Michigan university - organic-reaction.com

COMPOUNDS CAPABLE OF UNDERGOING SYMMETRY BREAKING INTRAMOLECULAR CHARGE TRANSFER IN A POLARIZING MEDIUM AND ORGANIC PHOTOVOLTAIC DEVICES COMPRISING THE SAME (Sat, 11 May 2013)
The present disclosure generally relates to chromophoric compounds that combine strong absorption of light at visible wavelengths with the ability to undergo symmetry-breaking intramolecular charge transfer (ICT), and their use for the generation of free carriers in organic photovoltaic cells (OPVs) and electric-field- stabilized geminate polaron pairs. The present disclosure also relates to the synthesis of such compounds, methods of manufacture, and applications in photovoltaic systems and organic lasers.
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GLUCOSYLCERAMIDE SYNTHASE INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 26 Apr 2013)
Glucosylceramide synthase inhibitore and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
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GLUCOSYLCERAMIDE SYNTHASE INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 19 Apr 2013)
Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
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LECTINS AND USES THEREOF (Fri, 19 Apr 2013)
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and re-search use. In particular, the present invention provides antiviral and antimicrobial lectin compounds (BanLec) isolated from bananas. These compounds have low mitogenicity and pro-inflammatory activity whilst maintaining anti-HIV-1 activity.
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POLYMERIC NANOPARTICLES FOR ULTRASOUND IMAGING AND THERAPY (Fri, 19 Apr 2013)
Provided herein are nanobubbles designed for use in ultrasound-mediated ablation of cancer cells. The nanobubbles undergo ultrasound-mediated cavitation at an ablation threshold which is significantly decreased, relative to standard ultrasound- mediated treatment of cancer cells. In exemplary embodiments, the nanobubbles comprise an amphiphilic ABC triblock copolymer, wherein block A comprises a hydrophilic polymer, block B comprises a crosslinking polymer, and block C comprises a hydrophobic copolymer comprising (i) methyl methacrylate (MMA) and (ii) a fluorinated monomer, wherein the fluorinated monomer is present in the hydrophobic copolymer of block C at 25 mole percent or less. Related treatment and diagnostic methods, as well as materials relating to the nanobubbles are provided herein. Methods of making a random copolymer are furthermore provided herein.
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CBP and p300-MEDIATED TRANSCRIPTION MODULATORS AND RELATED METHODS (Fri, 22 Mar 2013)
The present invention relates to gene regulation. In particular, the present invention provides small compounds capable of modulating p300 and/or CBP-mediated transcription and related methods of therapeutic and research use. In addition, the present invention provides methods for treating conditions associated with aberrant p300 and/or CBP -mediated transcription with p300 and/or CBP-mediated transcription modulators (e.g., p300 and/or CBP-mediated transcription inhibitors).
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THERAPEUTIC COMPOUNDS AND METHODS (Fri, 08 Mar 2013)
The invention provides compounds of formula I: and salts thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer using compounds of formula I.
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MICROPOROUS COORDINATION COMPLEX AND METHOD OF MAKING THE SAME (Fri, 11 Jan 2013)
Disclosed herein is a three-dimensional coordination complex that includes a plurality of inorganic centers; a plurality of a first bis(bidentate) linker; and a plurality of a second bis(bidentate) linker, where the first and the second bis(bidentate) linkers are have different lengths, and the bidentate binding sites on each linker face in opposite directions on an axis.
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COMPOUND AND METHOD FOR MODULATING OPIOID RECEPTOR ACTIVITY (Fri, 28 Dec 2012)
The invention provides a compound of formula (I), wherein R1 is H, C(NH)NH2, an amino acid, or a peptide; X is OH, NH2, NHR2, NR 2R 3, an amino acid, or a peptide; R 2 and R 3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R4 and R5 is independently H or CH3; Z is 2-amino-2,3-dihydro-lH- indene-2-carboxylic acid; 2-amino-l,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6- amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4- tetrahydroisoquinoline-3-carboxylic acid; or octahydro-lH-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NH2 when R1 is H, R4 is H, R5 is CH3, Z is Aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided.
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BINDING DOMAINS DIRECTED AGAINST GPCR:G PROTEIN COMPLEXES AND USES DERIVED THEREOF (Fri, 28 Dec 2012)
The present invention relates to the field of G protein coupled receptor (GPCR) structural biology and signaling. In particular, the present invention relates to binding domains directed against and/or specifically binding to GPCR:G protein complexes. Also provided are nucleic acid sequences encoding such binding domains and cells expressing or capable of expressing such binding domains. The binding domains of the present invention can be used as universal tools for the structural and functional characterization of G-protein coupled receptors in complex with downstream heterotrimeric G proteins and bound to various natural or synthetic ligands, for investigating the dynamic features of G protein activation, as well as for screening and drug discovery efforts that make use of GPCR:G protein complexes.
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ARBOVIRUS INHIBITORS AND USES THEREOF (Fri, 14 Dec 2012)
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.
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FLUORESCENT MOLECULAR PROBES FOR USE IN ASSAYS THAT MEASURE TEST COMPOUND COMPETITIVE BINDING WITH SAM-UTILIZING PROTEINS (Fri, 23 Nov 2012)
Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM-utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM- utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 16 Nov 2012)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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SELECTIVE LIGANDS FOR THE DOPAMINE 3 (D3) RECEPTOR AND METHODS OF USING THE SAME (Fri, 14 Sep 2012)
Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula (I), wherein R1 is C1-6alkyl or C3-6cycloalkyl; or formula (II) wherein R2 is A or B substituted with one or two halogen(s) or OC1-3alkyl.
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 31 Aug 2012)
The present invention provides polypeptides involved in cryptophycin biosynthesis and the nucleic acid molecules that encode such polypeptides. The nucleic acid molecules and polypeptides of the invention or variants thereof can be used in the methods of the invention to produce cryptophycins.
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COMPOSITIONS AND METHODS FOR THE TREATMENT OF OBESITY AND RELATED DISORDERS (Fri, 24 Aug 2012)
Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions.
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CRYSTALLINE EXPLOSIVE MATERIAL (Fri, 17 Aug 2012)
An explosive material in the form of a cocrystal comprising 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane (CL-20 or HNIW) and at least one energetic material. The energetic material is selected from 2,4,6-trinitrotoluene (TNT), and 1,3,5,7-tetranitro-1,3,5,7-tetrazocane (HMX).
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BCL-2/BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 03 Aug 2012)
Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
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Electrospray and nanospray ionization of discrete samples in droplet format (Fri, 22 Jun 2012)
Droplets or plugs within multiphase microfluidic systems have rapidly gained interest as a way to manipulate samples and chemical reactions on the femtoliter to microliter scale. Chemical analysis of the plugs remains a challenge. It has been discovered that nanoliter plugs of sample separated by air or oil can be analyzed by electrospray ionization mass spectrometry when pumped directly into a fused silica nanospray emitter nozzle. Using leu-enkephalin in methanol and 1% acetic acid in water (50:50 v:v) as a model sample, we found carry-over between plugs was <0.1% and relative standard deviation of signal for a series of plugs was 3%. Detection limits were 1 nM. Sample analysis rates of 0.8 Hz were achieved by pumping 13 nL samples separated by 3 mm long air gaps in a 75 μm inner diameter tube. Analysis rates were limited by the scan time of the ion trap mass spectrometer. The system provides a robust, rapid, and information-rich method for chemical analysis of sample in segmented flow systems.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Sat, 19 May 2012)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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NANOSCALE PHOTOLITHOGRAPHY (Sat, 19 May 2012)
A simple and practical method that can reduce the feature size of a patterned structure bearing surface hydroxyl groups is described. The patterned structure can be obtained by any patterning technologies, such as photo-lithography, e-beam lithography, nano-imprinting lithography. The method includes: (1) initially converting the hydroxyl or silanol-rich surface into an amine-rich surface with the treatment of an amine agent, preferably a cyclic compound; (2) coating an epoxy material on the top of the patterned structure; (3) forming an extra layer when applied heat via a surface-initiated polymerization; (4) applying an amine coupling agent to regenerate the amine-rich surface; (5) coating an epoxy material on the top of the patterned structure to form the next layer; (6) repeating step 4 and 5 to form multiple layers; This method allows the fabrication of feature sizes of various patterns and contact holes that are difficult to reach by conventional lithographic methods.
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PHOTOACTIVE DEVICES INCLUDING PORPHYRINOIDS COORDINATING ADDITIVES (Fri, 20 Apr 2012)
Coordinating additives are included in porpliyrinoid-based materials to promote intermolecular organization and improve one or more photoelectric characteristics of the materials, The coordinating additives are selected from fullerene compounds and organic compounds having free electron pairs. Combinations of different coordinating additives can be used to tailor the characteristic properties of such porphyrinoid-based materials, including porphyrin oligomers. Bidentate ligands are one type of coordinating additive that can form coordination bonds with a central metal ion of two different porphyrinoid compounds to promote porphyrinoid alignment and/or pi-stacking. The coordinating additives can shift the absorption spectrum of a photoactive material toward higher wa velengths, increase the external quantum efficiency of the material, or both.
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DEUBIQUITINASE INHIBITORS AND METHODS FOR USE OF THE SAME (Fri, 30 Mar 2012)
Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
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FUSING PORPHYRINS WITH POLYCYCLIC AROMATIC HYDROCARBONS AND HETEROCYCLES FOR OPTOELECTRIC APPLICATIONS (Fri, 27 Jan 2012)
A compound that can be used as a donor material in organic photovoltaic devices comprising a non-activated porphyrin fused with one or more non-activated polycyclic aromatic rings or one or more non-activated heterocyclic rings can be obtained by a thermal fusion process. By heating the reaction mixture of non-activated porphyrins with non-activated polycyclic aromatic rings or heterocyclic rings to a fusion temperature and holding for a predetermined time, fusion of one or more polycyciic rings or heterocyclic rings to the non-activated porphyrin core in meso,β fashion is achieved resulting in hybrid structures containing a distorted porphyrin ring with annulated aromatic rings. The porphyrin core can be olygoporphyrins.
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2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and -pyrimidines as antiviral agents (Fri, 11 Nov 2011)
Compounds which are active against viruses have the following formulas: <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="19.22mm" wi="56.56mm" file="US08232275-20120731-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines. 
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METHODS OF TREATING AUTOIMMUNE DISORDERS AND/OR INFLAMMATORY DISORDERS (Fri, 04 Nov 2011)
The present invention relates to dendrimer compositions configured for treating inflammatory disorders and autoimmune disorders, and related methods of synthesis. Specifically, the present invention relates to methods for treating rheumatoid arthritis with PAMAM dendrimers having functional ligands configured for treating rheumatoid arthritis (e.g., therapeutic agents, pro-drugs, targeting agents, trigger agents, imaging agents) (e.g., methotrexate).
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BANANA LECTINS AND USES THEREOF (Fri, 21 Oct 2011)
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides antiviral and antimicrobial lectin compounds (BanLec) isolated from bananas. These compounds have low mitogenicity and pro - inflammatory activity whilst maintaining anti-HIV-1 activity.
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ULTRASTRONG AND STIFF LAYERED POLYMER NANOCOMPOSITES AND HIERARCHICAL LAMINATE MATERIALS THEREOF (Fri, 14 Oct 2011)
A stiff layered polymer nanocomposite comprising a substrate adapted to receive a plurality of alternating layers of a first material and a second material; wherein the first material and second material are a polyelectrolyte, an organic polymer or an inorganic colloid and said first material and said second material have a chemical affinity for each other, said plurality of layers crosslinked using a chemical or physical crosslinking agent. Thin films that are consolidated and optionally crosslinked can be manufactured into hierarchical laminates with rigid and stress resistant properties.
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USING PHAGE EPITOPES TO PROFILE THE IMMUNE RESPONSE (Fri, 30 Sep 2011)
The present disclosure provides compositions and methods for using one or more polypeptide probes to profile an immune response. The polypeptide probe can be used to detect one or more antibodies from a sample. Furthermore, the present disclosure provides methods and compositions for characterizing a cancer based on the detection of one or more antibodies, such as autoantibodies.
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USING PHAGE EPITOPES TO PROFILE THE IMMUNE RESPONSE (Fri, 23 Sep 2011)
The present disclosure provides compositions and methods for using one or more polypeptide probes to profile an immune response. The polypeptide probe can be used to detect one or more antibodies from a sample. Furthermore, the present disclosure provides methods and compositions for characterizing a cancer based on the detection of one or more antibodies, such as autoantibodies.
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NANO-FIBROUS MICROSPHERES AND METHODS FOR MAKING THE SAME (Fri, 19 Aug 2011)
Nano-fϊbrous microspheres and methods for forming them are disclosed herein. In one embodiment the microsphere includes a plurality of nano-fibers aggregated together in a spherical shape; and a plurality of pores formed between at least some of the plurality of nano-fibers. The nano-fibers are formed of star-shaped polymers.
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Compositions and methods relating to novel compounds and targets thereof (Fri, 12 Aug 2011)
