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1. 发明申请

US20080039459A1 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US20080039459A1
公开(公告)日：2008-02-14
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： C07D413/14 , A61K31/5377 , A61P17/00 , A61P25/00 , A61P3/00 , A61P3/10 , C12N9/99 , A61P31/00 , A61P35/00 , A61P41/00 , A61P9/00
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，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种病症的方法。

2. 发明授权

US07846929B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US07846929B2
公开(公告)日：2010-12-07
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，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种病症的方法。

3. 发明申请

US20110105464A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：US20110105464A1
公开(公告)日：2011-05-05
申请号：US12916125
申请日：2010-10-29
申请人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
发明人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
IPC分类号： A61K31/5377 , A61P35/00 , A61P35/02 , A61P29/00 , A61P3/10 , A61P9/00
CPC分类号： C07D491/04 , C07D495/04
摘要： Methods of using compounds of Formula Ia and Ib 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：公开了将式Ia和Ib化合物用于体外，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种病症的方法。

4. 发明授权

US08450315B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US08450315B2
公开(公告)日：2013-05-28
申请号：US12916125
申请日：2010-10-29
申请人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
发明人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
IPC分类号： A61K31/5377
CPC分类号： C07D491/04 , C07D495/04
摘要： Methods of using compounds of Formula Ia and Ib 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：公开了将式Ia和Ib化合物用于体外，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种病症的方法。

5. 发明申请

US20080269210A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：US20080269210A1
公开(公告)日：2008-10-30
申请号：US11951189
申请日：2007-12-05
申请人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
发明人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D495/04 , C07D413/14 , A61P35/00 , A61K31/519
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。公开了使用式Ia-d化合物在体外，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种疾病的方法。

6. 发明授权

US09487533B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US09487533B2
公开(公告)日：2016-11-08
申请号：US11951189
申请日：2007-12-05
申请人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
发明人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
IPC分类号： C07D491/048 , C07D495/04
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

7. 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。

8. 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。

9. 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。

10. 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.

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