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11.发明授权Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效环状尿素衍生物，其制备方法及其作为激酶抑制剂的药物用途公开(公告)号：US07354933B2
公开(公告)日：2008-04-08
申请号：US10770382
申请日：2004-02-02
申请人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
发明人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
IPC分类号： C07D401/06 , C07D403/06 , A61K31/41
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译： 本发明涉及式I的环脲化合物：如本文所定义。 本发明还涉及其制备方法，包含其的药物组合物及其药物用途，作为蛋白激酶上的抑制剂。 因此，通过抑制蛋白激酶（例如实体瘤）的活性来预防或治疗能够调节的生理障碍是有用的。
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公开(公告)号：US20080070964A1
公开(公告)日：2008-03-20
申请号：US11857193
申请日：2007-09-18
申请人： William Welsh , Seong Yu , Anil Nair
发明人： William Welsh , Seong Yu , Anil Nair
IPC分类号： A61K31/4196 , A61P25/04 , C07D249/08
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/14
摘要： The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
摘要翻译： 本发明提供式I化合物：其中R 1至R 4和n具有说明书中定义的任何含义及其药学上可接受的盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体，以及用于治疗疼痛和治疗其它病症的治疗方法，所述治疗方法涉及例如使用 式I化合物。
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公开(公告)号：US07294720B2
公开(公告)日：2007-11-13
申请号：US11337366
申请日：2006-01-23
申请人： William J. Welsh , Seong Jae Yu , Anil Nair
发明人： William J. Welsh , Seong Jae Yu , Anil Nair
IPC分类号： C07D249/08 , A61K31/4196
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/14
摘要： The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
摘要翻译： 本发明提供式I化合物：其中R 1至R 4和n具有说明书中定义的任何含义及其药学上可接受的盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体，以及用于治疗疼痛和治疗其它病症的治疗方法，所述治疗方法涉及例如使用 式I化合物。
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公开(公告)号：US07164021B2
公开(公告)日：2007-01-16
申请号：US10665377
申请日：2003-09-18
申请人： William J. Welsh , Seong Jae Yu , Anil Nair
发明人： William J. Welsh , Seong Jae Yu , Anil Nair
IPC分类号： C07D471/02 , C07D471/08
CPC分类号： C07D471/10 , C07D498/08
摘要： Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the δ-opioid receptor have shown promise in providing enhanced analgesis without the addictive properties, the compounds of the present invention are better than morphine, naltrindole (NTI), spiroindanyloxymorphone (SIOM), and other known μ-opioid receptor selectors as analgesics.
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公开(公告)号：US20070105884A1
公开(公告)日：2007-05-10
申请号：US11507955
申请日：2006-08-22
申请人： William Welsh , Seong Yu , Anil Nair
发明人： William Welsh , Seong Yu , Anil Nair
IPC分类号： A61K31/485 , C07D489/02
CPC分类号： C07D471/10 , C07D498/08
摘要： Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the δ-opioid receptor have shown promise in providing enhanced analgesis without the addictive properties, the compounds of the present invention are better than morphine, naltrindole (NTI), spiroindanyloxymorphone (SIOM), and other known μ-opioid receptor selectors as analgesics.
