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11 条记录 (耗时 0.026 秒)

    NOVEL COMPOUNDS
    6.
    发明公开
    NOVEL COMPOUNDS 审中-公开
    新化合物

    公开(公告)号：EP1556140A2

    公开(公告)日：2005-07-27

    申请号：EP03776373.7

    申请日：2003-10-14

    申请人： Synta Pharmaceuticals Corporation

    发明人： SUN, Lijun ,  ONO, Mitsunori ,  WADA, Yumiko ,  YING, Weiwen ,  PRZEWLOKA, Teresa ,  KOSTIK, Elena

    IPC分类号： A61P19/02 ,  A61P17/06 ,  A61P3/10 ,  A61P1/00 ,  C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D401/10 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61K31/52 ,  A61K31/522 ,  A61K31/541 ,  A61K31/5355 ,  A61K31/4745 ,  A61K31/4743 ,  A61K31/496

    CPC分类号： C07D473/34 ,  C07D473/16 ,  C07D473/18

    摘要： 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.

    摘要翻译： 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。

    PYRIMIDINE COMPOUNDS AND USES THEREOF
    8.
    发明公开
    PYRIMIDINE COMPOUNDS AND USES THEREOF 审中-公开
    嘧啶化合物及其用途

    公开(公告)号：EP1827447A1

    公开(公告)日：2007-09-05

    申请号：EP05851852.3

    申请日：2005-11-18

    申请人： Synta Pharmaceuticals Corporation

    发明人： WADA, Yumiko ,  LU, Rongzhen ,  HSIA, Albert, Y.

    IPC分类号： A61K31/5377

    CPC分类号： A61K31/5377

    摘要： This invention features pyrimidine compounds of formula (I): Rl is formula (A), 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, SO2Rc, S(O2)NRc Rd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C=N-Rc, C=N-ORc, C=N-SRc, O, S, S(O), S(O2), 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(O2), 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 featured compounds inhibit the production of IL-12, IL-23 and IL-27 and are useful for treating disorders associated with IL- 12, IL-23 and IL-27 overproduction or misregulation, such as inflammatory and immune disorders.