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    AZINYLOXY- AND PHENOXYDIARYL DERIVATIVES OF CARBOXYLIC ACIDS, THEIR PREPARATION AND APPLICATION AS MIXED ETA/ETB ENDOTHELIN-RECEPTOR ANTAGONISTS
    82.
    发明专利
    AZINYLOXY- AND PHENOXYDIARYL DERIVATIVES OF CARBOXYLIC ACIDS, THEIR PREPARATION AND APPLICATION AS MIXED ETA/ETB ENDOTHELIN-RECEPTOR ANTAGONISTS 未知

    公开(公告)号：BG103258A

    公开(公告)日：2000-12-29

    申请号：BG10325899

    申请日：1999-03-16

    Applicant: BASF AG

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

    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

    Abstract: The derivatives of carboxylic acids have the formula where R1 means tetrazole or the group (a); R2 means hydrogen, hydroxy, amino, NH(C1-C4-alkyl), N(C1-C4-alkyl)2; halogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 halogenalkyl, C1-C4 alkoxy, C1-C4 halogenalkoxy or C1-C4 alkylthio, or CR2 together with CR10, as shown below, form 5- or 6-member ring, N is nitrogen or methine, Y is nitrogen or methine. Z is nitrogen or CR10, where R10 is hydrogen or C1-C4 alkyl or CR10 together with CR2 or with CR3 form 5- or 6-member alkylene or alkenyl ring where one or more methylene groups can be substituted with oxygen, sulphur, -NH or -N(C1-C4-alkyl), R3 is hydrogen, hydroxy, amino, NH(C1-C4-alkyl), N(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 hydroxyalkyl, C1-C4 halogenalkyl, C1-C4 alkoxy, C1-C4 halogenalkoxy, C1-C4 alkylthio or CR3 together with CR10, as indicated above, form 5- or 6-member ring, R4 & R5 (which can be the same or different) are phenyl, optionally substituted, or phenyl or naphthyl which are interconnected in orthoposition by a direct bond, by methylene, ethylene or ethenyl group, with oxygen or sulphur or by the group SO2-, NH- or N-alkyl, C3-C8-cycloalkyl, optionally substituted, R6 is C3-C8 cycloalkyl, optionally substituted, phenyl or naphthyl, optionally substituted, or 5- or 6-member heteroaromatic ring containing from one to three nitrogen atoms and/or one sulphur or oxygen atom, W is sulphur or oxygen, Q is a dividing group which by length corresponds to a C2-C4 chain. The invention also relates to physiologically acceptable salts of these compounds, as well as to their pure enantiomer or diastereomer forms, to their preparation and application as mixed ETA/ETB-receptor antagonists. 10 claims

    85.
    发明专利
    未知

    公开(公告)号：BR9907911A

    公开(公告)日：2000-10-24

    申请号：BR9907911

    申请日：1999-02-05

    Applicant: BASF AG

    Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  DER STEFAN HERGENR ,  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 ,  C07D239/36

    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.

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