BCL-2BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 25 Jul 2014)
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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SYNTHESIS AND ISOLATION OF DENDRIMER BASED IMAGING SYSTEMS (Fri, 18 Jul 2014)
The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).
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FLUOROGENIC DENDRIMER REPORTERS AND RELATED METHODS OF USE (Fri, 18 Jul 2014)
The present invention relates to fluorogenic dendrimer reporters. In particular, the present invention relates to dendrimer nanoparticles conjugated with 'click-on' fluorogenic reporters and related methods of use.
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BACTERIA TARGETING NANOPARTICLES AND RELATED METHODS OF USE (Fri, 20 Jun 2014)
The present invention relates to bacteria-targeting nanoparticles and related methods of use. In particular, the present invention relates to dendrimer nanoparticles conjugated with Vancomycin and/or Polymixin (e.g., Polymixin B, Polymixin E). In certain embodiments, such dendrimer nanoparticles are used to sequester and/or identify bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), screen liquid samples (e.g., water samples, food samples, pharmaceutical samples, blood samples, blood platelet samples, etc.) for the presence of bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), treat disorders associated with bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria), and/or identify, sequester, and remove bacteria (e.g., Gram-positive bacteria and/or Gram-negative bacteria) from a liquid sample (e.g., water sample, food sample, pharmaceutical sample, blood sample, blood platelet sample, etc.). In certain embodiments, iron oxide nanoparticles are coated with dendrimer nanoparticles conjugated with Vancomycin and/or Polymixin.
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COMPOUND AND METHOD FOR MODULATING OPIOID RECEPTOR ACTIVITY (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The invention provides a compound of formula (I), wherein R<sup>1 </sup>is H, C(NH)NH<sub>2</sub>, an amino acid, or a peptide; X is OH, NH<sub>2</sub>, NHR<sup>2</sup>, NR<sup>2</sup>R<sup>3</sup>, an amino acid, or a peptide; R<sup>2 </sup>and R<sup>3 </sup>are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R<sup>4 </sup>and R<sup>5 </sup>is independently H or CH<sub>3</sub>; Z is 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid; 2-amino-1,2,3,4-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-1H-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NH<sub>2 </sub>when R<sup>1 </sup>is H, R<sup>4 </sup>is H, R<sup>5 </sup>is CH<sub>3</sub>, 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.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.85mm" wi="75.10mm" file="US20140154272A1-20140605-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 30 May 2014)
<p id="p-0001" num="0000">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.</p>
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DENDRIMER CONJUGATES (Fri, 09 May 2014)
<p id="p-0001" num="0000">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.</p>
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PLASMINOGEN ACTIVATOR-1 INHIBITORS AND METHODS OF USE THEREOF (Fri, 09 May 2014)
The invention relates to plasminogen activator- 1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels.
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DIPYRIN BASED MATERIALS FOR PHOTOVOLTAICS, COMPOUNDS CAPABLE OF UNDERGOING SYMMETRY BREAKING INTRAMOLECULAR CHARGE TRANSFER IN A POLARIZING MEDIUM AND ORGANIC PHOTOVOLTAIC DEVICES COMPRISING THE SAME (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">The present disclosure generally relates to organic photosensitive optoelectronic devices comprising at least one boron dipyrrin compound. In addition, the present disclosure relates to methods of making organic photosensitive optoelectronic devices comprising at least one boron dipyrrin compound. The present disclosure also 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.</p>
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BIVALENT INHIBITORS OF IAP PROTEINS AND THERAPEUTIC METHODS USING THE SAME (Fri, 28 Feb 2014)
Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.
