7</sub>, —N(H)—R<sub>8</sub>, —N(H)—(CH<sub>2</sub>)<sub>n</sub>—NH<sub>2</sub>, —N(R<sub>9</sub>)(R<sub>10</sub>), or a piperazine cation; R<sub>2 </sub>is either covalently bound to R<sub>9</sub>, or is —H, or is covalently bound to R<sub>3 </sub>so as to form a substituted or unsubstituted pyrrole or R<sub>2 </sub>is covalently bound to R<sub>9 </sub>or R<sub>8 </sub>or R<sub>7</sub>; or R<sub>1 </sub>and R<sub>2 </sub>are covalently joined to form an aromatic ring; R<sub>3 </sub>is either covalently bound to R<sub>2 </sub>so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R<sub>3 </sub>is ═O; R<sub>4 </sub>is, inter alia, —H, —OH, or —R<sub>11</sub>NH<sub>2</sub>; R<sub>5 </sub>is, inter alia, —H, —OH, or —R<sub>12</sub>NH<sub>2</sub>, and R<sub>6 </sub>is either is covalently bound to R<sub>10 </sub>or is —H, or R<sub>6 </sub>is covalently bound to R<sub>10 </sub>or R<sub>8 </sub>or R<sub>7</sub>. 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.</p> <p id="p-0002" num="0000"><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> </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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</p> <p id="p-0002-en" num="0000"> <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> </p> <p id="p-0003-en" num="0000">which then may be used to make many other benzothiazepine compounds.</p>
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Method of preparing a star polymer macromonomer (Fri, 16 Oct 2009)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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METHODS FOR TESTING ANTI-THROMBOTIC AGENTS (Fri, 14 Aug 2009)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">A compound having the structure of the formula (genus of compound 1 excluding Tashironin or Debenzoyltashironin)</p> <p id="p-0002" num="0000"><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> <br/> and methods of the same. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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Methods of inhibiting binding of beta-sheet fibril to rage and consequences thereof (Fri, 30 Jan 2009)
<p id="p-0001-en" num="0000">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.</p> <p id="p-0002-en" num="0000">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.</p> <p id="p-0003-en" num="0000">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.</p> <p id="p-0004-en" num="0000">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.</p>
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Sensing devices from molecular electronic devices (Fri, 16 Jan 2009)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">Embodiments of the present invention relate to the removal of contaminants from water using sugar based surfactant enhanced ultrafiltration.</p> <p id="p-0002" num="0000">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.</p>
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Preparation Of Ginkgolide And F-Seco-Ginkgolide Lactols (Fri, 12 Dec 2008)
<p id="p-0001-en" num="0000">The present invention relates to synthesis of C<sub>11 </sub>natural ginkgolide derivatives and C<sub>11 </sub>f-seco-gingkolide derivatives from the corresponding lactols which are selectively obtained using NaBH<sub>4</sub>.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">Nucleic acid arrays and methods of using nucleic acid arrays are disclosed.</p>
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Polymeric Nanoparticles and Nanogels for Extraction and Release of Compounds (Fri, 24 Oct 2008)
<p id="p-0001-en" num="0000">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. <b>1</b>) 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.</p>
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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</p> <p>; prevent a decrease in the level of RyR -bound FKBPI2.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject;</p> <p>I and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention</p> <p>: further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these</p> <p><sub>!</sub> 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.</p> <p>O</p> <p>o
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Photolabile compounds (Fri, 25 Jul 2008)
<p id="p-0001" num="0000">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.</p>
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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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Radiolabeled compounds and uses thereof (Fri, 13 Jun 2008)
<p id="p-0001" num="0000">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.</p>
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Radiolabeled Arylsulfonyl Compounds and Uses Thereof (Fri, 13 Jun 2008)
<p id="p-0001-en" num="0000">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.</p>
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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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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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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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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. </p>
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Human chorionic gonadotropin antagonists and methods to prevent ovarian hyperstimulation (Fri, 15 Feb 2008)