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
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Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same (Fri, 29 Jul 2011)
Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C═O or SO2, R1 is C1-6 alkyl, R2 is aryl, heteroaryl, aryl, —(CH2)1-3aryl, or —(CH2)1-3heteroaryl, and n is 0 or 1. Methods of using the D3 receptor ligands in the treatment of diseases and conditions wherein modulation of the D3 receptor provides a benefit also are disclosed. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.45mm" wi="75.35mm" file="US20110184033A1-20110728-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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Indole antiviral compositions and methods (Fri, 22 Jul 2011)
The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 22 Jul 2011)
The present invention relates to cancer markers. In particular, the present invention provides metabolites and panels of metabolites that are differentially present in cancer (e.g., prostate or breast cancer).
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HIGH THROUGHPUT ENSEMBLE-BASED DOCKING AND ELUCIDATION OF THREE-DIMENSIONAL STRUCTURAL CONFIRMATIONS OF FLEXIBLE BIOMOLECULAR TARGETS (Fri, 15 Jul 2011)
Methods for generating putative ligand structures capable of altering the activity of a target effector molecule comprise: constructing an elongated monomer of the target effector molecule; constructing a three dimensional model of the target effector molecule under the influence of elongation using empirical three dimensional data, the model including a conformation revealing the binding portion of the target effector molecule to a putative ligand structure; generating a plurality of computational models of the target effector molecule; filtering the plurality of computational models against the three dimensional model created experimentally using a reiterative simulation analysis algorithm operable to identify and select a plurality of computational models having a root-mean square deviation below a predetermined threshold when compared to the three dimensional model of the target effector molecule; screening a plurality of ligands to rank the binding strength of each ligand with the plurality of computational models selected and selecting one or more ligands based on the ranking.
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Protein purification tags and uses thereof (Fri, 08 Jul 2011)
The present invention relates to fusion proteins. In particular, the present invention relates to protein tags for use in protein solubilization and purification.
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Pyrimidotriazinediones and Pyrimidopyrimidinediones and Methods of Using the Same (Fri, 08 Jul 2011)
The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="106.76mm" wi="55.37mm" file="US20110166144A1-20110707-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 24 Jun 2011)
The present invention relates to cancer markers. In particular, the present invention provides metabolites and panels of metabolites that are differentially present in cancer (e.g., prostate or breast cancer).
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TARGETED DENDRIMER-DRUG CONJUGATES (Fri, 17 Jun 2011)
V The invention provides for dendrimer conjugates useful for liver- specific delivery of therapeutic agents. The therapeutic agent is associated to the dendrimer through a enzyme-cleavable covalent linkage.
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PHOSPHORESCENT ORGANIC COMPOUNDS (Sat, 04 Jun 2011)
Compositions providing metal-independent phosphorescence due to a directed heavy atom effect are provided. Methods of providing a phosphorescent composition are also provided where a directed heavy atom effect is maintained to cause the composition to be phosphorescent. Manufacture of phosphorescent compositions using intermolecular and intramolecular directed heavy atom effects are disclosed.
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NOVEL GREB1A MONOCLONAL ANTIBODY (Fri, 27 May 2011)
The generation and validation of a novel monoclonal GREB1 antibody (GREB1ab). Methods for the prognosis, diagnosis, assessment of disease progression, severity and outcome utilize GREB1 molecules as biomarkers. The GREB1 antibody is also a useful tool for investigations focused on the expression, distribution and function of GREB1 in normal and cancer tissues.
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1,4-BENZODIAZEPINE-2,5-DIONES AND RELATED COMPOUNDS WITH THERAPEUTIC PROPERTIES (Fri, 27 May 2011)
The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.
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1,4-BENZODIAZEPINE-2,5-DIONES AND RELATED COMPOUNDS WITH THERAPEUTIC PROPERTIES (Fri, 27 May 2011)
The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.
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DENDRIMER COMPOSITIONS AND METHODS OF SYNTHESIS (Fri, 20 May 2011)
The present invention relates to novel dendrimer compounds and methods of synthesizing the same. In particular, the present invention is directed to novel polyamidoamine (PAMAM) dendrimers, novel dendrimer branching units, methods for synthesizing such novel PAMAM dendrimers and functionalized dendrimers, as well as systems and methods utilizing the dendrimers (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease diagnosis and/or therapy, etc.))).
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ANALYTICAL SYSTEM WITH PHOTONIC CRYSTAL SENSOR (Fri, 20 May 2011)
A system for determining whether interaction occurs between a trial substance and a target substance. The system includes a photonic crystal sensor having a photonic crystal structure and a defect member disposed adjacent the photonic crystal structure. The defect member defines an operative surface able to receive the target substance and the trial substance. The system further includes a light source that inputs a light signal to the photonic crystal structure and the defect member. The light signal is internally reflected, and a resultant output signal is outputted. The output signal relates to whether the trial substance interacts with the target substance at the operative surface. Furthermore, the system includes an identity detector that identifies the trial substance that interacts with the target substance.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 20 May 2011)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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MULTIFUNCTIONAL SMALL MOLECULES (Fri, 20 May 2011)
The present invention relates to dendrimer synthesis. Specifically, the present invention relates to triazine scaffolds capable of click chemistry for one-step synthesis of functionalized dendrimers, and methods of making and using the same.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 13 May 2011)
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
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COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION (Fri, 06 May 2011)
The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
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HYDROXYL-TERMINATED DENDRIMERS (Fri, 06 May 2011)
The present invention relates to dendrimer synthesis, dendrimer compositions, and related methods of use. Specifically, the present invention relates to hydroxyl-terminated PAMAM dendrimers bearing, e.g., multiple terminal hydroxyl groups and/or terminal oligo (ethylene glycol) groups. In some embodiments, the hydroxyl-terminated PAMAM dendrimers are further conjugated with functional ligands (e.g., therapeutic agents, pro-drugs, targeting agents, trigger agents, imaging agents).
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BIVALENT DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 29 Apr 2011)
The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
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METHOD FOR ENZYMATIC PRODUCTION OF DECARBOXYLATED POLYKETIDES AND FATTY ACIDS (Fri, 22 Apr 2011)
Disclosed herein are methods of preparing alkenes from beta-hydroxy or beta-sulfate carboxylic acid or carboxylic acid derivatives using thioesterase and optionally a sulfotransferase.
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SELECTIVE OXIDATION OF C-H BONDS OF MODIFIED SUBSTRATES BY P450 MONOOXYGENASE (Fri, 01 Apr 2011)
The present invention provides regio- and stereoselective oxidation of unactivated C-H bonds using an engineered mutant cytochrome P450 monooxygenase and an engineered substrate.
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BENZODIAZEPINONE COMPOUNDS AND METHODS OF TREATMENT USING SAME (Fri, 25 Mar 2011)
The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.
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METHODS AND COMPOSITIONS FOR INHIBITING RHO-MEDIATED DISEASES AND CONDITIONS (Fri, 25 Mar 2011)
The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research.
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COMPOSITIONS AND METHODS FOR TREATMENT OF LEUKEMIA (Fri, 18 Mar 2011)
The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.
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VISIBLE/NIR PHOTODETECTORS (Fri, 11 Mar 2011)
Porphyrin compounds are provided. The compounds may further comprise a fused polycyclic aromatic hydrocarbon or a fused heterocyclic aromatic. Fused polycyclic aromatic hydrocarbon s and fused heterocyclic aromatics may extend and broaden absorption, and modify the solubility, crystallinity, and film-forming properties of the porphyrin compounds. Additionally, devices comprising porphyrin compounds are also provided. The porphyrin compounds may be used in a donor/acceptor configuration with compounds, such as C60.
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SYNTHESIS AND ISOLATION OF DENDRIMER SYSTEMS (Fri, 11 Mar 2011)
The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).
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COMPOSITIONS AND METHODS FOR TREATMENT OF LEUKEMIA (Fri, 11 Mar 2011)
The invention relates generally to effective treatment leukemia. In particular, the present invention provides compositions and methods to inhibit the interaction of menin with MLL and MLL-fusion oncoproteins, and well as systems and methods to screen for such compositions.
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COMPOSITIONS AND METHODS FOR TARGETING TUMORS (Fri, 04 Mar 2011)
The present invention relates to functionalized magnetic nanoparticles. In particular, the present invention provides functionalized magnetic nanoparticles for research and clinical (e.g., targeted treatment) applications.
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HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 25 Feb 2011)
The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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SYNTHESIS OF DENDRIMER CONJUGATES (Fri, 28 Jan 2011)
The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
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METHOD FOR ENZYMATIC PRODUCTION OF DECARBOXYLATED POLYKETIDES AND FATTY ACIDS (Fri, 28 Jan 2011)
Disclosed herein are methods of preparing alkenes from beta-hydroxy or beta-sulfate carboxylic acid or carboxylic acid derivatives using thioesterase and optionally a sulfotransferase.
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PRO-DRUG COMPLEXES AND RELATED METHODS OF USE (Fri, 07 Jan 2011)
The present invention provides methods, compositions and applications for efficient, site-specific drug delivery using pro-drug complexes comprising therapeutic agents and one or more functional groups (e.g., imaging agents, targeting agents, and trigger agents). In particular, the present invention relates to pro-drug complexes comprising one or more functional groups conjugated with a therapeutic agent (e.g., a chemotherapeutic agent), methods of synthesizing the same, as well as systems and methods utilizing the therapeutic and diagnostic compositions (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).
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METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTION (Fri, 31 Dec 2010)
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.
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ELECTROSPRAY AND NANOSPRAY IONIZATION OF DISCRETE SAMPLES IN DROPLET FORMAT (Fri, 24 Dec 2010)
Droplets or plugs within multiphase microfluidic systems have rapidly gained interest as a way to manipulate samples and chemical reactions on the femtoliter to microliter scale. Chemical analysis of the plugs remains a challenge. It has been discovered that nanoliter plugs of sample separated by air or oil can be analyzed by electrospray ionization mass spectrometry when pumped directly into a fused silica nanospray emitter nozzle. Using leu-enkephalin in methanol and 1% acetic acid in water (50:50 v:v) as a model sample, we found carry-over between plugs was < 0.1% and relative standard deviation of signal for a series of plugs was 3%. Detection limits were 1 nM. Sample analysis rates of 0.8 Hz were achieved by pumping 13 nL samples separated by 3 mm long air gaps in a 75 μm inner diameter tube. Analysis rates were limited by the scan time of the ion trap mass spectrometer. The system provides a robust, rapid, and information-rich method for chemical analysis of sample in segmented flow systems.
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 17 Dec 2010)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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COMPOUNDS ACTING AS PEPTIDE GAP JUNCTION MODULATORS, AND USES THEREOF (Fri, 17 Dec 2010)
Compounds capable of modulating intracellular gap junctional communication, as well as their use in the treatment of diseases associated with impaired gap junction intracellular communication (GJIC)1 are disclosed.
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Pharmaceutical Co-Crystal Compositions (Fri, 10 Dec 2010)
A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, O-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
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PLASMINOGEN ACTIVATOR INHIBITOR AMELIORATION OF NEWBORN HYPOXIC ISCHEMIC BRAIN INJURY (Fri, 12 Nov 2010)
Plasminogen activators as potential therapeutic targets in neonatal hypoxia ischemia (HI) brain injury. Use of plasminogen activator inhibitor-1 (PAI-1) to ameliorate HI encephalopathy related disease. Use of PAI-1 as preventive treatment of cerebral palsy (CP).
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DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 29 Oct 2010)
The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 29 Oct 2010)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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1,4-BENZODIAZEPINONE COMPOUNDS AND THEIR USE IN TREATING CANCER (Fri, 22 Oct 2010)
The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.
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Block Coordination Copolymers (Fri, 03 Sep 2010)
The present invention provides compositions of crystalline coordination copolymers wherein multiple organic molecules are assembled to produce porous framework materials with layered or core-shell structures. These materials are synthesized by sequential growth techniques such as the seed growth technique. In addition, the invention provides a simple procedure for controlling functionality.
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Block coordination copolymers (Fri, 03 Sep 2010)
The present invention provides compositions of crystalline coordination copolymers wherein multiple organic molecules are assembled to produce porous framework materials with layered or core-shell structures. These materials are synthesized by sequential growth techniques such as the seed growth technique. In addition, the invention provides a simple procedure for controlling functionality.