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METABOLOMIC PROFILING OF CANCER (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to cancer markers. In particular, the present invention provides metabolites that are differentially present in prostate cancer.</p>
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DIPYRRIN BASED MATERIALS FOR PHOTOVOLTAICS, COMPOUNDS CAPABLE OF UNDERGOING SYMMETRY BREAKING INTRAMOLECULAR CHARGE TRANSFER IN A POLARIZING MEDIUM AND ORGANIC PHOTOVOLTAIC DEVICES COMPRISING THE SAME (Fri, 14 Feb 2014)
The present disclosure generally relates to organic photosensitive optoelectronic devices comprising at least one boron dipyrrin compound. In addition, the present disclosure relates to methods of making organic photosensitive optoelectronic devices comprising at least one boron dipyrrin compound. The present disclosure also 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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NON-SURGICAL METHOD OF TREATMENT FOR CATARACT (Fri, 31 Jan 2014)
<p id="p-0001" num="0000">The invention provides inhibitors of α-crystallin aggregation and methods of using α-crystallin aggregation inhibitors to, e.g., treat or prevent cataracts in a subject having or at risk of developing cataracts. The invention further provides high throughput methods of screening compounds for modulation of protein thermal stability, the method comprising contacting a protein with each of a plurality of test compounds; and (b) measuring the melting transition (T<sub>m</sub>) of the protein in the presence of each of the plurality of test compounds, wherein a compound that decreases or increases the apparent T<sub>m </sub>by at least 2 standard deviations is identified as a pharmacological protein chaperone.</p>
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INHIBITORS OF ALPHA-CRYSTALLIN AGGREGATION FOR THE TREATMENT FOR CATARACT (Fri, 24 Jan 2014)
The invention provides inhibitors of cc-crystallin aggregation and methods of using cc- crystallin aggregation inhibitors to, e.g., treat or prevent cataracts in a subject having or at risk of developing cataracts. The invention further provides high throughput methods of screening compounds for modulation of protein thermal stability, the method comprising contacting a protein with each of a plurality of test compounds; and (b) measuring the melting transition (Tm) of the protein in the presence of each of the plurality of test compounds, wherein a compound that decreases or increases the apparent Tm by at least 2 standard deviations is identified as a pharmacological protein chaperone.
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COMPOUNDS AND METHODS FOR ACTIVATING THE APOPTOTIC ARM OF THE UNFOLDED PROTEIN RESPONSE (Sat, 28 Dec 2013)
N-substituted sulfonylphenyl-5-nitrofuranyl-2- carboxamide derived compounds, which selectively activate the apoptotic, but not the adaptive arm, of the Unfolded Protein Response are provides as is their use in the treatment of diseases such as diabetes, Alzheimer's, Parkinson's, hemophilia, lysosomal storage diseases and cancer.
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SPIRO-OXINDOLE MDM2 ANTAGONISTS (Fri, 08 Nov 2013)
<p id="p-0001" num="0000">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.</p>
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MEAN DIFFUSIVITY MEASUREMENT CORRECTIONS FOR GRADIENT NON-LINEARITY (Fri, 08 Nov 2013)
Techniques for correcting gradient non-linearity bias in mean diffusivity measurements by MRI systems are shown and include minimal number of spatial correction terms to achieve sufficient error control using three orthogonal diffusion weighted imaging (DWI) gradients. The correction is based on rotation of system gradient nonlinearity tensor into a DWI gradient frame where spatial bias of b-matrix is described by its Euclidian norm. The techniques obviate time consuming multi-direction acquisition and noise-sensitive mathematical diagonalization of a full diffusion tensor for medium of arbitrary anisotropy.
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METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTION (Fri, 08 Nov 2013)
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 (e.g., biofilms).
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Method Of MRI Imaging Using Non-Slice-Selective, Spatially Tailored Tip-Up Pulse (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">A method of acquiring image data with an MRI system from an object using a sequence of tip-down and tip-up RF pulses is described. A slice-selective first pulse α rotates the in-slice spins from the longitudinal axis (z) toward a transverse plane (x, y). Image data is acquired from the in-slice spins during a free precession interval (T<sub>free</sub>) in which the in-slice spins precess along the transverse plane (x, y). A spatially tailored, non-slice-selective second pulse β({right arrow over (r)}) is applied for rotating the in-slice spins from the transverse plane (x, y) to at least substantially along the longitudinal axis (z). A third pulse S may be applied to the in-slice and out-of-slice spins to eliminate (spoil) residual transverse signal from out-of-slice spins.</p>
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Benzodiazepinone compounds useful in the treatment of skin conditions (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">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.</p>
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">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).</p>
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NANOPARTICLES COATED WITH AMPHIPHILIC BLOCK COPOLYMERS (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">The present provides amphiphilic block copolymer coated surfaces (e.g., nanoparticles, medical devices, etc.) and methods of preparing such surfaces. In certain embodiments, the present invention provides amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer (e.g., PBS) and have neutral but functionable surfaces, and methods of preparing the same.</p>
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Novel Strategies, Linkers and Coordination Polymers for High-Performance Sorbents (Fri, 13 Sep 2013)
<p id="p-0001" num="0000">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.</p>
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NANOPARTICLES COATED WITH AMPHIPHILIC BLOCK COPOLYMERS (Fri, 13 Sep 2013)
Amphiphilic block copolymer coated surfaces and methods of preparing such surfaces. Amphiphilic block copolymer coated single dispersed nanoparticles, which are stable in buffer and have neutral but functionable surfaces, and methods of preparing the same. Methods of producing stable amphiphilic block copolymer coated gold nanoparticles comprising: a) preparing a stable colloidal suspension of gold nanoparticles in an organic solvent by a top-down nanofabrication method using bulk gold as a source material and preparing a solution of amphiphilic block copolymers in the organic solvent; b) mixing the solution of amphiphilic block copolymer with the colloidal suspension of gold nanoparticles, then treating the mixture at elevated temperature, and then cooling the resultant mixture.
