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    • 9. 发明专利
    • HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE
    • CA2513141A1
    • 2004-08-12
    • CA2513141
    • 2004-01-23
    • PFIZER LTD
    • KUKI ATSUOZHANG JUNHUWANG HAIPLEWE MICHAEL BRUNOLI XINQIANG
    • A61P31/18C07D471/04A61K31/437
    • Beta-carboline hydroxamic acid compounds represented by formula (I) and formula (lb) are described, wherein: R1, R2, R3, R4, R5, and R6 are independently selected from hydrogen, halogen, C1_C6 alkyl, aikoxy C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -ORc, -NO2, and -N(Rc)2, each Rc is Independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-Ca alkynyl; R7 Is C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl, all of which ar e optionally substituted by one or more substituents independently selected fr om halogen, C1-C6 alkyl, C2-C6 alkenyl; C2-C6 alkynyl, aryl, cycloalkyl, heterocycioalkyl, and heteroaryl, wherein said aryl, cydoalkyi, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl; R8 and R9 are independently selected from hydrogen, C1-C6 alkyl, C2 - C6 alkenyl, and C2-C6 aikynyl, wherein said alkyl, alkenyl, and alkynyl are optionally substituted with one or more substituents independently selected from halogen, aryl, cycloalkyl, heterocycloalkyl, and heteroaryl group, wherein said aryl, cycloalkyl, and heterocycloalkyl are optionally substitut ed with one or more substituents independently selected from halogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase- mediated diseases and conditions.