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Block coordination copolymers (Fri, 03 Sep 2010)
The present invention provides compositions of crystalline coordination copolymers wherein multiple organic molecules are assembled to produce porous framework materials with layered or core-shell structures. These materials are synthesized by sequential growth techniques such as the seed growth technique. In addition, the invention provides a simple procedure for controlling functionality.
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Properties tailoring in silsesquioxanes (Fri, 03 Sep 2010)
Fluoride catalyzed rearrangement reactions of polymeric silsesquioxanes [RSiO1.5]n involve reacting at least one silsesquioxane material with a catalytic amount of an organic fluoride at a temperature ranging from about −50° C. to about 120° C. thereby forming a reaction mixture for a period ranging from 60 minutes to 48 hours. To the reaction mixture, a quenching agent is added to remove fluoride from the reaction mixture. A silsesquioxane cage compound can be isolated from the reaction mixture using a precipitation or other extraction process.
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F1F0-ATPase inhibitors and related methods (Fri, 03 Sep 2010)
The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
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BLOCK COORDINATION COPOLYMERS (Fri, 03 Sep 2010)
The present invention provides compositions of crystalline coordination copolymers and methods of making and using the compositions wherein multiple organic molecules are assembled to produce porous framework materials with layered or core-shell structures. These materials are synthesized by sequential growth techniques such as the seed growth technique. In addition, the invention provides a simple procedure for controlling functionality.
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METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTION (Fri, 13 Aug 2010)
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.
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SYSTEMS AND METHODS FOR IMAGING CHANGES IN TISSUE (Fri, 23 Jul 2010)
The present invention provides systems and methods for monitoring tissue regions. In particular, the present invention provides systems and methods for detecting changes in tissue regions over a period of time. In some embodiments, the systems and methods of the present invention are used to evaluate the effectiveness of a particular treatment of a tissue region. In some embodiments, the systems and methods of the present invention provide a parametric response map approach for detecting and analyzing changes in tissue regions over a period of time to detect and monitor disease or tissue health and to monitor the impact of therapeutic interventions.
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STAT3 INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 09 Jul 2010)
Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed.
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DENDRIMER BASED MODULAR PLATFORMS (Fri, 02 Jul 2010)
The present invention relates to novel therapeutic and diagnostic dendrimer based modular platforms (e.g., drug delivery platforms). In particular, the dendrimer based modular platforms are configured such that two or more dendrimers (e.g., PAMAM dendrimers) are coupled together (e.g., via a cycloaddition reaction) wherein each of the coupled dendrimers is functionalized (e.g., functionalized for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy). In some embodiments, the present invention provides dendrimer based modular platforms having coupled dendrimers (e.g., two or more coupled dendrimers) wherein each dendrimer is conjugated to one or more functional groups (e.g., therapeutic agent, imaging agent, targeting agent, triggering agent) (e.g., for specific targeting and/or therapeutic use of the dendrimer based modular platform). In some embodiments, the functional groups are conjugated to the dendrimers via a linker and/or a triggering agent. In addition, the present invention is directed to methods of synthesizing dendrimer based modular platforms, compositions comprising the dendrimer based modular platforms, as well as systems and methods utilizing the dendrimer based modular platforms (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).
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DENDRIMER BASED MODULAR PLATFORMS (Fri, 25 Jun 2010)
The present invention relates to novel therapeutic and diagnostic dendrimer based modular platforms (e.g., drug delivery platforms). In particular, the dendrimer based modular platforms are configured such that two or more dendrimers (e.g., PAMAM dendrimers) are coupled together (e.g., via a cycloaddition reaction) wherein each of the coupled dendrimers is functionalized (e.g., functionalized for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy). In some embodiments, the present invention provides dendrimer based modular platforms having coupled dendrimers (e.g., two or more coupled dendrimers) wherein each dendrimer is conjugated to one or more functional groups (e.g., therapeutic agent, imaging agent, targeting agent, triggering agent) (e.g., for specific targeting and/or therapeutic use of the dendrimer based modular platform). In some embodiments, the functional groups are conjugated to the dendrimers via a linker and/or a triggering agent. In addition, the present invention is directed to methods of synthesizing dendrimer based modular platforms, compositions comprising the dendrimer based modular platforms, as well as systems and methods utilizing the dendrimer based modular platforms (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).
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DENDRIMER CONJUGATES (Fri, 25 Jun 2010)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
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Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism (Fri, 04 Jun 2010)
The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
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PROPERTIES TAILORING IN SILSESQUIOXANES (Fri, 04 Jun 2010)
Fluoride catalyzed rearrangement reactions of polymeric silsesquioxanes [RSiO1.5]n involve reacting at least one silsesquioxane material with a catalytic amount of an organic fluoride at a temperature ranging from about -50C to about 120C thereby forming a reaction mixture for a period ranging from 60 minutes to 48 hours. To the reaction mixture, a quenching agent is added to remove fluoride from the reaction mixture. A silsesquioxane cage compound can be isolated from the reaction mixture using a precipitation or other extraction process.
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METHODS OF TREATING AUTOIMMUNE DISORDERS AND/OR INFLAMMATORY DISORDERS (Sat, 15 May 2010)
The present invention relates to dendrimer compositions configured for treating inflammatory disorders and autoimmune disorders, and related methods of synthesis. Specifically, the present invention relates to methods for treating rheumatoid arthritis with PAMAM dendrimers having functional ligands configured for treating rheumatoid arthritis (e.g., therapeutic agents, pro-drugs, targeting agents, trigger agents, imaging agents) (e.g., methotrexate).
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DENDRIMER CONJUGATES (Fri, 09 Apr 2010)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
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HIGH-THROUGHPUT ENSEMBLE-BASED DOCKING AND ELUCIDATION OF 3-DIMENSIONAL STRUCTURAL CONFORMATIONS OF FLEXIBLE BIOMOLECULAR TARGETS (Fri, 02 Apr 2010)
Methods for generating putative ligand structures capable of altering the activity of a target effector molecule comprise: constructing an elongated monomer of the target effector molecule; constructing a three dimensional model of the target effector molecule under the influence of elongation using empirical three dimensional data, the model including a conformation revealing the binding portion of the target effector molecule to a putative ligand structure; generating a plurality of computational models of the target effector molecule; filtering the plurality of computational models against the three dimensional model created experimentally using a reiterative simulation analysis algorithm operable to identify and select a plurality of computational models having a root-mean square deviation below a predetermined threshold when compared to the three dimensional model of the target effector molecule; screening a plurality of ligands to rank the binding strength of each ligand with the plurality of computational models selected and selecting one or more ligands based on the ranking.
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ANALYTICAL SYSTEM WITH PHOTONIC CRYSTAL SENSOR (Fri, 19 Mar 2010)
A system for determining whether interaction occurs between a trial substance and a target substance. The system includes a photonic crystal sensor having a photonic crystal structure and a defect member disposed adjacent the photonic crystal structure. The defect member defines an operative surface able to receive the target substance and the trial substance. The system further includes a light source that inputs a light signal to the photonic crystal structure and the defect member. The light signal is internally reflected, and a resultant output signal is outputted. The output signal relates to whether the trial substance interacts with the target substance at the operative surface. Furthermore, the system includes an identity detector that identifies the trial substance that interacts with the target substance.
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SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS (Fri, 19 Mar 2010)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
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SELECTIVE LIGANDS FOR THE DOPAMINE 3 (D3) RECEPTOR AND METHODS OF USING THE SAME (Fri, 05 Mar 2010)
Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C=O or SO2, R1 is C1-6 alkyl, R2 is aryl, heteroaryl, aryl, -(CH2)1-3aryl, or -(CH2)1-3heteroaryl, and n is 0 or 1. Methods of using the D3 receptor ligands in the treatment of diseases and conditions wherein modulation of the D3 receptor provides a benefit also are disclosed.
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Compositions and methods for treating inflammatory conditions of the bowel (Fri, 12 Feb 2010)
The present invention provides compositions and methods for treating inflammatory conditions (e.g., of the bowel). In particular, the present invention provides methods of treating (e.g., therapeutically and/or prophylactically treating) inflammatory conditions (e.g., of the bowel), compositions useful for such methods (e.g., antagonists and/or inhibitors of angiotensin II (AngII) receptor Type 1a (AT1a)), and methods of identifying, characterizing and/or optimizing such compositions. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine) and research applications.
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COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY CONDITIONS OF THE BOWEL (Fri, 12 Feb 2010)
The present invention provides compositions and methods for treating inflammatory conditions (e.g., of the bowel). In particular, the present invention provides methods of treating (e.g., therapeutically and/or prophylactically treating) inflammatory conditions (e.g., of the bowel), compositions useful for such methods (e.g., antagonists and/or inhibitors of angiotensin II (AngII) receptor Type 1a (AT1a)), and methods of identifying, characterizing and/or optimizing such compositions. Compositions and methods of the present invention find use in, among other things, clinical (e.g. therapeutic and preventative medicine) and research applications.
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PYRIMIDOTRIAZINEDIONES AND PYRIMIDOPYRIMIDINEDIONES AND METHODS OF USING THE SAME (Fri, 05 Feb 2010)
The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same.
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PROTEIN PURIFICATION TAGS AND USES THEREOF (Fri, 05 Feb 2010)
The present invention relates to fusion proteins. In particular, the present invention relates to protein tags for use in protein solubilization and purification.
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DENDRIMER CONJUGATES (Fri, 18 Dec 2009)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
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IKKi Inhibitor Therapies and Screening Methods, and Related IKKi Diagnostics (Fri, 11 Dec 2009)
The present invention provides diagnostics, screening methods, and treatment methods related to obesity, insulin resistance, diabetes, weight loss, and related disorders. In particular, the present invention provides methods of treating such conditions with IKKi inhibitors, methods of diagnosing such conditions based on IKKi status, and methods of screening candidate IKKi inhibitors.
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USE OF LEPTIN FOR THE TREATMENT OF FATTY LIVER DISEASES AND CONDITIONS (Fri, 11 Dec 2009)
The invention generally relates to the use of leptin in the treatment of a leptin- responsive disease or condition in a non-lipodystrophic subject. More particularly, the invention is directed to the use of leptin in the treatment of a fatty liver disease in a non- lipodystrophic subject with a relative leptin deficiency. The invention includes methods for the treatment of nonalcoholic steatohepatitis (NASH), alcoholic fatty liver disease (AFLD), and nonalcoholic fatty liver disease (NAFLD) in a non-lipodystrophic subject. The invention includes the treatment of conditions ranging from ectopic lipid accumulation (steatosis) to cirrhosis.
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POLYMER COMPOSITIONS, COATINGS AND DEVICES, AND METHODS OF MAKING AND USING THE SAME (Fri, 20 Nov 2009)
The disclosure provides for a biocompatible, thromboresistant coating including a chalcogenide compound that induces nitric oxide formation; and a biocompatible matrix incorporating the chalcogenide compound. Devices incorporating such coatings, and methods of making and using such coatings are also disclosed herein.
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Dendrimer conjugates (Fri, 20 Nov 2009)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
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Indole antiviral compositions and methods (Fri, 13 Nov 2009)
The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
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UV curable silsesquioxane resins for nanoprint lithography (Fri, 16 Oct 2009)
Radiation-curable silsesquioxane resin materials are employed for micro- and nanolithography. The resin materials can include a radiation-curable silsesquioxane resin and a photo-initiator having low viscosity. The low viscosity of the liquid system allows imprinting with low pressure and low temperature; e.g. room temperature. The resist's dry etching resistance is increased and the cured film is more easily separated from the mask. Due to its high modulus after cure, the material allows the fabrication of micro- and nano-features having high aspect ratios while providing a high throughput. Various pattern sizes, for example, ranging from tens of microns to as small as a few nanometers, may be achieved with the UV-curable material system.
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HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 16 Oct 2009)
The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
>> read more