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SYNTHESIZING FUNCTIONALIZED DENDRIMERS WITHIN BIOLOGICAL SETTINGS (Fri, 09 Aug 2013)
The present invention relates to compositions (e.g., dendrimer scaffolds) capable of click chemistry for use in synthesis of functionalized dendrimers within biological settings, and methods of use of the same.
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NICOTINIC RECEPTOR COMPOUNDS (Fri, 05 Jul 2013)
Compounds and compositions for promoting smoking cessation or descreasing tobacco use or nicotine addiction are provided. The compounds are 2'-fluoro-3'-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.
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ANTIMICROBIAL COMPOUNDS (Fri, 14 Jun 2013)
Provided herein is technology relating to antimicrobial compounds and particularly, but not exclusively, to analogs of rifalazil having increased inhibition of RNA polymerase and decreased induction of human cy-tochrome P450. The compounds have an increased affinity for a bacterial RNA polymerase (e.g., a MTB RNA polymerase) and a decreased affinity for a human pregnane X receptor. Thus, in some embodiments, the steric clash of A or R with residues in the binding pocket of the human pregnane X receptor reduces an affinity of the compound for the human pregnane X receptor. Consequently, in some embodiments the steric clash thus reduces the induction (e.g., an activity) of a cytochrome P450 and/or other related proteins.
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MULTIFUNCTIONAL SMALL MOLECULES (Fri, 14 Jun 2013)
The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.
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COMPOSITIONS AND METHODS FOR THE TREATMENT AND ANALYSIS OF NEUROLOGICAL DISORDERS (Fri, 07 Jun 2013)
Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-β (Aβ ) or metal-Aβ species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
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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)
<p id="p-0001" num="0000">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.</p>
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LECTINS AND USES THEREOF (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">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.</p>
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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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Process for the preparation of small molecule inhibitors of MDM2 and intermediates used therein (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">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).</p>
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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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Systems and methods for tissue imaging (Fri, 14 Dec 2012)
<p id="p-0001" num="0000">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.</p>
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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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Diazo bicyclic Smac mimetics and the uses thereof (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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Dendrimer conjugates (Fri, 02 Nov 2012)
<p id="p-0001" num="0000">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.</p>
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SMALL MOLECULE INHIBITORS OF RGS PROTEINS (Fri, 02 Nov 2012)
The invention relates to compositions having RGS (regulator of G-protein Signaling) inhibiting activity, and methods of use thereof. In some embodiments, RGS-inhibiting compositions find use in research on or treatment of disease states (e.g., diabetes, epilepsy, neuropathic pain, depression and other diseases).
