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    AZABICYCLO-OCTANE INHIBITORS OF IAP
    1.
    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
    2.
    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。

    Azabicyclo-octane inhibitors of IAP
    3.
    发明申请
    Azabicyclo-octane inhibitors of IAP 失效
    IAP的氮杂双环辛烷抑制剂

    公开(公告)号：US20050261203A1

    公开(公告)日：2005-11-24

    申请号：US11088008

    申请日：2005-03-22

    申请人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Keteltas ,  Vickie Tsui

    发明人： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Keteltas ,  Vickie Tsui

    IPC分类号： A61K31/403 ,  A61K38/04 ,  C07D203/02 ,  C07D209/02 ,  C07D409/12 ,  C07K5/06 ,  C07K14/47

    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。

    Fibroblast activation protein inhibitor compounds and methods
    10.
    发明申请
    Fibroblast activation protein inhibitor compounds and methods 有权
    成纤维细胞激活蛋白抑制剂化合物及方法

    公开(公告)号：US20060276435A1

    公开(公告)日：2006-12-07

    申请号：US11437182

    申请日：2006-05-18

    申请人： Frederick Cohen ,  Wayne Fairbrother ,  Clifford Quan ,  Daniel Sutherlin ,  Beni Wolf

    发明人： Frederick Cohen ,  Wayne Fairbrother ,  Clifford Quan ,  Daniel Sutherlin ,  Beni Wolf

    IPC分类号： C07F5/02 ,  A61K31/69

    CPC分类号： C07F5/025

    摘要： Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

    摘要翻译： 式I和II的氨基末端封闭的肽硼酸酯化合物可用于抑制成纤维细胞激活蛋白（FAP）和其它蛋白酶，以及用于治疗由FAP介导的病症。 使用氨基末端阻断肽硼酸酯化合物及其立体异构体，互变异构体，溶剂化物和其药学上可接受的盐的方法用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这些疾病。 披露