IKKI INHIBITOR THERAPIES AND SCREENING METHODS, AND RELATED IKKI DIAGNOSTICS (Fri, 02 Oct 2009)
The present invention provides diagnostics, screening methods, and treatment methods related to obesity, insulin resistance, diabetes, weight loss, and related disorders. In particular, the present invention provides methods of treating such conditions with IKKi inhibitors, methods of diagnosing such conditions based on IKKi status, and methods of screening candidate IKKi inhibitors.
>> read more

SYSTEMS AND METHODS FOR IMAGING CHANGES IN TISSUE (Fri, 18 Sep 2009)
The present invention provides systems and methods for monitoring tissue regions. In particular, the present invention provides systems and methods for detecting changes in tissue regions over a period of time. In some embodiments, the systems and methods of the present invention are used to evaluate the effectiveness of a particular treatment of a tissue region. In some embodiments, the systems and methods of the present invention provide a parametric response map approach for detecting and analyzing changes in tissue regions over a period of time to detect and monitor disease or tissue health and to monitor the impact of therapeutic interventions.
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Functionalized dendrimer-encapsulated and dendrimer-stabilized nanoparticles (Fri, 21 Aug 2009)
The present invention relates to compositions comprising functionalized dendrimer-stabilized nanoparticles (DSNPs), functionalized dendrimer-encapsulated nanoparticles (DENPs) (e.g., metal DENPs), and methods of generating and using the same.
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ULTRASTRONG AND STIFF LAYERED POLYMER NANOCOMPOSITES AND HIERARCHICAL LAMINATE MATERIALS THEREOF (Fri, 10 Jul 2009)
A stiff layered polymer nanocomposite comprising a substrate adapted to receive a plurality of alternating layers of a first material and a second material; wherein the first material and second material are a polyelectrolyte, an organic polymer or an inorganic colloid and said first material and said second material have a chemical affinity for each other, said plurality of layers crosslinked using a chemical or physical crosslinking agent. Thin films that are consolidated and optionally crosslinked can be manufactured into hierarchical laminates with rigid and stress resistant properties.
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PASSIVE WIRELESS READOUT MECHANISMS FOR NANOCOMPOSITE THIN FILM SENSORS (Fri, 15 May 2009)
A method for sensing a stimulus comprising providing a sensing assembly having a first structure and a second structure, wherein the first structure is made of a material different than the second structure and each of the first structure and the second structure is nanoscale. The method further includes providing an inductive antenna operably coupled to the sensing assembly, disposing the sensing assembly upon a spatial area, exposing the sensing assembly to the stimulus thereby producing a detectable change in the sensing assembly, and wirelessly coupling a reader with the inductive antenna to obtain a signal representative of the detectable change in the sensing assembly.
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Electrical impedance tomography of nanoengineered thin films (Fri, 15 May 2009)
The present teachings relate to the application of electrical impedance tomography (EIT) to demonstrate the multifunctionality of carbon nanocomposite thin films under various types of environmental stimuli. Carbon nanotube (CNT) thin films are fabricated by a layer-by-layer (LbL) technique or other techniques and mounted with electrodes along their boundaries. The response of the thin films to various stimuli determined by relying on electric current excitation and corresponding boundary potential measurements. The spatial conductivity variations are reconstructed based on a mathematical model for the EIT technique. Here, the ability of the EIT method to provide two-dimensional mapping of the conductivity of CNT thin films is validated by (1) electrically imaging intentional structural defects in the thin films and (2) mapping the film's response to various pH environments.
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Bivalent SMAC mimetics and the uses thereof (Fri, 15 May 2009)
The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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BENZODIAZEPINONE COMPOUNDS USEFUL IN THE TREATMENT OF SKIN CONDITIONS (Fri, 15 May 2009)
The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
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2,2-Bis-(hydroxymethyl)cyclopropylidenemethyl-Purines and -Pyrimidines As Antiviral Agents (Fri, 08 May 2009)
Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
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Benzodiazepinone compounds useful in the treatment of skin conditions (Fri, 08 May 2009)
The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
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MACROCYCLIZATION OF COMPOUNDS FROM SOLID SUPPORT USING THIOESTERASES (Fri, 08 May 2009)
A method of preparing macrocycles using solid support chemistry and thioesterases is disclosed. Also disclosed are novel macrocycles.
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ENANTIOSELECTIVE SYNTHESIS OF CERAMIDE-LIKE COMPOUNDS, NOVEL INTERMEDIATES, THEIR PREPARATION AND PYRROLE DERIVATIVES (Tue, 05 May 2009)

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Macrocyclization of compounds from solid support using thioesterases (Fri, 01 May 2009)
A method of preparing macrocycles using solid support chemistry and thioesterases is disclosed. Also disclosed are novel macrocycles.
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Small molecule antagonists of Bcl-2 family proteins (Fri, 10 Apr 2009)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
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DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME (Fri, 03 Apr 2009)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 20 Mar 2009)
The present invention relates to cancer markers. In particular, the present invention provides metabolites that are differentially present in prostate cancer.
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F1F0-ATPASE INHIBITORS AND RELATED METHODS (Fri, 20 Mar 2009)
The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
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COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION (Fri, 20 Mar 2009)
The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
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Strategies, linkers and coordination polymers for high-performance sorbents (Fri, 06 Mar 2009)
A linking ligand compound includes three bidentate chemical moieties distributed about a central chemical moiety. Another linking ligand compound includes a bidentate linking ligand and a monodentate chemical moiety. Coordination polymers include a plurality of metal clusters linked together by residues of the linking ligand compounds.
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NOVEL STRATEGIES, LINKERS AND COORDINATION POLYMERS FOR HIGH-PERFORMANCE SORBENTS (Fri, 06 Mar 2009)
A linking ligand compound includes three bidentate chemical moieties distributed about a central chemical moiety. Another linking ligand compound includes a bidentate linking ligand and a monodentate chemical moiety. Coordination polymers include a plurality of metal clusters linked together by residues of the linking ligand compounds.
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Dendrimer based compositions and methods of using the same (Fri, 27 Feb 2009)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 27 Feb 2009)
The present invention relates to cancer markers. In particular, the present invention provides metabolites that are differentially present in prostate cancer. The present invention further provides diagnostic, research, and therapeutic applications targeting cancer specific metabolites.
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METABOLOMIC CANCER TARGETS (Fri, 20 Feb 2009)
The present invention relates to cancer markers. In particular, the present invention provides metabolites that are differentially present in prostate cancer and methods of inhibiting the growth of a cell by altering the level of such metabolites.
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Systems and methods for tissue imaging (Fri, 06 Feb 2009)
The present invention provides systems and methods for monitoring tissue regions. In particular, the present invention provides systems and methods for detecting changes in tissue regions over a period of time. In some embodiments, the systems and methods of the present invention are used to evaluate the effectiveness of a particular treatment of a tissue region. In some embodiments, the systems and methods employ functional diffusion map algorithms for imaging changes in tissue regions over time and/or in response to therapeutic interventions.
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DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME (Fri, 16 Jan 2009)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
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Plasminogen Activator Inhibitor-1 Inhibitors And Methods Of Use Thereof To Modulate Lipid Metabolism (Fri, 09 Jan 2009)
The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 26 Dec 2008)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. In particular, the present invention provides methods and devices for generating a photogenerated reaction in solution on a substrate comprising generating a light beam using an optical device system comprising a light source and a computer-controlled spatial optical modulator comprising a digital micromirror device and using the spatial optical modulator to direct light to fluidly isolated reaction sites under conditions such that a photogenerated reaction takes place. The method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces.
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Protein MicroarraySystem (Fri, 14 Nov 2008)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of the phosphorylation status of protein samples, including the generation and analysis of protein microarrays.
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Compositions and methods relating to novel compounds and targets thereof (Fri, 31 Oct 2008)
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
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Conformationally constrained Smac mimetics and the uses thereof (Fri, 31 Oct 2008)
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF TO MODULATE LIPID METABOLISM (Fri, 31 Oct 2008)
The invention relates to plasminogen activator- 1 (PAl-1I) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.
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COMPOSITIONS AND METHODS FOR CHARACTERIZING, REGULATING, DIAGNOSING, AND TREATING CANCER (Fri, 24 Oct 2008)
The present invention relates to compositions and methods for characterizing, regulating, diagnosing, and treating cancer. For example, the present invention provides compositions and methods for inhibiting tumorigenesis of certain classes of cancer cells, including breast cancer cells and preventing metastasis. The present invention also provides systems and methods for identifying compounds that regulate tumorigenesis.
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DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 24 Oct 2008)
The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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SYSTEMS AND METHODS FOR TISSUE IMAGING (Fri, 24 Oct 2008)
The present invention provides systems and methods for monitoring tissue regions. In particular, the present invention provides systems and methods for detecting changes in tissue regions over a period of time. In some embodiments, the systems and methods of the present invention are used to evaluate the effectiveness of a particular treatment of a tissue region. In some embodiments, the systems and methods employ functional diffusion map algorithms for imaging changes in tissue regions over time and/or in response to therapeutic interventions.
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DELIVERY DEVICE AND METHOD FOR FORMING THE SAME (Fri, 24 Oct 2008)
A delivery device (10) includes a hollow container (20), and a plurality of biodegradable and/or erodible polymeric layers (22) established in the container (20). A layer (24) including a predetermined substance is established between each of the plurality of polymeric layers (22), whereby degradation of the polymeric layer (22) and release of the predetermined substance occur intermittently. Methods for forming the device (10) are also disclosed herein.
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Carboxylic acid-modified EDOT for bioconjugation (Fri, 19 Sep 2008)
An electroconductive carboxylic acid functionalized monomer corresponding to Formula (I), wherein A represents a hydrogen or a carboxyl group. Polymerized monomers of Formula (I) conjugated with a biomolecule result in conjugated PEDOT polymers of Formula (III) wherein A is a hydrogen or a carboxylic acid group and B is a biomolecule selected from the group consisting of a peptide, a protein, a lipid, a carbohydrate and a polynucleotide. The biomolecule conjugated polymers can be disposed onto an electrically conductive substrate wherein the substrate has a first layer of PEDOT polymerized on a surface of the substrate and a second layer of biomolecule conjugated PEDOT polymer of Formula (III) polymerized on the first layer of PEDOT. The first and second layers form a charge transport material in electrical communication with the conductive substrate. The electrically conductive substrate further comprises a dopant.
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COMPOSITIONS AND METHODS RELATING TO NOVEL COMPOUNDS AND TARGETS THEREOF (Fri, 19 Sep 2008)
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
>> read more

Methods for production and use of synthetic hydroxyapatite and fluorapatite nanorods, and superstructures assembled from the same (Fri, 12 Sep 2008)
Disclosed herein are methods directed toward the synthesis of ordered structures of hydroxyapatite and hydroxyapatite derivatives. More specifically, disclosed herein is a method of preparing ordered hydroxyapatite nanorod structures including the steps of suspending calcium and phosphate in a solvent, adjusting the pH to above 5, and heating to a temperature sufficient to support formation of the ordered hydroxyapatite nanorod structures. In some cases, the methods may include ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid derivatives. Also disclosed are methods that additionally involve a step of coating hydroxyapatite nanorods with a protein or an amphiphile such as a surfactant or polymer.
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CARBOXYLIC ACID-MODIFIED EDOT FOR BIOCONJUGATION (Fri, 05 Sep 2008)
An electroconductive carboxylic acid functionalized monomer corresponding to Formula (I), wherein A represents a hydrogen or a carboxyl group. Polymerized monomers of Formula (I) conjugated with a biomolecule result in conjugated PEDOT polymers of Formula (III) wherein A is a hydrogen or a carboxylic acid group and B is a biomolecule selected from the group consisting of a peptide, a protein, a lipid, a carbohydrate and a polynucleotide. The biomolecule conjugated polymers can be disposed onto an electrically conductive substrate wherein the substrate has a first layer of PEDOT polymerized on a surface of the substrate and a second layer of biomolecule conjugated PEDOT polymer of Formula (III) polymerized on the first layer of PEDOT. The first and second layers form a charge transport material in electrical communication with the conductive substrate. The electrically conductive substrate further comprises a dopant.
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Protein microarray system (Fri, 27 Jun 2008)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of protein samples. The present invention thus provides improved methods for the separation and analysis of samples containing a plurality of proteins (e.g., cells).
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Indole antiviral compositions and methods (Fri, 20 Jun 2008)
The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
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Conformationally constrained Smac mimetics and the uses thereof (Fri, 06 Jun 2008)
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
>> read more

