发明名称 Diazeniumdiolate heterocyclic derivatives
摘要 A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.;
申请公布号 US9108920(B2) 申请公布日期 2015.08.18
申请号 US201113881929 申请日期 2011.10.25
申请人 Merck Sharp & Dohme Corp. 发明人 Ali Amjad;Lo Michael Man-Chu;Baker Robert K.;Guo Zhiqiang;Whitehead Brent;Henderson Timothy J.;Metzger Edward;Yan Lin;Shah Shrenik K.;Dellureficio James;Wang Jun
分类号 A61K31/655;C07D207/12;C07D211/44;C07D205/04;C07D207/16;C07D207/273;C07D307/20;C07D309/12;C07D401/04;C07D401/12;C07D403/04;C07D403/10;C07D413/04;C07D413/10;C07D417/04 主分类号 A61K31/655
代理机构 代理人 Beeler Nicole M.;Fitch Catherine D.
主权项 1. A compound having the formula I: or a pharmaceutically acceptable salt thereof, wherein X is O or NR7; R1 is hydrogen, —C(O)OC1-6alkyl, or —C(O)OH, or together with R2, forms ═O; R2 is hydrogen, or together with R1, forms ═O; R3 and R4 are independently —C1-6alkyl,—CD2C1-5alkyl,—C2-5alkylene-OH,—C2-5alkylene-O—C(O)C1-6alkyl,—C1-6alkylene-aryl, or—CH2CH═CH2,or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R5 and R6, which are attached to any available carbon ring atom, are independently hydrogen, —C1-6alkyl,—C(O)OC1-6alkyl,—C(O)OH,aryl,or R5 and R6, when they are attached to the same carbon atom, together form ═O; R7 is hydrogen,deuterium,—C1-6alkyl,—C1-6alkylene-aryl,—C1-6alkyleneC(O)O—C1-6alkyl,—C1-6alkyleneCF3,—CN,—C(O)O—C1-6alkyl,—C(O)C1-6alkyl,—C(O)OC3-6carbocycle,—C(O)CHF2,—C(O)CHF3,—C(O)CH2OH,—C(O)aryl,—C(O)C1-6alkyleneOHC(O)C3-6carbocycle,—C(O)NH2,—C(O)NHC1-6alkyl,—C(O)heterocycle,—C(O)NHC3-6carbocycle,—C(O)N(C1-6alkyl)C1-6alkyl,—C(O)NHSO2aryl,—SOC1-6alkyl,—SO2C1-6alkyl,—SO2CF3,—SO2aryl,—SO2heteroaryl,aryl,heteroaryl,heterocycle, or—C3-6carbocycle;wherein aryl, alkyl, carbocycle, heteroaryl, and heterocycle are unsubstituted or substituted with 1, 2, 3 or 4 groups independently selected from —CN, halogen, —CF3, ═O, —C(O)OC1-6alkyl or —O—C1-6alkyl.
地址 Rahway NJ US