<p id="p-0001-en" num="0000">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. </p>
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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)
<p id="p-0001-en" num="0000">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. </p>
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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)
<p id="p-0001" num="0000">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.</p>
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Photocleavable fluorescent nucleotides for DNA sequencing on chip constructed by site-specific coupling chemistry (Fri, 30 Nov 2007)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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. </p>
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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)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">The present invention provides compounds of Formula I</p> <p id="p-0002" num="0000"><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> <br/> 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. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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 <i>Ginkgo biloba </i>and related compounds and uses thereof (Fri, 04 May 2007)
<p id="p-0001-en" num="0000">The subject invention provides compounds having the structure:</p> <p id="p-0002-en" num="0000"> <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 R<sub>1 </sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R<sub>2 </sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R<sub>3 </sub>is H or OH; R<sub>4 </sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, or R<sub>4 </sub>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 (C<sub>1</sub>-C<sub>5</sub>) alkyl group, (C<sub>2</sub>-C<sub>5</sub>) alkenyl, or a (C<sub>2</sub>-C<sub>5</sub>) alkynyl, (C<sub>1</sub>-C<sub>5</sub>) alkoxy, (C<sub>2</sub>-C<sub>5</sub>) alkenyloxy, or (C<sub>2</sub>-C<sub>5</sub>) 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 (C<sub>1</sub>-C<sub>5</sub>) alkyl, (C<sub>2</sub>-C<sub>5</sub>) alkenyl, or (C<sub>2</sub>-C<sub>5</sub>) 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, —SO<sub>2</sub>—Ar, or -A-NR<sub>5</sub>, or —R<sub>7</sub>, 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. </p>
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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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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.</p>
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Covalent methods for immobilization of thiolated biomolecules on siliceous and metallic surfaces (Fri, 30 Mar 2007)
<p id="p-0001-en" num="0000">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. </p>
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Agents for preventing and treating disorders involving modulation of the RyR receptors (Fri, 02 Mar 2007)
<p id="p-0001-en" num="0000">The present invention provides novel compounds of Formula I</p> <p id="p-0002-en" num="0000"> <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. </p>
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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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AGENTS FOR PREVENTING AND TREATING DISORDERS INVOLVING MODULATION OF THE RYR RECEPTORS (Fri, 02 Mar 2007)
<br/><br/><br/>The present invention provides compounds of Formula I, (I) and salts, <br/>hydrates, solvates, complexes, and prodrugs thereof. The present invention <br/>further provides methods for synthesizing compounds of Formula I. The <br/>invention additionally provides pharmaceutical compositions comprising the <br/>compounds of Formula I and methods of using the pharmaceutical compositions of <br/>Formula I to treat and prevent disorders and diseases associated with the RyR <br/>receptors that regulate calcium channel functioning in cells.<br/></p>
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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)
<p id="p-0001" num="0000">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.</p>
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Method and system of tracking an intracorporeal device with MR imaging (Fri, 12 Jan 2007)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">The present invention provides the compound having the formula:</p> <p id="p-0002-en" num="0000"> <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 R<sub>1 </sub>and R<sub>2 </sub>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 —CH<sub>2</sub>—; 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. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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Cross reactive arrays of three-way junction sensors for steroid determination (Fri, 15 Sep 2006)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">The present invention provides novel compounds of Formula I</p> <p id="p-0002" num="0000"><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> <br/> 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. </p>
