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US 2014/0005168 A1Published application
5-azaindazole compounds and methods of use
AssigneeGenentech, Inc.
InventorsSteven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang
Life of this patent
Estimating the term…
Abstract
5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, 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.
Claims20
A compound selected from Formula I:
- and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein:
- R1 is a five-membered or six-membered heteroaryl, optionally substituted with one or more groups independently selected from F, Cl, Br, —CN, —NO2, OH, C1-C12 alkyl, —NH(C1-C12 alkyl), —N(C1-C12 alkyl)2, —O(C1-C12 alkyl), —S(C1-C12 alkyl), —S(O)2(C1-C12 alkyl), —S(O)2N(C1-C12 alkyl)2, —(C1-C12 alkylene)-(C3-C12 carbocyclyl), —(C1-C12 alkylene)-(C2-C20 heterocyclyl), —(C2-C8 alkenylene)-(C3-C12 carbocyclyl), —(C2-C8 alkenylene)-(C2-C20 heterocyclyl), C6-C20 aryl, —(C6-C20 arylene)-(C2-C20 heterocyclyl), —(C6-C20 arylene)-(C1-C12 alkylene)-(C2-C20 heterocyclyl), C3-C12 carbocyclyl, C2-C20 heterocyclyl, and C1-C20 heteroaryl, where alkyl, alkenyl, alkynyl, alkylene, carbocyclyl, 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, —CH2CH2NH2, —CH2CHCH2NH2, —CH2CH(CH3)NH2, —CH2OH, —CH2CH2OH, —C(CH3)2OH, —CH(OH)CH(CH3)2, —C(CH3)2CH2OH, —CH2CH2SO2CH3, —CN, —CHF2, —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, —N(CH3)C(CH3)2CONH2, —N(CH3)CH2CH2S(O)2CH3, ═O, —OH, —OCH3, —OCH2CH3, —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;
- and
- R2 is phenyl or a six-membered heteroaryl, where the phenyl or the six-membered heteroaryl is optionally substituted with one or more groups independently selected from F, Cl, Br, —CN, —NO2, OH, C1-C12 alkyl, —NH(C1-C12 alkyl), —N(C1-C12 alkyl)2, —O(C1-C12 alkyl), —S(C1-C12 alkyl), —S(O)2(C1-C12 alkyl), —S(O)2N(C1-C12 alkyl)2, —(C1-C12 alkylene)-(C3-C12 carbocyclyl), —(C1-C12 alkylene)-(C2-C20 heterocyclyl), —O(C2-C20 heterocyclyl), —NH(C2-C20 heterocyclyl), —N(C1-C12 alkyl)(C2-C20 heterocyclyl), —(C2-C8 alkenylene)-(C3-C12 carbocyclyl), —(C2-C8 alkenylene)-(C2-C20 heterocyclyl), C6-C20 aryl, —(C6-C20 arylene)-(C2-C20 heterocyclyl), —(C6-C20 arylene)-(C1-C12 alkylene)-(C2-C20 heterocyclyl), C3-C12 carbocyclyl, C2-C20 heterocyclyl, and C1-C20 heteroaryl, where alkyl, alkenyl, alkynyl, alkylene, carbocyclyl, 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, —CH2CH2NH2, —CH2CHCH2NH2, —CH2CH(CH3)NH2, —CH2OH, —CH2CH2OH, —C(CH3)2OH, —CH(OH)CH(CH3)2, —C(CH3)2CH2OH, —CH2CH2SO2CH3, —CN, —CHF2, —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, —N(CH3)C(CH3)2CONH2, —N(CH3)CH2CH2S(O)2CH3, ═O, —OH, —OCH3, —OCH2CH3, —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.
1 more element
Dependencies are inferred from the claim text.