专利检索 ap:("Frederick Cohen" OR "Wayne J. Fairbrother" OR "Clifford Quan" OR "Daniel P. Sutherlin" OR "Beni B. Wolf") AND inv:"Daniel P. Sutherlin" 第 4 页

31.

发明授权
Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂

公开(公告)号：US06472393B1

公开(公告)日：2002-10-29

申请号：US09509104

申请日：2000-03-21

申请人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu

发明人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu

IPC分类号： A61K3118

CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51

摘要： Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

摘要翻译： 具有下述结构的化合物其中A，B，N1，N2，X，Y，Q，R2，R5和R6如本文所定义，可用于抑制丝氨酸蛋白酶，如TF /因子VIIa因子Xa，凝血酶和激肽释放酶。这些化合物可用于预防和/或治疗凝血障碍的方法。

32.

发明授权
Tyrosine derivatives 有权
标题翻译：酪氨酸衍生物

公开(公告)号：US06469047B1

公开(公告)日：2002-10-22

申请号：US09669779

申请日：2000-09-25

申请人： David Y. Jackson , Frederick C. Sailes , Daniel P. Sutherlin

发明人： David Y. Jackson , Frederick C. Sailes , Daniel P. Sutherlin

IPC分类号： A61K31535

CPC分类号： C07D213/75 , C07C233/87 , C07C271/22 , C07C271/44 , C07C271/48 , C07C271/54 , C07C271/56 , C07C271/58 , C07C311/06 , C07C311/09 , C07C311/58 , C07C323/43 , C07C323/59 , C07D207/16 , C07D207/22 , C07D207/28 , C07D211/46 , C07D211/60 , C07D211/62 , C07D215/36 , C07D217/06 , C07D217/14 , C07D217/22 , C07D231/16 , C07D235/06 , C07D235/26 , C07D249/18 , C07D277/12 , C07D277/56 , C07D295/205 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/72 , C07D471/10

摘要： The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

摘要翻译： 本发明的化合物是含有整合素介导的与配体如VCAM-1和MAdCAM结合的α4的抑制剂。

33.

发明授权
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.

34.

发明授权
Benzoxazepin compounds selective for PI3K P110 delta and methods of use 有权
标题翻译：苯并西泮化合物选择性PI3K P110 delta及其使用方法

公开(公告)号：US09090628B2

公开(公告)日：2015-07-28

申请号：US13424500

申请日：2012-03-20

申请人： Timothy Heffron , Brian Safina , Steven Staben , Daniel P. Sutherlin , BinQing Wei , Richard Elliott , Robert Heald , Eileen M. Seward , Emanuela Gancia , Bohdan Waszkowycz

发明人： Timothy Heffron , Brian Safina , Steven Staben , Daniel P. Sutherlin , BinQing Wei , Richard Elliott , Robert Heald , Eileen M. Seward , Emanuela Gancia , Bohdan Waszkowycz

IPC分类号： A61K31/553 , C07D498/04 , C07D498/14 , C07D519/00

CPC分类号： C07D498/14 , C07D498/04 , C07D519/00

摘要： Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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： 苯并西泮配方I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗脂质激酶如炎症，免疫学障碍和癌症介导的病症。公开了使用式I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病症的方法。

35.

发明授权
Pharmaceutical compounds 有权
标题翻译：药物化合物

公开(公告)号：US08802670B2

公开(公告)日：2014-08-12

申请号：US11789468

申请日：2007-04-24

申请人： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu

发明人： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Bing-Yan Zhu

IPC分类号： A61K31/535 , C07D413/14

CPC分类号： A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04

摘要： Compounds of Formulae Ia and Ib, and 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的化合物及其立体异构体，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。

36.

发明申请
HETEROCYCLIC COMPOUNDS AND METHODS OF USE 失效
标题翻译：杂环化合物和使用方法

公开(公告)号：US20120202785A1

公开(公告)日：2012-08-09

申请号：US13369016

申请日：2012-02-08

申请人： Robert Heald , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Bohdan Waszkowycz

发明人： Robert Heald , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Bohdan Waszkowycz

IPC分类号： A61K31/52 , C07D519/00 , C07D487/04 , C07D495/04 , C07D403/12 , C07D498/06 , A61K31/519 , A61K31/5377 , A61P35/00 , A61P37/00 , A61P9/00 , A61P31/12 , A61P29/00 , A61P3/00 , A61P5/00 , A61P25/00 , A61P19/02 , A61P37/08 , A61P1/04 , A61P11/06 , A61P17/06 , A61P35/02 , C07D473/34

CPC分类号： C07D473/34 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D473/16 , C07D473/32 , C07D473/40 , C07D487/04 , C07D495/04 , C07D498/06 , C07D513/04 , C07D519/00

摘要： Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。公开了使用式I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病症的方法。

37.

发明申请
BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 失效
标题翻译：用于P110 DELTA的双相PYRIMIDIN PI3K抑制剂化合物选择及使用方法

公开(公告)号：US20120178736A1

公开(公告)日：2012-07-12

申请号：US13427081

申请日：2012-03-22

申请人： Georgette Castanedo , Bryan Chan , David Goldstein , Rama Kondru , Matthew Lucas , Wylie Palmer , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Zachary K. Sweeney

发明人： Georgette Castanedo , Bryan Chan , David Goldstein , Rama Kondru , Matthew Lucas , Wylie Palmer , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Zachary K. Sweeney

IPC分类号： A61K31/5377 , C07D487/04 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P1/04 , A61P1/00 , A61P17/00 , A61P11/06 , A61P19/04 , A61P25/00 , A61P7/02 , A61P7/00 , A61P11/00 , A61P17/06 , A61P19/02 , C07D495/04

CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04

摘要： Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is 0, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I 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（Ib）化合物，其中（i）X1为N，X 2为S，（ii）X1为CR7，X2为S，（iii）X1为N，X2为NR2，或（iv）X1为CR7， X 2为0，包括立体异构体，互变异构体，代谢物和药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学和癌症介导的病症。公开了使用式I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病症的方法。