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1.发明申请QUINUCLIDINE DERIVATIVES AND THEIR USE AS MUSCARINIC M3 RECEPTOR ANTAGONISTS 失效喹啉衍生物及其作为MUSCARINIC M3受体拮抗剂的用途公开(公告)号：US20100168132A1
公开(公告)日：2010-07-01
申请号：US12721897
申请日：2010-03-11
申请人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungshul Kim , Dimitris Papoutsakis , Simon James Watson
发明人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungshul Kim , Dimitris Papoutsakis , Simon James Watson
IPC分类号： A61K31/439 , C07D453/00 , C07D401/14 , A61K31/497 , A61K31/506 , C07D409/14 , A61P29/00
CPC分类号： C07D453/02
摘要： Compounds of Formula (I) ; in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译： 式（I）化合物; 盐或两性离子形式，其中R 1，R 2，R 3和R 4具有说明书中指出的含义，可用于治疗由毒蕈碱M3受体介导的病症，特别是炎性或阻塞性气道疾病。 还描述了含有化合物的药物组合物和制备该化合物的方法。
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2.发明授权Quinuclidine derivatives and their use as muscarinic m3 receptor antagonists 有权奎宁环衍生物及其作为毒蕈碱咪唑受体拮抗剂的用途公开(公告)号：US07723356B2
公开(公告)日：2010-05-25
申请号：US11577417
申请日：2005-10-31
申请人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon James Watson
发明人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon James Watson
IPC分类号： A61K31/44
CPC分类号： C07D453/02
摘要： Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译： 式（I）化合物; 盐或两性离子形式，其中R 1，R 2，R 3和R 4具有说明书中指出的含义，可用于治疗由毒蕈碱M3受体介导的病症，特别是炎性或阻塞性气道疾病。 还描述了含有化合物的药物组合物和制备该化合物的方法。
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公开(公告)号：US20090048281A1
公开(公告)日：2009-02-19
申请号：US11577417
申请日：2005-10-31
申请人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon James Watson
发明人： Neil John Press , Stephen Paul Collingwood , Urs Baettig , Brian Cox , Sudhakar Devidasrao Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon James Watson
IPC分类号： C07D453/02 , A61K31/439 , A61K31/506 , A61P29/00 , A61P11/00
CPC分类号： C07D453/02
摘要： Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译： 式（I）化合物; 盐或两性离子形式，其中R 1，R 2，R 3和R 4具有说明书中指出的含义，可用于治疗由毒蕈碱M3受体介导的病症，特别是炎性或阻塞性气道疾病。 还描述了含有化合物的药物组合物和制备该化合物的方法。
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4.发明授权Quinuclidine derivatives and their use as muscarinic M3 receptor antagonists 失效奎宁环衍生物及其作为毒蕈碱M3受体拮抗剂的用途公开(公告)号：US08084463B2
公开(公告)日：2011-12-27
申请号：US12721897
申请日：2010-03-11
申请人： Neil J Press , Stephen P Collingwood , Urs Baettig , Brian Cox , Sudhakar D Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon J Watson
发明人： Neil J Press , Stephen P Collingwood , Urs Baettig , Brian Cox , Sudhakar D Garad , Hyungchul Kim , Dimitris Papoutsakis , Simon J Watson
IPC分类号： A61K31/44
CPC分类号： C07D453/02
摘要： Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译： 式（I）化合物; 盐或两性离子形式，其中R 1，R 2，R 3和R 4具有说明书中指出的含义，可用于治疗由毒蕈碱M3受体介导的病症，特别是炎性或阻塞性气道疾病。 还描述了含有化合物的药物组合物和制备该化合物的方法。
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![Polymorphic form of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic](/abs-image/US/2012/05/08/US08173634B2/abs.jpg.150x150.jpg)
5.发明授权Polymorphic form of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic 有权1-（4- {1 - [（E）-4-环己基-3-三氟甲基 - 苄氧亚氨基] - 乙基} -2-乙基 - 苄基） - 氮杂环丁烷-3-羧酸的多晶型公开(公告)号：US08173634B2
公开(公告)日：2012-05-08
申请号：US13140453
申请日：2009-12-17
IPC分类号： A61K31/397 , C07D205/04
CPC分类号： C07D205/04
摘要： This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment.
摘要翻译： 本发明涉及1-（4- {1 - [（E）-4-环己基-3-三氟甲基 - 苄氧基亚氨基] - 乙基} -2-乙基 - 苄基） - 氮杂环丁烷-3的新型结晶形式（A型） - 羧酸（化合物I），包含该结晶形式的药物组合物，其形成方法及其在医疗中的应用。
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公开(公告)号：US20100093749A1
公开(公告)日：2010-04-15
申请号：US12529943
申请日：2008-03-06
IPC分类号： A61K31/517 , C07D403/14 , A61P37/06 , A61P37/00 , A61P29/00
CPC分类号： C07D403/14
摘要： The invention provides acid addition salts of 3-(1.H.-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-pyrrole-2,5-dione, crystalline forms thereof, processes for the preparation thereof, pharmaceutical compositions comprising them and uses thereof in therapeutic treatment.
