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公开(公告)号：US08673978B2
公开(公告)日：2014-03-18
申请号：US13078039
申请日：2011-04-01
IPC分类号： A61K31/192 , A61P25/28 , C07C61/40
CPC分类号： A61K31/192 , A61K9/0053 , C07B2200/13 , C07C61/40 , C07C229/26 , C07C279/14 , C07C2601/02
摘要： Novel polymorphic forms and salts of 1-(3′,4′-dichloro-2-fluorobiphenyl-4-yl)cyclopropanecarboxylic acid are useful for the prevention or treatment of Alzheimer's Disease.
摘要翻译： 1-（3'，4'-二氯-2-氟联苯-4-基）环丙烷羧酸的新型多晶型物和盐可用于预防或治疗阿尔茨海默氏病。
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公开(公告)号：US20110245346A1
公开(公告)日：2011-10-06
申请号：US13078039
申请日：2011-04-01
IPC分类号： A61K31/192 , C07C61/40 , A61P25/28
CPC分类号： A61K31/192 , A61K9/0053 , C07B2200/13 , C07C61/40 , C07C229/26 , C07C279/14 , C07C2601/02
摘要： Novel polymorphic forms and salts of 1-(3′,4′-dichloro-2-fluorobiphenyl-4-yl)cyclopropanecarboxylic acid are useful for the prevention or treatment of Alzheimer's Disease.
摘要翻译： 1-（3'，4'-二氯-2-氟联苯-4-基）环丙烷羧酸的新型多晶型物和盐可用于预防或治疗阿尔茨海默病。
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3.发明申请Pharmaceutical aerosol formulations for pressurized metered dose inhalers comprising a sequestering agent 有权用于加压计量剂量吸入器的药物气溶胶制剂，其包含螯合剂公开(公告)号：US20060193785A1
公开(公告)日：2006-08-31
申请号：US11361562
申请日：2006-02-24
申请人： David Lewis , Brian Meakin , Maurizio Delcanale , Fausto Pivetti
发明人： David Lewis , Brian Meakin , Maurizio Delcanale , Fausto Pivetti
IPC分类号： A61K31/573 , A61K31/4704 , A61L9/04
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/573 , A61K31/58 , A61K47/02
摘要： Aerosol solution formulation for use in an aerosol inhaler which includes at least one active ingredient selected from 20-ketosteroids and quinolinone derivatives, a propellant containing a hydrofluoroalkane, a cosolvent, and a specific amount of a sequestering agent that stabilizes the formulation. By way of example, the stabilizing agent may be phosphoric acid or sulphuric acid.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含至少一种选自20-酮类和喹啉酮衍生物的活性成分，含有氢氟烷烃的助推剂，助溶剂和稳定该制剂的特定量的螯合剂。 举例来说，稳定剂可以是磷酸或硫酸。
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![Process for the preparation of 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride](/abs-image/US/2012/04/24/US08163922B2/abs.jpg.150x150.jpg)
4.发明授权Process for the preparation of 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride 有权制备8-羟基-5 - [（1R）-1-羟基-2 [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮的方法 一盐酸盐公开(公告)号：US08163922B2
公开(公告)日：2012-04-24
申请号：US12512187
申请日：2009-07-30
IPC分类号： C07D215/38
CPC分类号： C07D215/26
摘要： 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride of formula (I) may be conveniently prepared in a diastereomeric pure form from optically pure precursors that are readily available by simple resolution and asymmetric reduction.