Indole inhibitors of MDM2 and the uses thereof (Fri, 30 May 2008)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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Protein separation and analysis (Fri, 25 Apr 2008)
The present invention relates to multi-phase protein separation methods capable of resolving and characterizing large numbers of cellular proteins, including methods for efficiently facilitating the transfer of protein samples between separation phases. In particular, the present invention provides systems and methods for the differential display of protein samples from multiple cell types. The present invention thus provides improved methods for the analysis of multiple samples containing large numbers of proteins. 
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 18 Apr 2008)
The present invention provides polypeptides involved in cryptophycin biosynthesis and the nucleic acid molecules that encode such polypeptides. The nucleic acid molecules and polypeptides of the invention or variants thereof can be used in the methods of the invention to produce cryptophycins.
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Bivalent Smac mimetics and the uses thereof (Fri, 18 Apr 2008)
The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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NEW SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF (Fri, 28 Mar 2008)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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FRET-based apoptosis detector (Fri, 21 Mar 2008)
The present invention relates to compositions comprising a FRET-based substrate, a cell-targeting moiety and a dendrimer, and methods for generating and using the same. 
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Small molecule inhibitors targeted at Bcl-2 (Fri, 07 Mar 2008)
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs. 
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Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents (Fri, 29 Feb 2008)
This invention relates to a method of imaging vesicular monoamine transporters and to labeled compounds and pharmaceutical compositions thereof, and methods of making labeled compounds useful in imaging vesicular monoamine transporters. This invention also relates to compounds, and methods of monitoring progression of a disease related to vesicular monoamine transporters. 
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 29 Feb 2008)
The present invention provides polypeptides involved in cryptophycin biosynthesis and the nucleic acid molecules that encode such polypeptides. The nucleic acid molecules and polypeptides of the invention or variants thereof can be used in the methods of the invention to produce cryptophycins.
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Production of gossypol co-crystals (Fri, 25 Jan 2008)
This invention relates to relates to methods for producing gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals. The invention also relates to pharmaceutical compositions comprising gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals and the use of gossypol acetic acid co-crystals and (−)-gossypol acetic acid co-crystals for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
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Small molecule antagonists of XIAP family proteins (Fri, 25 Jan 2008)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
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DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME (Fri, 18 Jan 2008)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
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FRET-BASED APOPTOSIS DETECTOR (Fri, 18 Jan 2008)
The present invention relates to compositions comprising a FRET-based substrate, a cell-targeting moiety and a dendrimer, and methods for generating and using the same.
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Gossypol co-crystals and the use thereof (Fri, 21 Dec 2007)
This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
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PYRIMIDONE DERIVATIVES WHICH ARE MODULATORS OF HEAT SHOCK PROTEIN (HSP) 70 (Fri, 16 Nov 2007)
The present disclosure is directed to new compounds of formula (I) useful as modulators of Heat Shock Proteins (HSP). In particular, the present disclosure provides new small molecule peptide-derived compounds having HSP modulation activity, especially Hsp70 modulation activity, and methods of preventing or ameliorating beta-amyloid or polyglutamine aggregation, decreasing cell proliferation, or increasing chaperon activity of the HSPs.
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BIVALENT SMAC MIMETICS AND THE USES THEREOF (Fri, 16 Nov 2007)
The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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RADIOLABELED DIHYDROTETRABENAZINE DERIVATIVES AND THEIR USE AS IMAGING AGENTS (Fri, 16 Nov 2007)
This invention relates to a method of imaging vesicular monoamine transporters and to labeled compounds and pharmaceutical compositions thereof, and methods of making labeled compounds useful in imaging vesicular monoamine transporters. This invention also relates to compounds, and methods of monitoring progression of a disease related to vesicular monoamine transporters.
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Brain-Associated Inhibitor of Tissue-Type Plasminogen Activator (Fri, 09 Nov 2007)
The present invention relates to a novel BAIT protein which is a member of serpin superfamily which is expressed primarily in brain tissue. In particular, isolated nucleic acid molecules are provided encoding the human and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of BAIT activity. Also provided are diagnostic methods for detecting nervous system-related disorders and therapeutic methods for treating nervous system-related disorders. Additionally, the present invention is related to methods of treating patients with BAIT polynucleotides or polypeptides, wherein said patients have had seizures or epilepsy. 
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METHODS AND REAGENTS FOR ACTIVATING HEAT SHOCK PROTEIN 70 (Fri, 09 Nov 2007)
The present disclosure is directed to new compounds useful as modulators of Heat Shock Proteins (HSP). In particular, the present disclosure provides new small molecule peptide-derived compounds having HSP modulation activity, especially Hsp70 modulation activity, and methods of preventing or ameliorating beta-amyloid or polyglutamine aggregation, decreasing cell proliferation, or increasing chaperon activity of the HSPs. 
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PRODUCTION OF GOSSYPOL CO-CRYSTALS (Fri, 09 Nov 2007)
This invention relates to relates to methods for producing gossypol acetic acid co- crystals and (-)-gossypol acetic acid co-crystals. The invention also relates to pharmaceutical compositions comprising gossypol acetic acid co-crystals and (-)-gossypol acetic acid co-crystals and the use of gossypol acetic acid co-crystals and (-)-gossypol acetic acid co-crystals for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
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Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors (Fri, 31 Aug 2007)
Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
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VIABLE NON-TOXIC GRAM NEGATIVE BACTERIA (Fri, 27 Jul 2007)
The present invention provides non-toxic Gram-negative bacteria. In particular, the present invention provides viable Gram-negative bacteria (e.g., E. coli) substantially lacking lipopolysaccharide (LPS, endotoxin) within the outer membrane. The present invention further provides methods of generating viable non-toxic Gram-negative bacteria and uses thereof. The present invention also provides compositions and methods for inducing immune responses and for researching and developing therapeutic agents.
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METHODS AND COMPOSITIONS FOR DRUG DELIVERY ENHANCEMENT (Fri, 15 Jun 2007)
A method is provided for the delivery of a therapeutic to epithelial cells through the use of a bile acid conjugated to a peptide, the peptide being ionically charged at physiological pH. The complex is well suited for oral and other forms of therapeutic administration of therapeutic drugs known in the art in order to exact systemic and/or localized effect. Intestinal epithelial cells, as well as non-epithelial cells within the gastrointestinal tract and other target cells receive with greater efficiency a charged therapeutic when delivered with an oppositely charged bile acid conjugate (BAC) through oral administration, direct injection, or infusive administrations, thereby increasing bioavailability.
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POLYMER COMPOSITIONS, COATINGS AND DEVICES, AND METHODS OF MAKING AND USING THE SAME (Fri, 08 Jun 2007)
The disclosure provides for a biocompatible, thromboresistant coating including a chalcogenide compound that induces nitric oxide formation; and a biocompatible matrix incorporating the chalcogenide compound. Devices incorporating such coatings, and methods of making and using such coatings are also disclosed herein.
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Small molecule transcriptional activation domains (Fri, 11 May 2007)
The present invention relates to gene regulation. In particular, the present invention provides small molecule activation domain compositions and methods of making the same. The present invention further provides methods of regulating gene expression using the novel activation domains. The invention also provides methods of screening small molecule/compound libraries for identifying ligands of a protein or molecule of interest.
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Dendrimer based compositions and methods of using the same (Fri, 23 Feb 2007)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor). 
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NITRIC OXIDE COATINGS FOR MEDICAL DEVICES (Fri, 12 Jan 2007)
The disclosure provides for devices and coatings that are substantially free of organic solvent sand suitable for insertion into a patient, and that comprise a metal layer and a coating with a thickness of about 20 nm to about 2000 nm wherein the coating comprises a biocompatible polymer comprising at least one residue covalently bonded to a nitric oxide generating compound.
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Chromen-4-one inhibitors of anti-apoptotic Bcl-2 family members and the uses thereof (Fri, 03 Nov 2006)
The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death. 
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PROTEIN MICROARRAY SYSTEM (Fri, 06 Oct 2006)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of the phosphorylation status of protein samples, including the generation and analysis of protein microarrays.
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 22 Sep 2006)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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CHROMEN-4-ONE INHIBITORS OF ANTI-APOPTOTIC BCL-2 FAMILY MEMBERS AND THE USES THEREOF (Fri, 22 Sep 2006)
The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
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SMALL MOLECULE INHIBITORS OF MDM2 AND USES THEREOF (Fri, 01 Sep 2006)
The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
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INDOLE ANTIVIRAL COMPOUNDS AND COMPOSITIONS COMPRISING THEM (Mon, 21 Aug 2006)

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SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS (Thu, 27 Jul 2006)
 The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-XL proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-XL).
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ULTRAVIOLET TRANSMISSIVE POLYHEDRAL SILSESQUIOXANE POLYMERS (Fri, 16 Jun 2006)
Inorganic/organic hybrid polymers containing silsesquioxane cages are robust and exhibit desirable physical properties such as strength, hardness, and optical transparency at infrared and ultraviolet wavelengths. The polymers are prepared by polymerizing functionalized polyhedral silsesquioxane monomers such as polyhedral silsesquioxanes bearing two complementarily reactive functional groups bonded to cage silicon atoms by means of spacer moieties. The spacer moieties allow for steric mobility and more complete cure than polyhedral silsesquioxanes bearing reactive functional groups bound directly to cage silicon atoms.
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Ultraviolet transmissive polyhedral silsesquioxane polymers (Fri, 09 Jun 2006)
Inorganic/organic hybrid polymers containing silsesquioxane cages are robust and exhibit desirable physical properties such as strength, hardness, and optical transparency at infrared and ultraviolet wavelengths. The polymers are prepared by polymerizing functionalized polyhedral silsesquioxane monomers such as polyhedral silsesquioxanes bearing two complementarily reactive functional groups bonded to cage silicon atoms by means of spacer moieties. The spacer moieties allow for steric mobility and more complete cure than polyhedral silsesquioxanes bearing reactive functional groups bound directly to cage silicon atoms.
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METHODS FOR PRODUCTION OF SYNTHETIC HYDROXYAPATITE NANORODS (Fri, 12 May 2006)
Disclosed herein are methods directed toward the synthesis of ordered structures of hydroxyapatite and hydroxyapatite derivatives. More specifically, disclosed herein is a method of preparing ordered hydroxyapatite nanorod structures including the steps of suspending calcium and phosphate in a solvent, adjusting the pH to above 5, and heating to a temperature sufficient to support formation of the ordered hydroxyapatite nanorod structures. In some cases, the methods may include ethylenediamine tetraacetic acid or ethylenediamine tetraacetic acid derivatives. Also disclosed are methods that additionally involve a step of coating hydroxyapatite nanorods with a protein or an amphiphile such as a surfactant or polymer.
>> read more

Small molecule inhibitors of anti-apoptotic BCL-2 family members and the uses thereof (Fri, 21 Apr 2006)
The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death. 
>> read more

DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME (Fri, 31 Mar 2006)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
>> read more

Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 17 Mar 2006)
The present invention provides polypeptides involved in cryptophycin biosynthesis and the nucleic acid molecules that encode such polypeptides. The nucleic acid molecules and polypeptides of the invention or variants thereof can be used in the methods of the invention to produce cryptophycins.
>> read more

SMALL MOLECULE INHIBITORS OF ANTI-APOPTOTIC BCL-2 FAMILY MEMBERS AND THE USES THEREOF (Fri, 03 Mar 2006)
The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
>> read more

CONFORMATIONALLY CONSTRAINED SMAC MIMETICS AND THE USES THEREOF (Fri, 27 Jan 2006)
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
>> read more

