Patent ID: 6670359
Filing Date: 2003-12-30
Classification: A61P,C07D

Abstract:
A compound of formula (I): whereinX is CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is (CH2)n-phenyl wherein the phenyl may be mono- or di-substituted with R4 and/or R5; wherein R4 is selected from the group consisting of H, C1-C6 alkyl, C3-C6 cycloalkyl, halogen, CN, CF3, OH, C1-C6 alkoxy, NR6R7, OCF3, SO3CH3, SO3CF3, SO2NR6R7, phenyl, phenyl-C1-C6 alkyl, phenoxy, C1-C6 alkylphenyl, an optionally substituted heterocyclic ring containing one or two heteroatoms and selected from the group consisting of imidazolidinyl, imidazolinyl, morpholinyl, piperazinyl, piperidyl, piperidonyl, pyrazolidinyl, pyrazolinyl, pyrrolidinyl, pyrrolinyl, tetrahydropyranyl, thiomorpholinyl, and diazepinyl wherein the ring substituent(s) is(are) selected from the group consisting of C1-C6 alkyl, C3-C6 cycloalkyl, phenyl-C1-C6 alkyl, (CH2)mOR9 wherein m is 2-6 and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl or phenyl-C1-C6 alkyl, and COR8, an optionally substituted heteroaromatic ring containing one or two heteroatoms and selected from the group consisting of furyl, imidazolyl, isoxazolyl, isothiazolyl, oxazolyl, pyrazinyl, pyrazolyl, pyridazinyl, pyridyl, pyrimidyl, pyrrolyl, thiazolyl and thienyl wherein the ring substituent(s) is(are) selected from the group consisting of C1-C6 alkyl, C3-C6 cycloalkyl and phenyl-C1-C6 alkyl, and COR8; wherein R6 is H, C3-C6 alkyl or C3-C6 cycloalkyl; R7 is H, C1-C6 alkyl or C3-C6 cycloalkyl; and R8 is C1-C6 alkyl, C3-C6 cycloalkyl, CF3, NR6R7 or phenyl; R5 is H, OH, CF3, OCF3, halogen, C1-C6 alkyl or C1-C6 alkoxy; and n is 0-4; wherein the compound is an (R)-enantiomer, an (S)-enantiomer, or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof.