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公开(公告)号:EP1424321B1
公开(公告)日:2006-07-05
申请号:EP03104950.5
申请日:1999-10-22
申请人: SEPRACOR Inc
发明人: BAKALE, Roger, P. , LOPEZ, Jorge, L , McCONVILLE, Francis, X , VANDENBOSSCHE, Charles, P , SENANAYAKE, Chris, Hugh
IPC分类号: C07C51/487 , C07C59/54 , C07C67/12 , C07C213/06 , C07C219/20 , C07C69/96
CPC分类号: C07C69/96 , C07B2200/07 , C07C51/487 , C07C67/12 , C07C68/02 , C07C213/06 , C07C219/20 , C07C229/36 , C07C2601/14 , C07C59/54 , C07C69/732
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公开(公告)号:EP1082293B1
公开(公告)日:2004-02-18
申请号:EP99968848.4
申请日:1999-05-20
申请人: Sepracor Inc.
发明人: GAO, Yun , FANG, Kevin, Q. , HETT, Robert , REDMON, Martin, P. , SENANAYAKE, Chris, Hugh , WALD, Stephen, Alan
IPC分类号: C07C233/43 , A61K31/16
CPC分类号: C07C205/37 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/008 , C07C205/45 , C07C217/86 , C07C233/25 , C07C233/43
摘要: A method is disclosed for the preparation of optically pure isomers of formoterol and polymorphs of the novel L-tartrate salt of R,R-formoterol. Pharmaceutical compositions of the polymorphs and salts are also described.
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公开(公告)号:EP1424321A1
公开(公告)日:2004-06-02
申请号:EP03104950.5
申请日:1999-10-22
申请人: Sepracor, Inc.
发明人: BAKALE, Roger, P. , LOPEZ, Jorge, L , McCONVILLE, Francis, X , VANDENBOSSCHE, Charles, P , SENANAYAKE, Chris, Hugh
IPC分类号: C07C51/487 , C07C59/54 , C07C67/12 , C07C213/06 , C07C219/20 , C07C69/96
CPC分类号: C07C69/96 , C07B2200/07 , C07C51/487 , C07C67/12 , C07C68/02 , C07C213/06 , C07C219/20 , C07C229/36 , C07C2601/14 , C07C59/54 , C07C69/732
摘要: A process for the preparation of optically active cyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R) - or (S) -cyclohexylphenylglycolic acid (CHPGA) with 4- N , N -diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described.
摘要翻译: 描述了制备旋光环己基羟基乙酸酯的方法。 该方法利用羧酸活化将(R) - 或(S) - 环己基苯基乙醇酸(CHPGA)与4-N,N-二乙基氨基丁炔醇或其它炔丙醇衍生物偶联。 还描述了盐酸盐的制备。
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公开(公告)号:EP0956286B1
公开(公告)日:2003-04-02
申请号:EP98901831.2
申请日:1998-01-20
申请人: SEPRACOR, INC.
IPC分类号: C07D317/30 , C07D317/22 , C07D317/20 , C07D211/22 , C07D211/34 , C07D307/20 , C07C69/612 , C07C69/738
CPC分类号: C07D317/20 , C07C69/76 , C07D211/22 , C07D211/34 , C07D307/20 , C07D317/22 , C07D317/30
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公开(公告)号:EP1176952A2
公开(公告)日:2002-02-06
申请号:EP00930158.1
申请日:2000-04-26
申请人: Sepracor Inc.
IPC分类号: A61K31/00 , A61K31/496
CPC分类号: A61K31/675 , A61K9/2031 , A61K31/495 , A61K31/496 , A61K2300/00
摘要: A method of treating fungal infections with a mixture of isomers of 2R,4S-hydroxyitraconazole and their sulfate and phosphate derivatives is disclosed. Pharmaceutical compositions containing these compounds are also disclosed.
摘要翻译: 公开了用2R,4S-羟基伊曲康唑及其硫酸盐和磷酸盐衍生物的异构体混合物治疗真菌感染的方法。 还公开了含有这些化合物的药物组合物。
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公开(公告)号:EP1082293A2
公开(公告)日:2001-03-14
申请号:EP99968848.4
申请日:1999-05-20
申请人: Sepracor Inc.
发明人: GAO, Yun , FANG, Kevin, Q. , HETT, Robert , REDMON, Martin, P. , SENANAYAKE, Chris, Hugh , WALD, Stephen, Alan
IPC分类号: C07C233/43 , A61K31/16
CPC分类号: C07C205/37 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/008 , C07C205/45 , C07C217/86 , C07C233/25 , C07C233/43
摘要: A method is disclosed for the preparation of optically pure isomers of formoterol and polymorphs of the novel L-tartrate salt of R,R-formoterol. Pharmaceutical compositions of the polymorphs and salts are also described.
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公开(公告)号:EP0956286A1
公开(公告)日:1999-11-17
申请号:EP98901831.0
申请日:1998-01-20
申请人: SEPRACOR, INC.
CPC分类号: C07D317/20 , C07C69/76 , C07D211/22 , C07D211/34 , C07D307/20 , C07D317/22 , C07D317/30
摘要: Processes for preparing compounds having general formula (1), wherein R1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of general formula (II), and elaborate the product by reductive amination of an aldehyde of formula (IVa) with α,α-diphenyl-4-piperidinemethanol.
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公开(公告)号:EP1093450B1
公开(公告)日:2003-04-23
申请号:EP99930556.8
申请日:1999-06-22
申请人: Sepracor Inc.
IPC分类号: C07C215/78 , C07C213/02 , A61K31/135
CPC分类号: C07C213/04 , C07B2200/07 , C07C217/60 , C07C217/70
摘要: The (R, R) -, (S, S) -, (R, S) -, ($I(R, S)) - isomers of 3 - amino- 4- hydroxy-α- [[[2- (4- methoxyphenyl)- 1-methylethyl]amino]methyl] -benzenemethanol (D) are disclosed, as well as an efficient method for their stereoselective synthesis. A method and composition are also disclosed utilizing desformoterol (D) as a bronchodilator, having high selectivity for β2 receptors.
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公开(公告)号:EP1093450A1
公开(公告)日:2001-04-25
申请号:EP99930556.8
申请日:1999-06-22
申请人: Sepracor Inc.
IPC分类号: C07C215/78 , C07C213/02 , A61K31/135
CPC分类号: C07C213/04 , C07B2200/07 , C07C217/60 , C07C217/70
摘要: The (R, R) -, (S, S) -, (R, S) -, ($I(R, S)) - isomers of 3 - amino- 4- hydroxy-α- [[[2- (4- methoxyphenyl)- 1-methylethyl]amino]methyl] -benzenemethanol (D) are disclosed, as well as an efficient method for their stereoselective synthesis. A method and composition are also disclosed utilizing desformoterol (D) as a bronchodilator, having high selectivity for β2 receptors.
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