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    • 5. 发明申请
    • AZABICYCLO-OCTANE INHIBITORS OF IAP
    • 化学文摘AZABICYCLO-OCTANE抑制剂
    • US20080146808A1
    • 2008-06-19
    • US12019003
    • 2008-01-24
    • Frederick CohenWayne FairbrotherJohn FlygareStephen Franz KeteltasVickie Hsiao-Wei Tsui
    • Frederick CohenWayne FairbrotherJohn FlygareStephen Franz KeteltasVickie Hsiao-Wei Tsui
    • C07D403/12C07D209/52C07D401/12
    • 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: X1 and X2 are independently O or S; L is a bond or —C(X3)—, —C(X3)NR12, —C(X3)O— wherein X3 is O or S and R12 is H or R1; R1 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; R2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R3 is H or alkyl; R4 and R4′ 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; R5, and R5′ are each independently H or alkyl; R6 is H or alkyl; and salts and solvates thereof.
    • 本发明提供可用作治疗恶性肿瘤的治疗剂的IAP的新型抑制剂,其中化合物具有通式I:X 1和X 2独立地为O或S ; -C(X 3) - , - C(X 3)NR 12,-C(X 3) 3其中X 3是O或S,R 12是H或R 1; 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; R 2是烷基,环烷基,环烷基烷基,芳基,芳烷基,杂环或杂环基烷基; R 3是H或烷基; R 4和R 4'独立地为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; R 5和R 5'各自独立地为H或烷基; R 6是H或烷基; 及其盐和溶剂合物。