摘要翻译： 已经设计了选择性结合δ-阿片受体的新型化合物。 这些化合物具有更大的选择性，改善的水（血液）溶解度，并且作为镇痛药具有增强的治疗价值。 由于对δ-阿片样物质受体具有选择性的激动剂显示出提供增强镇痛而没有上瘾性质的希望，本发明的化合物比吗啡，纳曲酮（NTI），螺茚二氧基吗啡（SIOM）和其他已知的μ-阿片受体 选择剂作为镇痛药。
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16.发明申请1,4-Dihydropyridine-Fused Heterocycles, Process for Preparing the Same, Use and Compositions Containing Them 有权1,4-二氢吡啶稠合杂环，其制备方法，含有它们的用途和组合物公开(公告)号：US20080261969A1
公开(公告)日：2008-10-23
申请号：US12014516
申请日：2008-01-15
申请人： Jacques MAUGER , Anil NAIR , Nina MA , Kirsten BJERGARDE , Bruno FILOCHE-ROMME , Odile ANGOUILLANT-BONIFACE , Serge MIGNANI , Jean-Christophe CARRY , Francois CLERC , Herve MINOUX , Laurent SCHIO , Cecile COMBEAU
发明人： Jacques MAUGER , Anil NAIR , Nina MA , Kirsten BJERGARDE , Bruno FILOCHE-ROMME , Odile ANGOUILLANT-BONIFACE , Serge MIGNANI , Jean-Christophe CARRY , Francois CLERC , Herve MINOUX , Laurent SCHIO , Cecile COMBEAU
IPC分类号： A61K31/5377 , C07D471/12 , A61K31/4353 , C07D471/02 , A61P35/00 , A61K31/519 , C07D295/00
CPC分类号： C07D471/04 , C07D471/14
摘要： This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
摘要翻译： 本发明涉及式（I）化合物，其用于制备这些化合物的方法，包含这些化合物的药物组合物，以及涉及治疗方法，包括施用这些化合物。
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公开(公告)号：US08420824B2
公开(公告)日：2013-04-16
申请号：US13156947
申请日：2011-06-09
申请人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
发明人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
IPC分类号： C07D401/00
CPC分类号： C07C273/18 , C07D231/38 , C07C275/38
摘要： The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
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18.发明授权1,4-dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them 有权1,4-二氢吡啶稠合的杂环，其制备方法，用途和含有它们的组合物公开(公告)号：US08163768B2
公开(公告)日：2012-04-24
申请号：US12014516
申请日：2008-01-15
申请人： Jacques Mauger , Anil Nair , Nina Ma , Kirsten Bjergarde , Bruno Filoche-Romme , Odile Angouillant-Boniface , Serge Mignani , Jean-Christophe Carry , Francois Clerc , Herve Minoux , Laurent Schio , Cecile Combeau
发明人： Jacques Mauger , Anil Nair , Nina Ma , Kirsten Bjergarde , Bruno Filoche-Romme , Odile Angouillant-Boniface , Serge Mignani , Jean-Christophe Carry , Francois Clerc , Herve Minoux , Laurent Schio , Cecile Combeau
IPC分类号： A61K31/437 , A61K31/4375 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
摘要翻译： 本发明涉及式（I）化合物，其用于制备这些化合物的方法，包含这些化合物的药物组合物，以及涉及治疗方法，包括施用这些化合物。
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公开(公告)号：US07776898B2
公开(公告)日：2010-08-17
申请号：US11857193
申请日：2007-09-18
申请人： William J. Welsh , Seong Jae Yu , Anil Nair
发明人： William J. Welsh , Seong Jae Yu , Anil Nair
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/14
摘要： The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
摘要翻译： 本发明提供式I化合物：其中R 1至R 4和n具有本说明书中定义的任何含义及其药学上可接受的盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体，以及用于治疗疼痛和治疗其它病症的治疗方法，所述治疗方法涉及例如使用 式I化合物。
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20.发明申请Cyclic Urea Compounds, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors 失效循环脲类化合物，其制备方法及其药物用途作为激酶抑制剂公开(公告)号：US20080108654A1
公开(公告)日：2008-05-08
申请号：US11972314
申请日：2008-01-10
申请人： Marcel PATEK , Anil NAIR , Augustin HITTINGER , Conception NEMECEK , Daniel BOND , Greg HARLOW , Herve BOUCHARD , Jacques MAUGER , Jean-Luc MALLERON , Mark PALERMO , Fahad AL-OBEIDI , Thomas FAITG , Hartmut STROBEL , Sven RUF , Kurt RITTER , Youssef EL-AHMAD , Dominique LESUISSE
发明人： Marcel PATEK , Anil NAIR , Augustin HITTINGER , Conception NEMECEK , Daniel BOND , Greg HARLOW , Herve BOUCHARD , Jacques MAUGER , Jean-Luc MALLERON , Mark PALERMO , Fahad AL-OBEIDI , Thomas FAITG , Hartmut STROBEL , Sven RUF , Kurt RITTER , Youssef EL-AHMAD , Dominique LESUISSE
IPC分类号： A61K31/47 , C07D401/02 , C07D401/14 , A61K31/444 , A61P11/06 , A61P25/00 , A61P35/00 , C12N9/99 , A61K31/4439
CPC分类号： C07D401/06 , C07D401/14
摘要： The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译： 本公开涉及式I的环脲化合物：如本文所定义，其制备方法，包含其的药物组合物及其作为蛋白激酶上的抑制剂的药物用途。 因此，式I化合物可用于预防或治疗能够通过抑制蛋白激酶如实体瘤的活性而被调节的生理障碍。
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