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filingDate 1992-09-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f227666e2ef9c122feae2fde74089412
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8c65ba2e5228b24e9111a69f6651fcb8
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publicationDate 1993-03-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0532410-A1
titleOfInvention N-substituted heterocyclic derivatives as angiotensin II inhibitors
abstract R₁ et R₂ sont semblables ou différents et représentent chacun indépendamment l'hydrogène ou un groupe choisi parmi un alkyle en C₁-C₆, un alcoxy en C₁-C₄, un amino, un aminométhyle, un carboxy, un alcoxycarbonyle dans lequel l'alcoxy est en C₁-C₄, un cyano, un tétrazolyle, un méthyltétrazolyle, un méthylsulfonylamino, un trifluorométhylsulfonylamino, un trifluorométhylsulfonylaminométhyle, un N-cyano-acétamide, un N-hydroxy-acétamide, un N-((carboxy-4) thiazol- 1,3-yl-2 acétamide, un ureido, un cyano-2 guanidinocarbonyle, un cyano-2 guanidinométhyle, un imidazol-1-yl-carbonyle, un cyano-3 méthyl-2 isothioureidométhyle, à la condition qu'au moins l'un des substituants R₁ ou R₂ soit différent de l'hydrogène ; R₃ représente un hydrogène, un alkyle en C₁-C₆, non substitué ou substitué par un ou plusieurs atomes d'halogène, un alcényle en C₂-C₆, un cycloalkyle en C₃-C₇, un phényle, un phénylalkyle dans lequel l'alkyle est en C₁-C₃, un phénylalcényle dans lequel l'alcényle est en C₂-C₃, lesdits groupes phényles étant non substitués ou substitués une ou plusieurs fois par un atome d'halogène, un alkyle en C₁-C₄, un halogénoalkyle en C₁-C₄, un polyhalogénoalkyle en C₁-C₄, un hydroxyle ou un alcoxy en C₁-C₄; R₄ représente un alkyle en C₁-C₆, non substitué ou substitué par un ou plusieurs atomes d'halogène ; R₅ représente un cycloalkyle ou un cycloalkylméthyle, ledit cycloalkyle étant en C₃-C₇ non substitué ou substitué par un ou plusieurs atomes d'halogène ; ou R₄ et R₅ représentent chacun un cyclopropyle ; X représente un atome d'oxygène ou un atome de soufre ; z et t sont nuls ou l'un est nul et l'autre représente un ; n et ses sels.The subject of the invention is N-substituted heterocyclic derivatives of formula : in which : R₁ and R₂ are the same or different and each independently represents hydrogen or a group chosen from C₁-C₆ alkyl, C₁-C₄ alkoxy, amino, aminomethyl, carboxy, alkoxycarbonyl in which the alkoxy is in C₁-C₄, cyano, tetrazolyl, methyltetrazolyl, methylsulfonylamino, trifluoromethylsulfonylamino, trifluoromethylsulfonylaminomethyl, N-cyano-acetamide, N-hydroxy-acetamide, N - ((carboxy-4) thiazol- 3-yl-2 acetamide, ureido, 2-cyano guanidinocarbonyl, 2-cyano guanidinomethyl, imidazol-1-yl-carbonyl, 3-cyano-methyl isothioureidomethyl, provided that at least one of the substituents R₁ or R₂ is different from hydrogen; R₃ represents 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, a C₁-C₄ alkyl, a C₁-C₄ haloalkyl , C₁-C₄ polyhaloalkyl, hydroxyl or C₁-C₄ alkoxy; R₄ represents C₁-C₆ alkyl, unsubstituted or substituted by one or more halogen atoms; R₅ represents a cycloalkyl or a cycloalkylmethyl, said cycloalkyl being C₃-C₇ unsubstituted or substituted by one or more halogen atoms; or R₄ and R₅ each represents a cyclopropyl; X represents an oxygen atom or a sulfur atom; z and t are zero or one is zero and the other represents one; and its salts.n n n Application: Angiotensin II antagonists
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