abstract |
A compound of formula (I)n n n <Formula I>n n n n n n n n Wherein R 1 is optionally substituted (C 2 -C 9 ) heteroaryl; R 2 is optionally substituted phenyl- (CH 2 ) m- , naphthyl- (CH 2 ) m- , (C 3 -C 10 ) cycloalkyl- (CH 2 ) m- , (C 1 -C 6 ) alkyl Or (C 2 -C 9 ) heteroaryl- (CH 2 ) m- , where m is an integer from 0 to 4, R 3 is hydrogen, optionally substituted (C 1 -C 10 ) alkyl, (C 3- C 10 ) cycloalkyl- (CH 2 ) n- , (C 2 -C 9 ) heterocycloalkyl (CH 2 ) n- , (C 2 -C 9 ) heteroaryl- (CH 2 ) n -or aryl- ( CH 2 ) n −, where n is an integer from 0 to 6; R 4 is hydrogen, (C 1 -C 6 ) alkyl, hydroxy, (C 1 -C 6 ) alkoxy, hydroxy (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkoxy (C = O) -, (C 3 -C 10 ) cycloalkyl- (CH 2 ) p- , optionally substituted (C 2 -C 9 ) heterocycloalkyl- (CH 2 ) p- , (C 2 -C 9 ) heteroaryl- (CH 2 ) p- , phenyl- (CH 2 ) p -or naphthyl- (CH 2 ) p- , where p is an integer from 0 to 4, or R 4 and R 5 are combined with the nitrogen atom to which they are attached Together form a (C 2 -C 9 ) heterocycloalkyl group, R 5 is hydrogen, (C 1 -C 6 ) alkyl or amino.n n n Compounds of the invention are potent selective inhibitors of MIP-1α that bind to the CCR1 receptor and are therefore useful for treating inflammation and other immune diseases. |