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公开(公告)号:US20050009887A1
公开(公告)日:2005-01-13
申请号:US10911361
申请日:2004-08-04
申请人: Chris Senanayake , Gerald Tanoury , Harold Wilkinson , Roger Bakale , Andrei Zlota , Kostas Saranteas
发明人: Chris Senanayake , Gerald Tanoury , Harold Wilkinson , Roger Bakale , Andrei Zlota , Kostas Saranteas
IPC分类号: A61K31/4422 , A61P9/10 , A61P9/12 , C07D211/90 , C07D211/82
CPC分类号: C07D211/90
摘要: The invention relates to methods of resolving racemic amlodipine into enantiomerically enriched compositions by precipitation with tartaric acid in the presence of a non-aqueous solvent, such as N,N′-dimethylacetamide. The molar ratio of tartaric acid:amlodipine is preferably less than 0.25:1.0 or greater than 0.75:1.0.
摘要翻译: 本发明涉及通过在非水溶剂如N,N'-二甲基乙酰胺的存在下用酒石酸沉淀来将外消旋氨氯地平拆分成对映异构体富集的组合物的方法。 酒石酸:氨氯地平的摩尔比优选小于0.25:1.0或大于0.75:1.0。
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公开(公告)号:US20060035940A1
公开(公告)日:2006-02-16
申请号:US11082253
申请日:2005-03-16
申请人: Sharon Laughlin , Roger Bakale , Harold Wilkinson , Andrei Zlota
发明人: Sharon Laughlin , Roger Bakale , Harold Wilkinson , Andrei Zlota
IPC分类号: C07D211/82 , A61K31/455
CPC分类号: A61K31/455 , C07D211/90
摘要: One aspect of the present invention relates to optically pure (S)-amlodipine malate. Another aspect of the present invention relates to (rac)-amlodipine malate. In a preferred embodiment, the compound is optically pure (S)-amlodipine L-malate. Another aspect of the present invention relates to a pharmaceutical composition comprising optically pure (S)-amlodipine malate. Another aspect of the present invention relates to a method of preparing optically pure (S)-amlodipine malate, comprising admixing optically pure (S)-amlodipine with malic acid. Another aspect of the present invention relates to the various polymorphic and solvated forms of optically pure (S)-amlodipine malate. In another prefered embodiment the invention relates to polymorphic and solvated forms A-G. The present invention also relates to a method of preparing optically pure (S)-amlodipine malate, comprising combining a salt of optically pure (S)-amlodipine with a malate salt to give optically pure (S)-amlodipine malate. In a preferred embodiment, the malate salt is an optically pure L-malate salt.
摘要翻译: 本发明的一个方面涉及光学纯的(S) - 麦草碱苹果酸盐。 本发明的另一方面涉及(外消旋) - 苹果酸麦草碱。 在优选的实施方案中,该化合物是光学纯的(S) - 氨氯地平L-苹果酸盐。 本发明的另一方面涉及一种药物组合物,其包含光学上纯的(S) - 氨氯地平苹果酸盐。 本发明的另一方面涉及一种制备旋光纯(S) - 马洛替灵苹果酸盐的方法,其包括将旋光纯(S) - 氨氯地平与苹果酸混合。 本发明的另一方面涉及光学纯(S) - 氨氯地平苹果酸盐的各种多晶型和溶剂化形式。 在另一个优选的实施方案中,本发明涉及多晶型和溶剂化形式A-G。 本发明还涉及一种制备光学纯的(S) - 氨氯地平苹果酸盐的方法,其包括将光学纯的(S) - 氨氯地平的盐与苹果酸盐组合以得到光学纯的(S) - 氨氯地平苹果酸盐。 在优选的实施方案中,苹果酸盐是光学上纯的L-苹果酸盐。
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公开(公告)号:US20060030602A1
公开(公告)日:2006-02-09
申请号:US11082252
申请日:2005-03-16
申请人: Sharon Laughlin , Roger Bakale , Harold Wilkinson , Andrei Zlota
发明人: Sharon Laughlin , Roger Bakale , Harold Wilkinson , Andrei Zlota
IPC分类号: A61K31/455
CPC分类号: A61K31/455 , C07D211/90
摘要: One aspect of the present invention relates to optically pure (S)-amlodipine malate. Another aspect of the present invention relates to (rac)-amlodipine malate. In a preferred embodiment, the compound is optically pure (S)-amlodipine L-malate. Another aspect of the present invention relates to a pharmaceutical composition comprising optically pure (S)-amlodipine malate. Another aspect of the present invention relates to a method of preparing optically pure (S)-amlodipine malate, comprising admixing optically pure (S)-amlodipine with malic acid. Another aspect of the present invention relates to the various polymorphic and solvated forms of optically pure (S)-amlodipine malate. In another prefered embodiment the invention relates to polymorphic and solvated forms A-G. The present invention also relates to a method of preparing optically pure (S)-amlodipine malate, comprising combining a salt of optically pure (S)-amlodipine with a malate salt to give optically pure (S)-amlodipine malate. In a preferred embodiment, the malate salt is an optically pure L-malate salt.