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Phosphorescent organic compounds (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">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.</p>
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Selective ligands for the dopamine 3 (D<sub>3</sub>) receptor and methods of using the same (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">Potent and selective ligands for the dopamine 3 (D<sub>3</sub>) receptor are disclosed. The D<sub>3 </sub>receptor ligands have a structural formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="31.16mm" wi="76.20mm" file="US08486981-20130716-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>1 </sup>is C<sub>1-6 </sub>alkyl or C<sub>3-6</sub>cycloalkyl; or </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="33.78mm" wi="75.35mm" file="US08486981-20130716-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> wherein R<sup>2 </sup>is </p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00003" num="00003"> <img id="EMI-C00003" he="12.36mm" wi="35.22mm" file="US08486981-20130716-C00003.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> substituted with one or two halogen(s) or OC<sub>1-3</sub>alkyl. </p>
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Benzodiazepinone compounds and methods of treatment using same (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same (Fri, 27 Jul 2012)
<p id="p-0001" num="0000">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.</p>
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Electrospray and nanospray ionization of discrete samples in droplet format (Fri, 22 Jun 2012)
<p id="p-0001" num="0000">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.</p>
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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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Spiro-oxindole MDM2 antagonists (Fri, 18 May 2012)
<p id="p-0001" num="0000">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.</p>
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1,4-benzodiazepinone compounds and their use in treating cancer (Fri, 20 Apr 2012)
<p id="p-0001" num="0000">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.</p>
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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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Benzodiazepinone compounds useful in the treatment of skin conditions (Fri, 17 Feb 2012)
<p id="p-0001" num="0000">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.</p>
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<i>Methylocystis </i>strain SB2 materials and methods (Fri, 10 Feb 2012)
<p id="p-0001" num="0000">The present disclosures provides isolated or purified compounds, each of which bind to a metal atom. Generally, the compounds are small in size (e.g, molecular weight of less than about 1 kDa) and peptidic in nature, inasmuch as the compounds comprise amino acids. In some embodiments, the compound comprises a structure of Formula I: <br/> <?in-line-formulae description="In-line Formulae" end="lead"?>M<sub>1</sub>-P<sub>1</sub>-M<sub>2</sub>-P<sub>2 </sub><?in-line-formulae description="In-line Formulae" end="tail"?> <br/> wherein each of P<sub>1 </sub>and P<sub>2 </sub>is a peptide comprising at least two amino acids, M<sub>1 </sub>is a first metal binding moiety comprising a substituted imidazolone ring, M<sub>2 </sub>is a second metal binding moiety comprising a substituted oxazolone ring, and wherein M<sub>1 </sub>and M<sub>2 </sub>bind to a single metal atom. Also provided are related complexes, conjugates, cells which synthesize the compounds of the present disclosures, substantially homogenous cultures thereof, kits and compositions, and methods of making or using the materials of the present disclosures. </p>
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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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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,ß fashion is achieved resulting in hybrid structures containing a distorted porphyrin ring with annulated aromatic rings. The porphyrin core can be olygoporphyrins.</p>
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2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and -pyrimidines as antiviral agents (Fri, 11 Nov 2011)
<p id="p-0001" num="0000">Compounds which are active against viruses have the following formulas:</p> <p id="p-0002" num="0000"><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> <br/> 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. </p>
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METHODS OF TREATING AUTOIMMUNE DISORDERS AND/OR INFLAMMATORY DISORDERS (Fri, 04 Nov 2011)
<p id="p-0001" num="0000">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).</p>
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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)
<p id="p-0001" num="0000">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.</p>
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USING PHAGE EPITOPES TO PROFILE THE IMMUNE RESPONSE (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same (Fri, 29 Jul 2011)
<p id="p-0001" num="0000">Potent and selective ligands for the dopamine 3 (D<sub>3</sub>) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C═O or SO<sub>2</sub>, R<sup>1 </sup>is C<sub>1-6 </sub>alkyl, R<sup>2 </sup>is aryl, heteroaryl, aryl, —(CH<sub>2</sub>)<sub>1-3</sub>aryl, or —(CH<sub>2</sub>)<sub>1-3</sub>heteroaryl, and n is 0 or 1. Methods of using the D<sup>3 </sup>receptor ligands in the treatment of diseases and conditions wherein modulation of the D<sub>3 </sub>receptor provides a benefit also are disclosed.</p> <p id="p-0002" num="0000"><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> </p>
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Indole antiviral compositions and methods (Fri, 22 Jul 2011)
<p id="p-0001" num="0000">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.</p>
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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 3-dimensional structural conformations of flexible biomolecular targets (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">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.</p>
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Protein purification tags and uses thereof (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to fusion proteins. In particular, the present invention relates to protein tags for use in protein solubilization and purification.</p>
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Pyrimidotriazinediones and Pyrimidopyrimidinediones and Methods of Using the Same (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">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.</p> <p id="p-0002" num="0000"><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> </p>
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 24 Jun 2011)
<p id="p-0001" num="0000">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).</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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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.</p>
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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.</p>
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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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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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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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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.))).</p>
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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.</p>
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Spiro-oxindole MDM2 antagonists (Fri, 13 May 2011)
<p id="p-0001" num="0000">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.</p>
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COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION (Fri, 06 May 2011)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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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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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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COMPOSITIONS AND METHODS FOR TREATMENT OF LEUKEMIA (Fri, 18 Mar 2011)