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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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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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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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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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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 AND ERASTIN BINDING PROTEINS, AND USES THEREOF (Fri, 04 Aug 2006)
<br/><br/><br/>The invention relates to methods of screening for binding partners, especially <br/>binding partners essential for the biological activity of erastin (e.g. VDACs <br/>such as VDAC3) . The invention also provides reagents and methods for <br/>effective killing of cancer cells with erastin and related compounds or <br/>derivatives, such like the compounds (1).<br/></p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">This invention provides methods, kits and automated systems for identifying a reagent in which a compound crystallizes, and methods for crystallizing a compound.</p>
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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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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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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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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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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. </p>
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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)
<p id="p-0001-en" num="0000">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 R<sup>10</sup>CHO to form the alcohol. X<sub>3 </sub>is one of O and C(R<sup>4</sup>)(R<sup>5</sup>). Each of X<sub>1 </sub>and X<sub>2 </sub>is independently O or N—R. Each of C<sub>a </sub>and C<sub>b </sub>is independently an achiral center, an (S) chiral center or an (R) chiral center. R<sub>a </sub>and R<sub>b </sub>are (i) each independently C<sub>1-10 </sub>alkyl, C<sub>6-10 </sub>aryl or C<sub>3-9 </sub>heteroaryl, or (ii) taken together to form a C<sub>3</sub>—C<sub>4 </sub>alkylene chain which together with C<sub>a </sub>and C<sub>b </sub>forms a 5-membered or 6-membered aliphatic ring. R<sub>c </sub>and R<sub>d </sub>are each independently hydrogen, C<sub>1-10 </sub>alkyl, C<sub>6-10 </sub>aryl or C<sub>3-9 </sub>heteroaryl. R is C<sub>1-10 </sub>alkyl, C<sub>6-10 </sub>aryl or C<sub>3-9 </sub>heteroaryl. Each of R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5 </sup>is independently hydrogen, C<sub>1</sub>—C<sub>10 </sub>alkyl, C<sub>6-10 </sub>aryl, C<sub>3-9 </sub>heteroaryl, C<sub>1-10 </sub>alkoxy, C<sub>6-10 </sub>aryloxy, C<sub>1-10 </sub>dialkylamino, C<sub>1-10 </sub>alkyl-C<sub>6-10 </sub>arylamino, C<sub>1-10 </sub>diarylamino, or halogen. R<sup>6 </sup>is halogen, hydrogen, C<sub>1-10 </sub>alkyl, C<sub>6-10 </sub>aryl, C<sub>3-9 </sub>heteroaryl, C<sub>1-10 </sub>alkoxy, C<sub>6-10 </sub>aryloxy, C<sub>1-10 </sub>alkyl-C<sub>6-10 </sub>arylamino, C<sub>1-10 </sub>diarylamino, OSO<sub>2</sub>CF<sub>3 </sub>or SR. R<sup>10 </sup>may be C<sub>1-10 </sub>alkyl, C<sub>6-10 </sub>aryl, or C<sub>3-9 </sub>heteroaryl.</p> <p id="p-0002-en" num="0000"> <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> </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) (Fri, 26 Aug 2005)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">The subject invention provides ginkgolide C derivatives compounds having the structure:</p> <p id="p-0002-en" num="0000"> <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, —CH<sub>2</sub>CO<sub>2</sub>R<sup>4</sup>, and —CH<sub>2</sub>CONR<sup>5</sup>R<sup>6</sup>; <ul id="ul0003-en" list-style="none"><li>where R<sup>4 </sup>is an alkyl group; and</li><li>R<sup>5 </sup>and R<sup>6 </sup>are each, independently, hydrogen or a branched or unbranched alkyl group;</li></ul></li></ul></li> <li>wherein R<sup>1 </sup>is H or —COR<sup>7</sup>, <ul id="ul0004-en" list-style="none"><li>where R<sup>7 </sup>is alkyl, aryl or amino;</li></ul></li> <li>wherein R<sup>2 </sup>is present or absent, and when present is H, —COR<sup>8 </sup>or —CO—Z—R<sup>8</sup>; <ul id="ul0005-en" list-style="none"><li>where R<sup>8 </sup>is alkyl, aryl or amino; and</li><li>Z is oxygen;</li></ul></li> <li>wherein R<sup>3 </sup>is present or absent, and when present is —COR<sup>9</sup>; <ul id="ul0006-en" list-style="none"><li>where R<sup>9 </sup>is alkyl or aryl;</li></ul></li> <li>wherein only one of R<sup>2 </sup>or R<sup>3 </sup>is present in the compound;</li> <li>wherein only two of R, R<sup>1</sup>, R<sup>2 </sup>and R<sup>3 </sup>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 R<sup>3 </sup>is absent and bond b is present when R<sup>2 </sup>is absent; <br/> 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> </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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COMPOUNDS AND METHODS FOR TREATING AND PREVENTING EXERCISE-INDUCED CARDIAC ARRHYTHMIAS (Fri, 29 Apr 2005)