Amino ceramide-like compounds and therapeutic methods of use (Fri, 02 Dec 2005)
The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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ANTIHELMINTHIC ANTHRAQUINONES AND METHOD OF USE THEROF (Thu, 01 Dec 2005)
y roxy, aogen, a y, su s a , n , u , , ry, su stituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, 15 carbohydrate, or combination thereof, and the halogen is I, F, Br, or CI.
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Amino ceramide-like compounds and therapeutic methods of use (Fri, 28 Oct 2005)
 Novel amino ceramide-like compounds (1) are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels. <chemistry id="chem-us-00001-en" num="1"><img id="emi-c00001" he="50.63mm" wi="76.20mm" file="US20050239862A1-20051027-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry>
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Protein microarray system (Fri, 21 Oct 2005)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of the phosphorylation status of protein samples, including the generation and analysis of protein microarrays. 
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Compositions and methods for characterizing, regulating, diagnosing, and treating cancer (Fri, 21 Oct 2005)
The present invention relates to compositions and methods for characterizing, regulating, diagnosing, and treating cancer. For example, the present invention provides compositions and methods for inhibiting tumorigenesis of certain classes of cancer cells, including breast cancer cells and preventing metastasis. The present invention also provides systems and methods for identifying compounds that regulate tumorigenesis. 
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Gossypol co-crystals and the use thereof (Fri, 21 Oct 2005)
This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
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Mixed-metal oxide particles by liquid feed flame spray pyrolysis of oxide precursors in oxygenated solvents (Fri, 14 Oct 2005)
Liquid feed flame spray pyrolysis of solutions of a metal oxide precursor which is an alkoxide or C1-6 carboxylate and at least one second metal oxide precursor and/or second metal compound dissolved in oxygenated solvent by combustion with oxygen lead to the formation of sub-micron mixed-metal oxide powders not accessible by other processes or by the pyrolysis of metal chlorides or nitrates. The powders have numerous uses in advanced materials applications including particulate solid state lasers, advanced ceramic materials, and as catalysts in organic synthesis and automobile exhaust systems.
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GOSSYPOL CO-CRYSTALS AND THE USE THEREOF (Fri, 14 Oct 2005)
This invention relates to compositions comprising co-crystals of (-)- gossypol with a C 1-8 carboxylic acid or C 1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of cocrystals of (-)-gossypol with a C 1-8 carboxylic acid or C 1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
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Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors (Fri, 07 Oct 2005)
Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
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SMALL MOLECULE ANTAGONISTS OF XIAP FAMILY PROTEINS (Fri, 07 Oct 2005)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).
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Noninvasive method to determine fat content of tissues using MRI (Fri, 30 Sep 2005)
The present invention relates to systems and methods for generating high resolution MR images of the fractional amount or percentage of fat content in an imaged object. In particular, the present invention relates to systems and methods for obtaining high resolution MR images of fat content with reduced NMR relaxation effects. Moreover, the present invention relates to systems and methods for obtaining high resolution MR images of fat content with reduced fat-percentage ambiguity. Furthermore, the present invention relates to systems and methods for diagnostic, and prognostic imaging where knowledge of fat content within tissues, organs, and lesions is beneficial to improve diagnostic accuracy, aid in risk assessment of future disease, and aid in assessment of therapeutic intervention. 
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Eglin c based drugs for treatment of disease (Fri, 16 Sep 2005)
The present invention relates to eglin c variants which inhibit proteases, and in particular to eglin c mutants at adventitious contact sites. The present invention also relates to eglin c variants which comprise mutations in both adventitious contact sites and at reactive loop sites. The present invention further relates to methods of preparing the eglin c variants, and methods of using the eglin c variants for treatment of diseases including acute bacterial, viral, and fungal infections.
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COMPOSITIONS AND METHODS FOR CHARACTERIZING, REGULATING, DIAGNOSING, AND TREATING CANCER (Fri, 19 Aug 2005)
The present invention relates to compositions and methods for characterizing, regulating, diagnosing, and treating cancer. For example, the present invention provides compositions and methods for inhibiting tumorigenesis of certain classes of cancer cells, including breast cancer cells and preventing metastasis. The present invention also provides systems and methods for identifying compounds that regulate tumorigenesis.
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SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS (Fri, 05 Aug 2005)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the nati-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2 Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotheratpeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
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CONFORMATIONALLY CONSTRAINED SMAC MIMETICS AND THE USES THEREOF (Fri, 05 Aug 2005)
The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
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Facile synthesis of polyhedral silsesquioxane anions and use thereof (Fri, 01 Jul 2005)
Polyhedral silsesquioxane anions are economically prepared by reaction of a silica source derived from combusted organic material with a quaternary ammonium hydroxide compound. Reaction of the resulting anions with chlorosilanes may be effected in near stoichiometric fashion in organic solvent containing reactive quantities of organic acids such as formic acid. The functional groups on the resulting functionalized silsesquioxanes may be substituted for other functional groups by reaction with di- or polysiloxanes in the presence of a synthetic ion exchange resin.
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2-amino-9-[(2-hydroxymethyl) cyclopropylidenemethyl] purine antiviral agents (Fri, 10 Jun 2005)
Compounds which are active against viruses have the following Formulas: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="44.53mm" wi="55.88mm" file="us07183268-20070227-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 B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR1, OR2, or SR3;</li> <li>R1 is selected from the group consisting of alkyl, alkenyl, alkynyl, and C4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl;</li> <li>R2 is selected from the group consisting of C2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and</li> <li>R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.</li> </ul> </li> </ul> 
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Azaborolyl group 4 metal complexes, catalysts and olefin polymerization process (Fri, 03 Jun 2005)
Metal complexes, catalysts derived therefrom, and polymerization processes using the same, characterized by the presence of one or more nitrogen and boron containing, anionic 5-membered cyclic ligand groups, especially 1,2-azaborolyl groups, are disclosed.
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2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents (Fri, 27 May 2005)
Compounds which are active against viruses have the following formulas: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="19.47mm" wi="65.19mm" file="US07393855-20080701-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines. 
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Amino ceramide-like compounds and therapeutic methods of use (Wed, 11 May 2005)
Novel amino ceramide-like compounds (1) are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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FACILE SYNTHESIS OF POLYHEDRAL SILSESQUIOXANE ANIONS AND USE THEREOF (Sat, 07 May 2005)
Polyhedral silsesquioxane anions are economically prepared by reaction of a silica source derived from combusted organic material with a quaternary ammonium hydroxide compound. Reaction of the resulting anions with chlorosilanes may be effected in near stoichiometric fashion in organic solvent containing reactive quantities of organic acids such as formic acid. The functional groups on the resulting functionalized silsesquioxanes may be substituted for other functional groups by reaction with di- or polysiloxanes in the presence of a synthetic ion exchange resin.
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INDOLE ANTIVIRAL COMPOSITIONS AND METHODS (Fri, 22 Apr 2005)
The present invention provides novel chemical compounds and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
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Methods for incorporating non-perfectly matched oligonucleotides into target-specific hybridization sequences (Fri, 25 Mar 2005)
The present invention provides a method of designing target-specific hybridization sequences which include one or more mutations. The method of the invention comprises selecting a candidate target nucleotide sequence in a subject nucleotide sequence. A first complementary nucleotide sequence to the target nucleotide sequence is identified by applying the known bonding relationships of the nucleotides. Next, a second complementary nucleotide sequence having one or more mutations is constructed. The amount of the “target-second complementary nucleotide sequence” hybrid formed when the candidate target nucleotide sequence and second complementary nucleotide sequences are combined in the presence of interfering sequences is characterized and used to assess utility of the second complementary nucleotide sequence. The present invention also provides the target-specific hybridization sequences designed by the methods of the invention.
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Replication deficient adenovirus vectors and methods of making and using them (Wed, 16 Mar 2005)
The invention provides novel replication deficient adenovirus vectors and methods for making and using these viruses. The invention also provides vector systems and kits using a serotype specific strategy for making adenoviral vector preparations substantially free of replication competent “helper” virus. The helper virus-free preparations provide novel pharmaceutical compositions substantially free of helper virus for use in gene transfer and gene therapy.
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CHEMICAL ADDRESS TAGS (Fri, 11 Mar 2005)
The present invention provides methods and compositions related to the fields of chemoinformatics, chemogenomics, drug discovery and development, and drug targeting. In particular, the present invention provides subcellular localization signals (e.g., chemical address tags) that influence (e.g., direct) subcellular and organelle level localization of associated compounds (e.g., drugs and small molecule therapeutics, radioactive species, dyes and imagining agents, proapoptotic agents, antibiotics, etc) in target cells and tissues. The compositions of the present invention modulate the pharmacological profiles of associated compounds by influencing the compound's accumulation, or exclusion, from subcellular loci such as mitochondria, endoplasmic reticulum, cytoplasm, vesicles, granules, nuclei and nucleoli and other subcellular organelles and compartments. The present invention also provides methods for identifying chemical address tags, predicting their targeting characteristics, and for rational designing chemical libraries comprising chemical address tags.
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Amino ceramide-like compounds and therapeutic methods of use (Fri, 04 Mar 2005)
The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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Drug delivery compositions (Fri, 25 Feb 2005)
The present invention relates to multicomponent compositions and methods of administering these compositions, which specifically translocate therapeutic molecules (e.g., drugs or prodrugs) across biological membranes thus reducing potential toxic side effects on nontargeted cells and tissues.
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2-hydroxymethylcyclopropylidene methylpurines and -pyrimidines as antiviral agents (Fri, 14 Jan 2005)
Compounds which are active against viruses have the following Formulas: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="57.49mm" wi="64.43mm" file="US06958345-20051025-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH. 
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Blood-pool carrier for lipophilic imaging agents (Fri, 24 Dec 2004)
A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
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METHODS FOR INCORPORATING NON-PERFECTLY MATCHED OLIGONUCLEOTIDES INTO TARGET-SPECIFIC HYBRIDIZATION SEQUENCES (Fri, 17 Dec 2004)
The present invention provides a method of designing target-specific hybridization sequences which include one or more mutations. The method of the invention comprises selecting a candidate target nucleotide sequence in a subject nucleotide sequence. A first complementary nucleotide sequence to the target nucleotide sequence is identified by applying the known bonding relationships of the nucleotides. Next, a second complementary nucleotide sequence having one or more mutations is constructed. The amount of the 'target-second complementary nucleotide sequence' hybrid formed when the candidate target nucleotide sequence and second complementary nucleotide sequences are combined in the presence of interfering sequences is characterized and used to assess utility of the second complementary nucleotide sequence. The present invention also provides the target-specific hybridization sequences designed by the methods of the invention.
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Protein microarray system (Fri, 29 Oct 2004)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of protein samples. The present invention thus provides improved methods for the separation and analysis of samples containing a plurality of proteins (e.g., cells). 
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Small molecule antagonists of Bcl-2 family proteins (Fri, 29 Oct 2004)
The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
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Brain-associated inhibitor of tissue-type plasminogen activator (Fri, 15 Oct 2004)
The present invention relates to a novel BAIT protein which is a member of serpin superfamily which is expressed primarily in brain tissue. In particular, isolated nucleic acid molecules are provided encoding the human and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of BAIT activity. Also provided are diagnostic methods for detecting nervous system-related disorders and therapeutic methods for treating nervous system-related disorders. Additionally, the present invention is related to methods of treating patients with BAIT polynucleotides or polypeptides, wherein said patients have had seizures or epilepsy.
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NON-TOXIC MEMBRANE-TRANSLOCATING PEPTIDES (Fri, 24 Sep 2004)
Compositions for transport across a biological membrane include a membrane-translocating LMWP peptide and a cargo molecule. Methods for transporting a cargo molecule across a biological membrane are also described.
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PHARMACEUTICAL CO-CRYSTAL COMPOSITIONS OF DRUGS SUCH AS CARBAMAZEPINE, CELECOXIB, OLANZAPINE, ITRACONAZOLE, TOPIRAMATE, MODAFINIL, 5-FLUOROURACIL, HYDROCHLOROTHIAZIDE, ACETAMINOPHEN, ASPIRIN, FLURBIPROFEN, PHENYTOIN AND IBUPROFEN (Fri, 17 Sep 2004)
A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
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Lithium-based zeolites containing silver and copper and use thereof for selective absorption (Wed, 25 Aug 2004)
The invention provides new methods for separating nitrogen from a mixture. The invention provides adsorbents specifically for accomplishing nitrogen separation. The adsorbents and separation methods are particularly useful for the selective adsorption of nitrogen from air. In one aspect, the adsorbent comprises an ion exchange zeolite X and preferably zeolite LSX (low silica zeolite X). The zeolite is most preferably a lithium-based zeolite. Further, the zeolite has exchangeable cationic sites, with silver cation or copper cation occupying at least some of the exchangeable cationic sites. The Ag/Cu exchanged zeolite is heat-treated under specific conditions as per the invention. The presence of the silver cation or copper cation at any of the sites will provide an improvement over the non-exchanged zeolite.
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Methods of using latent TGF-β binding proteins (Wed, 11 Aug 2004)
Disclosed are novel nucleic acid and peptide compositions comprising latent TGFβ binding proteins (LTBPs). Also disclosed are methods of using LTBP-2 and LTBP-3 peptides and the DNA segments which encode them.
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Antihelminthic anthraquinones and method of use thereof (Fri, 06 Aug 2004)
Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="24.64mm" wi="36.66mm" file="US07132403-20061107-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl. 
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Biocompatible dendrimers (Fri, 06 Aug 2004)
The present invention relates to compositions and methods involving biocompatible dendrimers. In particular, the present invention provides dendrimeric copolymers with poly(propyleneimine) (POPAM) interiors and poly(amidoamine) (PAMAM) exteriors for use in transfection and imaging applications.
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Crosslinked DNA condensate compositions and gene delivery methods (Wed, 04 Aug 2004)
Disclosed are improved compositions and methods for use in gene delivery and expression. A range of surprisingly effective cross-linking agents and peptides are provided, as are peptide-DNA carrier compositions and condensed particles with reduced toxicity and increased stability. Advantageous methods of using such compositions in gene delivery and gene expression are further disclosed, which may be used in combination with biocompatible matrices, carriers and/or targeting agents.
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METHOD TO FORM A PROTEIN MICROARRAY SYSTEM (Fri, 30 Jul 2004)
The present invention relates to automated methods, systems, and apparatuses protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of protein samples. The present invention thus provides improved methods for the separation and analysis of samples containing a plurality of proteins (e.g., cells).
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Multidimensional protein separation system (Fri, 16 Jul 2004)
The present invention relates to systems, apparatuses and methods for multidimensional protein separation. In particular, the present invention relates to 3-dimension protein separation and characterization systems and methods. 
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Antihelminthic anthraquinones and method of use thereof (Fri, 18 Jun 2004)
Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="24.55mm" wi="36.66mm" file="US06838443-20050104-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl. 
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Antihelminthic anthraquinones and method of use thereof (Fri, 04 Jun 2004)
Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: <chemistry id="chem-us-00001-en" num="00001"><img id="emi-c00001-en" he="24.55mm" wi="36.83mm" file="US06903076-20050607-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/></chemistry> wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl. 
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PROCESS FOR PRODUCING POLYALKYLENE CARBONATES (Fri, 07 May 2004)
The present invention relates to a process for the preparation of polyalkylene carbonate, an alternating copolymer, obtainable from the ring opening of an alkene oxide or an alkene oxide precursor in the presence of carbon dioxide or any substance delivering carbon oxide, in the presence of at least one catalyst containing a metal-organic framework material, wherein said framework material comprises pores and a metal ion and an at least bidentate organic compound, said bidentate organic compound being coordinately bound to the metal ion.
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MULTIDIMENSIONAL PROTEIN SEPARATION SYSTEM (Fri, 30 Apr 2004)
The present invention relates to systems, apparatuses and methods for multidimensional protein separation. In particular, the present invention relates to 3-dimension protein separation and characterization systems and methods.
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Benzimidazole derivatives. (Wed, 17 Mar 2004)
The present invention relates to certain benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
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Method and apparatus for chemical and biochemical reactions using photo-generated reagents (Fri, 27 Feb 2004)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. Specifically, the method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces. 
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Automated protein analysis system (Fri, 20 Feb 2004)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis. In particular, the present invention provides an automated system for the separation, identification, and characterization of protein samples. The present invention thus provides improved methods for the separation and analysis of samples containing a plurality of proteins (e.g., cells). 
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 06 Feb 2004)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. Specifically, the method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces. 
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Thiomolybdate analogues and uses thereof (Fri, 30 Jan 2004)
The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation.
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THIOMOLYBDATE ANALOGUES AND USES THEREOF (Fri, 30 Jan 2004)
The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation.
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2-AMINO-9-[(2-HYDROXYMETHYL) CYCLOPROPYLIDENEMETHYL] PURINE ANTIVIRAL AGENTS (Fri, 23 Jan 2004)
Compounds which are active against viruses have the Formulas (I) and (II), wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR1, OR2, or SR3; Rl is selected from the group consisting of alkyl, alkenyl, alkynyl, and C4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl; R2 is selected from the group consisting of C2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.
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Protein mapping (Fri, 16 Jan 2004)
The present invention relates to multiphase protein separation methods capable of resolving large numbers of cellular proteins. The methods of the present invention provide protein profile maps for imaging and comparing protein expression patterns. The present invention provides alternatives to traditional 2-D gel separation methods for the screening of protein profiles. 
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2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS (Fri, 19 Dec 2003)
Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
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AUTOMATED PROTEIN ANALYSIS SYSTEM COMPRISING CAPILLARY ELECTROPHORESIS-TANDEM MASS SPECTROMETRY (Fri, 12 Dec 2003)
The present invention relates to automated methods, systems, and apparatuses for protein separation and analysis, based on capillary electrophoresis-tandem mass spectrometry, according to the Scheme represented in Figure 30. Proteins can be preliminary separated using multidimensional chromatography or 2D gel electrophoresis with isoelectric point in a first dimension and hydrophobicity in a second dimension. The present invention thus provides improved methods for the separation and analysis of samples containing a plurality of proteins (e.g. of cells).
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Blood-pool selective carrier for lipophilic imaging agents (Wed, 12 Nov 2003)
A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
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Polymers containing polysaccharides such as alginates or modified alginates (Wed, 05 Nov 2003)
Materials which contain polysaccharide chains, particularly alginate or modified alginate chains. The polysaccharide chains may be included as side chains or auxiliary chains from a backbone polymer chain, which may also be a polysaccharide. Further, the polysaccharide chains may be cross-linked between side chains, auxiliary chains and/or backbone chains. These materials and non-modified or otherwise modified alginate materials are advantageously modified by covalent bonding thereto of a biologically active molecule for cell adhesion or other cellular interaction. Processes for preparation of these alginate materials and methods for using them, particularly for cell transplantation and tissue engineering applications.
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ANTIHELMINTHIC ANTHRAQUINONES AND METHOD OF USE THEREOF (Fri, 31 Oct 2003)
Anthraquinones are described wnicn are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. In vitro or in vivo. The preferred anthraquinones have the formula (I) wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, 15 carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.
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Small molecule inhibitors targeted at Bcl-2 (Fri, 24 Oct 2003)
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
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AZABOROLYL GROUP 4 METAL COMPLEXES, CATALYSTS AND OLEFIN POLYMERIZATION PROCESS (Fri, 24 Oct 2003)
Metal complexes, catalysts derived therefrom, and polymerization processes using the same, charaterized by the presence of one or more nitrogen and boron containing, anionic, 5-membered cyclic ligand groups, especially 1,2-azaborolyl groups, are disclosed.
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6-and 7-substituted analogs of swainsonine their preparation and therapeutic use (Wed, 08 Oct 2003)
This invention relates to 6 or 7 substituted swainsonine analogues, processes for their preparation and use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 03 Oct 2003)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. Specifically, the method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces. 
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Copolymers derived from vinyl dicyanoimidazoles and other monomers (Wed, 24 Sep 2003)
A copolymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions together with a non-imidazole monomer capable of undergoing addition polymerization. In the imidazole, G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The invention also provides a method for using the co-polymers as a coupling/activator for synthon synthesis.
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 01 Aug 2003)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. In particular, the present invention provides methods and devices for selectively converting photogenerated reagent precursors to photogenerated reagents comprising a substrate comprising at least one solid surface containing a plurality of isolated reaction sites; and an optical system operably linked to the substrate comprising a light source and a computer-controlled spatial optical modulator to form an irradiation pattern, wherein the irradiation pattern selectively irradiates a plurality of reaction sites without use of a photolithographic mask. The method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces.
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 25 Jul 2003)
This invention provides method and apparatus for performing chemical and biochemical reactions in solution using in situ generated photo-products as reagent or co-reagent. In some embodiments, the present invention provides methods and devices for generating one or more selected multimers at specific reaction sites on a substrate comprising contacting the substrate with a liquid solution comprising photo-reagent precursors, isolating the reaction sites, selectively irradiating the reaction sites with a digital micromirror device, and contacting the substrate with monomers. The method and apparatus of the present invention have applications in parallel synthesis of molecular sequence arrays on solid surfaces.
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Well-defined nanosized building blocks for organic/inorganic nanocomposites (Fri, 27 Jun 2003)
Functionalized silsesquioxanes containing from 6 to 24 silicon atoms and minimally about 67 mol percent RSiO3/2 moieties where R is a phenyl group bearing a chemically reactive functional group are highly suitable for use as nanoparticles in producing highly ordered nanocomposites of many types, containing a high proportion of interphase. The nanocomposites have unusual physicochemical properties due to the use of uniform, highly functionalized nanoparticles.
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Imaging system, computer, program product and method for detecting changes in rates of water diffusion in a tissue using magnetic resonance imaging (MRI) (Wed, 21 May 2003)
The invention provides a computer-implemented method for detecting changes in rates of water diffusion in a tissue. The invention also provides a computer program product for use in the detection of changes in rates of water diffusion in a tissue using magnetic resonance imaging (MRI) comprising a computer useable medium comprising a computer readable program code embodied therein, wherein the computer program product is capable of storing and analyzing data input from a MRI device. The invention also provides a computer system, comprising a processor and a computer program product of the invention. The invention also provides a tissue imaging system, comprising a magnetic resonance imaging (MRI) device capable of outputting data to a processor; a processor; and, a computer program product of the invention embodied within the processor.
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SMALL MOLECULE INHIBITORS TARGETED AT BCL-2 (Fri, 09 May 2003)
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/BcI-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
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Amino ceramide-like compounds and therapeutic methods of use (Fri, 18 Apr 2003)
The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels. 
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A COMPOSITION COMPRISING A DENDRITIC POLYMER COMPLEXED WITH ATLEAST ONE UNIT OF BIOLOGICAL RESPONSE MODIFIER AND A PRPCESS FORTHE PREPAR (Fri, 11 Apr 2003)