摘要翻译： 本发明提供了3-（1H-吲哚-3-基）-4- [2-（4-甲基 - 哌嗪-1-基） - 喹唑啉-4-基] - 吡咯-2-甲酸的酸加成盐， 5-二酮，其结晶形式，其制备方法，包含它们的药物组合物及其在治疗性治疗中的用途。
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![Crystal modifications-3-(1H-indol-3-yl)-4- [4-methyl-piperazin-1-yl)-quinazolin-4-yl] -pyrrole-2, 5-D ione](/abs-image/US/2014/10/21/US08865897B2/abs.jpg.150x150.jpg)
7.发明授权Crystal modifications-3-(1H-indol-3-yl)-4- [4-methyl-piperazin-1-yl)-quinazolin-4-yl] -pyrrole-2, 5-D ione 有权晶体修饰3-（1H-吲哚-3-基）-4- [4-甲基 - 哌嗪-1-基） - 喹唑啉-4-基] - 吡咯-2,5-D离子公开(公告)号：US08865897B2
公开(公告)日：2014-10-21
申请号：US12445371
申请日：2007-10-18
IPC分类号： C07D403/14
CPC分类号： C07D403/14
摘要： The invention relates to a new crystalline form of the acetate salt of which may be used, for example, for prevention or treatment of transplant rejection.
摘要翻译： 本发明涉及一种新的乙酸盐结晶形式，其可用于例如预防或治疗移植排斥反应。
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8.发明申请NEW POLYMORPHIC FORM OF 1-(4--2-ETHYL-BENZYL)-AZETIDINE-3-CARBOXYLIC 有权1-（4-（2-乙基苯基） - 苯并三唑-3-羧酸的新型多晶型公开(公告)号：US20110251170A1
公开(公告)日：2011-10-13
申请号：US13140453
申请日：2009-12-17
IPC分类号： A61K31/397 , A61P37/06 , A61P35/00 , C07D205/04
CPC分类号： C07D205/04
摘要： This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment.
摘要翻译： 本发明涉及1-（4- {1 - [（E）-4-环己基-3-三氟甲基 - 苄氧基亚氨基] - 乙基} -2-乙基 - 苄基） - 氮杂环丁烷-3的新型结晶形式（A型） - 羧酸（化合物I），包含该结晶形式的药物组合物，其形成方法及其在医疗中的应用。
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![Salts of N-Hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide](/abs-image/US/2011/05/12/US20110112308A1/abs.jpg.150x150.jpg)
9.发明申请Salts of N-Hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide 审中-公开N-羟基-3- [4 - [[[2-（2-甲基-1H-吲哚-3-基）乙基]氨基]甲基]苯基] -2E-2-丙烯酰胺的盐公开(公告)号：US20110112308A1
公开(公告)日：2011-05-12
申请号：US13006485
申请日：2011-01-14
申请人： Murat Acemoglu , Joginder S. Bajwa , Piotr Karpinski , Dimitris Papoutsakis , Joel Slade , Frank Stowasser
发明人： Murat Acemoglu , Joginder S. Bajwa , Piotr Karpinski , Dimitris Papoutsakis , Joel Slade , Frank Stowasser
IPC分类号： C07D209/14
CPC分类号： C07D209/14
摘要： Salts of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide are prepared and characterized.
摘要翻译： 制备N-羟基-3- [4 - [[[2-（2-甲基-1H-吲哚-3-基）乙基]氨基]甲基]苯基] -2E-2-丙烯酰胺的盐。
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![Polymorphs of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide](/abs-image/US/2011/08/02/US07989494B2/abs.jpg.150x150.jpg)
10.发明授权Polymorphs of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide 有权N-羟基-3- [4 - [[[2-（2-甲基-1H-吲哚-3-基）乙基]氨基]甲基]苯基] -2E-2-丙烯酰胺的多晶型物公开(公告)号：US07989494B2
公开(公告)日：2011-08-02
申请号：US12302564
申请日：2007-06-07
申请人： Murat Acemoglu , Joginder S. Bajwa , Piotr Karpinski , Dimitris Papoutsakis , Joel Slade , Frank Stowasser
发明人： Murat Acemoglu , Joginder S. Bajwa , Piotr Karpinski , Dimitris Papoutsakis , Joel Slade , Frank Stowasser
IPC分类号： A61K31/404 , C07D209/10 , C07D209/12 , C07D209/14
CPC分类号： C07D209/16 , C07D209/14 , C07D209/20
摘要： Polymorphic forms of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide free base and salts thereof are prepared by various processes.
摘要翻译： N-羟基-3- [4 - [[[2-（2-甲基-1H-吲哚-3-基）乙基]氨基]甲基]苯基] -2E-2-丙烯酰胺游离碱及其盐的多晶型形式为 由各种过程准备。
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