Patent ID: 6667316
Filing Date: 2003-12-23
Classification: A61P,C07D

Abstract:
A compound selected from the group consisting of (a) an isoindoline of the formula I: wherein:each of R1 and R2, independently of the other, is alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, cyano, cycloalkoxy of 3 to 18 carbon atoms, cycloalkyl of 3 to 18 carbon atoms, or cycloalkylmethoxy in which cycloalkyl has from 3 to 18 carbon atoms; one of X and Xâ€² is &boxH;C&boxH;O and the other of X and Xâ€² is &boxH;C&boxH;O or &boxH;CH2; R3 is â€”SO2â€”Y, â€”COZ, â€”CN, or hydroxyalkyl of 1 to 6 carbon atoms in which Y is alkyl of 1 to 6 carbon atoms, phenyl, or benzyl; Z is â€”NR6â€³R7â€³, alkyl of 1 to 6 carbon atoms, phenyl, or benzyl; R6â€³ is hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl of 3 to 18 carbon atoms; phenyl, benzyl, or alkanoyl of 2 to 5 carbon atoms, each of which is unsubstituted or substituted with halo, amino, or alkylamino of 1 to 4 carbon atoms; R7â€³ is alkyl of 1 to 4 carbon atoms; n has a value of 1, 2, or 3; one of R4 and R5 is hydrogen and the other of R4 and R5 is, imidazolyl, pyrrolyl, oxadiazolyl, triazolyl, or â€ƒin which z is 0 or 1; R6 when taken independently of R7, is cycloalkanoyl of 2 to 6 carbon atoms each of which is unsubstituted or substituted with halo, amino, monoalkylamino or dialkylamino in which each alkyl group contains 1 to 4 carbon atoms; and R7 is hydrogen, alkyl of 1 to 4 carbon atoms, methylsufonyl; or alkoxyalkylcarbonyl of 2 to 5 carbon atoms; or, R6 and R7 taken together are alkylidene of 1 or 2 carbon atoms substituted by amino, alkylamino, or dialkylamino in which each alkyl group has from 1 to 4 carbon atoms or, provided z is 1, â€”CH&boxH;CHâ€”CH&boxH;CHâ€”, â€”CH&boxH;CHâ€”N&boxH;CHâ€”; and, the carbon atom designated * constitutes a center of chirality; and (b) the acid addition salts of said isoindoline derivatives which are susceptible of protonation.