Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed.

Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present invention relates to Myosin II ATPase inhibitor compounds, including substituted 3a-hydroxy-1,2,3,3a-tetrahydro-4H-pyrrolo [2,3b] quinolin-4-one compounds which are blebbistatin derivatives.

Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Abstract: Disclosed are a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, a preparation method thereof, pharmaceutical compositions and uses thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO, wherein in the formula (I), R1 and R2 are each independently hydrogen; R3 is hydrogen or C1-3 alkyl; and Ar is an aromatic ring or an heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring.

Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.

Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.

Abstract: Aromatic diimide chromophores and methods for using the chromophores for the detection of volatile organic compounds are described. The chromophores are able to reversibly change colors in the presence or absence of volatile organic compounds.

Abstract: The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1-R9, Y, Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things, novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.

Abstract: The invention relates to salt forms of (3R,4S)-1-((4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl)-4-(methyl-thiomethyl)pyrrolidin-3-ol, as well as polymorphic forms of the salts. The invention further relates to processes for preparing the salt forms and to the use of the salt forms in the treatment of diseases and disorders where it is desirable to inhibit 5?-methylthioadenosine phosphorylase (MTAP).

Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.

Abstract: The present disclosure provides compounds of Formula (II) as disclosed herein, and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i), for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases.

Abstract: The present invention relates to a new benzodiazepine derivative, pharmaceutically acceptable salt thereof, preparation method therefor, and use thereof. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have obvious anesthetic effect and low toxicity in body, thereby enhancing the medication safety. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have sedative, hypnotic, and anesthetic effect, and can be used as sedative, hypnotic, and anesthetic drugs.

Abstract: The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.

Abstract: Provided is a phthalocyanine compound which has a green hue without having a halogen atom, and exhibits high luminance and an excellent coloring force at the time of being used for preparing a green pixel unit of a color filter. The phthalocyanine compound of the present invention has green hues without having a halogen atom, and exhibits high luminance and an excellent coloring force at the time of being used for preparing the green pixel unit of the color filter. In addition, the phthalocyanine compound can be used not only for the color filter, but also as a colorant for a wide range of applications as a general colorant such as printing ink, paint, colored plastic, toner, and ink for ink jet.

Abstract: The present invention provides for compounds of formula (I) wherein Rx, X, Y, Y1, L1, A1, A2, A3, A4, A5, A6, A7, and A8, have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract: Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the ?-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.

Abstract: The present invention relates to a method for preparing a curable bicyclic compound derived from biomass. The method includes preparing starting materials furan and methyl acrylate by preparing furan from hemicellulose extracted from biomass, and methyl acrylate from glycerol generated from biomass, preparing an intermediate compound comprising a bicycle and an alcohol functional group by reacting the furan and the methyl acrylate through a Diels-Alder reaction and consecutive reduction, and preparing a curable bicyclic compound that includes the bicycle and an epoxide functional group by reacting the intermediate compound and epichlorohydrin.

Abstract: The present invention provides a process for producing the compound having the structure: comprising (a) reacting a compound having the structure: with a compound having the structure: in the presence of a first organic solvent under conditions sufficient to produce the compound, wherein the first organic solvent is a substituted benzene.

Abstract: Embodiments of the present invention are directed to methods and dosage forms for treating inflammation and rejection in transplantation injuries with Bryostatin-1, Bryostatin-1 analogs and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a compound of Formula XXVIII: werein R1is H or CH3, and optionally including a salt or a hydrate of said compound.

Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2?±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.

Abstract: Described herein are novel compounds and methods for the treatment and/or prevention of cerebral amyloidoses such as Alzheimer's disease (AD) and/or cerebral amyloid angiopathy (CAA).

Abstract: Provided herein are substituted [1,2,4]triazlolo[1,5-?]pyrazine compounds, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorders.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.

Abstract: A method for treating a proliferative disease, disorder, or condition comprising administering a gold(III) complex such as [Au(npen)Cl2]Cl.2H2O (1) or [Au(npen)2]Cl3 (2); the complexes, and methods for making them.

