Abstract: The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Abstract: The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R1, R2, R3, R4, R5, R6, R7 and Ar1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.

Abstract: A method for preparing indenoisoquinoline derivatives represented by the following formula (I) is disclosed, which comprises the following steps: (A) providing a first reactant represented by the following formula (II) and a second reactant represented by the following formula (III): and (B) reacting the first reactant represented by the formula (II) and the second reactant represented by the formula (III) in a solvent and selectively adding R2NH2 therein, to obtain the indenoisoquinoline derivatives represented by the formula (I), wherein, R1, R2, R3, A, X, Y, Z, m and n are defined in the specification.

Abstract: An electrically conducting organic oligomer comprising 4-nitro-1H-pyrazole-3-yl-amine, 4-trifluoromethyl-1H-pyrazol-3-yl-amine, 4-trichloromethyl-1H-pyrazol-3-yl-amine, 4-tribromomethyl-1H-pyrazol-3-yl-amine, 4-ammonium-1H-pyrazol-3-yl-amine, 4-trimethylammonium-1H-pyrazol-3-yl-amine, 4-triethylammonium-1H-pyrazol-3-yl-amine, or 4-tripropylammonium-1H-pyrazol-3-yl-amine. An electrically conducting organic oligomer made from the steps of preparing an acidic aqueous solution with a monomer, preparing the acidic aqueous solution by mixing water with a monomer (3-amino-1H-pyrazole-4-carbonitrile), forming a solution preparing a second aqueous solution, mixing the acidic aqueous solution with the second aqueous solution, and allowing a reaction to proceed at about 40° C.

Abstract: The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation.

Abstract: The present invention relates to novel heterocyclic derivatives having general formula (I) and their therapeutic use for diseases such as cancer, inflammation, pain, autoimmune diseases or neurodegenerative diseases like Alzheimer's or Parkinson's disease that can be treated by modulation of certain protein kinases. Compounds of formula (I) can be used for treatment of patients who do not respond to kinase inhibition therapy that comprises currently available medications.

Abstract: A novel imidazole compound that yields a surface treatment liquid that is very effective at suppressing migration and oxidation of a wiring surface; a metal surface treatment liquid that contains the imidazole compound; a metal surface treatment method that uses the metal surface treatment liquid; and a laminate production method that uses the surface treatment liquid. A metal is surface-treated using the surface treatment liquid which includes a saturated fatty acid or a saturated fatty acid ester of a specific structure, in which a prescribed position is substituted by an aromatic group of a prescribed structure and an imidazolyl group that may have a substituent group.

Abstract: Provided herein are lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitors, pharmaceutical compositions thereof, and methods of their use for the treatment of disease.

Abstract: The present invention belongs to the pharmaceutical field, and relates to a preparation method for a series of benzimidazole derivatives, their pharmaceutical salts and pharmaceutically acceptable prodrugs, a pharmaceutical composition containing the derivatives, and the uses of the derivatives and pharmaceutical composition in the preparation of antigout drugs and in the treatment of related diseases.

Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The applicant provides a compound for enhancing the space coupling degree of an endothelial cell ion channel complex TRPV4-KCa2.3 and anti-hypertension applications thereof. By finding the structural domains of the interacting sites of the endothelial cell ion channel complex TRPV4-KCa2.3, a compound with specificity which can act at the two interacting sites is prepared in the present invention. It is found that the compound can enhance the space coupling degree of the TRPV4-KCa2.3 complex and has great significance for the research and development of anti-hypertension drugs.

Abstract: Triazole-based molecules, methods of making and using the same are provided. Triazole-based molecules may be used as reading molecules and incorporated into or operatively-linked with electrodes, for example, and used in recognition tunneling systems to identify individual and/or sequences of molecules (e.g., DNA bases, carbohydrates, proteins, peptides, and/or amino-acids).

Abstract: A crystalline form of metsulfuron-methyl of formula (I), the crystal preparation process, the analyses of the crystal through various analytical methods and using the crystal to prepare stable agrochemical formulation. The invention also describes the use of various solvents towards the crystalline form preparation conditions.

Abstract: The present invention is directed to a process for the preparation of phosphoric acid loaded covalent organic framework (PA@Tp-Azo and PA@Tp-Stb) with high stability and high proton conductivity.

Abstract: A thermodynamically stable crystal modification of 2-methyl-N-(5-methyl-1,3,4-oxadiazol-2-yl)-3-(methylsulfonyl)-4-(trifluoromethyl)benzamide is described. This thermodynamically stable crystal modification has particular advantages in the stability of suspension formulations.

Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.

Abstract: It is possible to produce an optically active fluoroalkyl chloromethyl alcohol with a high optical purity and a good yield by treating a fluoroalkyl chloromethyl ketone with a microorganism having an activity for asymmetrically reducing the ketone or an enzyme having the activity. Then, it is possible to obtain a fluoroalkyl ethylene oxide by treating the alcohol with a base. Industrial implementation of the production method of the present invention is easy.

