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    New amido-substituted (hetero)aryloxy-alkanoic acid derivative endothelin receptor antagonists for treating e.g. cardiovascular disorders
    1.
    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：DE19752904A1

    公开(公告)日：1999-07-15

    申请号：DE19752904

    申请日：1997-11-28

    Applicant: BASF AG

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

    IPC: C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  A61K31/505 ,  C07D213/63 ,  C07D239/80 ,  C07D239/96 ,  C07D251/12 ,  C07D491/04

    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.

    New carbocyclic and heterocyclic carboxylic acid or tetrazolyl compounds
    7.
    发明专利
    New carbocyclic and heterocyclic carboxylic acid or tetrazolyl compounds 未知

    公开(公告)号：DE19652763A1

    公开(公告)日：1998-06-25

    申请号：DE19652763

    申请日：1996-12-18

    Applicant: BASF AG

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

    IPC: C07D237/14 ,  C07D237/16 ,  C07D241/18 ,  C07D253/07 ,  C07D253/075 ,  C07D253/10 ,  C07D491/04 ,  A61K31/195 ,  A61K31/53 ,  C07D241/14 ,  C07D241/36 ,  C07D255/00 ,  C07D487/06 ,  C07D493/04 ,  C07D495/04

    Abstract: Heterocyclic compounds of formula (I) and their salts are new. R1 = tetrazolyl, or COR; R = OR6, O(CH2)pS(O)kR7, NHS(O)2R8 or a 5-membered azaheteroaryl; R2 = 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl (all optionally substituted), H, halo, 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl, NH(1-4C alkyl), N(1-4C alkyl)2, OH, carboxy or amino; R3, R4 = phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted); or R3+R4 = two of phenyl, naphthyl linked at the o-position by a bond, methylene, ethylene, ethenyl, S, SO2, NH or N-alkyl; R5 = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl, Ph, naphthyl, 5-6 membered heteroaromatic (containing 1-3 N, S and/or O), or 3-8C cycloalkyl (all optionally substituted); R6 = H, alkali metal or earth-alkali metal, organic ammonium, 3-8C cycloalkyl, 1-8C alkyl, or (all optionally substituted) benzyl, 3-8C alkenyl, 3-8C alkynyl or phenyl; R7 = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; R8 = 1-4C alkyl, 3-8C alkenyl, 3-8C alkynyl, 3-8C cycloalkyl (all optionally substituted by 1-4C alkoxy, 1-4C alkylthio and/or phenyl), 1-4C haloalkyl or optionally substituted phenyl; X = N, Y = N or CR9 and Z = N; or X = CH, Y = N or CR9 and Z = N or CR10 provided that Y or Z = N; R9, R10 = 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted), H, OH, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, halo, 1-4C alkoxy, 1-4C haloalkoxy or 1-4C alkylthio; or CR2+CR9 or CR2+CR10 completes a 5-6 membered alkylene or alkenyl ring (optionally substituted) with one or more CH2 optionally replaced by O, S, NH or N(1-4C alkyl); Q = N and W = bond; or Q = O and W = S, O or a bond; k = 0-2; and p = l-4.

    8.
    发明专利
    未知

    公开(公告)号：DE19636046A1

    公开(公告)日：1998-03-12

    申请号：DE19636046

    申请日：1996-09-05

    Applicant: BASF AG

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

    IPC: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D491/04 ,  C07D491/048 ,  C07D405/10 ,  C07D403/12 ,  C07D251/12 ,  C07C59/64 ,  A61K31/41

    Abstract: Carboxylic acid derivatives have the formula (I), in which R stands for tetrazole or a group (a); R stands for hydrogen, hydroxy, NH2, NH(C1-c4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-alkyl halide, C1-C4-alkoxy, C1-C4-alkoxy halide or C1-C4-alkylthio, or CR is linked with CR , as indicated below, into a 5- or 6-membered ring; X stands for nitrogen or methine; Y stands for nitrogen or methine; Z stands for nitrogen or CR , wherein R is hydrogen or C1-C4-alkyl or CR forms together with CR or CR an optionally substituted 5- or 6-membered alkylene or alkenylene ring, and wherein one or more methylene groups can be substituted by hydrogen, sulphur, -NH or -N(C1-C4-alkyl); R stands for 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-alkyl halide, C1-C4-alkoxy, C1-C4-alkoxy halide, C1-C4-alkylthio; or CR is linked to CR as indicated above into a 5- or 6-membered ring, R and R (which may be identical or different) stand for optionally substituted phenyl or naphthyl, or for phenyl or naphthyl which are linked to each other at the ortho-position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulphur atom or an SO2, NH or N-alkyl group; optionally substituted C3-C8-cycloalkyl; R stands for optionally substituted C3-C8-cycloalkyl; optionally substituted phenyl or naphthyl, a 5- or 6-membered, optionally substituted heteroaromatic compound containing one to three nitrogen atoms and/or one sulphur or oxygen atom; W stands for sulphur or oxygen; Q is a spacer with a length that corresponds to a C2-C4 chain. Also disclosed are the physiologically tolerable salts of these compounds, as well as their pure enantiomer and diastereoisomer forms, their preparation and use as mixed ETA/ETB-receptor antagonists.

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