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    Benzo-1, 3-dioxolyl- and benzofuranyl substituted pyrrolidine derivatives as endothelin antagonists
    100.
    发明专利
    Benzo-1, 3-dioxolyl- and benzofuranyl substituted pyrrolidine derivatives as endothelin antagonists 未知

    公开(公告)号：NZ514170A

    公开(公告)日：2005-02-25

    申请号：NZ51417097

    申请日：1997-02-12

    Applicant: ABBOTT LAB

    Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN SOO ,  TASKER ANDREW S ,  VON GELDERN THOMAS V ,  KESTER JEFFREY A ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

    IPC: A61K31/40 ,  A61P9/00 ,  A61P19/00 ,  C07D207/16 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07F9/572

    Abstract: A process for preparing a compound of formula (I), wherein: E is a carboxy-protecting group and R1 and R2 are loweralkyl, alkoxyalkyl, alkoxycarbonylalkyl, hydroxyalkyl, haloalkyl, haloalkoxyalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl,aminocarbonyalkenyl, alkylaminocarbonylalkenyl, dialkylaminocarbonylalkenyl, aryl, arylalkyl, aryloxyalkyl, arylalkoxyalkyl, heterocyclic and (heterocyclic)alkyl Wherein cycloalkyl, aryl and heterocyclic may be optionally substituted, provided at least one of the following conditions apply: (a) R1 is selected from haloalkyl, haloalkoxyalkyl, cycloalkylalkyl, arylalkyl, aryloxyalkyl, and (heterocyclic)alkyl, (b) R2 is selected from haloalkyl, haloalkoxyalkyl, cycloalkylalkyl, arylalkyl, aryloxyalkyl, (c) at least on of the optionally substituted aryl groups has at least on substituent selected from hydroxyalkyl and cyano or (d) at least one of the optionally substituted heterocyclic groups has at least one substituent selected from alkyloxycarbonyl, nitro and cyano; comprises a) catalytic hydrogenation of a compound of Formula (II) b)catalytic hydrogenation of the product of step a) in the presence of an acid or a mixture of acids, and c) epimerization of the product of step b) with a base. Also described is the compound (2R, 3R, 4S)-(+)-2-(4-methoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(N,N-di(n-butyl-aminocarbonylmethyl)-pyrrolidine-3-carboxylic acid. This compound can be used in the manufacture of a medicament for antagonizing endothelin treating hypertension, congestive heart failure, restinosis cerebral or myocardial ischemia or atherosclerosis, treating coronary angina, cerebral vasospasm, acute and chronic renal failure, gastric ulceration, cyclosporine-induced nephrotoxicity, endotoxin-induced toxicity, asthma, LPL-related lipoprotein disorders, proliferative diseases, acute or chronic pulmonary hypertension, platelet aggregation, thrombosis, IL-2 mediated cardio toxicity nociception, colitis, vascular permeability disorders, ischemia-reperfusion injury raynaud's disease, migraine and for treating bone pain. (62) Divided out of 503365

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