N-substituted heterocyclic derivatives, their preparation...

Details N-substituted heterocyclic derivatives, their preparation... N-substituted heterocyclic derivatives, their preparation...

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/41 (2006.01) A61K 31/505 (2006.01) C07D 233/66 (2006.01) C07D 233/70 (2006.01) C07D 233/84 (2006.01) C07D 239/22 (2006.01) C07D 403/10 (2006.01) C07D 417/06 (2006.01) C07D 417/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2077967

IN THE UNITED STATES PATENT & TRADEMARK OFFICE PATENT APPLICATION entitled: N-Substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present in the name of: Pierre PERREAUT Claude MUNEAUX Yvette MUNEAUX Assignee: ELF SANOFI ABSTRACT The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula Image (I) in which: - R1 and R2 are similar or different and are each independently hydrogen or a group selected from a C1- C6 alkyl ; a C1-C4 alkoxy, an amino, an amino-methyl, a carboxyl, an alkoxycarbonyl in which the alkoxy is C1-C4, a cyano, a tetrazolyl, a methyltetrazolyl, a methylsulfonylamino, a trifluoromethylsulfo-nylamino, a tri-fluoromethylsulfonylaminomethyl, an N-cyano acetamide, an N-hydroxyacetamide, an N-(4-carboxy-1,3- thiazol-2-yl)acetamide, a ureido, a 2-cyano- guanidinocarbonyl, a 2-cyano-guanidinomethyl, an imi- dazol-l-yl carbonyl and a 3-cyano-2- methylisothioureidomethyl, with the proviso that at least one of the substituents R1 or R2 is other than hydrogen ; - R3 is a hydrogen, a C1-C6 alkyl which is unsubstituted or substituted by one or more halogen atoms, a C2-C6 alkenyl, a C3-C7 cycloalkyl, a phenyl, a phenylalkyl in which the alkyl is C1-C3, or a phenylalkenyl in which the alkenyl is C1-C3, said phenyl groups being unsubstituted or monosubstituted or polysubstituted by a halogen atom, a Cl-C4 alkyl, a C1-C4 halogenoalkyl, a C1-C4 polyhalogenoalkyl, a hydroxyl or a C1-C4 alkoxy; -R4 is a C1-C6 alkyl which is unsubstituted ot substituted by one of more halogen atoms ; and - R5 is a cycloalkyl or a cycloalkylmethyl, said cycloalkyl being C3-C7, which is unsubstituted or substituted by one or more halogen atoms ; - or R4 and R5 are each a cyclopropyl ; - X is an oxygen atom or sulfur atom; and - z and t are zero or one is zero and the other is one. Application: Angiotensin II antagonists N-substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present.

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