Abstract: The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGF?R1), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, preferably colon cancer, melanoma, hepatocellular carcinoma, renal cancer, glioblastoma, pancreatic cancer, myelodysplastic syndrome, lung cancer, and gastric cancer, and/or fibrosis, preferably liver fibrosis and chronic kidney disease.

Abstract: Provided herein are compounds useful for kinase inhibition.

Abstract: The present disclosure provides novel furanone compounds, or pharmaceutically acceptable salts, solvates or prodrugs thereof, as Raf kinase, especially BRAF kinase, inhibitors, which are useful therapeutic agents for treatment of Raf kinase related diseases or disorders, such as melanomas, cancers, and leukemia. The disclosure also provides methods and processes for preparing these novel furanone compounds, pharmaceutical compositions containing these furanone compounds, and methods of treatment using these furanone compounds.

Abstract: The present invention refers to co-crystals of monoacid salts of the pharmaceutical active ingredient named Lapatinib and to processes for the preparation thereof and medical uses.

Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:

Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.

Abstract: The present invention relates to compounds of the formula I wherein the substituents are defined in the claims and the specification.

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions.

Abstract: The present invention relates to imidazo pyridine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:

Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Crystalline form, Form T2H1.5-4, of N,Ndicyclopropyl-4-(1,5-dimethyl-1 Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, (Compound (I)) is provided. Also provided is a pharmaceutical composition and an oral dosage form comprising Form T2H1.5-4 of Compound (I) as well as a method of using the Form T2H1.5-4 of Compound (I) in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to processes for preparing enantiopure Lupanine and Sparteine.

Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

Abstract: Disclosed are novel compounds comprising an imino-ribose derivative covalently linked to a carbocycle or heterocycle. Pharmaceutical compositions comprising the compounds of the invention are also described. Methods of inhibition, treatment and/or suppression of viral infections with the compounds of the invention are also described. The compositions or methods may optionally comprise one or more additional anti-viral agents.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the pyrazolo-pyrrolidin-4-one derivatives, and their use as BET inhibitors for the treatment of conditions or diseases such as cancer. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.

Abstract: The invention relates to a multilayer superoleophobic and/or superhydrophobic material comprising: on the one hand, a first constituent that is a conductive substrate or a substrate that has previously been rendered conductive (1): the surface of which is modified by chemical and/or physical treatment (2) and that incorporates a first adhesion-promoting conductive layer (3); or that incorporates a first adhesion-promoting conductive layer (3); and, on the other hand, at least one other constituent that is a superoleophobic and/or superhydrophobic polymer or copolymer layer (4, 5 or 6) composed of one or more monomers based on an aromatic or heteroaromatic ring substituted by one or more fluorocarbon and/or hydrocarbon chains. It is characterized in that the various constituents of said material comply with an increasing hydrophobicity gradient between the first layer deposited on the conductive substrate or substrate previously rendered conductive (1) and the last layer of said material.

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP 17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract: The present invention provides a compound of formula (I) or the salt thereof: wherein R is at least one selected from the group consisting of unsubstituted C1-4 alkyl, C1-4 alkyl substituted by C6-18 aryl or —OR1, and —C(?O)Z. The compound is a type-S protein kinase inhibitor, which binds to an ATP-binding site and a substrate-recognition site of a protein kinase simultaneously. The present invention further provides a pharmaceutical composition, which includes a compound of formula (I) or a salt and a pharmaceutically acceptable carrier thereof. The present invention further provides a use of a compound of formula (I) or a salt thereof, which is for the manufacture of a protein kinase inhibitor as a drug.

Abstract: The present disclosure relates to a benzoyl substituted carbazole-dioxazine pigment and its preparation. The process involves benzoylation of 3-nitro-N-ethylcarbazole in monochlorobenzene using benzoylchloride and ferric chloride to yield 3-nitro-6-benzoyl-N-ethyl carbazole, which on catalytic hydrogenation and subsequent condensation with chloranil and cyclisation yields benzoyl substituted carbazole-dioxazine pigment.

Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate salt was synthesized and isolated. The pentafluorosulfanyl salt was examined in a wide assortment of reactions to form novel SF5-bearing alkenes, alkynes, and biaryl derivatives using Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation of the salt furnished the corresponding p-SF5—C6H4X,C6H4OS(O)(CF3)?NSO2CF3, and p-SF5—C6H4—NTf2 derivatives. The azide derivative p-SF5—C6H4N3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. Various SF5-bearing alkenes were synthesized by coupling reactions using a metal catalyst. Fluorodediazoniation selectively furnished the fluoro derivative p-SF5—C6H4F. Homolytic dediazoniation gave the unsymmetrical biaryls, thus demonstrating the broad utility of pentafluorosulfanyl diazonium salts as building blocks of SF5-aromatics that are in high demand in many branches of chemistry including biomedicine and materials chemistry.

Abstract: The present disclosure relates, in exemplary embodiments, to compositions of matter comprising synthetic blends of at least two feedstocks that produce a distribution of fluorinated polyhedral oligomeric silsesquioxane molecule structures. The present disclosure also relates, in exemplary embodiments, to methods of making such synthetic blends.

Abstract: [PROBLEM] To provide a novel method for suppressing heat discoloration of lecithin and a novel lecithin or lecithin preparation having resistance to heat discoloration. [SOLUTION] A method for suppressing heat discoloration of lecithin, comprising adding a fatty acid metal salt to lecithin, and a lecithin or lecithin preparation having resistance to heat discoloration and containing a fatty acid metal salt. Preferably, the metal constituting the fatty acid metal salt is at least one selected from the group consisting of lithium, beryllium, sodium, magnesium, aluminum, potassium, calcium, iron, cobalt, nickel, copper, zinc, silver, barium, thallium, and lead, and the fatty acid of the fatty acid metal salt is at least one selected from saturated fatty acids and unsaturated fatty acids having 3 to 36 carbon atoms.

Abstract: The present invention relates to the use of certain platinum compounds including [PtCb(cis-1,4-diaminocyclohexane)], or combinations of these compounds with a variety of other agents for treating and/or preventing the progression of colorectal cancer in mammals. In particular, the invention provides methods of treating and/or preventing oxaliplatin-refractory colorectal cancer in mammals.

Abstract: A method for the purification of idraparinux sodium includes: passing a solution including a crude idraparinux sodium through a column including a sodium ion exchange resin to obtain a first mixture; passing a solution including the first mixture through a gel chromatogaphy column to obtain a second mixture; and precipitating a purified idraparinux sodium from a solution including the second mixture.

Abstract: Systems for converting aldose sugars to ketose sugars and separating and/or concentrating these sugars using differences in the sugars' abilities to bind to specific affinity ligands are described.

Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Abstract: It has been found that adding carbon dioxide or the like to a solution containing arbekacin free base makes it possible to produce arbekacin derivatives including arbekacin carbonate and carbamic acid of arbekacin. Moreover, it has been found that the arbekacin derivatives have a high stability, and that the use thereof enables efficient productions of highly-pure arbekacin free base and pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a preparation method of trihydroxyethyl rutoside. In the method, rutin is firstly prepared into 7-monohydroxyethyl rutoside with a purity of greater than or equal to 98% by weight, and then 7-monohydroxyethyl rutoside is hydroxyethylated to give troxerutin having less than 2% of non-hydroxyethylated rutoside derivatives. The amount of 7,3?,4?-trihydroxyethyl rutoside in troxerutin is more than 80% by weight. The product is further purified so that 7,3?,4?-trihydroxyethyl rutoside with a purity of greater than or equal to 98% by weight could be obtained.

Abstract: Provided is a compound of the general formula (I): The compound of formula (I) is suitable for treating pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a mammal. Also provided is a method for treatment of pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a human subject having a galectin-3 level indicative of pulmonary fibrosis or exacerbation of symptoms as well as a method for making said compound.

