TRPV4 antagonists,申请号US201214125370-传众专利搜索

TRPV4 antagonists

申请公布号：US9487507(B2)

申请号：US201214125370

申请日期：2012.06.15

申请公布日期：2016.11.08

申请人：

GlaxoSmithKline Intellectual Property (No. 2) Limited

发明人：Brooks Carl;Cheung Mui;Eidam Hilary Schenck;Goodman Krista B.;Hammond Marlys;Hilfiker Mark A.;Patterson Jaclyn R.;Stoy Patrick;Ye Guosen

分类号：A01N43/76;A61K31/42;C07D263/52;C07D498/00;C07D413/14;C07D413/06;C07D413/08

主分类号：A01N43/76

代理人：Dustman Wayne J.;Gimmi Edward R.

地址：Brentford, Middlesex GB

摘要：The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

主权项：1. A compound of Formula (I): wherein: R1 is hydrogen, C1-3 alkyl, CH2OH, CH2—O—CH3, CH2OCH2Ph, CH2CN, CN, halo, or C(O)OCH3; R2 is independently hydrogen, CN, halo or C1-3 alkyl R3 is hydrogen; X is N; A is (CH2)n-phenyl, (CH2)n-naphthyl, (CH2)n—C(O)-phenyl, (CH2)n-dihydroindenyl, (CH2)n-tetrahydronaphthalenyl, (CH2)n-dihydrobenzodioxinyl, (CH2)n-dihydroindenyl, or (CH2)n-dimethyldihydrobenzofuranyl; wherein phenyl may be substituted by one or more substituents chosen from: halo, OH, OCF3, OC1-3 alkyl, C1-4 alkyl, C(CH3)2CN, CH2CN, OCH2CN, C3-6 cycloalkyl, phenyl, CF3, O-phenyl, CN, OCH2-phenyl, CH2O-phenyl, piperidinyl, piperazinyl, het, O-het, O—CH2-het, or CH2-het; het is pyridine, pyrimidine, pyridazine, pyrazine, or isoxazole; and further wherein the phenyl or het substituent on A may be further substituted by one or two: halo, OC1-3 alkyl, CN, C1-4 alkyl, or C(O)NH2; n is 0 or 1; and y is 1 or 2; or a pharmaceutically acceptable salt thereof.