| 摘要 |
This invention features pyrimidine compounds of formula (I): R1 is formula (II), aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, S02Rc, S(O)Rc, S(02)NRcRd, SRc, NRcR d, NRcCORd, NRcC(O)ORd, NR cC(O)NRcRd, NRcS02Rd, CORc, C(O)ORc, or C(O)NRcRd; R 5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(02), or NRc; Y is a covalent bond, CH2, C(O), C=N-R c, C=N-ORc, C=N-SRc, O, S, S(O), S(02), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(02), NRc, or NC(O) Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
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