Abstract: The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

Abstract: The disclosure relates to a cyclic carbonate monomer containing double iodine, a biodegradable polymer prepared thereby and use. The polymer can be obtained by ring-opening polymerization of the cyclic carbonate monomer containing double iodine, without affecting the ring-opening polymerization and without a protection and deprotection process. The polymer which is obtained by ring-opening polymerization of the cyclic carbonate monomer of the present disclosure can be assembled into a nano-vesicle and a micelle as a drug carrier, a biological tissue scaffold or a CT contrast media.

Abstract: The present disclosure describes biaryl triazole compounds, as well as their compositions and methods of use. The compounds inhibit the activity of macrophage migration inhibitory factor and are useful for the treatment of diseases, e.g., inflammatory diseases and cancer.

Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.

Abstract: The present invention is directed to the compounds of Formula I which are inhibitors of tropomyosin-related kinase A (TrkA): Formula (I) or stereoisomers, tautomers or a pharmaceutically acceptable salts, metabolites, isotopes, solvates or prodrugs thereof, wherein, Ra, Rb, Rc, Rd, R1, R2, L and Het-Ar are as defined herein.

Abstract: The present invention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: each of A, B, C, D, and E, independently, is C, N, N—H, O, S, or absent; is a single bond or a double bond; each of X, Y, and Z, independently, is aryl, heteroaryl, aralkyl, H, or absent; each of L1 and L2, independently, is a moiety selected from O, CH2, C?O, C2-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, —((CH2)n—W)—, wherein n=0, 1, 2, 3, 4, or 5, and W is O or S, or absent; and when L2 is absent, Z is aryl or heteroaryl fused with BC. Also provided in the present invention is a method for inhibiting, treating and/or reducing the risk of a neuropsychiatric disorder, comprising administering a subject in need a composition comprising a compound of Formula (I).

Abstract: The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).

Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt or hydrate thereof, useful as a CGRP receptor antagonist.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine 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 to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

Abstract: The invention relates to new benzonitrile derivatives of the formula (I) wherein R1 to R3 and A are as defined in the description and Claims, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention provides compounds of Formula (I): (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: Provided is a compound having formula (I): wherein R2 is selected from —C1, —Br and —CN; R1 and R4 are independently selected from H and —F; R631, R632, R641 and R642 are independently selected from —H, —F and substituted or unsubstituted C1-C3 alkyl groups; and R651 and R652 are independently selected from H and substituted or unsubstituted C1-C3 alkyl groups and substituted or unsubstituted phenyl groups; and wherein at least one of R631, R632, R641, R642 and R652 is not —H, or wherein when all of R631, R632, R641, R642 and R652 are —H, R651 is not Me or Et.

Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, Ra, R1, R2, R3, R4, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis, metabolic syndrome, atherosclerosis, and cancer.

Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of ACK1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new ACK1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I are disclosed.

Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.

Abstract: Compounds are provided as chemokine inhibitors having the structure:

Abstract: Described herein is the development of an arenophile-mediated, nickel-catalyzed dearomative trans-1,2-carboamination protocol. A range of readily available aromatic compounds was converted to the corresponding dienes using Grignard reagents as nucleophiles. This strategy provided products with exclusive trans-selectivity and high enantioselectivity was observed in case of benzene and naphthalene. The utility of this methodology was showcased by controlled and stereoselective preparation of small, functionalized molecules. A concise synthesis of (+)-pancratistatin and (+)-7-deoxypancratistatin from benzene using an enantioselective, dearomative carboamination strategy has been achieved. This approach, in combination with the judicious choice of subsequent olefin-type difunctionalization reactions, permits rapid and controlled access to a hexasubstituted core. Finally, minimal use of intermediary steps as well as direct, late stage C-7 hydroxylation provides both natural products in six and seven operations.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

Abstract: The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.

Abstract: The present invention relates to a novel process for preparing thiazole derivatives.

Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.

Abstract: The present invention relates to compounds, 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, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

Abstract: A two-photon absorbing (TPA) compound is provided along with a method of making same. The TPA compound has a general structural formula: where R1 and R2 are independently selected from the group consisting of linear or branched alkyl chains having a general formula CnH2n+1, n ranges from about 6 to about 20, and ethoxylated alkyls having a general formula R3(OCH2CH2)mOCH2CH2—, where R3 is a C1 to C4 alkyl group, and where m ranges from 0 to about 3; and where Y is selected from the group consisting of H, OH, and alkoxyl groups.

Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

Abstract: Pyrimido[4,5-b]indole derivatives are provided. These compounds are useful to expand hematopoietic stem cell populations, particularly, human hematopoietic stem cell populations. The compounds are also useful in the medical treatment of diseases that involve hematopoietic stem cells.

Abstract: The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)

Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.

Abstract: The invention provides novel compounds having the general formula: wherein R1 to R7 are as described herein, compositions including the compounds and methods of using the compounds.