IMIDAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY
    62.
    发明申请
    IMIDAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
    调节HSP90活性的咪唑化合物

    公开(公告)号:US20140094436A1

    公开(公告)日:2014-04-03

    申请号:US14103420

    申请日:2013-12-11

    摘要: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.

    摘要翻译: 式(I)化合物,包含式(I)化合物的药物组合物和抑制细胞中Hsp90的方法,治疗或预防哺乳动物中的增殖病症并治疗哺乳动物的癌症,其包括给予式(I)化合物至 患者或细胞。 变量R5是任选取代的杂芳基; 任选取代的6至14元芳基; 任选在任何可取代的氮或碳原子上取代的双环9元杂环; 或本文定义的取代基R18。 环A是除了R3之外任选进一步被一个或多个取代基取代的芳基或杂芳基。 取代基R 3在本文中定义。

    TRICYCLIC TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY
    64.
    发明申请
    TRICYCLIC TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
    调节HSP90活性的TRICYCLIC TRIAZOLE化合物

    公开(公告)号:US20110152310A1

    公开(公告)日:2011-06-23

    申请号:US12992448

    申请日:2009-05-15

    CPC分类号: C07D487/04 C07D471/04

    摘要: The present invention relates to substituted tricyclic triazole compounds and compositions comprising substituted tricyclic triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.

    摘要翻译: 本发明涉及取代的三环三唑化合物和包含取代的三环三唑化合物的组合物。 本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法以及在有需要的受试者中预防或治疗过度增殖性疾病如癌症的方法,其包括向受试者施用本发明化合物或 包含这种化合物的组合物。

    Heterocyclic compounds
    67.
    发明授权

    公开(公告)号:US07122665B2

    公开(公告)日:2006-10-17

    申请号:US10686505

    申请日:2003-10-14

    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)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C═NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, 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.