发明名称 Inhibitors of the Renal Outer Medullary Potassium Channel
摘要 The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.;
申请公布号 US2014206618(A1) 申请公布日期 2014.07.24
申请号 US201214239649 申请日期 2012.08.16
申请人 Pasternak Alexander;Blizzard Timothy;Chobanian Harry;de Jesus Reynalda;Ding Fa-Xiang;Dong Shuzhi;Gude Candido;Kim Dooseop;Tang Haifeng;Walsh Shawn;Pio Barbara;Jiang Jinlong 发明人 Pasternak Alexander;Blizzard Timothy;Chobanian Harry;de Jesus Reynalda;Ding Fa-Xiang;Dong Shuzhi;Gude Candido;Kim Dooseop;Tang Haifeng;Walsh Shawn;Pio Barbara;Jiang Jinlong
分类号 C07D498/04;A61K45/06;A61K31/4985;C07D513/04;A61K31/542;C07D487/04;A61K31/5383;A61K31/553 主分类号 C07D498/04
代理机构 代理人
主权项 1. A compound having structural Formula Ia: or a pharmaceutically acceptable salts thereof wherein: Z is R1 is wherein *** indicates attachment to the carbonyl carbon and ** indicates attachment to the tetrazolyl ring in Formula Ia; X is O, NH or S; m is an integer selected from 1 or 2; n is an integer selected from 1 or 2; X1, X2 and X3 are each independently selected from C(R7) or N, provided that at least one of X1, X2 and X3 must be N and at most two of X1, X2 and X3 are N; Ra is —CN; Rb is —H or —C1-6alkyl; R2 is —H, —F, —Cl, —C1-6alkyl, —C3-6cycloalkyl or —OC1-6alkyl; R3 is —H, —F, —Cl, —CN, —C1-6alkyl, —C3-6cycloalkyl or —OC1-6alkyl; R4 is —F, —Cl, —CN, —C1-6alkyl, —C3-6cycloalkyl, —OC1-4alkyl or N-tetrazolyl; or R3 and R4 are joined together with the carbon atoms in the phenyl ring to which they are attached to form: wherein R is —H or —C1-4alkyl; R5 is —H, —Cl, —F, —CN, —C1-4alkyl, —C3-6cycloalkyl or —OC1-4alkyl; provided that when R3 and R4 are not joined together, then one and only one of R3, R4 or R5 is —CN; R6 is —H or —C1-4alkyl; and R7 is —H, —F, —Cl or —C1-4alkyl.
地址 Princeton NJ US