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公开(公告)号：US07265146B2
公开(公告)日：2007-09-04
申请号：US11111105
申请日：2005-04-20
申请人： Dean R. Artis , David Y. Jackson , Thomas E. Rawson , Mark E. Reynolds , Daniel P. Sutherlin , Mark S. Stanley
发明人： Dean R. Artis , David Y. Jackson , Thomas E. Rawson , Mark E. Reynolds , Daniel P. Sutherlin , Mark S. Stanley
IPC分类号： A61K31/403 , C07D207/04 , C07D209/82
CPC分类号： C07D403/12 , C07C233/25 , C07C233/60 , C07C233/81 , C07C237/04 , C07C237/20 , C07C237/22 , C07C2601/08 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/48 , C07D209/88 , C07D405/12
摘要： Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.
摘要翻译： 提供式（I）的化合物，其中A，Q，W，X，Y，Z，R 1至R 4，m和n如本文所定义。 本发明的化合物结合α4H整联蛋白受体，从而抑制用于α4A整联蛋白的配体的结合，其可用于预防和/或治疗与 α4整联蛋白或其配体。
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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。
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公开(公告)号：US06469047B1
公开(公告)日：2002-10-22
申请号：US09669779
申请日：2000-09-25
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。
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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。
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公开(公告)号：US20120094980A1
公开(公告)日：2012-04-19
申请号：US13273945
申请日：2011-10-14
申请人： Janet L. Gunzner , Daniel P. Sutherlin , Mark S. Stanley , Liang Bao , Georgette Castanedo , Rebecca Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F.T. Koehler
发明人： Janet L. Gunzner , Daniel P. Sutherlin , Mark S. Stanley , Liang Bao , Georgette Castanedo , Rebecca Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F.T. Koehler
IPC分类号： A61K31/551 , A61K31/5377 , C07D401/14 , A61K31/444 , C07D213/56 , A61K31/44 , C07D409/12 , A61K31/4436 , C07D413/12 , A61K31/4439 , C07D403/14 , A61K31/496 , C07D401/12 , A61K31/506 , C07D417/12 , A61K31/541 , A61K31/4545 , C12N5/07 , A61P35/00 , A61P9/00 , C07D413/14
CPC分类号： C07D213/16 , C07D213/06 , C07D213/56 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A，X，Y R1，R2，R3，R4，m和n如本文所述。
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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
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。
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公开(公告)号：US20090281089A1
公开(公告)日：2009-11-12
申请号：US12420746
申请日：2009-04-08
申请人： Janet L. Gunzner , Daniel P. Sutherlin , Mark S. Stanley , Liang Bao , Georgette Castanedo , Rebecca L. LaLonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina
发明人： Janet L. Gunzner , Daniel P. Sutherlin , Mark S. Stanley , Liang Bao , Georgette Castanedo , Rebecca L. LaLonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina
IPC分类号： A61K31/444 , C07D413/14 , C07D401/14 , C07D213/56 , C07D417/12 , C07D413/12 , C07D401/12 , A61P35/00 , A61K31/5377 , A61K31/4402 , A61K31/496 , A61K31/541 , A61K31/4439 , A61K31/506 , A61K31/551
CPC分类号： C07D213/16 , C07D213/06 , C07D213/56 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A，X，Y R1，R2，R3，R4，m和n如本文所述。
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公开(公告)号：US07595399B2
公开(公告)日：2009-09-29
申请号：US10772678
申请日：2004-02-04
IPC分类号： C07D211/06 , C07D295/027 , C07D217/12
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.
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公开(公告)号：US07273886B2
公开(公告)日：2007-09-25
申请号：US10850231
申请日：2004-05-19
IPC分类号： A61K31/64
CPC分类号： C07D405/12 , C07D307/81
摘要： Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 式I的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶，并具有改善的药代动力学性质。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US06706753B2
公开(公告)日：2004-03-16
申请号：US10313147
申请日：2002-12-06
申请人： Dean R. Artis , David Y. Jackson , Thomas E. Rawson , Mark E. Reynolds , Daniel P. Sutherlin , Mark S. Stanley
发明人： Dean R. Artis , David Y. Jackson , Thomas E. Rawson , Mark E. Reynolds , Daniel P. Sutherlin , Mark S. Stanley
IPC分类号： A61K314025
CPC分类号： C07D403/12 , C07C233/25 , C07C233/60 , C07C233/81 , C07C237/04 , C07C237/20 , C07C237/22 , C07C2601/08 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/48 , C07D209/88 , C07D405/12
摘要： Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to &agr;4 integrin receptors and thereby inhibit binding of ligands for &agr;4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with &agr;4 integrins or their ligands.
摘要翻译： 提供式（I）的化合物，其中A，Q，W，X，Y，Z，R 1至R 4，m和n如本文所定义。 本发明的化合物结合α4整联蛋白受体，从而抑制用于α4整联蛋白的配体的结合，其可用于与α4整联蛋白或其配体相关的疾病和病症的预防和/或治疗性治疗。
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