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    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF
    4.
    发明申请
    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF 审中-公开
    GLUCOCORTICOID受体的调节剂，AP-1和/或NF-κB活性及其用途

    公开(公告)号：WO2008057862A2

    公开(公告)日：2008-05-15

    申请号：PCT/US2007/083094

    申请日：2007-10-31

    申请人： BRISTOL-MYERS SQUIBB COMPANY ,  YANG, Bingwei Vera ,  DOWEYKO, Lidia M. ,  VACCARO, Wayne ,  HUYNH, Tram N. ,  TORTOLANI, David R. ,  DHAR, T.g. Murali

    发明人： YANG, Bingwei Vera ,  DOWEYKO, Lidia M. ,  VACCARO, Wayne ,  HUYNH, Tram N. ,  TORTOLANI, David R. ,  DHAR, T.g. Murali

    IPC分类号： C07C235/36 ,  C07D213/75 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D241/20

    CPC分类号： C07D211/58 ,  C07C235/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/75 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D277/46 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R 6 and R 7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C 1 -C 4 alkyl, and substituted C 1 -C 4 alkyl; or (ii) Q and R 6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and M a M are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO 2 , and N which ring may be optionally substituted with 0-2 R 5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and M a , Z a , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.

    摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病， 对映体，非对映异构体，互变异构体，溶剂化物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基，则 R 6和R 7与它们所连接的碳原子一起选自除环烷基之外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基 烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和M a a M与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自 由O，S，SO 2和N组成的基团可以任选地被0-2个R 5基团或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 和M a a，Z a，R 1，R 2，R 3， R 4，R 6，R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。