<p id="p-0001" num="0000">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.</p>
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Functionalized polydiacetylene sensors (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">A microarray includes a solid substrate having a surface, the surface having a plurality of binding spots and a plurality of reaction moieties bound to the binding spots. A reaction moiety includes a plurality of polyacetylene monomers, the polyacetylene monomers having a first coupling region and a second coupling region, the first coupling region having a first functional group operable to bind to the binding spot and the second coupling region comprising a second functional group operable to bind to an accessory molecule; and an accessory molecule having a binding region and an analyte reaction region, the analyte reaction region operable to selectively bind to the target analyte, and the binding region operable to bind to the second coupling region of the polyacetylene monomer. Upon binding a target analyte with the reaction moiety, a color change from the polyacetylene monomer occurs and the reaction moiety produces fluorescence.</p>
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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 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.</p>
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COMPOSITIONS AND METHODS FOR TARGETING TUMORS (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">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.</p>
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Heteroaryl-substituted bicyclic Smac mimetics and the uses thereof (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">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.</p>
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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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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 ?m 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.</p>
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 17 Dec 2010)
<p id="p-0001" num="0000">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).</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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PLASMINOGEN ACTIVATOR INHIBITOR AMELIORATION OF NEWBORN HYPOXIC ISCHEMIC BRAIN INJURY (Fri, 12 Nov 2010)
<p id="p-0001-en" num="0000">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).</p>
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DIAZO BICYCLIC SMAC MIMETICS AND THE USES THEREOF (Fri, 29 Oct 2010)
<p id="p-0001-en" num="0000">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.</p>
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 29 Oct 2010)
<p id="p-0001" num="0000">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).</p>
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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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Properties tailoring in silsesquioxanes (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">Fluoride catalyzed rearrangement reactions of polymeric silsesquioxanes [RSiO<sub>1.5</sub>]<sub>n </sub>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.</p>
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Block coordination copolymers (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">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.</p>
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Block coordination copolymers (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">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.</p>
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Block Coordination Copolymers (Fri, 03 Sep 2010)
<p id="p-0001-en" num="0000">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.</p>
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F<sub>1</sub>F<sub>0</sub>-ATPase inhibitors and related methods (Fri, 03 Sep 2010)
<p id="p-0001" num="0000">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.</p>
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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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BLOCK COORDINATION COPOLYMERS (Fri, 03 Sep 2010)
<br/><br/><br/> The present invention provides <br/>composi-tions of crystalline coordination copolymers and methods <br/>of making and using the compositions wherein multiple <br/>organic molecules are assembled to produce porous <br/>framework materials with layered or core-shell structures. <br/>These materials are synthesized by sequential growth <br/> tech-niques such as the seed growth technique. In addition, the <br/>invention provides a simple procedure for controlling <br/>functionality.<br/><br/><br/><br/><br/></p>
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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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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 inven-tion provides systems and methods for detecting changes in tissue regions over a period of time. In some embodiments, the sys-tems 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 im-pact of therapeutic interventions. </p>
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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)
<p id="p-0001-en" num="0000">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.)).</p>
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DENDRIMER CONJUGATES (Fri, 25 Jun 2010)
<p id="p-0001-en" num="0000">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.</p>
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Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism (Fri, 04 Jun 2010)
<p id="p-0001-en" num="0000">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.</p>
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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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SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS (Fri, 19 Mar 2010)
<p id="p-0001-en" num="0000">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-X<sub>L, </sub>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.</p>
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Analytical system with photonic crystal sensor (Fri, 19 Mar 2010)
<p id="p-0001" num="0000">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.</p>
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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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Hydrophilic copolymers and assemblies containing the same (Fri, 26 Feb 2010)
<p id="p-0001" num="0000">A water soluble copolymer includes first and second hydrophilic block segments or graft chains. The first hydrophilic block segment or graft chain contains cyclodextrin groups in at least a majority of its repeating units, and the second hydrophilic block segment or graft chain contains repeating units other than cyclodextrin groups. The first and second block segments or graft chains are covalently linked.</p>
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Compositions and methods for treating inflammatory conditions of the bowel (Fri, 12 Feb 2010)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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Dendrimer conjugates (Fri, 20 Nov 2009)
<p id="p-0001" num="0000">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.</p>
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POLYMER COMPOSITIONS, COATINGS AND DEVICES, AND METHODS OF MAKING AND USING THE SAME (Fri, 20 Nov 2009)
<p id="p-0001-en" num="0000">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.</p>
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Indole antiviral compositions and methods (Fri, 13 Nov 2009)
<p id="p-0001" num="0000">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.</p>
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UV curable silsesquioxane resins for nanoprint lithography (Fri, 16 Oct 2009)
<p id="p-0001" num="0000">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.</p>
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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.
