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US 9,260,425 B2Granted
Pyrazolo[3,4-c]pyridine compounds and methods of use
AssigneeGenetech, Inc.
InventorsSteven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
Life of this patent
Estimating the term…
Abstract
Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Claims14
A compound selected from Formula I:
- and stereoisomers, geometric isomers, tautomers, or pharmaceutically acceptable salts thereof, wherein:
- R1 is selected from C2-C20 heterocyclyl, C1-C20 heteroaryl, —(C1-C20 heteroaryl)-(C1-C20 heteroaryl), —(C1-C20 heteroaryl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-O—(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-O—(C1-C12 alkylene)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-NR3—(C2-C20 heterocyclyl), and —(C1-C20 heteroaryl)-NR3—(C1-C12 alkylene)-(C2-C20 heterocyclyl);
- R2 is selected from C2-C20 heterocyclyl, C1-C20 heteroaryl, C6-C20 aryl, —(C6-C20 aryl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-(C1-C20 heteroaryl), —(C1-C20 heteroaryl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-(C2-C20 heterocyclyl)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-NR3—(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-(C1-C12 alkylene)-(C2-C20 heterocyclyl), —(C1-C20 heteroaryl)-NR3—(C1-C12 alkylene)-(C2-C20 heterocyclyl), and —(C1-C20 heteroaryl)-NR3—(C1-C12 alkylene)-(C1-C20 heteroaryl);
- R3 is independently selected from H and C1-C12 alkyl optionally substituted with F, Cl, CN, —CO2H, —COCH3, —CO2CH3, —CO2C(CH3)3, —COCH(OH)CH3, —CONH2, —CONHCH3, —CON(CH3)2, —NO2, —NH2, —NHCH3, —N(CH3)2, —NHCOCH3, —N(CH3)COCH3, —NHS(O)2CH3, —NHCH2CH2NH2, —NHCH2CH2CH2NH2, —NHCH2CH2CH2CH2NH2, —N(CH3)C(CH3)2CONH2, —N(CH3)CH2CH2S(O)2CH3, ═O, —OH, —OCH3, —OCH2CH2OCH3, —OCH2CH2NH2, —S(O)2N(CH3)2, —SCH3, and —S(O)2CH3;
- where alkyl, alkylene, heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from F, Cl, Br, I, —CH3, —CH2CH3, —CH(CH3)2, —CH2CH(CH3)2, —CH2NH2, —CH2NHCH3, —CH2N(CH3)2, —CH2CH2NH2, —CH2CHCH2NH2, —CH2CHCH2CH2NH2, —CH2CH(CH3)NH2, —CH2CONH2, —CH2OH, —CH2CH2OH, —C(CH3)2OH, —CH(OH)CH(CH3)2, —C(CH3)2CH2OH, —CH2C(CH3)2OH, —CH2CH2SO2CH3, —CN, —CF3, —CO2H, —COCH3, —CO2CH3, —CO2C(CH3)3, —COCH(OH)CH3, —CONH2, —CONHCH3, —CON(CH3)2, —C(CH3)2CONH2, —NO2, —NH2, —NHCH3, —N(CH3)2, —NHCOCH3, —N(CH3)COCH3, —NHS(O)2CH3, —NHCH2CH2NH2, —NHCH2CH2CH2NH2, —NHCH2CH2CH2CH2NH2, —N(CH3)C(CH3)2CONH2, —N(CH3)CH2CH2S(O)2CH3, ═O, —OH, —OCH3, —OCH2CH2OCH3, —OCH2CH2NH2, —S(O)2N(CH3)2, —SCH3, —CH2OCH3, —S(O)2CH3, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, azetidinyl, azepanyl, oxetanyl, pyrrolidinyl, piperazinyl, piperidinyl, (piperidin-4-yl)ethyl), pyranyl, (piperidin-4-ylmethyl), morpholinomethyl, and morpholino.
2 more elements
Dependencies are inferred from the claim text.