摘要翻译: 本发明的一个方面涉及光学纯的(S) - 麦草碱苹果酸盐。 本发明的另一方面涉及(外消旋) - 苹果酸麦草碱。 在优选的实施方案中,该化合物是光学纯的(S) - 氨氯地平L-苹果酸盐。 本发明的另一方面涉及一种药物组合物,其包含光学上纯的(S) - 氨氯地平苹果酸盐。 本发明的另一方面涉及一种制备旋光纯(S) - 马洛替灵苹果酸盐的方法,其包括将旋光纯(S) - 氨氯地平与苹果酸混合。 本发明的另一方面涉及光学纯(S) - 氨氯地平苹果酸盐的各种多晶型和溶剂化形式。 在另一个优选的实施方案中,本发明涉及多晶型和溶剂化形式A-G。 本发明还涉及一种制备光学纯的(S) - 氨氯地平苹果酸盐的方法,其包括将光学纯的(S) - 氨氯地平的盐与苹果酸盐组合以得到光学纯的(S) - 氨氯地平苹果酸盐。 在优选的实施方案中,苹果酸盐是光学上纯的L-苹果酸盐。
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公开(公告)号:US07256310B2
公开(公告)日:2007-08-14
申请号:US10728873
申请日:2003-12-08
申请人: Paul McGlynn , Roger Bakale , Craig Sturge
发明人: Paul McGlynn , Roger Bakale , Craig Sturge
IPC分类号: C07C215/00 , C07C205/00
CPC分类号: C07C215/60 , A61K9/008 , A61K9/14 , A61K31/205 , A61M15/002 , A61M15/009 , A61M2202/0484 , A61M2202/0488 , A61M2202/064 , C07B2200/07 , C07B2200/13 , C07C59/255 , C09K3/30
摘要: Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
摘要翻译: 莱伐珠特醇L-酒石酸盐提供具有期望用于计量剂量吸入器的性质的晶体。
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公开(公告)号:US20060025418A1
公开(公告)日:2006-02-02
申请号:US11229699
申请日:2005-09-20
申请人: Thomas Jerussi , Chrisantha Senanayake , Paul Rubin , Yaping Hong , Roger Bakale , Tingjian Xiang , Fran McConville
发明人: Thomas Jerussi , Chrisantha Senanayake , Paul Rubin , Yaping Hong , Roger Bakale , Tingjian Xiang , Fran McConville
IPC分类号: A61K31/498
CPC分类号: A61K31/4985 , A61K31/498 , C07B2200/07 , C07D487/04
摘要: The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (+)-N-desmethylzopiclone, and optically pure (−)-N-desmethylzopiclone.
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公开(公告)号:US20130028845A1
公开(公告)日:2013-01-31
申请号:US13633801
申请日:2012-10-02
申请人: Paul McGlynn , Roger Bakale , Craig Sturge
发明人: Paul McGlynn , Roger Bakale , Craig Sturge
IPC分类号: A61K31/137 , A61P11/06 , A61P11/00 , A61K9/12
CPC分类号: C07C215/60 , A61K9/008 , A61K9/14 , A61K31/205 , A61M15/002 , A61M15/009 , A61M2202/0484 , A61M2202/0488 , A61M2202/064 , C07B2200/07 , C07B2200/13 , C07C59/255 , C09K3/30
摘要: Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
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公开(公告)号:US20100272654A1
公开(公告)日:2010-10-28
申请号:US12833882
申请日:2010-07-09
申请人: Paul McGlynn , Roger Bakale , Craig Sturge
发明人: Paul McGlynn , Roger Bakale , Craig Sturge
IPC分类号: A61K9/12 , A61K31/138 , A61P11/00
CPC分类号: C07C215/60 , A61K9/008 , A61K9/14 , A61K31/205 , A61M15/002 , A61M15/009 , A61M2202/0484 , A61M2202/0488 , A61M2202/064 , C07B2200/07 , C07B2200/13 , C07C59/255 , C09K3/30
摘要: Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
摘要翻译: 莱伐珠特醇L-酒石酸盐提供具有期望用于计量剂量吸入器的性质的晶体。
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公开(公告)号:US20080119564A1
公开(公告)日:2008-05-22
申请号:US11891048
申请日:2007-08-08
申请人: Paul McGlynn , Roger Bakale , Craig Sturge
发明人: Paul McGlynn , Roger Bakale , Craig Sturge
IPC分类号: A61K31/137 , C07C215/00
CPC分类号: C07C215/60 , A61K9/008 , A61K9/14 , A61K31/205 , A61M15/002 , A61M15/009 , A61M2202/0484 , A61M2202/0488 , A61M2202/064 , C07B2200/07 , C07B2200/13 , C07C59/255 , C09K3/30
摘要: Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
摘要翻译: 莱伐珠特醇L-酒石酸盐提供具有期望用于计量剂量吸入器的性质的晶体。
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