abstract |
Orthosubstituted aryl- or heteroarylamide compounds, their use in pharmaceutical compositions, and in the manufacture of medicaments. Claim 1: A compound of the formula (1) in which: X represents -CH- or a nitrogen atom; Y represents NR4, an oxygen atom or a sulfur atom; R4 represents a hydrogen atom or a C1-3 alkyl group; Z represents a hydrogen atom or a halogen atom; R1 represents a C1-6 alkyl group optionally substituted with 1 to 2 groups independently selected from a C1-6 alkoxy group, a trifluoromethyl group, a C2-5 alkanoyl group, a C3-7 cycloalkyl group, a phenyl group, a phenoxy group , a heterocyclic group and a heteroaryl group; a C3-7 cycloalkyl group optionally substituted with a C1-3 alkyl group; or a heterocyclic group; R2 and R3 independently represent a hydrogen atom or a C1-3 alkyl group; or groups R2 and R3 together form a C3-6 alkylene chain; said heteroaryl group is a 4- to 7-membered aromatic ring system having either 1 to 4 ring nitrogen heteroatoms or 0 to 2 nitrogen ring heteroatoms and 1 oxygen ring heteroatom or 1 sulfur ring heteroatom ; said heterocyclic group is a 4 to 7-membered saturated ring system that has either 1 to 4 ring nitrogen heteroatoms or 0 to 2 nitrogen ring heteroatoms and 1 oxygen ring heteroatom or 1 sulfur ring heteroatom ; said phenyl groups, said phenoxy group, and said heteroaryl groups mentioned in the definitions of R1 are unsubstituted or substituted with at least one substituent selected from the group consisting of alpha substituents; said alpha substituent is selected from the group consisting of halogen atoms, C1-4 alkyl groups, C1-4 haloalkyl groups, hydroxy groups, C1-4 alkoxy groups, C1-4 haloalkoxy groups, cyano groups, C1-4 hydroxyalkyl groups, groups C1-4 alkoxy-C1-4 alkyl, C1-4 alkylsulfonyl groups, C2-5 alkanoyl groups, C2-4 alkenyl groups, C2-4 alkynyl groups, C1-4 alkylthio groups, nitro groups, amino groups, mono- or C1-4 dialkylamino, aminosulfonyl groups, C1-4 alkoxycarbonyl groups, C1-4 alkylsulfonylamino groups, C3-7 cycloalkyl groups and C1-6 mono- or dialkylaminocarbonyl groups; or a pharmaceutically acceptable ester of such compound; or a pharmaceutically acceptable salt thereof. |