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    AZABICYCLO-OCTANE INHIBITORS OF IAP
    3.
    发明申请
    AZABICYCLO-OCTANE INHIBITORS OF IAP 审中-公开
    化学文摘AZABICYCLO-OCTANE抑制剂

    公开(公告)号：US20080146808A1

    公开(公告)日：2008-06-19

    申请号：US12019003

    申请日：2008-01-24

    申请人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Franz Keteltas ,  Vickie Hsiao-Wei Tsui

    发明人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Franz Keteltas ,  Vickie Hsiao-Wei Tsui

    IPC分类号： C07D403/12 ,  C07D209/52 ,  C07D401/12

    CPC分类号： C07K5/06026 ,  C07K14/4747

    摘要： 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.

    摘要翻译： 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。

    Azabicyclo-octane inhibitors of IAP
    6.
    发明授权
    Azabicyclo-octane inhibitors of IAP 失效
    IAP的氮杂双环辛烷抑制剂

    公开(公告)号：US07345081B2

    公开(公告)日：2008-03-18

    申请号：US11088008

    申请日：2005-03-22

    申请人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Franz Keteltas ,  Vickie Hsiao-Wei Tsui

    发明人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Franz Keteltas ,  Vickie Hsiao-Wei Tsui

    IPC分类号： A61K31/403 ,  C07D209/02

    CPC分类号： C07K5/06026 ,  C07K14/4747

    摘要： 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.

    摘要翻译： 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。