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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. </p>
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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.
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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. </p>
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SYSTEMS AND METHODS FOR IMAGING CHANGES IN TISSUE (Fri, 18 Sep 2009)
<p id="p-0001-en" num="0000">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.</p>
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Functionalized dendrimer-encapsulated and dendrimer-stabilized nanoparticles (Fri, 21 Aug 2009)
<p id="p-0001-en" num="0000">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.</p>
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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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Electrical impedance tomography of nanoengineered thin films (Fri, 15 May 2009)
<p id="p-0001" num="0000">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.</p>
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Bivalent SMAC mimetics and the uses thereof (Fri, 15 May 2009)
<p id="p-0001" num="0000">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.</p>
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Passive wireless readout mechanisms for nanocomposite thin film sensors (Fri, 15 May 2009)
<p id="p-0001" num="0000">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.</p>
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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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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 psonasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone. </p>
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Benzodiazepinone compounds useful in the treatment of skin conditions (Fri, 08 May 2009)
<p id="p-0001" num="0000">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.</p>
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2,2-Bis-(hydroxymethyl)cyclopropylidenemethyl-Purines and -Pyrimidines As Antiviral Agents (Fri, 08 May 2009)
<p id="p-0001-en" num="0000">Compounds which are active against viruses have the following formulas:</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">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.</p>
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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)
<p id="p-0001" num="0000">A method of preparing macrocycles using solid support chemistry and thioesterases is disclosed. Also disclosed are novel macrocycles.</p>
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Small molecule antagonists of Bcl-2 family proteins (Fri, 10 Apr 2009)
<p id="p-0001" num="0000">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-X<sub>L</sub>, 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.</p>
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DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME (Fri, 03 Apr 2009)
<p id="p-0001-en" num="0000">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).</p>
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METABOLOMIC PROFILING OF PROSTATE CANCER (Fri, 20 Mar 2009)
<p id="p-0001-en" num="0000">The present invention relates to cancer markers. In particular, the present invention provides metabolites that are differentially present in prostate cancer.</p>
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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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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. </p>
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Strategies, linkers and coordination polymers for high-performance sorbents (Fri, 06 Mar 2009)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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).</p>
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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 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. </p>
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METABOLOMIC CANCER TARGETS (Fri, 20 Feb 2009)
<p id="p-0001-en" num="0000">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.</p>
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Systems and methods for tissue imaging (Fri, 06 Feb 2009)
<p id="p-0001" num="0000">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.</p>
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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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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).</p>
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Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism (Fri, 09 Jan 2009)
<p id="p-0001" num="0000">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.</p>
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Device for chemical and biochemical reactions using photo-generated reagents (Fri, 26 Dec 2008)
<p id="p-0001-en" num="0000">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.</p>
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Protein MicroarraySystem (Fri, 14 Nov 2008)
<p id="p-0001-en" num="0000">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.</p>
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Conformationally constrained Smac mimetics and the uses thereof (Fri, 31 Oct 2008)
<p id="p-0001" num="0000">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.</p>
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Compositions and methods relating to novel compounds and targets thereof (Fri, 31 Oct 2008)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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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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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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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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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.</p>
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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.</p>
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Delivery device and method for forming the same (Fri, 17 Oct 2008)
<p id="p-0001" num="0000">A delivery device includes a hollow container, and a plurality of biodegradable and/or erodible polymeric layers established in the container. A layer including a predetermined substance is established between each of the plurality of polymeric layers, whereby degradation of the polymeric layer and release of the predetermined substance occur intermittently. Methods for forming the device are also disclosed herein.</p>
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Carboxylic acid-modified EDOT for bioconjugation (Fri, 19 Sep 2008)
<p id="p-0001-en" num="0000">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.</p>
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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.
