发明名称 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
摘要 The present invention provides compounds of Formula I;and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
申请公布号 US2014336177(A1) 申请公布日期 2014.11.13
申请号 US201214364908 申请日期 2012.12.11
申请人 MERCK SHARP & DOHME CORP. 发明人 Pio Barbara;Pasternak Alexander;Shahripour Aurash;Tang Haifeng;Walsh Shawn
分类号 C07D513/04;A61K31/5383;A61K45/06;A61K31/542;C07D487/04;A61K31/4985;C07D498/04;A61K31/553 主分类号 C07D513/04
代理机构 代理人
主权项 1. A compound having structural Formula I: or a pharmaceutically acceptable salt thereof wherein: X is O, NH, S or SO2; R1 is —C(R9)(R10)— or —N(R13)—; m 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, Z is R2 is —H, —F, —Cl, —C1-6 alkyl, —C3-6 cycloalkyl or —OC1-6 alkyl; R3 and R3a are each independently —H, —F, —Cl, —CN, —C1-6 alkyl, —C3-6 cycloalkyl or —OC1-6 alkyl; R4 and R4a are each independently —F, —Cl, —CN, —C1-6 alkyl, —C3-6 cycloalkyl, —OC1-4 alkyl 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 —C1-4 alkyl; R5 and R5a are each independently —H, —F, —Cl, —CN, —C1-4 alkyl, —C3-6 cycloalkyl or —OC1-4 alkyl; provided that when R3 and R4 are not joined together, then one and only one of R3, R4 or R5 is —CN; and provided that one and only one of R3a, R4a or R5a is —CN; R6 is —H or —C1-4 alkyl; each R7 is independently —H, —F, —Cl, —CF3, —C1-4 alkyl or —OC1-4 alkyl; R8 is —H, —F, —Cl, —CF3, —C1-4 alkyl or —OC1-4 alkyl; R9 is —H, —F or —C1-4 alkyl; R10 is —H or —F; R11 is —H or —CH3; R12 is —H or —CH3; and R13 is —H or —C1-4 alkyl.
地址 Rahway NJ US