发明名称 Cyclohexylamine isoquinolone derivatives
摘要 The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I); or isoquinoline derivatives of the formula (I′) ; useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
申请公布号 US8796458(B2) 申请公布日期 2014.08.05
申请号 US201113161003 申请日期 2011.06.15
申请人 Sanofi 发明人 Plettenburg Oliver;Hofmeister Armin;Kadereit Dieter;Brendel Joachim;Loehn Matthias;Altenburger Jean-Michel
分类号 C07D217/22;A61K31/545;C07D217/24 主分类号 C07D217/22
代理机构 Scully, Scott, Murphy & Presser, P.C. 代理人 Scully, Scott, Murphy & Presser, P.C.
主权项 1. A method of treating pulmonary hypertension, glaucoma, neuronal degeneration or Alzheimer's disease in a patient comprising administering to said patient an effective amount of at least one compound of the formulae (I) or (I′):wherein R1 is H; R2 is H; R3 is H; R4 is H, halogen, OH, CN, (C1-C6)alkyl; R5 is H, halogen, CN, NO2, (C1-C6)alkyl, (C2-C6)alkenyl, —NH2, NH—SO2H, NH—SO2—(C1-C6)alkyl, NH—C(O)—(C1-C6)alkyl, C(O)N[(C1-C6)alkyl]2, C(O)OH or C(O)O—(C1-C6)alkyl; R6 and R6′ are independently of each other H, R′, (C1-C8)alkyl, (C1-C6)alkylene-R′, (C1-C6)alkylene-O—(C1-C6)alkyl, (C1-C6)alkylene-O—R′, (C1-C6)alkylene-CH[R′]2, (C1-C6)alkylene-C(O)—R′, (C1-C6)alkylene-C(O)NH2, (C1-C6)alkylene-C(O)NH—R′, or (C1-C6)alkylene-C(O)N[R′]2; R7 and R8 are independently of each other H, halogen, CN, NO2, (C1-C6)alkyl, O—(C1-C6)alkyl, (C2-C6)alkenyl, NH2, NH—SO2H, NH—SO2—(C1-C6)alkyl, SO2—NH2, NH—C(O)—(C1-C6)alkyl, C(O)N[(C1-C6)alkyl]2, C(O)OH, or C(O)O—(C1-C6)alkyl; R9 is halogen or (C1-C6)alkyl; R′ is (C3-C8)cycloalkyl, (C5-C10)heterocyclyl or (C6-C10)aryl; n is 0; and L is O or O—(C1-C6)alkylene; wherein in residues R4, R5, R7 and R8 one alkyl or alkylene hydrogen atom can optionally be substituted by OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 or CON(CH3)2, or a pharmaceutically acceptable salt thereof, or a stereoisomeric form thereof, or a pharmaceutically acceptable salt of a stereoisomeric form thereof.
地址 Paris FR