发明名称 Ring-substituted N-pyridinyl amides as kinase inhibitors
摘要 The present invention provides a compound of formula (A):; as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
申请公布号 US9173883(B2) 申请公布日期 2015.11.03
申请号 US201314402541 申请日期 2013.05.20
申请人 NOVARTIS AG 发明人 Burger Matthew;Drumm, III Joseph E.;Nishiguchi Gisele;Rico Alice;Simmons Robert Lowell;Taft Benjamin;Tanner Huw
分类号 C07D403/12;C07D401/14;C07D401/12;C07D403/14;C07D407/14;C07D409/14;C07D417/12;C07D417/14;C07D213/81;C07D405/14;A61K31/506;A61K31/4439;A61K31/444;A61K31/4545;A61K31/675;A61K45/06;C07F9/6558 主分类号 C07D403/12
代理机构 代理人 Nardone Rona
主权项 1. A compound of Formula (A) wherein: groups attached to the ring containing Q that are depicted inside the ring are all syn to each other, and all groups attached to that ring that are depicted outside the ring are syn to one another; Q is C or N; Rq is H when Q is C, and Rd is absent when Q is N; R1 is selected from H, C1-4 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, —(CR′2)1-3—OR′ and —OR′, where each R′ is independently H or C1-4 alkyl, and each alkyl, cycloalkyl and heterocyclyl is optionally substituted with up to two groups selected from halo, CN, NH2, hydroxy, oxo, C1-4 haloalkyl, C1-4 alkoxy, and C1-4 haloalkoxy; R1b, R1c, and R1d are each independently selected from H, halo, OR′, R′, —(CH2)1-2OR′, and CONR′2; one of R2a and R2b is H, and the other of R2a and R2b is selected from CN, azido, amino, —OR, —O(CH2)1-3OR, —NRC(O)R, —NRC(O)OR, —NHSO2R, —SO2R, —OSO2R, —SR, —S(O)R, —OP(O)R2, and 1-pyridonyl or 1-triazolyl optionally substituted with up to two groups selected from halo, C1-4 alkyl, hydroxy-substituted C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, C1-4 alkoxy, and C5-6 heteroaryl; where each R is independently C5-6 heteroaryl or C1-4 alkyl optionally substituted with up to three groups selected from cyano, halo, hydroxy, carboxy, C1-4 alkylsulfonyl, and C1-4 alkoxy; or R2a and R2b taken together may form a dialkyl ketal or 5-6 membered cyclic ketal, ═O or ═N—OR″, where R″ is H or C1-4 alkyl; ring A is selected from pyridinyl, pyrimidinyl, and pyrazinyl, each having N positioned as shown in Formula (I); and Ring A is optionally substituted with 1 or 2 groups selected from halo, CN, NH2, hydroxy, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, and C1-4 haloalkoxy;or a pharmaceutically acceptable salt thereof.
地址 Basel CH