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Proteomic differential display (Fri, 04 Apr 2003)
The present invention relates to multi-phase protein separation methods capable of resolving and characterizing large numbers of cellular proteins, including methods for efficiently facilitating the transfer of protein samples between separation phases. In particular, the present invention provides systems and methods for the differential display of protein samples from multiple cell types. The present invention thus provides improved methods for the analysis of multiple samples containing large numbers of proteins. 
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Three dimensional protein mapping (Fri, 28 Mar 2003)
The present invention relates to multi-phase protein separation methods capable of resolving and characterizing large numbers of cellular proteins, including methods for efficiently facilitating the transfer of protein samples between separation phases. In particular, the present invention provides systems and methods for the generation of multi-dimensional protein maps. The present invention thus provides improved methods for the analysis of samples containing large numbers of proteins.
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Treatment of idiopathic pulmonary fibrosis using IP-10 (Fri, 14 Feb 2003)
Disclosed are various discoveries concerning the angiogenic and angiostatic properties of the CXC chemokines, including the finding that the ELR motif controls the ability of these molecules to induce angiogenesis. Aspects of the invention include, for example, the identification of IP-10, MIG and certain IL-8 analogues as angiostatic agents, and their use in inhibiting angiogenesis in various systems.
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SYNTHESIS OF UDP-GLUCOSE: N-ACYLSPHINGOSINE GLUCOSYLTRANSFERASE INHIBITORS (Fri, 31 Jan 2003)
Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
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Small molecule antagonists of Bcl-2 family proteins (Fri, 10 Jan 2003)
The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-XL proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-XL). 
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EGLIN C BASED DRUGS FOR TREATMENT OF DISEASE (Sat, 28 Dec 2002)
The present invention relates to eglin c variants which inhibit proteases, and in particular to eglin c mutants at adventitious c ontact sites. The present invention also relates to eglin c variants which comprise mutations in both adventitious contact sites and at reactive loop sites. The present invention further relates to methods of preparing the eglin c variants, and methods of using the eglin c variants for treatment of diseases including acute bacterial, viral, and fungal infections.
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2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents (Fri, 20 Dec 2002)
Compounds which are active against viruses have the following Formulas:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06790841-20040914-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1and R2are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
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WELL-DEFINED NANOSIZED BUILDING BLOCKS FOR ORGANIC/INORGANIC NANOCOMPOSITES (Fri, 20 Dec 2002)
Functionalized silsesquioxanes containing from 6 to 24 silicon atoms and minimally about 67 mol percent RSiO3/2 moieties where R is a phenyl group bearing a chemically reactive functional group are highly suitable for use as nanoparticles in producing highly ordered nanocomposites of many types, containing a high proportion of interphase. The nanocomposites have unusual physicochemical properties due to the use of uniform, highly functionalized nanoparticles.
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CXC chemokines as regulators of angiogenesis (Wed, 11 Dec 2002)
Disclosed are various discoveries concerning the angiogenic and angiostatic properties of the CXC chemokines, including the finding that the ELR motif controls the ability of these molecules to induce angiogenesis. Aspects of the invention include, for example, the identification of IP-10, MIG and certain IL-8 analogues as angiostatic agents, and their use in inhibiting angiogenesis in various systems.
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SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS (Fri, 06 Dec 2002)
The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-XL proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-XL).
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METHODS OF MULTI-PHASE PROTEIN ANALYSIS (Fri, 08 Nov 2002)
The present invention relates to multi-phase protein separation methods capable of resolving and characterizing large numbers of cellular proteins, including methods for efficiently facilitating the transfer of protein samples between separation phases. In particular, the present invention provides systems and methods for the generation of multi-dimensional protein maps. The present invention further provides systems and methods for the differential display of protein samples from multiple cell types. The present invention thus provides improved methods for the analysis of samples containing large numbers of proteins.
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Multifunctional nanodevice platform (Wed, 30 Oct 2002)
The present invention relates to novel therapeutic and diagnostic arrays. More particularly, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems generally comprise two or more separate components for targeting, imaging, sensing, and/or triggering release of a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
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Methods and products for the synthesis of oligosaccharide structures on glycoproteins, glycolipids, or as free molecules, and for the isolation of cloned genetic sequences that determine these structures (Fri, 02 Aug 2002)
A method for isolating a gene, comprising: (i) isolating a cell possessing a post-translational characteristic of interest, said post-translational characteristic being the presence of a membrane-bound oligosaccharide or polysaccharide of interest on the surface of said cell, the presence of a soluble oligosaccharide or polysaccharide of interest in an extract of said cell, or the presence of a particularly glycosyltransferase activity in an extract of said cell; (ii) creating a genetic library of either cDNA or genomic DNA from the genetic material of said isolated cell; (iii) transforming host cells with said genetic library; and (iv) screening said transformed host cells for a host cell containing said post-translational characteristic, thereby obtaining a cell containing said gene, is disclosed. The method can be used to obtain genes encoding glycosyltransferases. 
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Protein separation and display (Fri, 26 Jul 2002)
The present invention relates to multi-phase protein separation methods capable of resolving and characterizing large numbers of cellular proteins, including methods for efficiently facilitating the transfer of protein samples between separation phases. In particular, the present invention provides an automated system for the separation, identification, and characterization of protein samples. The present invention thus provides improved methods for the analysis of samples containing large numbers of proteins. 
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Benzimidazole derivatives for the treatment of viral infections (Wed, 03 Jul 2002)
According to a first aspect of the invention there is provided compounds of formula (I):<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06413938-20020702-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein: R1is hydroxy; O-acetyl; or a halo atom; R2is hydroxy; O-acetyl; or a halo atom; R3is hydrogen; a halo atom; azido; C2-6alkenyl; C2-6alkynyl; C6-14aryl C2-6alkenyl; C6-14arylC2-6alkynyl —NR8R9(where R8and R9may be the same or different and are hydrogen, C1-8alkyl, cyanoC1-8alkyl, hydroxyC1-8alkyl, haloC1-8alkyl, C3-7cycloalkyl, C1-8alkylC3-7cycloalkyl, C2-6alkenyl, C3-7cycloalkylC1-8alkyl, C2-6alkynyl, C6-14aryl, C6-14arylC1-8alkyl, heterocycleC1-8alkyl, C1-8alkylcarbonyl, C6-14arylsulfonyl, C1-8alkysulfonyl, or R8R9together with the N atom to which they are attached form a 3,4,5 or 6 membered heterocyclic ring); —OR10(where R10is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl, C2-6alkenyl, C2-6alkynyl, C6-14aryl C2-6alkenyl or C6-14arylC2-6alkynyl); or —SR11(where R11is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl).
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Radioiodinated phospholipid ether analogs and methods of using the same (Fri, 31 May 2002)
The present invention provides improved radioiodinated phospholipid ether analogs which demonstrate significant tumor avidity and longer plasma half-life than shorter-chain analogs. The radioiodinated phospholipid ether analogs of the present invention provide superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy. 
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Catalyst compositions comprising bridged metal complexes and an activating cocatalyst (Wed, 24 Apr 2002)
A catalyst and process of polymerizing olefins using it are described, the catalyst comprising a cocatalyst and a metal complex preferably of the formulas 4-9,<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06376406-20020423-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein M is a group 4 metal, Z is a boron atom, and T is one of<chemistry id="chem-us-00002-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00002-en" file="US06376406-20020423-C00002.TIF" img-content="chem" alt="embedded image"/></chemistry>
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Heterocyclic metal complexes and olefin polymerization process (Wed, 13 Mar 2002)
Racemic isomers of metal complexes of Groups 3, 4 or the Lanthanides, addition polymerization catalysts containing the same and olefin polymerization processes using the same comprising a boratabenzene group or divalent derivative thereof are disclosed.
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2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents (Wed, 06 Mar 2002)
Compounds which are active against viruses have the following Formulas:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06352991-20020305-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1and R2are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
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Pyrrolo[2,3-d] pyrimidines as antiviral agents (Wed, 30 Jan 2002)
This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by the following formula:<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06342501-20020129-C00001.TIF" img-content="chem" alt="embedded image"/></chemistry> wherein: R4is —NR1R2or oxo; R5is —CN, or —CSNR1R2, or —CONR1R2; R6is —H, or halo, or —NR1R2; wherein R1and R2are independently —H or an aliphatic group; and R7is of the formula R3—Ar, wherein R3is an aliphatic group and Ar is an unsubstituted aryl or an aryl independently substituted with halo, nitro, amino, or aliphatic groups; provided that when R5is a —CN or —CSNH2, and R6is a —H or —NH2, and Ar is a —C6H5or a phenyl substituted with only one aliphatic group, R3is an aliphatic group other than methyl such that —R3— is not a —CH2—; and pharmaceutically acceptable salts, prodrugs and derivatives thereof.
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Imidazole containing compounds having relatively low hydrogen content and relatively high nitrogen content and polymers and copolymers formed therefrom (Fri, 21 Dec 2001)
In one embodiment, the invention provides a polymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions. G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The polymers formed by at least two of the cyclic imidazole units. In another embodiment, the invention provides new imidazole compounds usable as monomers to form the polymers. In still another embodiment, the invention provides a method for using the polymers as a coupling/activator for synthon synthesis.
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MULTIFUNCTIONAL NANODEVICE PLATFORM (Fri, 23 Nov 2001)
The present invention relates to novel therapeutic and diagnostic arrays. More particularly, the present invention is directed to dendrimer based multifuntional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems generally comprise two or more separate components for targeting, imaging, sensing, and/or triggering release of a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
>> read more

