Abstract: Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C1-C8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.

Abstract: Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

Abstract: The present disclosure provides compounds represented by Formula I: wherein R1, R2a, R2b, R2c, R2d, R3, R4a, R4b, A, L, X, Y, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are BCR-ABL inhibitors. BCR-ABL inhibitors are useful for the treatment of cancer and other diseases.

Abstract: The present disclosure provides compounds represented by Formula I: wherein R3, A, A1, A2, A3, E, E1, E2, L, Q, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are KRAS inhibitors and are thus useful to treat cancer and other diseases.

Abstract: Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

Abstract: The present disclosure provides compounds represented by Formula I: wherein R3, A, A1, A2, A3, E, E1, E2, L, Q, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are KRAS inhibitors and are thus useful to treat cancer and other diseases.

Abstract: A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.

Abstract: A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.

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: A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.

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: A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.

Abstract: Disclosed herein are certain indoloquinolone compounds, methods of preparation thereof, pharmaceutical compositions thereof, and uses thereof, such as their uses as ALK inhibitors.

Abstract: Disclosed herein are certain indoloquinolone compounds, methods of preparation thereof, pharmaceutical compositions thereof, and uses thereof, such as their uses as ALK inhibitors