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    • 5. 发明申请
    • HIV INTEGRASE INHIBITORS
    • 艾滋病毒整合抑制剂
    • US20100216834A1
    • 2010-08-26
    • US12445594
    • 2007-10-15
    • Richard C. A. IsaacsJohn S. WaiLinda S. PayneThorsten E. Fisher
    • Richard C. A. IsaacsJohn S. WaiLinda S. PayneThorsten E. Fisher
    • A61K31/4375C07D471/14C07D471/04A61P31/18
    • C07D471/14
    • Stereoisomers of compounds of Formula I are disclosed: wherein V1, V2, R5a, R5b, R5c, R8 and R9b are defined herein and wherein the stereoisomer contains 2 chiral centers in the 8-membered ring and one of the chiral centers is due to the presence of a chiral ring carbon. The isomers are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    • 公开了式I化合物的立体异构体:其中V1,V2,R5a,R5b,R5c,R8和R9b在本文中定义,其中立体异构体在8元环中含有2个手性中心,并且其中一个手性中心是由于 存在手性环碳。 异构体是HIV整合酶和HIV复制抑制剂的抑制剂,可用于预防或治疗艾滋病毒感染以及艾滋病的发病或进展的预防,治疗或延迟。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。