The present invention provides a method for limiting or preventing a decrease in the level of RyR2-bound FKBP12.6 in a subject, a method for treating or preventing exercise-induced cardiac arrhythmia in a subject, and a method for preventing exerciseinduced sudden cardiac death in a subject. Also provided are uses of JTV-519 in these methods. The present invention further provides methods for identifying agents for use in preventing exercise-induced sudden cardiac death, as well as agents identified by such methods. Also provided are methods for preventing exercise-induced sudden cardiac death by administering these agents. Additionally, the present invention provides methods for synthesizing JTV-519, radio-labeled JTV-519, and 1,4~benzothiazepine intermediates and derivatives. </p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING HEART TISSUE DEGENERATION, AND USES THEREOF (Fri, 07 Jan 2005)
<br/><br/><br/>The present invention provides methods for promoting generation of heart <br/>tissue, and for treating and preventing heurt tissue degeneration. <br/>Additionally, the present invention provides a therapeutic composition <br/>comprising a cyclin-associated agent, and a kit comprising the composition. <br/>The present invention further provides a heart tissue tell, a side~population <br/>progenitor tell, and a stem tell in which cyclin is augmented. Also provided <br/>are tell lins comprising these tells, screening methods using the tell lins, <br/>and drugs identified by these methods. The present invention further provides <br/>in vitro systems for use in screening candidate drugs for at least one <br/>cardiotoxic effect and/or for synergy with cyclin in the treatment and <br/>prevention of heart tissue degeneration. Finally, the present invention <br/>provides use of a cyclin-associated agent in the generation of heart tissue, <br/>and use of a cyclin~ associated agent in the treatment or prevention of heart <br/>tissue degeneration.<br/></p>
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Hydroxamic acid compounds and methods of use thereof (Fri, 31 Dec 2004)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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Synthetic receptors (Wed, 29 Sep 2004)
<p id="p-00001-en">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.</p>
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Method of re-sensitizing vancomycin resistant bacteria which selectively cleave a cell wall depsipeptide (Fri, 17 Sep 2004)
<p id="p-0001-en" num="0000">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 C<sub>1 </sub>to C<sub>6 </sub>straight chain or branched alkyl group, and wherein when n=1, R=CH<sub>3 </sub>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. </p>
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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)
<p id="p-0001-en" num="0000">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 R<sub>1 </sub>and R<sub>4 </sub>is H, a C<sub>1 </sub>to C<sub>4 </sub>alkyl group, or an acyl group;</li><li>wherein R<sub>2 </sub>is an ether, ester, amide, or a phthalimide group;</li><li>wherein R<sub>3 </sub>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 R<sub>5 </sub>is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R<sub>6 </sub>is ═O, OH, OCH<sub>3</sub>, CN, or an acyloxy group;</li><li>wherein R<sub>7</sub>, is ═O, OH, halogen, an ether group, or an acyl group; wherein R<sub>8 </sub>and R<sub>9 </sub>are independently H, CH<sub>3</sub>, OCH<sub>3</sub>, OC<sub>2</sub>H<sub>5</sub>, CF<sub>3</sub>, halogen such as Br and F, or R<sub>8 </sub>and R<sub>9 </sub>are joined together as a methylenedioxy group, or other five or six membered ring; wherein R<sub>10 </sub>and R<sub>11 </sub>are independently CH<sub>3</sub>, OCH<sub>3</sub>, OC<sub>2</sub>H<sub>5</sub>, SCH<sub>3</sub>, or SC<sub>2</sub>H<sub>5</sub>; wherein R<sub>12 </sub>is H, a C<sub>1 </sub>to C<sub>4 </sub>alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.</li></ul></li></ul></p>
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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)
<p id="p-00001-en" num="00001">A method of isolating terpene trilactones from <i>Ginkgo biloba </i>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.</p>
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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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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 anab 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. </p>
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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)
<p id="p-00001-en">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 (T<sub>I</sub>), 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.</p>
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Total synthesis of merrilactone A (Fri, 09 Jan 2004)
<p id="p-0001-en" num="0000">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.</p>
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Protein/solubility folding assessed by structural complementation (Fri, 02 Jan 2004)
<p id="p-00001-en">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.</p>
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Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof (Fri, 02 Jan 2004)
<p id="p-0001-en" num="0000">The present invention provides the compound having the formula:</p> <p id="p-0002-en" num="0000"> <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> <br/> wherein each of R<sub>1 </sub>and R<sub>2 </sub>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 —CH<sub>2</sub>—; 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. </p>
