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公开(公告)号：US08278446B2
公开(公告)日：2012-10-02
申请号：US11766257
申请日：2007-06-21
IPC分类号： C07D239/48 , C07D239/50 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D413/04 , C07D417/12
摘要： The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.
摘要翻译： 本发明涉及一种在具有多个反应位点和随后的立体选择性肟形成的卤代嘧啶甲醛上进行化学选择性取代的方法。
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公开(公告)号：US20080249304A1
公开(公告)日：2008-10-09
申请号：US11766257
申请日：2007-06-21
IPC分类号： C07D295/00 , C07D239/24
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D413/04 , C07D417/12
摘要： The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.
摘要翻译： 本发明涉及一种在具有多个反应位点和随后的立体选择性肟形成的卤代嘧啶甲醛上进行化学选择性取代的方法。
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3.发明授权Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors 失效氧基哌嗪 - 氮杂环丁烷酰胺和氧代二氮杂吖啶啶酰胺作为单酰基甘油脂肪酶抑制剂公开(公告)号：US08637498B2
公开(公告)日：2014-01-28
申请号：US13246232
申请日：2011-09-27
IPC分类号： A61K31/496 , A61K31/506 , A61K31/551 , C07D403/04 , C07D403/14 , C07D409/14 , C07D417/14
CPC分类号： C07D403/14 , C07D403/04 , C07D409/14 , C07D417/14
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.
摘要翻译： 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物和对映体，非对映异构体及其药学上可接受的盐由式（Ia）和式（Ib）表示如下：其中Y，Z和n如本文所定义; 并且其中Yb和Zb如本文所定义。
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4.发明授权Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors 有权氨基 - 吡咯烷 - 氮杂环丁烷二酰胺作为单酰基甘油脂肪酶抑制剂公开(公告)号：US08575363B2
公开(公告)日：2013-11-05
申请号：US13277734
申请日：2011-10-20
IPC分类号： C07D207/10 , A61K31/397
CPC分类号： A61K31/4025 , A61K31/404 , A61K31/416 , A61K31/427 , A61K31/428 , A61K31/4725 , A61K31/506 , A61K31/517 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.
摘要翻译： 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物和对映异构体，非对映异构体及其药学上可接受的盐由式（I）表示如下：其中Y，Z和R 1和R 2在本文中定义。
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5.发明申请PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS 有权哌可啶-4-Y-AZETIDINE DIAMIDES作为单羟乙基脂肪酶抑制剂公开(公告)号：US20130102584A1
公开(公告)日：2013-04-25
申请号：US13277702
申请日：2011-10-20
申请人： Peter J. Connolly , Haiyan Bian , Xun Li , Li Liu , Mark J. Macielag , Mark E. McDonnell
发明人： Peter J. Connolly , Haiyan Bian , Xun Li , Li Liu , Mark J. Macielag , Mark E. McDonnell
IPC分类号： A61K31/454 , A61P25/00 , A61P25/06 , C07D417/14
CPC分类号： C07D417/14
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
摘要翻译： 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物和对映体，非对映异构体及其药学上可接受的盐由式（I）表示如下：其中Y，Z和R在本文中定义。
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6.发明申请SUBSTITUTED PYRIMIDINE-5-CARBOXAMIDE AND 5-CARBOXYLIC ESTER KINASE INHIBITORS 审中-公开取代的吡咯烷-5-羧酰胺和5-羧基酯激酶抑制剂公开(公告)号：US20090111810A1
公开(公告)日：2009-04-30
申请号：US12252718
申请日：2008-10-16
IPC分类号： A61K31/5377 , C07D401/12 , C07D413/12 , A61P25/00 , A61K31/506
CPC分类号： C07D239/48
摘要： The present invention is directed to substituted pyrimidine-5-carboxamide and 5-carboxylic ester compounds of Formula (I): and forms thereof wherein R1, R2, R3, R4, R5, R6, R7 and L are as defined herein and their synthesis and use as kinase inhibitors for treating a chronic or acute protein kinase mediated disease.
