abstract |
SUMMARY OF THE INVENTION The present invention relates to imidazolidine derivatives of formula I wherein preferred substituents are as follows: W is a divalent radical of formula R 1 -A-C (R 13); Y is carbonyl; A is a direct bond; B is methylene substituted with isobutyl or cyclopropylmethyl; E is R10CO or HO-CH2; R is hydrogen; R 1 is methyl or trifluoromethyl; R2 is hydrogen; R3 is hydrogen, (C1-C8) -alkyl optionally substituted with 1 to 6 fluorine atoms, optionally substituted with (C6-C10) -aryl, (C6-C10) -aryl- (C1-C4) -alkyl a group optionally substituted on the aryl, an optionally substituted heteroaryl, a heteroaryl (C1-C4) alkyl group optionally substituted on the heteroaryl, a (C3-C8) cycloalkyl group or a (C3-C8) ) -cycloalkyl- (C1-C4) alkyl; R10 is hydroxy, (C1-C8) -alkoxy, (C6-C10) -aryl (C1-C6) -alkoxy optionally substituted with aryl, optionally substituted (C6-C10) -aryloxy, (C1-C6) a) alkylcarbonyloxy (C1-C6) alkoxy or (C1-C6) alkoxycarbonyloxy (C1-C6) alkoxy; R13 is methyl or trifluoromethyl; R30 is selected from the group consisting of R32 (R) N-CO-N (R) -R31 and R32 (R) N-CS-N (R) -R31; R31 is a divalent phenylene methyl optionally substituted on the phenyl moiety wherein the methylene of the phenylene methyl is bonded to the nitrogen of the imidazolidine ring of formula (I); e is 0 and h is 1. The compounds of formula I are valuable pharmaceutical agents useful in the treatment of inflammatory diseases such as rheumatoid arthritis, polyarthritis, inflammatory bowel syndrome, systemic lupus erythematosus, multiple sclerosis, or inflammatory diseases of the central nervous system. The invention further relates to a single process for the preparation of the compounds of formula I, to the use of the compounds and to pharmaceutical compositions containing the compounds of formula I. SHE |