发明名称 BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS
摘要 The present invention provides compounds of Formula I,;;and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
申请公布号 US2014371201(A1) 申请公布日期 2014.12.18
申请号 US201414302337 申请日期 2014.06.11
申请人 AMGEN INC. 发明人 WEISS Matthew;BOEZIO Alessandro;BOEZIO Christiane;BUTLER John R.;CHU-MOYER Margaret Yuhua;DIMAURO Erin F.;DINEEN Thomas;GRACEFFA Russell;GUZMAN-PEREZ Angel;HUANG Hongbing;KREIMAN Charles;LA Daniel;MARX Isaac E.;MILGRIM Benjamin Charles;NGUYEN Hanh Nho;PETERSON Emily;ROMERO Karina;SPARLING Brian
分类号 C07D471/04;C07D401/12;C07D215/227;C07D417/12;C07C53/18;C07D413/12;C07D413/14 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of Formula I, or a pharmaceutically acceptable salt thereof,wherein: each of A1 and A2 is, independently, CRa or N, provided no more than one of A1and A2 is N; wherein each Ra is independently H, halo, —NRcRc, —OH, hydroxyC1-6alkyl, —C1-6alkyl, —OC1-6alkyl, —C1-6haloalkyl, —OC1-6haloalkyl or —CN, andRa is H, —C1-6alkyl or acetyl; R1 is a 6 membered aryl or heteroaryl, wherein the aryl or heteroaryl is substituted with from 1 to 4 substituents independently selected from A, halo, OH, —NRbRb, —C1-6alkyl, —OC1-6alkyl, —OC1-6alkylCF3, —OC1-6alkylCN, —(CRcRc)mCN, —C1-6alkylOC1-6alkyl, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, —OCH2F, —(CRcRc)mA, —N(Rc)(CRcRc)mA, —O(CRcRc)mA, —O(CRcRc)mOA or —C(═O)A, provided at least one substituent on R1 is —(CRcRc)mA, —N(Rc)(CRcRc)mA, —O(CRcRc)mA, —O(CRcRc)mOA or —C(═O)A; A is a 4 to 9 membered aryl, heteroaryl or heterocycloalkyl group, where the heteroaryl or heterocycloalkyl group can have from 1 to 3 heteroatoms independently selected from O, N or S, or a 3 to 6 membered cycloalkyl group, and the aryl, heteroaryl, heterocycloalkyl or cycloalkyl group can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo, —NRbRb, —C1-6alkyl, —OC1-6alkyl, —(CRcRc)mOH, hydroxyC1-6alkyl, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, —OCH2F, —CN, —C(═O)NRbRb, —O(CRcRc)mB or —(CRcRc)mB; B is a 3 to 5 membered cycloalkyl group that can be unsubstituted or substituted with from 1 to 4 substituents independently selected from Cl, F, Br, —NHCH3, —N(CH3)2, —C1-4alkyl, —OC1-4alkyl, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, —OCH2F or —CN; R2 is a 5 to 6 membered aryl or heteroaryl, where the heteroaryl can have from 1 to 3 heteroatoms independently selected from O, N or S, and the aryl and heteroaryl group can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo, —NRbRb, —C1-6alkyl, —OC1-6alkyl, —(CRcRc)nNRbRb, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, —OCH2F, —CN or —C(═O)NRbRb; each Rb is independently H or —C1-6alkyl; each Rc is independently H or —C1-6alkyl; and each Rd is independently H, halo, —CN, —NRcRc, —OH, —C1-6alkyl, —C1-6haloalkyl, —OC1-6haloalkyl or —OC1-6alkyl; each Re is independently H, halo, —CN, —NRcRc, —OH, —C1-6alkyl or —OC1-6alkyl; each n is independently 0, 1, 2, 3 or 4; and each m is independently 0, 1, 2, 3 or 4.
地址 Thousand Oaks CA US
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