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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.</p>
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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. </p>
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Methods for production and use of synthetic hydroxyapatite and fluorapatite nanorods, and superstructures assembled from the same (Fri, 12 Sep 2008)
<p id="p-0001" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000">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).</p>
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Indole antiviral compositions and methods (Fri, 20 Jun 2008)
<p id="p-0001-en" num="0000">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.</p>
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Conformationally constrained Smac mimetics and the uses thereof (Fri, 06 Jun 2008)
<p id="p-0001-en" num="0000">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.</p>
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Indole inhibitors of MDM2 and the uses thereof (Fri, 30 May 2008)
<p id="p-0001-en" num="0000">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).</p>
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Protein separation and analysis (Fri, 25 Apr 2008)
<p id="p-0001-en" num="0000">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. </p>
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Bivalent Smac mimetics and the uses thereof (Fri, 18 Apr 2008)
<p id="p-0001" num="0000">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.</p>
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 18 Apr 2008)
<p id="p-0001-en" num="0000">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.</p>
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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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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).</p>
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FRET-based apoptosis detector (Fri, 21 Mar 2008)
<p id="p-0001-en" num="0000">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. </p>
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Small molecule inhibitors targeted at Bcl-2 (Fri, 07 Mar 2008)
<p id="p-0001-en" num="0000">The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X<sub>L</sub>. 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-X<sub>L </sub>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-X<sub>L</sub>, 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. </p>
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 29 Feb 2008)
<p id="p-0001-en" num="0000">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.</p>
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Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents (Fri, 29 Feb 2008)
<p id="p-0001" num="0000">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.</p>
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Small molecule antagonists of XIAP family proteins (Fri, 25 Jan 2008)
<p id="p-0001" num="0000">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).</p>
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Production of gossypol co-crystals (Fri, 25 Jan 2008)
<p id="p-0001-en" num="0000">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.</p>
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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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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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Gossypol co-crystals and the use thereof (Fri, 21 Dec 2007)
<p id="p-0001-en" num="0000">This invention relates to compositions comprising co-crystals of (−)-gossypol with a C<sub>1-8 </sub>carboxylic acid or C<sub>1-8 </sub>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 C<sub>1-8 </sub>carboxylic acid or C<sub>1-8 </sub>sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.</p>
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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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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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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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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.</p>
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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.</p>
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METHODS AND REAGENTS FOR ACTIVATING HEAT SHOCK PROTEIN 70 (Fri, 09 Nov 2007)
<p id="p-0001-en" num="0000">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. </p>
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Brain-Associated Inhibitor of Tissue-Type Plasminogen Activator (Fri, 09 Nov 2007)
<p id="p-0001-en" num="0000">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. </p>
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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)
<p id="p-0001-en" num="0000">Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.</p>
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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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VIABLE NON-TOXIC GRAM NEGATIVE BACTERIA (Fri, 27 Jul 2007)
<br/><br/><br/>The present invention provides non-toxic Gram-negative bacteria. In <br/>particular, the present invention provides viable Gram-negative bacteria <br/>(e.g., E. coli) substantially lacking lipopolysaccharide (LPS, endotoxin) <br/>within the outer membrane. The present invention further provides methods of <br/>generating viable non-toxic Gram-negative bacteria and uses thereof. The <br/>present invention also provides compositions and methods for inducing immune <br/>responses and for researching and developing therapeutic agents.<br/></p>
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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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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. </p>
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Small molecule transcriptional activation domains (Fri, 11 May 2007)
<p id="p-0001-en" num="0000">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.</p>
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Dendrimer based compositions and methods of using the same (Fri, 23 Feb 2007)
<p id="p-0001-en" num="0000">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). </p>
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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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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. </p>
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Chromen-4-one inhibitors of anti-apoptotic Bcl-2 family members and the uses thereof (Fri, 03 Nov 2006)
<p id="p-0001-en" num="0000">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. </p>
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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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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. </p>
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Small molecule inhibitors of MDM2 and the uses thereof (Fri, 22 Sep 2006)
<p id="p-0001-en" num="0000">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).</p>
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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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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. </p>
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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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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). </p>
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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)
</p> <p>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-X<sub>L</sub> proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-X<sub>L</sub>).
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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)
<p id="p-0001" num="0000">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.</p>
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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.
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Small molecule inhibitors of anti-apoptotic BCL-2 family members and the uses thereof (Fri, 21 Apr 2006)
<p id="p-0001" num="0000">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.</p>
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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).