摘要翻译： （I）的8-羟基-5 - [（1R）-1-羟基-2 [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮一盐酸盐 ）可以以通过简单拆分和不对称还原容易获得的光学纯前体的非对映体纯形式方便地制备。
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5.发明授权Process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity 失效制备具有选择性脑抗胆碱酯酶活性的赖烯罗林的氨基羰基衍生物的方法公开(公告)号：US06297237B1
公开(公告)日：2001-10-02
申请号：US09319693
申请日：1999-08-02
申请人： Paolo Chiesi , Paolo Ventura , Vittorino Servadio , Roberto Pighi , Fausto Pivetti , Bluetta Salsi , Maurizio Delcanale , Gabriele Amari , Claudio Pietra
发明人： Paolo Chiesi , Paolo Ventura , Vittorino Servadio , Roberto Pighi , Fausto Pivetti , Bluetta Salsi , Maurizio Delcanale , Gabriele Amari , Claudio Pietra
IPC分类号： A61K315365
CPC分类号： C07D498/04 , Y02P20/55
摘要： A process for the preparation of compounds of formula (I), wherein R is C2-C20 linear or branched alkyl, C3-C7 cycloalkyl, phenyl or benzyl, which can optionally be substituted by C1-C4 alkyl, halogen or C1-C4 alkoxy group, said process comprising: a) oxidation of eserine with hydrogen peroxide in the presence of a base and subsequent hydrolysis to geneseroline, without isolating the intermediate geneserine; b) acylation of geneseroline with an isocyanate of formula R—N═C═O, wherein R is as defined above, in the presence of a basic catalyst; c) optional transformation into a pharmaceutically acceptable salt. Compounds of formula (I) wherein R is a phenyl or benzyl, which can be optionally substituted by alkyl, halogen or alkoxy, are selective, potent brain anticholinesterase inhibitors.
摘要翻译： 制备式（I）化合物的方法，其中R是C2-C20直链或支链烷基，C3-C7环烷基，苯基或苄基，其可任选被C 1 -C 4烷基，卤素或C 1 -C 4烷氧基 所述方法包括：a）在碱的存在下用过氧化氢氧化埃乐林，然后在不分离中间生物素的情况下水解成基因异烯; b）在碱性催化剂的存在下，用式R-N = C = O的异氰酸酯，其中R如上定义， c）任选转化成药学上可接受的盐。 其中R为苯基或苄基的式（I）化合物，其可任选被烷基，卤素或烷氧基取代，是选择性有效的脑抗胆碱酯酶抑制剂。
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6.发明授权Pharmaceutical aerosol formulations for pressurized metered dose inhalers comprising a sequestering agent 有权用于加压计量剂量吸入器的药物气溶胶制剂，其包含螯合剂公开(公告)号：US08877164B2
公开(公告)日：2014-11-04
申请号：US11361562
申请日：2006-02-24
IPC分类号： A61K31/573 , A61K47/04 , A61K47/02 , A61K9/12 , A61K9/72 , A61K31/58 , A61K31/4704 , A61K9/00
CPC分类号： A61K9/008 , A61K31/4704 , A61K31/573 , A61K31/58 , A61K47/02
摘要： Aerosol solution formulation for use in an aerosol inhaler which includes at least one active ingredient selected from 20-ketosteroids and quinolinone derivatives, a propellant containing a hydrofluoroalkane, a cosolvent, and a specific amount of a sequestering agent that stabilizes the formulation. By way of example, the stabilizing agent may be phosphoric acid or sulphuric acid.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含至少一种选自20-酮类和喹啉酮衍生物的活性成分，含有氢氟烷烃的助推剂，助溶剂和稳定该制剂的特定量的螯合剂。 举例来说，稳定剂可以是磷酸或硫酸。
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![PROCESS FOR THE PREPARATION OF 8-HYDROXY-5-[(1R)-1-HYDROXY-2[[(1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-2(1H)-QUINOLINONE MONOHYDROCHLORIDE](/abs-image/US/2009/12/31/US20090326231A1/abs.jpg.150x150.jpg)
7.发明申请PROCESS FOR THE PREPARATION OF 8-HYDROXY-5-[(1R)-1-HYDROXY-2[[(1R)-2-(4-METHOXYPHENYL)-1-METHYLETHYL]AMINO]ETHYL]-2(1H)-QUINOLINONE MONOHYDROCHLORIDE 有权制备8-羟基-5 - [（1R）-1-羟基-2 [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮的方法 MONOHYDROCHLORIDE公开(公告)号：US20090326231A1
公开(公告)日：2009-12-31
申请号：US12512187
申请日：2009-07-30
IPC分类号： C07D215/227
CPC分类号： C07D215/26
摘要： 8-hydroxy-5-[(1R)-1-hydroxy-2[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone monohydrochloride of formula (I) may be conveniently prepared in a diastereomeric pure form from optically pure precursors that are readily available by simple resolution and asymmetric reduction.
