[EN] AZABICYCLO-OCTANE INHIBITORS OF IAP<br/>[FR] INHIBITEURS AZABICYCLO-OCTANE DE L'IAP
申请人:GENENTECH INC
公开号:WO2005094818A1
公开(公告)日:2005-10-13
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 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.
该发明提供了新型IAP抑制剂,可作为治疗恶性肿瘤的治疗剂,其中化合物具有通式(I),其中X1和X2独立地为O或S;L为键或-C(X3)-,-C(X3)NR12,-C(X3)O-,其中X3为O或S,R12为H或R1;R1为烷基,碳环,碳环取代烷基,杂环或杂环取代烷基,其中每个可选择地取代为卤素,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;R2为烷基,环烷基,环烷基烷基,芳基,芳基烷基,杂环或杂环烷基;R3为H或烷基;R4和R4'独立地为H,烷基,芳基,芳基烷基,环烷基,环烷基烷基,杂芳基,或杂芳基烷基,其中每个可选择地取代为卤素,羟基,巯基,羧基,烷基,烷氧基,氨基和硝基;R5和R5'各自独立地为H或烷基;R6为H或烷基;以及其盐和溶剂化合物。