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    • 8. 发明公开
    • NOVEL COMPOUNDS
    • 新化合物
    • EP1556140A2
    • 2005-07-27
    • EP03776373.7
    • 2003-10-14
    • Synta Pharmaceuticals Corporation
    • SUN, LijunONO, MitsunoriWADA, YumikoYING, WeiwenPRZEWLOKA, TeresaKOSTIK, Elena
    • A61P19/02A61P17/06A61P3/10A61P1/00C07D487/04C07D471/04C07D498/04C07D513/04C07D401/10C07D405/10C07D407/10C07D409/10C07D413/10C07D417/10A61K31/52A61K31/522A61K31/541A61K31/5355A61K31/4745A61K31/4743A61K31/496
    • C07D473/34C07D473/16C07D473/18
    • This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)Rb, NRaS(O)2Rb, NRaC(O)NRbRc NRaC(S)NRbR°, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NTRaRt, S(O)2NRSRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is 0, S, S(O), S(O)2, or NW; B is N or CRC; X is 0, S, S(O), S(O)2, NR, or C(O); Y is a covalent bond, C(O), C=NR a, O, S, S(O), S(O)2, or NW; Z is N or CH; each of U and V, independently, is N or CR; and W is 0, S, or NR'; in which each of Ra, Rb, Re, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl., aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin- 12 overproduction-related disorder.
    • 本发明的特征在于式(I)的化合物:R 1是芳基或杂芳基; R 2和R 4中的每一个独立地为H,卤素,CN,烷基,ORa或NRaRb; (O)R a,OC(O)NR a R b,NR a R b,NR a C(O)R b,NR a S(O)R b,其中R b是H,卤素,CN,烷基,烯基,炔基,芳基,杂芳基, (O)2Rb,NRaC(O)NRbRc,NRaC(S)NRbR°,NRaC(NRb)NRcRd,NRaC(O)ORb,S(O)NTRaRt,S(O)2NRSRb,S(O)Ra,S O)2Ra,C(O)R a,C(O)ORa或C(O)NR a R 1; R5是H或烷基; n是0,1,2,3,4,5或6; A是O,S,S(O),S(O)2或NW; B是N或CRC; X是O,S,S(O),S(O)2,NR或C(O); Y是共价键,C(O),C = NR a,O,S,S(O),S(O)2或NW; Z是N或CH; U和V中的每一个独立地是N或CR; 和W是0,S或NR'; 其中Ra,Rb,Re和Rd中的每一个独立地为H,烷基,芳基,杂芳基,环基或杂环基; Re是H,烷基,芳基,酰基或磺酰基; Rf为H,烷基,芳基,酰基,磺酰基,烷氧基,氨基,酯,酰胺,CN或卤素。 该化合物可用于治疗白介素-12过量产生相关疾病。