摘要翻译： 本发明涉及式（I）的取代的嘧啶-5-甲酰胺和5-羧酸酯化合物及其形式，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和L如本文所定义， 并用作治疗慢性或急性蛋白激酶介导的疾病的激酶抑制剂。
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![Substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds](/abs-image/US/2009/04/14/US07517885B2/abs.jpg.150x150.jpg)
7.发明授权Substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds 有权取代的[4-（4-苯基 - 哌嗪-1-基） - 环己基] - 脲化合物公开(公告)号：US07517885B2
公开(公告)日：2009-04-14
申请号：US11453128
申请日：2006-06-14
申请人： George Chiu , Peter J. Connolly , Jessica J. Liu , Steven A. Middleton , Virginia L. Pulito , Shengjian Li
发明人： George Chiu , Peter J. Connolly , Jessica J. Liu , Steven A. Middleton , Virginia L. Pulito , Shengjian Li
IPC分类号： A61K31/495 , C07D295/155
CPC分类号： C07D295/155 , C07D295/135
摘要： The present invention relates to substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.
摘要翻译： 本发明涉及用于治疗良性前列腺肥大的α1a/α1d肾上腺素受体调节剂的式（I）的取代的[4-（4-苯基 - 哌嗪-1-基） - 环己基] - 脲化合物及其药学上可接受的形式 和下尿路症状。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。
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公开(公告)号：US20090076037A1
公开(公告)日：2009-03-19
申请号：US11858609
申请日：2007-09-20
IPC分类号： A61K31/519 , C07D487/04 , A61P35/02 , A61P35/00 , A61P25/28 , A61P17/00
CPC分类号： C07D487/04 , C07D498/04
摘要： The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.
摘要翻译： 本发明涉及式（I）的新型双环嘧啶化合物或其形式或组合物及其作为ATP-蛋白激酶相互作用抑制剂的用途。
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公开(公告)号：US20080108611A1
公开(公告)日：2008-05-08
申请号：US11621610
申请日：2007-01-10
申请人： Kathleen A. Battista , Gilles C. Bignan , Peter J. Connolly , Stuart L. Emanuel , Stuart Hayden , Sigmond G. Johnson , Ronghui Lin , Steven A. Middleton , Niranjan B. Pandey , Mark T. Powell
发明人： Kathleen A. Battista , Gilles C. Bignan , Peter J. Connolly , Stuart L. Emanuel , Stuart Hayden , Sigmond G. Johnson , Ronghui Lin , Steven A. Middleton , Niranjan B. Pandey , Mark T. Powell
IPC分类号： A61K31/519 , C07D495/04 , A61K31/5377 , A61P35/00 , A61P17/00 , A61P9/00 , C07D413/14
CPC分类号： C07D495/04
摘要： The present invention is directed to thienopyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.
摘要翻译： 本发明涉及式（I）的噻吩并嘧啶化合物及其形式，其合成和用途，用于治疗，预防或改善慢性或急性蛋白激酶介导的疾病，病症或病症。
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公开(公告)号：US06924302B2
公开(公告)日：2005-08-02
申请号：US10029750
申请日：2001-12-21
申请人： Ronghui Lin , Peter J. Connolly , Steven K. Wetter , Shenlin Huang , Stuart L. Emanuel , Robert H. Gruninger , Steven A. Middleton
发明人： Ronghui Lin , Peter J. Connolly , Steven K. Wetter , Shenlin Huang , Stuart L. Emanuel , Robert H. Gruninger , Steven A. Middleton
IPC分类号： A61K31/4178 , A61K31/4196 , A61K31/427 , A61K31/4439 , C07D249/14 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , A61K31/496 , A61P35/00 , C07D249/08
CPC分类号： C07D401/06 , A61K31/4178 , A61K31/4196 , A61K31/427 , A61K31/4439 , C07D249/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The present invention provides substituted triazole diamine derivatives as selective kinase or dual-kinase inhibitors and a method for treating or ameliorating a selective kinase or dual-kinase mediated disorder.
摘要翻译： 本发明提供了作为选择性激酶或双重激酶抑制剂的取代的三唑二胺衍生物以及治疗或改善选择性激酶或双重激酶介导的病症的方法。
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