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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 <i>Ginkgo biloba </i>and related compounds and uses thereof (Fri, 05 Dec 2003)
<p id="p-0001-en" num="0000">The subject invention provides compounds having the structure:</p> <p id="p-0002-en" num="0000"> <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> <br/> wherein R<sub>1 </sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R<sub>2 </sub>is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R<sub>3 </sub>is H or OH; R<sub>4 </sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, or R<sub>4 </sub>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 (C<sub>1</sub>–C<sub>5</sub>) alkyl group, (C<sub>2</sub>–C<sub>5</sub>) alkenyl, or a (C<sub>2</sub>–C<sub>5</sub>) alkynyl, (C<sub>1</sub>–C<sub>5</sub>) alkoxy, (C<sub>2</sub>–C<sub>5</sub>) alkenyloxy, or (C<sub>2</sub>–C<sub>5</sub>) 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 (C<sub>1</sub>–C<sub>5</sub>) alkyl, (C<sub>2</sub>–C<sub>5</sub>) alkenyl, or (C<sub>2</sub>–C<sub>5</sub>) 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, —SO<sub>2</sub>—Ar, or -A-NR<sub>5</sub>, or —R<sub>7</sub>, 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. </p>
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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)
<p id="p-00001-en">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.</p>
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Bacterial small-molecule three-hybrid system (Fri, 31 Oct 2003)
<p id="p-0001-en" num="0000">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></p>
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Analogs of terpene trilactones from Ginkgo biloba for bioorganic and imaging studies (Fri, 17 Oct 2003)
<p id="p-00001-en">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></p> <p id="p-00002-en">wherein R<sub>1</sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety;</p> <p id="p-00003-en">wherein R<sub>2</sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety;</p> <p id="p-00004-en">wherein R<sub>3</sub>is H or OH;</p> <p id="p-00005-en">wherein R<sub>4</sub>is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and</p> <p id="p-00006-en">wherein at least one of R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, or R<sub>4</sub>is 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.</p>
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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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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. </p>
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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)
<p id="p-00001-en">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.</p>
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Method for re-sensitizing vancomycin resistant bacteria which selectively cleave a cell wall depsipeptide (Fri, 04 Jul 2003)
<p id="p-00001-en">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.</p>
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Complex combinatorial chemical libraries encoded with tags (Fri, 27 Jun 2003)
<p id="p-0001-en" num="0000">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.</p>
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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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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; wherein each of R1 and RZ is H or R1 and R2 together are =0; wherein each of R3 and R4 is H or R3 and R4 together are =0; wherein each of R5 and R6 is, independently, H, alkyl, aralkyl, or aryl; wherein each of R7 and R8 is, independently, H or OR14, where R14 is alkyl or -C (O) R15, where R15 is H, -CH2R16, -CHR16R16, - CR16R17R16, -OR16, alkenyl or alkynyl, cycloalkyl, aryl, heterocycloalkyl, heteroaryl, aralkyl, amino, alkyl amino, or dialkyl amino, wherein each R16 is straight or branched, substituted or unsubstituted alkyl, alkenyl or alkynyl, cycloalkyl, aryl heterocycloalkyl, heteroaryl, aralkyl, or amino; and wherein R17 is straight or branched, unsubstituted alkyl, alkenyl or alkynyl, cycloalkyl, aryl, heterocycloalkyl, heteroaryl, aralkyl, or amino, or wherein R7 and R9 together are >0; wherein each of R9 and Rio is, independently, H, alkyl, OH, or OR13, where R13 is an alkyl, an acyl, or an amide, or R9 and R10 together are =CH2, or wherein R8 and Rio together are >0; wherein if one of R7 or R8 and one of R9 or R10 is absent, a double bond is for med as indicated by the broken line; and wherein each of Ril and R12 is, independently, H, OH, or OR13, where R13 is an alkyl, an acyl, or an amide, or R11 and R12 together are =0, or wherein R12 and R10 together are >0, including intermediates in the synthesis. </p>
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Synthetic receptors, libraries and uses thereof (Fri, 06 Jun 2003)
<p id="p-0001-en" num="0000">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.</p>
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Catalytic antibodies against cocaine and methods of using and producing same (Wed, 21 May 2003)
<p id="p-00001-en">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.</p>
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Anti-cocaine catalytic antibody (Fri, 25 Apr 2003)
