Abstract: The present disclosure provides compounds represented by Formula I, or an enantiomer or diastereomer, or a pharmaceutically acceptable salt thereof, wherein X, Y, Z, L, Ar, R1, R2, R3 R4, R5, R6, m, and p are defined herein. Compounds of Formula I are BCR-ABL inhibitors. BCR-ABL inhibitors are useful for the treatment of cancer and other diseases.

Abstract: The present invention relates to a pharmaceutical composition comprising a sulfonamide as an inhibitor of Bcl-2/Bcl-xL, especially compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl)-5-fluorophenyl)piperazin-1-yl)-phenylaminosulfonyl)-2-trifluoromethyl sulfonyl-anilino)-4-phenylthio-butyl)-piperidine-4-carboxylic acid 3-phosphonopropyl ester or a pharmaceutically acceptable salt thereof and suitable excipients, preferably a pharmaceutical composition in the form of a lyophilized powder. The invention also relates to a method for preparing the pharmaceutical composition.

Abstract: Provided herein is a method of treating, preventing, or alleviating one or more symptoms of a disorder, disease, or condition mediated by an MDM2 with an MDM2 inhibitor, e.g., a compound of Formula (I), and a platinum compound. Also provided herein is a method of inhibiting the growth of a cell with an MDM2 inhibitor and a platinum compound.

Abstract: Disclosed is a method for preparing 2-indolinospirone compound and intermediate thereof, specifically disclosed is a method for preparing a compound of formula 5. The method is relatively simple and has high stereoselectivity and yield.

Abstract: Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, R1h, L2, L3, #, #, # are as defined as set forth in the re) specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

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: The present invention provides crystalline forms or amorphous forms of N-(phenylsulfonyl) benzoamide compound or its salts or solvates used as a Bcl-2 inhibitor, and the preparation method and the application thereof.

Abstract: Amorphous form or crystalline form of a 2-indolinolinololylspironone compound or its salt and solvate used as an MDM2 inhibitor, a preparation method and an application thereof. The amorphous form or crystalline form of the invention has good stability and is of great value for drug development, preparation development and production.

Abstract: Provided herein is a combination product comprising a Bcl-2 inhibitor, an anti-CD20 antibody and/or bendamustine or a combination product comprising a Bcl-2 inhibitor and CHOP, the combination product provides a use of the combination product for prevention and/or treatment of a disease (e.g., cancer, rheumatoid arthritis (RA), granulomatosis with polyangiitis (GPA), and microscopic polyangiitis).

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 a pharmaceutical composition comprising a Bcl-2/Bcl-xL inhibitor, a chemotherapeutic agent, and a pharmaceutically acceptable carrier. The present disclosure also provides a method of treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a Bcl-2/Bcl-xL inhibitor alone or in combination with a therapeutically effective amount of a chemotherapeutic agent. The present disclosure also provides use of a combination of a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent in the manufacture of an anti-tumor medicament. In the present disclosure, a significantly enhanced anti-tumor effect can be achieved by administration of a Bcl-2/Bcl-xL inhibitor in combination with a chemotherapeutic agent.

Abstract: The present invention relates to a combination product comprising a Bcl-2 inhibitor and a chemotherapeutic agent, and the combination product provides a use in the prevention and/or treatment of diseases (e.g., cancer).

Abstract: The present invention pertains to the biomedical field, and particularly relates to a method for treating or suppressing a cancer, reducing its severity, lowering its risk or inhibiting its metastasis in an individual. The method comprises administering to the individual a therapeutically effective amount of one or more of a FAK inhibitor, an ALK inhibitor and a ROS1 inhibitor, and a therapeutically effective amount of an EGFR inhibitor. The invention also relates to a pharmaceutical composition or kit comprising one or more of a FAK inhibitor, an ALK inhibitor and a ROS1 inhibitor, and an EGFR inhibitor.

Abstract: Provided herein is a combination product comprising a Bcl-2 inhibitor (or a Bc1-2/Bc1-xl dual inhibitor) and a BTK inhibitor, the combination product providing a use in the prevention and/or treatment of a disease (e.g., cancer, autoimmune disease and inflammatory disease.).

Abstract: Provided herein is a combination product comprising a Bcl-2 inhibitor and an MDM-2 inhibitor, the combination product providing a use in the prevention and/or treatment of diseases (e.g., cancer).

Abstract: Disclosed is a pharmaceutical composition comprising (i) a compound of formula (I) or a pharmaceutically acceptable salt thereof; (ii) a CDK inhibitor or a pharmaceutically acceptable salt thereof, for the prevention and/or treatment of a disease mediated by MDM2 and/or CDK activity.

Abstract: The present invention relates to a method for preparing sulfonamides which are inhibitors of Bcl-2/Bcl-xL, comprising the compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl)-5-fluorophenyl)piperazin-1-yl)-phenylaminosulfonyl)-2-trifluoro methylsulfonyl-anilino)-4-phenylthio-butyl)-4-hydroxyl-piperidine, and the present invention also relates to intermediates for the preparation of the sulfonamides, a new final product and its therapeutic use, and pharmaceutical use.

Abstract: The present invention relates to a compound for treating or preventing osteoarthritis. The compound relieves the joint pain, inhibits and attenuates the development of post-traumatic osteoarthritis in mouse model. The present invention also provides a pharmaceutical composition comprising the compound for treating or preventing osteoarthritis. The present invention further provides a method for treating or preventing osteoarthritis by administrating to the patient in need thereof with the pharmaceutical composition.

Abstract: The present invention relates to a process for preparing a sulfonamide compound which is an inhibitor of Bcl-2/Bcl-xL, including the compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl)-5-fluorophenyl)piperazine-1-yl)-phenylaminosulfonyl)-2-trifluoromethanesulfonyl-anilino)-4-phenylthio-butyl)-piperidine-4-carboxylic acid 3-phosphonopropyl ester. The present invention also relates to an intermediate for preparing the sulfonamide compound and a preparation process thereof.