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    Carboxylic acid derivatives as endothelin receptor antagonists
    39.
    发明专利
    Carboxylic acid derivatives as endothelin receptor antagonists 未知

    公开(公告)号：NZ331735A

    公开(公告)日：2000-06-23

    申请号：NZ33173597

    申请日：1997-04-04

    Applicant: BASF AG

    Inventor： RIECHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  HILLEN HEINZ ,  UNGER LILIANE ,  ELGER BERND

    IPC: C07D251/30 ,  A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61K31/529 ,  A61K31/53 ,  A61P7/00 ,  A61P9/00 ,  A61P9/02 ,  A61P9/12 ,  A61P13/00 ,  A61P13/08 ,  A61P13/12 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/48 ,  C07D403/12 ,  C07D491/044

    Abstract: Carboxylic acid derivatives of the formula described, useful as inhibitors of endothelin receptors. The derivatives may be useful for diseases such as hypertension, myocardial infarct, heart failure, kidney failure, pulmonary hypertension, Raynaud's syndrome, cerebral vasospasms, atherosclerosis, stroke, benign prostrate hypertrophy and asthma. Wherein: R is a tetrazole, nitrile or C-CO-R1 R1 is (a) H; (b) succinylimidoxy group; (c) 5 membered heteroaromatic system linked via a nitrogen atom (ie pyrrolyl), C1-4alkyl, C1-4haloalkyl, C1-4haloalkoxy, C1-4alkoxy, C1-4alkylthio; (e) -(O)m-N(R7)-R8, wherein m is 0 or 1, R7 and R8 is H, C1-8alkyl, C3-6alkenyl, C3-6alkynyl, C3-8cycloalkyl, C1-4alkylcarbonyl, C1-4alkoxycarbonyl, C3-6alkenylcarbonyl, C3-6alkynylcarbonyl, C3-6alkenyloxycarbonyl, C3-6alkynyloxycarbonyl, phenyl or R7 and R8 together may form C4-7alkylene chain; (d) -O-(CH2)p-S(O)k-R9, wherein k is 0-2, p is 1-4, R9 is C1-4alkyl, C1-4haloalkyl, C3-6alkenyl, C3-6alkynyl or substituted or unsubstituted phenyl; (e) -OR10; wherein R10 is H, cation of an alkali metal, C3-8cycloalkyl, C1-8alkyl, C1-4alkoxy, C1-4alkylthio, cyano, C1-4alkylcarbonyl, C3-8cycloakyl, C1-4alkoxycarbonyl, phenyl, phenoxy or phenylcarbonyl, -N=C(R11)-R12; (f) -NH-S(O)2-R13, wherein R13 is C1-4alkyl, C3-6alkenyl, C3-6alkynyl, C3-8cycloalkyl; (g) CH2-SO2-R13. R2 is halogen, C1-4alkyl, C1-4haloaklyl, C1-4alkoxy, C1-4haloalkoxy or C1-4alkylthio; X is nitrogen, CR14, wherein R14 is H or C1-5alkyl or CR14 forms together with CR3 a 5- or 6-membered alkylene or alkenylene ring; R3 is halogen, C1-4alkyl, C1-4haloaklyl, C1-4alkoxy, C1-4haloalkoxy, -NH-O-C1-4alkyl, C1-4alkylthio or CR3 is linked to CR14 to form a 5- or 6-membered ring; R4 and R5 is identical or different; phenyl or naphthyl; R6 is C1-10alkyl, C3-10alkenyl or C3-10alkynyl; Z is sulfur or oxygen.

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