Abstract: This invention provides a copper compound represented by General Formula (I) below. In General Formula (I), R1 to R3 independently represent a linear or branched alkyl group with a carbon number of 1 to 5; provided that R1 and R2 are a methyl group, R3 represents a linear or branched alkyl group with a carbon number of 2 to 5; and provided that R1 is a methyl group and R2 is an ethyl group, R3 represents a methyl group or a linear or branched alkyl group with a carbon number of 3 to 5. A starting material for forming a thin film of the present invention includes the copper compound represented by General Formula (I). The present invention can provide a copper compound which has a low melting point, can be conveyed in a liquid state, has a high vapor pressure, and is easily vaporizable, and also a starting material for forming a thin film which uses such a copper compound.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Abstract: Described herein is the fusion of two families of unique carbon-containing molecules that readily disregard the tendency of carbon to form four chemical bonds, namely N-heterocyclic carbenes (NHCs) and carborane anions. Deprotonation of an anionic imidazolium salt with lithium diisopropylamide at room temperature leads to a mixture of lithium complexes of C-2 and C-5 dianionic NHC constitutional isomers as well as a trianionic (C-2, C-5) adduct. Judicious choice of the base and reaction conditions allows for the selective formation of all three stable polyanionic carbenes. In solution, the so-called abnormal C-5 NHC lithium complex slowly isomerizes to the normal C-2 NHC, and the process can be proton catalyzed by the addition of the anionic imidazolium salt. These results indicate that the combination of two unusual forms of carbon atoms can lead to unexpected chemical behavior, and that this strategy paves the way for the development of a broad new generation of NHC ligands for catalysis.

Abstract: A composition containing 2-ethylhexyl silicate, is produced by heating a reaction mixture of ethyl silicate with an excess amount of 2-ethylhexanol in the presence of titanium tetrabutoxide as catalyst to a temperature below the boiling point of 2-ethylhexanol while mixing, allowing the reaction mixture to react and, after the reaction, removing ethanol and excess 2-ethylhexanol from the reaction mixture by distillation and obtaining the composition containing 2-ethylhexyl silicate.

Abstract: Inorganic siloxane ladder polymers with metal-aza/thio crown complexes, and methods of making and using such siloxane ladder polymers are disclosed. The polymers described herein may exhibit self-healing properties, a low dielectric constant, and a low refractive index. These siloxane ladder polymers are anchored to transparent, high-refractive index (RI) metal nanoparticles, such as ZrO2, via aza/thio crown macromolecules. The siloxane ladder polymers may be considered as “living polymer network” since the polymer active chain ends may further undergo anionic polymerization.

Abstract: Disclosed are a polyene compound, preparation method and use thereof. Provided in the present invention is the preparation method of a polyene compound I, comprising the following steps: under an action of a base and in an organic solvent, conducting a Witting reaction on a compound II and a compound III to obtain the polyene compound I. By the preparation method in the present invention, a coupling reaction results in good product purity without producing an obvious by-product and involves no heavy metal, thus facilitating a control over product quality and costs, having a simple operation and mild reaction condition, enabling high reaction conversion, a high yield, few by-products, high resultant product purity, low production costs and simple post-processing, and being suitable for industrial production.

Abstract: Embodiments of the present disclosure provide for biaryl ligands (also referred to herein as “biaryl compound”), biaryl complexes, methods of making biaryl compounds, methods of making single enantiomers of these biaryl compounds, methods of use (e.g., catalysis) and the like.

Abstract: Provided herein are cyclic phosphorus-containing prodrug compounds, their preparation and their uses, such as treating diseases via modulating molecular targets in the liver.

Abstract: Provided is a process for depolymerizing lignin, the process comprising exposing a liquid feed comprising lignin and a solvent to a metal-incorporated solid mesoporous silicate catalyst under conditions sufficient to depolymerize the lignin to produce one or more aromatic monomers.

Abstract: We claim a simple strategy for the synthesis of a collection of C(3?)-spirodihydroisobenzo-furannulated and C(3?)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diastereoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library.

Abstract: The present invention relates to a process for an epimerization of a saccharide in a microdevice consisting of a network of micron-sized channels in presence of molybdenum containing catalyst. It further relates to the use of a microdevice consisting of a network of micron-sized channels for the epimerization reaction of saccharides and the oligomerization of the thus obtained epimerized saccharide, preferably into manno-oligosaccharides.

Abstract: The present invention relates to pyrazolotriazolyl nucleoside analogs, such as oligonucleotide comprising them, and uses in treatment of hepatitis C virus infections. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide.

Abstract: The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substituents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone.

Abstract: There is provided processes for the purification of rebaudioside A from Steviol glycoside compositions, such as Stevia extracts. Also provided are pure compositions and formulations thereof of rebaudioside A with traces amounts of remaining steviol glycosides of less than 1%. Also provided are prepared foods, beverages, medicines and dietary supplements containing pure rebaudioside A.

Abstract: A compound of Formula (I) wherein Y1, Y2, X1, X2, R1, R2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.

Abstract: The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17?-ethynyl-androst-5-ene-3?,7?,17?-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

Abstract: Various aspects and embodiments of the present disclosure relate to the purification antibodies by hydrophobic interaction chromatography under no-salt conditions.