<p id="p-0001-en" num="0000">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.</p>
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Method for isolating terpene trilactones (ginkgolides, bilobalide) from leaves and pharmaceutical powders of ginkgo biloba (Fri, 14 Feb 2003)
<p id="p-00001-en">A method of isolating terpene trilactones from<i>Ginkgo biloba</i>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.</p>
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Process for pan-genomic determination of macromolecular atomic structures (Fri, 31 Jan 2003)
<p id="p-a-0001-en">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. </p>
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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)
<p id="p-00001-en">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></p> <p id="p-00002-en">wherein each of R<sub>1</sub>and R<sub>2</sub>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 —CH<sub>2</sub>—; 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.</p>
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Oligonucleotide inhibitors of bcl-xL (Fri, 24 Jan 2003)
<p id="p-0001-en" num="0000">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. <b>1.</b> 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. <b>2</b>A and <b>2</b>B. 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.</p>
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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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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. </p>
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Complex combinatorial chemical libraries encoded with tags (Wed, 08 Jan 2003)
<p id="p-00001-en">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.</p>
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Synthesis of dysidiolide and uses thereof (Wed, 20 Nov 2002)
<p id="p-00001-en">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.</p>
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Oligonucleotide inhibitors of bcl-xL (Fri, 26 Jul 2002)
<p id="p-a-0001-en">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. <b>1</b>. 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. <b>2</b>A and <b>2</b>B. 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. </p>
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Intermediates for the synthesis of vitamin D and steroid derivatives and process for preparation thereof (Wed, 05 Jun 2002)
<p id="p-00001-en">A process for preparing a compound having structure (I) wherein n is an integer from 1-5; each of R<sub>1</sub>and R<sub>2</sub>independently is optionally substituted C<sub>1</sub>-C<sub>6</sub>alkyl; each of W and X is independently hydrogen or C<sub>1</sub>-C<sub>6</sub>alkyl; Y is O, S or NR<sub>3</sub>where R<sub>3</sub>is hydrogen, C<sub>1</sub>-C<sub>6</sub>alkyl 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, R<sub>1</sub>and R<sub>2</sub>are as defined above, and E is an eliminating group.</p>
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Method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal circulation (Wed, 22 May 2002)
<p id="p-00001-en">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.</p>
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Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof (Fri, 01 Mar 2002)
<p id="p-00001-en">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></p> <p id="p-00002-en">wherein R<sub>1</sub>and R<sub>4</sub>is H, a C<sub>1</sub>to C<sub>4</sub>alkyl group, or an acyl group;</p> <p id="p-00003-en">wherein R<sub>2</sub>is an ether, ester, amide, or a phthalimide group; wherein R<sub>3</sub>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 R<sub>5</sub>is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R<sub>6</sub>is ═O, OH, OCH<sub>3</sub>, CN, or an acyloxy group; wherein R<sub>7</sub>, is ═O, OH, halogen, an ether group, or an acyl group; wherein R<sub>8</sub>and R<sub>9</sub>are independently H, CH<sub>3</sub>, OCH<sub>3</sub>, OC<sub>2</sub>H<sub>5</sub>, CF<sub>3</sub>, halogen such as Br and F, or R<sub>8</sub>and R<sub>9</sub>are joined together as a methylenedioxy group, or other five or six membered ring; wherein R<sub>10</sub>and R<sub>11</sub>are independently CH<sub>3</sub>, OCH<sub>3</sub>, OC<sub>2</sub>H<sub>5</sub>, SCH<sub>3</sub>, or SC<sub>2</sub>H<sub>5</sub>; wherein R<sub>12</sub>is H, a C<sub>1</sub>to C<sub>4</sub>alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.</p>
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Helical discotic switch (Wed, 06 Feb 2002)
<p id="p-00001-en">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></p> <p id="p-00002-en">wherein X is O, or S and Y is —O—C(═O)CH<sub>2</sub>—O—R<sub>5</sub>, wherein R<sub>5</sub>is H, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, wherein R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>and R<sub>4</sub>are independently the same or different and are substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.</p>
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Hydrophilic carrier for photosensitizers that cleaves when they catalyze the formation of singlet oxygen (Wed, 19 Dec 2001)
<p id="p-00001-en">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.</p>
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