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    61.
    发明专利
    未知

    公开(公告)号：NO20004075D0

    公开(公告)日：2000-08-15

    申请号：NO20004075

    申请日：2000-08-15

    Applicant: BASF AG

    Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

    IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D

    Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

    New amido-substituted (hetero)aryloxy-alkanoic acid derivative endothelin receptor antagonists for treating e.g. cardiovascular disorders
    65.
    发明专利
    New amido-substituted (hetero)aryloxy-alkanoic acid derivative endothelin receptor antagonists for treating e.g. cardiovascular disorders 未知

    公开(公告)号：DE19809376A1

    公开(公告)日：1999-09-09

    申请号：DE19809376

    申请日：1998-03-05

    Applicant: BASF AG

    Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

    IPC: C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D239/34 ,  A61K31/505 ,  C07B41/04 ,  C07C69/734 ,  C07C235/06 ,  C07C271/48 ,  C07C311/17 ,  C07D251/12 ,  C07D319/12

    Abstract: Amido-substituted (hetero)aryloxy-alkanoic acid derivatives (I) are new. Carboxylic acid derivatives of formula (I), and their salts and pure enantiomers or diastereomers, are new: R1 = tetrazole or -CO-R; R = OR9, N-bonded 5-membered heteroaryl, -O(CH2)p-S(O)k-R10 or -NHSO2R11; R9 = H; alkali metal, alkaline earth metal or organic ammonium cation; cycloalkyl; alkyl; or (all optionally substituted) benzyl, 3-6C alkenyl, 3-6C alkynyl or phenyl; k = 0-2; p = 1-4; R10 = A, cycloalkyl, 3-6C alkenyl, 3-6C alkynyl or optionally substituted phenyl; A = 1-4C alkyl; R11 = A, 3-6C alkenyl, 3-6C alkynyl or cycloalkyl (all optionally substituted by OA, SA and/or phenyl); or optionally substituted phenyl; R2, R3 = H, OH, NH2, NHA, N(A)2, halo, A', 2-4C alkenyl, 2-4C alkynyl, OA' or SA; A' = A or 1-4C haloalkyl; X, Y = CH or N; Z' = N or CR12; R12 = H, halo or A; or R2+R12 or R3+R12 = alkylene or alkenylene (both optionally substituted and optionally having one or more CH2 replaced by O, S, NH or NA), completing a 5- or 6-membered ring; R4, R5 = phenyl, naphthyl or cycloalkyl (all optionally substituted); or phenyl or naphthyl bonded together in the ortho-position via a direct bond, CH2, CH2CH2, CH=CH, O, S, SO2, NH or N-alkyl (C number not given); R6 = -CO-NR13R14 or -CR21R20-NR18R19; R13, R14 = H (but not both H) or (all optionally substituted) alkyl, cycloalkyl, alkenyl, alkynyl, benzyl, phenyl or naphthyl; or R13+R14 = optionally substituted 3-7C alkylene (optionally with one CH2 replaced by O, S or N or carrying an optionally substituted fused benzene ring); or optionally substituted 3-7C alkenylene carrying an optionally substituted fused benzene ring; R7, R8, R21 = H or A; R18 = H or (all optionally substituted) alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or naphthyl; R19 = alkylcarbonyl, (2-8C) alkenylcarbonyl, (2-8C) alkynylcarbonyl, benzyloxycarbonyl, cycloalkylcarbonyl, benzoyl, naphthoyl, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, phenylsulfonyl or naphthylsulfonyl (all optionally substituted); or cycloalkylsulfonyl; R20 = H or A (optionally substituted); W = O or S; alkyl moieties = 1-8C and alkenyl, alkynyl or cycloalkyl moieties = 3-8C unless specified otherwise. Independent claims are included for: (i) the use of alcohols of formula (V) as starting materials for the synthesis of endothelin (ET) receptor antagonists; (ii) structural fragments of formula (II); (iii) the use of (II) as a structural component of ET receptor antagonists; (iv) ET receptor antagonists consisting of a fragment of formula (III) covalently bonded with a group having molecular weight at least 30 or a fragment of formula (IV) covalently bonded via N to a group of molecular weight at least 58; and (v) new amines of formula (I'). N.B. The additional CO groups attached to R6 in (V) and (II) have been omitted in the disclosure.

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