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US 2008/0176867 A1Published application
N-[(4,5-diphenylpyrimidin-2-yl)methyl]amine derivatives, the preparation thereof and their therapeutic use
AssigneeSanofi-Aventis
InventorsFrancis BARTH, Christian CONGY, Patrick GUEULE, Murielle RINALDI-CARMONA
Life of this patent
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Abstract
The invention relates to compounds of formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to a method for preparing the aforementioned compounds and to their therapeutic use.
Claims25
A compound of formula (I):
- in which:
- X represents a group
- R1 represents:
- a (C1-C12)-alkyl, unsubstituted or substituted one or more times with substituents selected independently from a fluorine atom, a hydroxyl, a (C1-C4)-alkoxy, a (C1-C4)-alkylthio, a phenoxy, a trifluoromethoxy radical, a difluoromethoxy radical, a difluoromethylthio radical or a trifluoromethylthio radical;
- a non-aromatic (C3-C12)-carbocyclic radical, unsubstituted or substituted one or more times with substituents selected independently from a (C1-C4)-alkyl, a (C1-C4)-alkoxy, a fluorine atom, a hydroxyl, a trifluoromethyl radical, a trifluoromethoxy radical or a (C1-C4)-alkylthio;
- a (C3-C7)-cycloalkylmethyl, unsubstituted or substituted one or more times on the cycloalkyl with substituents selected independently from a (C1-C4)-alkyl, a (C1-C4)-alkoxy, a fluorine atom, a hydroxyl, a trifluoromethyl radical or a trifluoromethoxy radical;
- a phenyl, unsubstituted or substituted one or more times with substituents selected independently from a halogen atom, a hydroxyl, an Alk group, an OAlk group, a methylenedioxy, a (C1-C4)-alkylamino, a di-(C1-C4)-alkylamino, a cyano, a nitro, an S(O)nAlk group, an OS(O)nAlk group, a (C1-C4)-alkylcarbonyl group;
- or from a phenyl, phenoxy, pyrrolyl, imidazolyl, pyridyl or pyrazolyl radical, said radical being unsubstituted or substituted one or more times with a (C1-C4)-alkyl;
- a benzyl, unsubstituted or substituted one or more times on the phenyl with substituents selected independently from a halogen atom, an Alk group, a hydroxyl, an OAlk group, a methylenedioxy, an S(O)nAlk group or an OS(O)nAlk group and unsubstituted or substituted on alpha-methyl by one or two similar or dissimilar groups selected from a (C1-C4)-alkyl, a (C3-C7)-cycloalkyl;
- a phenethyl, unsubstituted or substituted one or more times on the phenyl with substituents selected independently from a halogen atom, a (C1-C4)-alkyl, a (C1-C4)-alkoxy, a trifluoromethyl radical or a trifluoromethoxy radical;
- a benzhydryl or a benzhydrylmethyl;
- a 1,2,3,4-tetrahydronaphthalenyl, unsubstituted or substituted one or more times with a (C1-C4)-alkyl;
- or
- an aromatic heterocyclic radical selected from pyrrolyl, imidazolyl, furyl, thienyl, pyrazolyl, oxazolyl, pyridyl, indolyl, said radical being unsubstituted or substituted one or more times with substituents selected independently from a halogen atom, a (C1-C4)-alkyl, a (C1-C4)-alkoxy, a trifluoromethyl radical, a trifluoromethoxy radical, a cyano, a nitro or a (C1-C4)-alkylthio;
- R2 represents a hydrogen atom or a (C1-C3)-alkyl;
- R3 represents a hydrogen atom or a (C1-C5)-alkyl;
- R4 represents a phenyl, unsubstituted or substituted one or more times with substituents selected independently from a halogen atom, Alk group, OAlk group, S(O)nAlk group or OS(O)nAlk group;
- R5 represents a phenyl, unsubstituted or substituted one or more times with substituents selected independently from a halogen atom, Alk group, OAlk group, S(O)nAlk group or OS(O)nAlk group;
- R6 represents a hydrogen atom or a (C1-C3)-alkyl;
- n represents 0, 1 or 2;
- and
- Alk represents a (C1-C4)-alkyl, unsubstituted or substituted one or more times with a fluorine atom;
- with the proviso that R4 and R5 do not simultaneously represent a phenyl substituted with a (C1-C4)-alkoxy.
20 more elements
Dependencies are inferred from the claim text.