摘要翻译： （I）的8-羟基-5 - [（1R）-1-羟基-2 [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮一盐酸盐 ）可以以通过简单拆分和不对称还原容易获得的光学纯前体的非对映体纯形式方便地制备。
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8.发明授权Stable pharmaceutical solution formulations for pressurized metered dose inhalers 失效用于加压计量剂量吸入器的稳定的药物溶液制剂公开(公告)号：US07381402B2
公开(公告)日：2008-06-03
申请号：US11065569
申请日：2005-02-25
IPC分类号： A61K9/12 , A61K9/08 , A61K31/47 , A61K31/4704 , A61M11/00 , A61M11/04 , A61M15/00 , A61M15/06
CPC分类号： A61K9/008 , A61K31/137 , A61K31/47 , A61K31/4704 , A61K47/02 , A61M15/009 , A61M2205/0222 , A61K2300/00
摘要： Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]-ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid exhibit improved shelf life. The formulation may be optionally contained in a can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基] - 乙基 ] -2（1H） - 喹啉酮或其盐，特别是盐酸盐（TA 2005）作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度 磷酸表现出改善的保质期。 制剂可以任选地包含在其内部具有惰性有机涂层的部分或全部内部金属表面的罐中。
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9.发明申请Stable Pharmaceutical Solution Formulations for Pressurized Metered Dose Inhalers 审中-公开用于加压计量吸入器的稳定的药物溶液制剂公开(公告)号：US20070025920A1
公开(公告)日：2007-02-01
申请号：US11467515
申请日：2006-08-25
IPC分类号： A61L9/04 , A61K31/4704
CPC分类号： A61K31/4704 , A61K9/008 , A61K47/02 , A61M15/009
摘要： Aerosol solution formulations for use in an aerosol inhaler include 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methyl ethyl]amino]ethyl]-2(1H)-quinolinone or a salt thereof, preferably the hydrochloride thereof, as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid and optionally by the use of a suitable can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂包括8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基]乙基] -2（1H） - 喹啉酮或其盐，优选其盐酸盐作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度磷酸和任选地通过 使用合适的罐，其具有内部具有惰性有机涂层的部分或全部内部金属表面。
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10.发明申请Stable pharmaceutical solution formulations for pressurized metered dose inhalers 失效用于加压计量剂量吸入器的稳定的药物溶液制剂公开(公告)号：US20050220718A1
公开(公告)日：2005-10-06
申请号：US11065569
申请日：2005-02-25
CPC分类号： A61K9/008 , A61K31/137 , A61K31/47 , A61K31/4704 , A61K47/02 , A61M15/009 , A61M2205/0222 , A61K2300/00
摘要： Aerosol solution formulations for use in an aerosol inhaler which comprise 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]-ethyl]-2(1H)-quinolinone or a salt thereof, in particular the hydrochloride salt (TA 2005), as an active ingredient, a propellant containing a hydrofluoroalkane, and a cosolvent, stabilized by addition of a specific small amount of a high concentrated phosphoric acid exhibit improved shelf life. The formulation may be optionally contained in a can having part or all of its internal metallic surfaces lined with an inert organic coating.
摘要翻译： 用于气溶胶吸入器的气溶胶溶液制剂，其包含8-羟基-5 - [（1R）-1-羟基-2 - [[（1R）-2-（4-甲氧基苯基）-1-甲基乙基]氨基] - 乙基 ] -2（1H） - 喹啉酮或其盐，特别是盐酸盐（TA 2005）作为活性成分，含有氢氟烷烃和助溶剂的推进剂，通过加入特定量的高浓度 磷酸表现出改善的保质期。 制剂可以任选地包含在其内部具有惰性有机涂层的部分或全部内部金属表面的罐中。
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