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    • 4. 发明申请
      WO1991014679A1 HETEROCYCLIC N-SUBSTITUTED DERIVATIVES, THEIR PREPARATION AND THEPHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    • HETEROCYCLIC N-SUBSTITUTED DERIVATIVES, THEIR PREPARATION AND THEPHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 杂环N-取代衍生物，其制备和含有它们的药物组合物
    • WO1991014679A1
    • 1991-10-03
    • PCT/FR1991000224
    • 1991-03-20
    • SANOFI , BERNHART, Claude , BRELIERE, Jean-Claude , CLEMENT, Jacques , NISATO, Dino , PERREAUT, Pierre
    • SANOFI
    • C07D235/02
    • C07D235/02 , C07D231/12 , C07D233/56 , C07D233/70 , C07D239/70 , C07D249/08 , C07D403/10 , C07D417/12 , C07D471/10 , C07D491/10 , Y02P20/55
    • The invention concerns heterocyclic N-substituted derivatives. These derivatives meet the formula (I) in which: R1 and R2 are similar or different and each independently is hydrogen or a group selected from among C1-C6 alkyl, C1-C4 alkoxy, amino, aminomethyl, carboxy, alkoxycarbonyl in which the alkoxy is C1-C4, cyano, tetrazolyl, methyltetrazolyl, methyl-sulphonylamino, trifluoromethyl-sulphonylamino, N-cyano acetamide, N hydroxy acetamide, N-((carboxy-4) thiazol-1,3-2yl) acetamide, ureido, cyano-2 guanidinocarbamonyl, cyano-2 guanidinomethyl, imidazol-1-yl carbonyl or cyano-3 methyl-2 isothioureidomethyl, provided that at least one of the substituents R1 or R2 is different from hydrogen; R3 is hydrogen, C1-C6 alkyl, unsubstituted or substituted by one or more halogen atoms, C2-C6 alkenyl, C3-C7 cycloalkyl, phenyl, phenylalkyl in which the alkyl is C1-C3, phenylalkenyl in which the alkenyl is C2-C3, said phenyl groups being unsubstituted or substituted one or more times by a halogen atom, C1-C4 alkyl, C1-C4 halogenoalkyl, C1-C4 polyhalogenoalkyl, hydroxyl or C1-C4 alkoxy; R4 and R5 are each independently C1-C6 alkyl, phenyl, phenylalkyl in which the alkyl is C1-C3, said alkyl, phenyl and phenylalkyl groups being unsubstituted or substituted by one or several halogen atoms or by a group selected from among C1-C4 perfluoroalkyl, hydroxyl or C1-C4 alkoxy; or R4 and R5 together are either a group of formula (CH2)n or one of formula (CH2)pY(CH2)q, where Y is either oxygen or a sulphur atom or a carbon atom substituted by a C1-C4 alkyl group, a phenyl or a phenylalkyl in which the alkyl is C1-C3,, or an N-R6 group in which R6 is a hydrogen, C1-C4 alkyl, a phenylalkyl in which the alkyl is C1-C3, C1-C4 alkylcarbonyl, C1-C4 halogenoalkyl carbonyl, C1-C6 polyhalogenoalkyl carbonyl, a benzoyl, an alpha aminoacyl or an N-protector group, or R4 and R5 together with the carbon atom to which they are bonded constitute an indame or adamantame; p + q = m; n is an integer between 2 and 5; X is an oxygen or sulphur atom; z and t are zero or one is zero and the other is unity; and their salts. Application: antagonists to angiotensin II.
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