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    New 2-(1,3,5-triazin-2-yloxy)-3,3-diaryl-propionic acid derivatives, are selective ET-A receptor antagonists useful e.g. for treating cardiac insufficiency, hypertension, liver cirrhosis, prostate cancer or pancreatitis
    115.
    发明专利
    New 2-(1,3,5-triazin-2-yloxy)-3,3-diaryl-propionic acid derivatives, are selective ET-A receptor antagonists useful e.g. for treating cardiac insufficiency, hypertension, liver cirrhosis, prostate cancer or pancreatitis 未知

    公开(公告)号：DE10004052A1

    公开(公告)日：2001-08-02

    申请号：DE10004052

    申请日：2000-02-01

    Applicant: BASF AG

    Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG ,  KLING ANDREAS ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  UNGER LILIANE

    IPC: C07D251/18 ,  C07D251/20 ,  C07D251/22 ,  C07D251/12 ,  A61K31/53 ,  C07D251/14 ,  C07D403/12

    Abstract: 2-(1,3,5-Triazin-2-yloxy)-3-(oxy or thio)-3,3-diaryl-propionic acid derivatives (I) are new. Triazine derivatives of formula (I) are new: [Image] R1tetrazolyl or -C(O)R; R : OR7; an N-bonded 5-membered heteroaromatic ring such as pyrrolyl, pyrazolyl, imidazolyl or triazolyl, optionally substituted (os) by 1 or 2 halo, 1 or 2 T or 1 or 2 COOT; -O-(CH2)p-S(O)kR8; or -NHSO2R9; R7H, alkali(ne earth) metal cation, organic ammonium (e.g. N(T)4) or NH4; alkyl, cycloalkyl or benzyl (all os by one or more of halo, NO2, T', OH, OT, SH, ST, NH2, NHT and NT2); 2-6C alkenyl or 3-6C cycloalkyl (both os by 1-5 halo); or phenyl (os by 1-5 halo and/or 1-3 of NO2, CN, T', OH, OT, SH, ST, NH2, NHT and NT2); T : 1-4C alkyl; T' : T or 1-4C haloalkyl; k : 0-2; p : 1-4; R8T, cycloalkyl, 2-6C alkenyl, 2-6C alkynyl or phenyl (os by one or more of halo, NO2, CN, T', OH, OT, ST, SH, NH2, NHT or NT2); R9T, 2-6C alkenyl, 2-6C alkynyl or cycloalkyl (all os by OT, ST and/or phenyl (itself os as in R8)); or phenyl (os by 1-3 of halo, NO2, CN, T', OH, OT, ST, NH2, NHT or NT2); R2T; R3H, alkyl, OT, ST, NHT, NT2, NH2 or OH; R4, R5phenyl or naphthyl (both os by one or more of halo, NO2, CN, T' and OT'); R6H; alkyl, 3-6C alkenyl, 3-6C alkynyl or cycloalkyl (all os by one or more of halo, OT', ST, COT, 3-8C alkylcarbonylalkyl and NT2); or phenyl or naphthyl (both os by one or more of halo, NO2, CN, T', OT', OPh, ST, NHT, NT2, OCH2O or OCH2CH2O); and A : O or S. Unless specified otherwise alkyl moieties have 1-8C and cycloalkyl moieties 3-8C. An independent claim is included for the use of a triazinyloxyethyl fragment of formula (VII) as a structural component of compounds having selective ET-A receptor antagonist action: [Image] ACTIVITY : Cardiant; vasotropic; hypotensive; nephrotropic; hepatotropic; cerebroprotective; cytostatic; antiinflammatory; antianginal; antiarrhythmic; hemostatic; antimigraine; antiasthma; antiarteriosclerotic; anticoagulant; ophthalmological; antiulcer. MECHANISM OF ACTION : Endothelin (ET) receptor antagonist. In particular (I) are selective ET-A receptor antagonists. In receptor binding assays, 2-(4,6-diethyl-1,3,5-triazin-2-yloxy)-3-ethoxy-3,3-diphenyl-propionic acid (Ia) had K1 values of 3.05 nM for ET-A receptors and 2250 for ET-B receptors; the corresponding values for the (S)-enantiomer of (Ia) were 1.95 nM and 1500 nM.

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