Abstract: The invention relates to compounds of Formula A: or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including obesity, insulin sensitivity, inflammation, cholestasis, and bile desaturation.

Abstract: A method of preparing a thioic acid intermediate of fluticasone propionate includes: treating a 17?-[(N,N-dimethyl carbamoyl)thio]carbonyl compound in a solution including an alcohol and an alkali metal hydroxide, an alkaline-earth metal hydroxide, or a mixture thereof to cleave an amide from the 17?-[(N,N-dimethyl carbamoyl)thio]carbonyl compound; treating the solution to separate an aqueous portion; and adding an acid to the aqueous portion to obtain the thioic acid intermediate of fluticasone propionate. A method of preparing fluticasone propionate includes preparing the thioic acid intermediate of fluticasone propionate, and alkylating the thioic acid intermediate of fluticasone propionate to prepare the fluticasone propionate.

Abstract: Prodrugs or pharmaceutically acceptable salts, stereoisomers, solvates, or polymorphs thereof include a pharmaceutically and/or diagnostically active cationic steroidal antimicrobial (hereinafter “CSA”) compound or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof, and one or more cleavable groups (C.G.). Some embodiments include a CSA compound prepared in an inactive or less active form and that is capable of conversion to a fully active form upon administration to a subject, upon preparation of a pharmaceutical formulation containing the CSA composition, and/or upon exposure to physiological conditions. Pharmaceutical compositions include the prodrug or pharmaceutically acceptable salt, stereoisomer, solvate, or polymorph thereof and one or more pharmaceutically acceptable excipients.

Abstract: The invention relates to novel peptide-silane “hybrid block” molecules, to the synthesis thereof and to the use of same for producing novel peptide-silica hybrid materials that can be used in various applications.

Abstract: Compounds comprising peptides and peptidomimetics capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. Methods of making and using the compounds are also disclosed.

Abstract: The present invention relates to ?-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.

Abstract: The present invention relates to a fusion protein comprising a mussel adhesive protein and a silica-binding peptide linked to the mussel adhesive protein, a silica nanoparticle a silica connected to the fusion protein, a fusion protein-silica nanoparticle complex comprising the silica nanoparticle having bioactivity and adhesiveness for cell proliferation and accelerating the differentiation, a surface coating composition including the complex, its use, and a method of coating a surface using the surface coating composition.

Abstract: Compositions, formulations and kits comprising chlorotoxin conjugate compounds are provided, including native and modified variants of chlorotoxin peptide conjugated to reporter molecules including fluorescent dyes. Methods of detecting and treating cancers and tumors with chlorotoxin conjugate compounds are also provided, including methods of imaging tumor tissues and cells. Dosing and pharmacokinetic profiles for therapeutic and diagnostic applications using chlorotoxin conjugate compounds are also provided.

Abstract: The invention relates to complement inhibitors that inhibit both the classical and alternative complement pathways. In particular, the invention relates to complement inhibitors derived from the salivary glands of haematophagous arthropods that inhibit both the classical and alternative complement pathways. The invention also relates to the use of such complement inhibitors in the treatment and prevention of diseases.

Abstract: The invention relates to Factor H gene polymorphisms and haplotypes associated with an elevated or a reduced risk of AMD. The invention provides methods and reagents for diagnosis and treatment of AMD.

Abstract: The present invention provides a method for producing peptides by recombinant means. The peptides are expressed as part of a fusion protein comprising the target peptide and an engineered intein. The invention also provides the engineered inteins, fusion proteins comprising these, and DNA constructs coding for these fusion proteins. Upon thiol-induced cleavage of the fusion protein the carboxy-terminal a-thioester of the target peptide is obtained. The carboxy-terminal ct-thioester can in principle react with any nucleophile and the strategy therefore allows a wider range of carboxy-terminal modifications such as chemical ligation, bioconjugation, or amidation.