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PARTIALLY ACETYLATED DENDRIMERS AND RELATED METHODS OF USE (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). </p>
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Nucleic acids and polypeptides involved in the production of cryptophycin (Fri, 17 Mar 2006)
<p id="p-0001-en" num="0000">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.</p>
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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.
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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. </p>
>> 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.
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Amino ceramide-like compounds and therapeutic methods of use (Fri, 02 Dec 2005)
<p id="p-0001-en" num="0000">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.</p>
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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)
<p id="p-0001-en" num="0000"> 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></p>
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Protein microarray system (Fri, 21 Oct 2005)
<p id="p-0001-en" num="0000">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. </p>
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Compositions and methods for characterizing, regulating, diagnosing, and treating cancer (Fri, 21 Oct 2005)
<p id="p-0001-en" num="0000">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. </p>
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Gossypol co-crystals and the use thereof (Fri, 21 Oct 2005)
<p id="p-0001-en" num="0000">This invention relates to compositions comprising co-crystals of (−)-gossypol with a C<sub>1-8 </sub>carboxylic acid or C<sub>1-8 </sub>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 C<sub>1-8 </sub>carboxylic acid or C<sub>1-8 </sub>sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.</p>
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Mixed-metal oxide particles by liquid feed flame spray pyrolysis of oxide precursors in oxygenated solvents (Fri, 14 Oct 2005)
<p id="p-0001-en" num="0000">Liquid feed flame spray pyrolysis of solutions of a metal oxide precursor which is an alkoxide or C<sub>1-6 </sub>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.</p>
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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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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 co~crystals of (-)-gossypol with a C 1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death. </p>
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Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors (Fri, 07 Oct 2005)
<p id="p-0001-en" num="0000">Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.</p>
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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)
<p id="p-0001-en" num="0000">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. </p>
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Eglin c based drugs for treatment of disease (Fri, 16 Sep 2005)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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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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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. </p>
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Facile synthesis of polyhedral silsesquioxane anions and use thereof (Fri, 01 Jul 2005)
<p id="p-0001-en" num="0000">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.</p>
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AMINO CERAMIDE-LIKE COMPOUNDS AND THERAPEUTIC METHODS OF USE (Sat, 25 Jun 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. </p>
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2-amino-9-[(2-hydroxymethyl) cyclopropylidenemethyl] purine antiviral agents (Fri, 10 Jun 2005)
<p id="p-0001-en" num="0000">Compounds which are active against viruses have the following Formulas:</p> <p id="p-0002-en" num="0000"> <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 NHR<sub>1</sub>, OR<sub>2</sub>, or SR<sub>3</sub>;</li> <li>R<sub>1 </sub>is selected from the group consisting of alkyl, alkenyl, alkynyl, and C<sub>4-18 </sub>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>R<sub>2 </sub>is selected from the group consisting of C<sub>2-18 </sub>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>R<sub>3 </sub>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> </p>
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Azaborolyl group 4 metal complexes, catalysts and olefin polymerization process (Fri, 03 Jun 2005)
<p id="p-0001-en" num="0000">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.</p>
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2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents (Fri, 27 May 2005)
<p id="p-0001-en" num="0000">Compounds which are active against viruses have the following formulas:</p> <p id="p-0002-en" num="0000"> <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. </p>
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Amino ceramide-like compounds and therapeutic methods of use (Wed, 11 May 2005)
<p id="p-0001-en" num="0000">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.</p>
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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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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. </p>
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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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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. </p>
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Methods for incorporating non-perfectly matched oligonucleotides into target-specific hybridization sequences (Fri, 25 Mar 2005)
<p id="p-0001-en" num="0000">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.</p>
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Replication deficient adenovirus vectors and methods of making and using them (Wed, 16 Mar 2005)
<p id="p-00001-en" num="00001">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.</p>
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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)
<p id="p-0001-en" num="0000">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.</p>
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Drug delivery compositions (Fri, 25 Feb 2005)
<p id="p-0001-en" num="0000">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.</p>
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2-hydroxymethylcyclopropylidene methylpurines and -pyrimidines as antiviral agents (Fri, 14 Jan 2005)
<p id="p-0001-en" num="0000">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, R<sub>1 </sub>and R<sub>2 </sub>are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R<sub>1</sub>X and/or R<sub>2</sub>X can also be amino acid residues with X as NH. </p>
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