发明名称 Aminopyrazine compounds
摘要 A compound of formula (I):; wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
申请公布号 US8962623(B2) 申请公布日期 2015.02.24
申请号 US201214001936 申请日期 2012.02.29
申请人 Locus Pharmaceuticals, Inc. 发明人 Shetty Rupa S.;Moriarity Kevin J.;Kelly Martha J.;Liu Bin;Zou Jinming;Moffett Kristofer K.;Lee Younghee
分类号 A61K31/5377;C07D487/04;C07D491/056;C07D401/12;C07D413/14;C07D403/12;C07D401/14;C07D407/14;C07D409/14;C07D417/14 主分类号 A61K31/5377
代理机构 Sughrue Mion, PLLC 代理人 Sughrue Mion, PLLC
主权项 1. A compound represented by formula (I) wherein G represents N, CH or CR6-2; ring1 represents benzene, pyridine, piperidine, cyclohexene, or cyclohexane, any of which is optionally substituted with 1-4 substituent(s) selected from among (1) C1-4 alkyl, (2) C1-4 alkoxy, (3) halogen, and (4) oxo;ring2 represents 5-10 membered aromatic monocyclic or bicyclic aromatic heterocyclic ring containing 1-4 heteroatom(s) selected from a nitrogen atom, an oxygen atom and/or a sulfur atom optionally oxidized;R1 represents cyclopropane, cyclobutane, cyclopentane, cyclohexane, cyclobutene, cyclopentene, cyclohexene, cyclobutadiene, cyclopentadiene, cyclohexadiene, benzene or pyridine, any ring of which is optionally substituted with 1-5 substituent(s) selected from among (1) C1-4 alkyl, (2) C1-4 alkoxy, (3) halogen, (4) CF3, and (5) CN;R2 and R3 each independently represent (1) CF3, or (2) C1-4 alkyl optionally substituted with 1-3 substituent(s) selected from among (1) OR2-1, (2) NR2-2R2-3 and (3) halogen;R4 represents (1) halogen, (2) C1-4 alkyl, (3) C1-4 alkoxy, (4) CF3, (5) OH, (6) CN, (7) ring3, (8) NR4-1R4-2, or (9) NO2;R5 represents (1) ring3, (2) C1-4 alkyl optionally substituted with halogen, OH, C1-4 alkoxy, CN, COOR5-8, or NR5-1R5-2, (3) C2-4 alkenyl, (4) C1-4 alkoxy, (5) NR5-3R5-4, (6) OH, (7) SO2R5-5, (8) SO2NR5-6R5-7, (9) COOR5-8, (10) COR5-9, (11) CONR5-10R5-11, (12) halogen, or (13) hydrogen;R6-1 and R6-2 each independently represent (1) hydrogen, (2) C1-4 alkyl, or (3) NH2;L represents (1) —O—, (2) —C1-6 alkylene-, (3) —C(O)—, (4) —O—C1-6 alkylene-, (5) —C1-6 alkylene-O—, (6) —NR7-1—, (7) —S—, (8) —SO—, (9) —SO2—, (10) —CNH— (11) —NR7-2C(O)—, (12) —NR7-3C(O)NR7-4—, (13) —C(O)NR7-5—, (14) —SO2NR7-6—, (15) —NR7-7SO2—, (16) C2-4 alkenylene, or (17) C2-4 alkynylene, wherein C1-6 alkylene is optionally substituted with OH;ring3 represents (1) C3-7 carbocyclic ring selected from among cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, cyclobutene, cyclopentene, cyclohexene, cycloheptene, cyclobutadiene, cyclopentadiene, cyclohexadiene, cycloheptadiene, and benzene, or (2) 3-7 membered monocyclic unsaturated or saturated heterocyclic ring containing 1-4 heteroatom(s) selected from a nitrogen atom, an oxygen atom and/or a sulfur atom optionally oxidized, any of which is optionally substituted with 1-5 substituent(s) selected from among (1) halogen, (2) C1-4 alkyl optionally substituted with OH, C1-4 alkoxy, or NR8-1R8-2, (3) oxo, (4) OH, (5) C1-4 alkoxy, (6) C(O)CH3, (7) NR8-3R8-4, (8) SO2CH3, (9) COOR8-5, and (10) C(O)NR8-6R8-7;R2-1, R2-2 and R2-3 each independently represent hydrogen, or C1-4 alkyl;R4-1 and R4-2 each independently represent hydrogen or C1-4 alkyl;R5-1, R5-2, R5-3, R5-4, R5-5, R5-6, R5-7, R5-8, R5-9, R5-10 and R5-11 each independently represent hydrogen or C1-6 alkyl;R7-1, R7-2, R7-3, R7-4 R7-5, R7-6 and R7-7 each independently represent hydrogen or C1-4 alkyl;R8-1, R8-2, R8-3, R84, R8-5, R8-6 and R8-7 each independently represent hydrogen or C1-4 alkyl;m represents 0 or an integer of 1-3, wherein when m is more than 1, each R4 may be same or different;n represents 0 or an integer of 1-2, wherein n is 2, each LR5 may be same or different;p represents 0 or 1; or a pharmaceutically acceptable salt thereof.
地址 Blue Bell PA US