Amino ceramide-like compounds and therapeutic methods of use (Fri, 16 Nov 2001)
Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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Bridged metal complexes (Wed, 05 Sep 2001)
A Group 4 transition metal complex containing a boron or aluminum bridging group containing a nitrogen containing electron donating group, especially an amido group.
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Cyclic imidazole compounds having relatively low hydrogen content and relatively high nitrogen content and polymers and copolymers formed therefrom (Wed, 15 Aug 2001)
In one embodiment, the invention provides a polymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions. G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The polymers formed by at least two of the cyclic imidazole units. In another embodiment, the invention provides new imidazole compounds usable as monomers to form the polymers. In still another embodiment, the invention provides a method for using the polymers as a coupling/activator for synthon synthesis.
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Methods and products for the synthesis of oligosaccharide structures on glycoproteins, glycolipids, or as free molecules, and for the isolation of cloned genetic sequences that determine these structures (Wed, 01 Aug 2001)
A method for isolating a gene, comprising: (i) isolating a cell possessing a post-translational characteristic of interest, said post-translational characteristic being the presence of a membrane-bound oligosaccharide or polysaccharide of interest on the surface of said cell, the presence of a soluble oligosaccharide or polysaccharide of interest in an extract of said cell, or the presence of a particularly glycosyltransferase activity in an extract of said cell; (ii) creating a genetic library of either cDNA or genomic DNA from the genetic material of said isolated cell; (iii) transforming host cells with said genetic library; and (iv) screening said transformed host cells for a host cell containing said post-translational characteristic, thereby obtaining a cell containing said gene, is disclosed. The method can be used to obtain genes encoding glycosyltransferases.
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COPOLYMERS DERIVED FROM VINYL DICYANOIMIDAZOLES AND OTHER MONOMERS (Fri, 20 Jul 2001)
A copolymer comprising imidazole ring units having nitrogen at the 1 and 3 positions of the ring; a carbon at each of the 2, 4 and 5 positions of the ring; and radical substituents G1 and G2 carried at the 4 and 5 positions together with a non-imidazole monomer capable of undergoing addition polymerization. In the imidazole, G1 and G2 are each independently selected from cyano, substituents derived from cyano, and substituents which replace cyano. The invention also provides a method for using the copolymers as a coupling/activator for synthon synthesis.
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Swainsonine derivatives and methods for preparing the same (Wed, 18 Jul 2001)
Compound of the formula (I):<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06262065-20010717-C00001.TIF" img-content="chem"/></chemistry> wherein: R is defined in the specification; each R′, independently of the other, is H, acetyl, benzyl, methoxymethyl, tosyl, mesyl, trifluoromesyl, tri(C1-4alkyl)silyl, di(C1-4alkyl)phenylsilyl, diphenyl(C1-4alkyl)silyl, or triphenylsilyl, or both R together from an alkylidene protecting group; R″ is H, acetyl, benzyl, methoxymethyl, tosyl, mesyl, trifluoromesyl, tri(C1-4alkyl)silyl, di(C1-4alkylsilyl)phenylsilyl, diphenyl(C1-4alkyl)silyl, or triphenylsilyl; X is H, Cl, Br, or R4(where R4is C1-22-alkyl); Y is H, Cl, Br, or —CHR2OH, —CR2R3OH, —CH2CHR2OH, —CH2CR2R3OH, —SR2, —SeR2, —OH, —NH2, —R5(where R2, R3, and R5are independently of each other C1-22-alkyl); or X and Y together form a covalent bond; A and A′ are both H or together A and A′ form ═O, are useful as anticancer agents and as glycosidase inhibitors.
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Amino ceramide-like compounds and therapeutic methods of use (Wed, 04 Jul 2001)
Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
>> read more

Radioiodinated phospholipid ether analogs and methods of using the same (Wed, 04 Jul 2001)
Improved radioiodinated phospholipid ether analogs are described which exhibit significant tumor avidity and longer plasma half-life relative to shorter chain analogs. Use of these compounds results in superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.
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TOPICAL COMPOSITIONS COMPRISING THALIDOMIDE FOR THE TREATMENT OF INFLAMMATORY DISEASES (Fri, 15 Jun 2001)
Compositions and methods are provided for treating inflammatory diseases in mammals by inhibiting TNFα expression. The methods comprise the step of topically administrating a composition of the present invention comprising thalidomide, N-alkyl analogs of thalidomide and combinations thereof.
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COMPOSITION COMPRISING A DENDRITIC POLYMER IN COMPLEX WITH AT LEAST ONE UNIT OF BIOLOGICAL RESPONSE MODIFIER AND A PROCESS FOR THE PREPARATION THEREOF (Mon, 21 May 2001)
A dense star polymer conjugate which comprises at least one dense star polymer associated with at least one unit of at least one biological response modifier.
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COMPOSITION COMPRISING A DENDRITIC POYMER IN COMPLEX WITH AT LEAST ONE UNIT OF BIOLOGICAL RESPONSE MODIFIER AND A PROCESS FOR THE PREPARATION THEREOF (Mon, 21 May 2001)
A dense star polymer conjugate of the formula: (T)e * (P)x * (M)y wherein: each P represents a dense star polymer; x represents an integer of 1 or greater; each M represents at least one unit of a biological response modifier, said biological response modifier can be the same biological response modifier or a different biological response modifier; y represents an integer of 1 or greater; each T represents one or more target directors; e represents an integer of 1 or greater; and * indicates that the biological response modifier is associated with the dense star polymer; with the proviso that the biological response modifier maintains its effectiveness. 138 כ" ז בסיון התשס" א - May 20, 2001
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COMPOSITION COMPRISING A DENDRITIC POLYMER IN COMPLEX WITH AT LEAST ONE UNIT OF BIOLOGICAL RESPONSE MODIFIER AND A PROCESS FOR THE PREPARATION THEREOF (Mon, 21 May 2001)
A dense star polymer conjugate of the formula [(T)e - (C')f]g * (P)x * [(C" )h - (M)y]k wherein: each C' represents the same or different connecting group; each C" represents the same or different connecting group; g and k each individually represent an integer of 1 or greater; e represents an integer of 1 or greater; f and h each individually represent an integer of 0 or greater; - indicates a covalent bond in instances where a connecting group is present; each P represents a dense star polymer; x represents an integer of 1 or greater; T represents a target director; each M represents at least one unit of a carried biological response modifier; y represents an integer of 1 or greater; and * indicates that the carried biological response modifier is associated with the polymer; with the proviso that the carried biological response modifier maintains its effectiveness. 137 כ" ז בסיון התשס" א - May 20, 2001
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Imidazo[1,2-a]pyridine C-nucleosides as antiviral agents (Wed, 11 Apr 2001)
This invention pertains to nucleoside analogs that have antiviral activity and improved metabolic stability, compositions comprising them, and methods of antiviral treatment employing them. More particularly, this invention pertains to imidazo[1,2-a]pyridine C-nucleosides, as exemplified by compounds such as imidazo[l,2-a]pyridine C5-nucleosides and imidazo[1,2-a]pyridine C3-nucleosides, and may be represented by formula (I), wherein exactly one of Q3and Q5is a sugar-like moiety; exactly one of Q3and Q5is —H; and Q2, Q6, Q7and Q8are independently imidazo[1,2-a]pyridine substituents, such as —H, —F, —Cl, —Br and —I.<chemistry id="chem-us-00001-en"><img he="N/A" wi="N/A" img-format="tif" id="emi-c00001-en" file="US06214801-20010410-C00001.TIF" img-content="chem"/></chemistry>
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Germanes and doping with germanes (Wed, 07 Mar 2001)
The present invention provides germanium-containing compounds which can function as dopants and where the methods for their use are flexible, reliable and environmentally safe. The process includes the ability to make bisamidegermanes under relatively mild conditions, usually standard temperature and pressure, without toxic by-products, giving pure products at satisfactory yields.
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AMINO CERAMIDE-LIKE COMPOUNDS AND THERAPEUTIC METHODS OF USE (Fri, 19 Jan 2001)
Novel amino ceramide-like compounds (1) are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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CROSSLINKED DNA CONDENSATE COMPOSITIONS AND GENE DELIVERY METHODS (Fri, 19 Jan 2001)
Disclosed are improved compositions and methods for use in gene delivery and expression. A range of surprisingly effective cross-linking agents and peptides are provided, as are peptide-DNA carrier compositions and condensed particles with reduced toxicity and increased stability. Advantageous methods of using such compositions in gene delivery and gene expression are further disclosed, which may be used in combination with biocompatible matrices, carriers and/or targeting agents.
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Method for performing magnetic resonance angiography using a contrast agent (Wed, 27 Dec 2000)
A 3DFT MRA dynamic study is performed using a contrast agent to enhance image contrast. A monitor pulse sequence is performed at a high temporal rate to monitor the magnitude of the NMR signal produced in a monitor region after the contrast agent is injected into the patient. When the monitor signal reaches a threshold value, the patient is signaled and the 3DFT image data set is acquired. -GOVT PAR This invention was made with government support under Grant No. HL 46384 awarded by the National Heart Lung and Blood Institute. The government has certain rights in the invention.
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