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3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide derivatives, preparation thereof and therapeutic use thereof
专利权人:
SANOFI
发明人:
RAVET ANTOINE,PACAUD CHRISTOPHE,PUECH FREDERIC,MARGUET FRANK,COTE-DES-COMBES SYLVAIN,FROISSANT JACQUES,GIBERT JEAN-FRANCOIS
申请号:
NZ60394711
公开号:
NZ603947A
申请日:
2011.06.01
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are 7-phenyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide derivaives as represented by the general formula (I), in which R2 represents: alkyl, cycloalkyl-alkyl, alkylthio-alkyl, alkoxy-alkyl, hydroxy-alkyl, hydroxy-alkyl-cycloalkyl-alkyl, fluoroalkyl, alkyl-oxyimino-alkyl, cycloalkyl, fluorocycloalkyl, hydroxy-cycloalkyl, a heterocyclic group comprising a saturated carbon-based cyclic group comprising from 3 to 8 carbon atoms and at least one heteroatom chosen from nitrogen, oxygen, sulfur and the oxide or dioxide form of sulfur, an alkyl-heterocyclic group comprising a saturated carbon-based cyclic group comprising from 3 to 8 carbon atoms and at least one heteroatom chosen from nitrogen, oxygen, sulfur and the oxide or dioxide form of sulfur, X6 represents a hydrogen, fluorine, chlorine or bromine atom or alkyl, cycloalkyl, cycloalkylalkyl, fluoroalkyl or cyano R7 represents an optionally substituted phenyl or naphthyl group, and wherein the remaining substituents are as defined herein. Representative compounds include N2-tert-butyl-6-chloro-7-phenyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, N2-tert-butyl-6-fluoro-7-phenyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, N2-tert-butyl-7-(4-methoxyphenyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, N2-6-di-cyclopropyl-7-(4-methoxyphenyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, 6-cyclopropyl-7-(4-methoxyphenyl)-N2-(isopropyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, N2-tert-butyl-6-cyclopropyl-7-[4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide, 6-chloro-N2-iso-butyl-7-phenyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide and 6-chloro-7-(3-fluorophenyl)-N2-{ [1-(hydroxymethyl)cyclopropyl]methyl} -3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1H)-dicarboxamide. Also disclosed is a medicament comprising a compound of formula (I) as defined above, in the form of the base or of an ad
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