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    • 9. 发明申请
    • AZABICYCLO-OCTANE INHIBITORS OF IAP
    • 化学文摘AZABICYCLO-OCTANE抑制剂
    • WO2005094818A1
    • 2005-10-13
    • PCT/US2005/009328
    • 2005-03-22
    • GENENTECH, INC.COHEN, FrederickFAIRBROTHER, WayneFLYGARE, JohnTSUI, Vickie, Hsiao-WeiKETELTAS, Stephen, Franz
    • COHEN, FrederickFAIRBROTHER, WayneFLYGARE, JohnTSUI, Vickie, Hsiao-WeiKETELTAS, Stephen, Franz
    • A61K31/403
    • C07K5/06026C07K14/4747
    • The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X 1 and X 2 are independently O or S; L is a bond or -C(X 3 )-, -C(X 3 )NR 12 , -C(X 3 )O- wherein X 3 is O or S and R 12 is H or R 1 ; R 1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R 2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R 3 is H or alkyl; R 4 and R 4' are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R 5 , and R 5' are each independently H or alkyl; R 6 is H or alkyl; and salts and solvates thereof.
    • 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂,其中化合物具有其中X 1和X 2独立地为O或S的通式(I); L是键或-C(X3) - , - C(X3)NR12,-C(X3)O-,其中X3是O或S,R12是H或R1; R 1是烷基,碳环,碳环取代的烷基,杂环或杂环取代的烷基,其中各自任选被卤素,羟基,巯基,羧基,烷基,卤代烷基,烷氧基,烷基磺酰基,氨基,硝基,芳基和杂芳基取代; R2是烷基,环烷基,环烷基烷基,芳基,芳烷基,杂环或杂环基烷基; R3是H或烷基; R 4和R 4'独立地是H,烷基,芳基,芳烷基,环烷基,环烷基烷基,杂芳基或杂芳烷基,其中各自任选被卤素,羟基,巯基,羧基,烷基,烷氧基,氨基和硝基取代; R5和R5'各自独立地为H或烷基; R6是H或烷基; 及其盐和溶剂合物。