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    Derivatives of 5-benzylisoquinoline for the treatment of cardiovascular diseases
    66.
    发明专利
    Derivatives of 5-benzylisoquinoline for the treatment of cardiovascular diseases 未知

    公开(公告)号：NZ722513A

    公开(公告)日：2019-08-30

    申请号：NZ72251315

    申请日：2015-02-20

    Applicant: SERVIER LAB

    Inventor： VILLENEUVE NICOLE ,  CHIMENTI STEFANO ,  COURCHAY CHRISTINE ,  DESSINGES AIMÉE ,  GELLIBERT FRANÇOISE ,  GOUMENT BERTRAND ,  KONNERT MARC ,  PEGLION JEAN-LOUIS ,  POITEVIN CHRISTOPHE ,  VILAINE JEAN-PAUL

    IPC: C07D217/02 ,  A61K31/472 ,  A61K31/4725 ,  A61P9/00 ,  C07D217/24 ,  C07D405/06

    Abstract: Described herein are (phenyl)(isoquinolin-5-yl)methanone derivatives of formula (I), wherein X represents a carbonyl (C(=O)) group; Ri1 represents a hydrogen atom or a hydroxyl group; Ri3 represents a hydrogen atom or an alkyl group; Ri2, Ri6, Ri7 and Ri8 each represent a hydrogen atom; Ra1 and Ra5, each represent hydrogen, fluorine or an alkyl group; Ra2 represents a hydrogen atom or an alkyl group; Ra3 represents a hydrogen atom, a piperidine ring, or a group -CRy1Ry2NH(Ry3); Ra4 represents a hydrogen atom or a group -CRy1Ry2NH(Ry3); it being understood that Ra1, Ra2, Ra3, Ra4 and Ra5 may not simultaneously represent a hydrogen atom; Ra3 and Ra4 may not simultaneously represent a group -CRy1Ry2NH(Ry3); when Ra3 represents a group -CRy1Ry2NH(Ry3), Ra1 and Ra2 can form together with the carbon atoms carrying them a tetrahydrofuran, a 1,4-dioxane or a tetrahydropyran ring; when Ra3 represents a hydrogen atom, Ra1 and Ra2 can form together with the carbon atoms carrying them a tetrahydro-2H-pyran-4-amine or a 1-(tetrahydro-2H-pyran-4-yl)methanamine ring; and Ra2 and Ra3 can form together with the carbon atoms carrying them a cyclopentanamine, or a 1-methylcyclopentanamine ring. Representative compounds include [4-(1-aminoethyl)-2,6-difluorophenyl](1-hydroxyisoquinolin-5-yl)methanone and 5-{ [(3R)-3-amino-4,6-difluoro-2,3-dihydro-1H-inden-5-yl]carbonyl} isoquinolin-1(2H)-one. The compounds of the invention can be useful in the treatment or prevention of pathologies which are the result of activation of the RhoA/ROCK pathway and phosphorylation of the myosin light chain, for example systemic arterial hypertension, pulmonary arterial hypertension, angina, myocardial infarction, post-angioplasty restenosis, aortic aneurysm, occlusion of the peripheral arteries, atherosclerosis, cardiac fibrosis and heart failure, glaucoma or pathologies of the cornea.

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