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: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste

Abstract: Provided herein are compounds of Formula (I?) or (A?), pharmaceutical compositions comprising the compounds, and methods of use thereof. The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including PI3 kinase activity.

Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.

Abstract: Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill A. baumannii. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.

Abstract: Disclosed are a compound, a stereisomer and a tautomer thereof, a pharmaceutically acceptable salt thereof, and a solvate or a prodrug thereof, which can be used for preventing or treating a ROR? mediated disease. The compound has the structural formula (I).

Abstract: The present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in reducing uric acid level, preventing or reducing inflammations, and preventing or treating uratic or gouty diseases. In particular, the present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in the manufacture of a medicament for the treatment or prevention of hyperuricemia, gout, gouty inflammations, pain and uric acid nephropathy. R1 represents hydrogen, C1-4 alkyl or the like. R2 represents C1-10 alkyl or the like. R3 represents halogen or the like.

Abstract: The present invention relates to compounds of formula (I): and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The disclosure relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.

Abstract: The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.

Abstract: The present invention relates to a novel polymorph of nilotinib hydrochloride (Form X), to processes for its preparation, to pharmaceutical compositions containing the same and to its use in medicine.

Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

Abstract: A compound of formula (I), having histone deacetylase 6 (HDAC6) inhibitory activity, wherein X, Q, N, R1, R2, L, and n are as described, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.

Abstract: A process for preparing a compound of formula (I): or a pharmaceutically acceptable salt thereof includes reacting a compound of formula (6): (wherein R is H) with 2-aminocyclohexanol or a salt thereof.

Abstract: A pyridine compound represented by formula (I), or an N-oxide thereof is provided, wherein the variable groups are as defined in the specification. The pyridine compound of formula has excellent control effects against harmful arthropods.

Abstract: The present invention relates to a liquid pharmaceutical composition suitable for parenteral administration comprising: a) pemetrexed diacid; b) at least one organic amine; c) at least one antioxidant; d) 10-200 mg/ml of propylene glycol; and e) one or more parenteral solvents, wherein the preparation thereof is conducted in an atmosphere of inert gas and wherein the organic amine(s) is present in an amount sufficient to reach a pH of the composition in the range from 8.3 to 9.1.

Abstract: The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.

Abstract: The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.

Abstract: A compound having formula I for histone deacetylase inhibition is provided: or a pharmaceutically acceptable salt or hydrate thereof wherein R is alkyl, C6-18 aryl, C5-18 heteroaryl, C8-22 alkylaryl, C8-22 alkylheteroaryl, or halo.