Pyrazole compounds
AssigneeKinetek Pharmaceuticals, Inc.
InventorsZaihui Zhang, Jun Yan, Danny Leung, Penelope C. Costello, Jasbinder Sanghera
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Abstract
Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
Claims18
A composition comprising a compound of formula (1)
- or a stereoisomer, solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient, where
- R1 and R2 are selected from H and direct bond;
- R3 and R4 are selected from —NH2, NHC(═O)R5, and ═O;
- R5 is selected from R6, R7, and R8, where R6) is selected from alkyl, heteroalkyl, aryl and heteroaryl;
- R7 is selected from (R6)k-alkylene, (R6)k-heteroalkylene, (R6)k-arylene and (R6)k-heteroarylene;
- R8 is selected from (R7)k-alkylene, (R7)k-heteroalkylene, (R7)k-arylene, and (R7)k-heteroarylene;
- and k is selected from 0, 1, 2, 3, 4 and 5;
- and
- n is selected from 0, 1, 2, 3, 4 or 5.
A method of treating a hyperproliferative disorder, the method comprising:
- contacting a patient suffering from said hyperproliferative disorder with an effective dose of a compound of the formula:
- or a stereoisomer, solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient, where
- R1 and R2 are selected from H and direct bond;
- R3 and R4 are selected from —NH2, NHC(═O)R5, and ═O;
- R5 is selected from R6, R7, and R8, where R6 is selected from alkyl, heteroalkyl, aryl and heteroaryl;
- R7 is selected from (R6)k-alkylene, (R6)k-heteroalkylene, (R6)k-arylene and (R6)k-heteroarylene;
- R8 is selected from (R7)k-alkylene, (R7)k-heteroalkylene, (R7)k-arylene, and (R7)k-heteroarylene;
- and k is selected from 0, 1, 2, 3, 4 and 5;
- and
- n is selected from 0, 1, 2, 3, 4 or 5.
Dependencies are inferred from the claim text.