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1. 发明申请

US20050261203A1 Azabicyclo-octane inhibitors of IAP 失效
标题翻译： 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。

2. 发明申请

US20060014700A1 Inhibitors of IAP 有权
标题翻译： IAP抑制剂
公开(公告)号：US20060014700A1
公开(公告)日：2006-01-19
申请号：US11174784
申请日：2005-07-05
申请人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
发明人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
IPC分类号： A61K38/05 , C07K5/04 , A61K31/421 , A61K31/426
CPC分类号： C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.
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：其中X，Y，A，R 1，R 2， R 3，R 4，R 4，R 5，R 5，R 5， R 6，R 6和R 6'如本文所述。

3. 发明申请

US20070299052A1 Inhibitors of IAP 审中-公开
公开(公告)号：US20070299052A1
公开(公告)日：2007-12-27
申请号：US11739030
申请日：2007-04-23
申请人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
发明人： Frederick Cohen , Kurt Deshayes , Wayne Fairbrother , Bainian Feng , John Flygare , Lewis Gazzard , Vickie Tsui
IPC分类号： A61K31/55 , A61K31/351 , A61K31/40 , A61K31/41 , A61P35/00 , C07D207/30 , C07D223/14 , C07D277/02 , C07D309/02 , C12N9/00 , C12N5/00 , C07D285/06 , C07D231/02 , C07D221/00 , A61P43/00 , A61K31/415 , A61K31/426 , A61K31/445
CPC分类号： C07D417/14 , A61K31/55 , A61K38/177 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/0827 , C07K7/06 , C12N5/0693
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4′, R5, R5′, R6 and R6′ are as described herein.

4. 发明申请

US20060167066A1 Pyrrolidine inhibitors of IAP 审中-公开
标题翻译： IAP吡咯烷抑制剂
公开(公告)号：US20060167066A1
公开(公告)日：2006-07-27
申请号：US11312063
申请日：2005-12-19
申请人： Frederick Cohen , Vickie Tsui , Cuong Ly , John Flygare
发明人： Frederick Cohen , Vickie Tsui , Cuong Ly , John Flygare
IPC分类号： A61K31/427 , A61K31/422 , C07D417/02 , C07D413/02
CPC分类号： C07D471/04 , C07D417/04 , C07D417/14
摘要： The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4′, R5, R6′ and R6′ are as described herein.
摘要翻译：本发明提供新的IAP抑制剂，其可用作治疗恶性肿瘤的治疗剂，其中化合物具有通式I：其中A，Q，X 1，X 2， Y，R 1，R 2，R 3，R 4，R 4， R 5，R 6和R 6'如本文所述。

5. 发明申请

US20080146808A1 AZABICYCLO-OCTANE INHIBITORS OF IAP 审中-公开
标题翻译：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。

6. 发明授权

US07345081B2 Azabicyclo-octane inhibitors of IAP 失效
标题翻译： 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。

7. 发明申请

US20110098305A1 ARYLSULFONAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：芳香酰胺化合物，组合物和使用方法
公开(公告)号：US20110098305A1
公开(公告)日：2011-04-28
申请号：US12993574
申请日：2009-05-20
申请人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne Fairbrother , John Flygare , Michael F.T. Koehler
发明人： Jonathan Bayldon Baell , Guillaume Laurent Lessene , Brad Edmund Sleebs , Wayne Fairbrother , John Flygare , Michael F.T. Koehler
IPC分类号： A61K31/501 , C07D239/88 , A61K31/497 , C07D237/30 , A61P35/00
CPC分类号： C07D215/38
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有化合物的组合物和该化合物用于制备用于治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

8. 发明申请

US20090148921A1 Compositions and methods for enhancing apoptosis 审中-公开
标题翻译：用于增强凋亡的组合物和方法
公开(公告)号：US20090148921A1
公开(公告)日：2009-06-11
申请号：US11521722
申请日：2006-09-14
申请人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
发明人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
IPC分类号： C12N9/00 , C07K5/10 , C12N5/06 , C07K7/06
CPC分类号： A61K38/08 , A61K38/00 , C07K7/08 , C07K14/001 , C07K14/4747 , C07K2319/00
摘要： The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译：本发明涉及用于增强哺乳动物细胞凋亡的物质组合物，以及使用这些物质组合物的方法。

9. 发明申请

US20120058953A1 COMPOSITIONS AND METHODS FOR ENHANCING APOPTOSIS 审中-公开
标题翻译：组合物和增强抗病毒的方法
公开(公告)号：US20120058953A1
公开(公告)日：2012-03-08
申请号：US13274142
申请日：2011-10-14
申请人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
发明人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
IPC分类号： A61K38/08 , C07K5/103 , C07K7/06 , A61P35/02 , C12N9/96 , C12N5/09 , A61K38/07 , A61P35/00 , C07K4/00 , C07K19/00
CPC分类号： A61K38/08 , A61K38/00 , C07K7/08 , C07K14/001 , C07K14/4747 , C07K2319/00
摘要： The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译：本发明涉及用于增强哺乳动物细胞凋亡的物质组合物，以及使用这些物质组合物的方法。

10. 发明申请

US20110039324A1 COMPOSITIONS AND METHODS FOR ENHANCING APOPTOSIS 审中-公开
标题翻译：组合物和增强抗病毒的方法
公开(公告)号：US20110039324A1
公开(公告)日：2011-02-17
申请号：US12835605
申请日：2010-07-13
申请人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
发明人： Kurt Deshayes , Wayne Fairbrother , John Flygare , Matthew C. Franklin , Saloumeh Fischer , Domagoj Vucic
IPC分类号： C12N9/96 , C07K2/00 , C07K5/103 , C07K7/06 , C12N5/071
CPC分类号： A61K38/08 , A61K38/00 , C07K7/08 , C07K14/001 , C07K14/4747 , C07K2319/00
摘要： The present invention is directed to compositions of matter useful for the enhancement of apoptosis in mammals and to methods of using those compositions of matter for the same.
摘要翻译：本发明涉及用于增强哺乳动物细胞凋亡的物质组合物，以及使用这些物质组合物的方法。

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