公开(公告)号：WO1994007476A1

公开(公告)日：1994-04-14

申请号：PCT/US1993009463

申请日：1993-10-05

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  BARBERICH, Timothy, J. ,  YOUNG, James, W.

IPC: A61K31/04

CPC classification number: A61K31/44

Abstract: Methods and compositions are disclosed utilizing the optically pure S(-) isomer of nitrendipine. This compound is a potent drug for the treament of hypertension while avoiding the concomitant liability of adverse effects associated with the administration of the racemic mixture of nitrendipine. The S(-) isomer of nitrendipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(-) nitrendipine as a calcium channel antagonist without the concomitant liability of adverse effects associated with the racemic mixture of nitrendipine.

Abstract translation: 公开利用尼群地平的光学纯的S（ - ）异构体的方法和组合物。 该化合物是高血压治疗的有效药物，同时避免与施用尼群地平的外消旋混合物相关的副作用的伴随责任。 尼群地平的S（ - ）异构体也可用于治疗心绞痛和其他可能与作为钙通道拮抗剂的S（ - ）尼群地平的活性有关的其他病症，而与外消旋混合物有关的不良反应的伴随责任 尼群地平。

公开(公告)号：WO1993010787A1

公开(公告)日：1993-06-10

申请号：PCT/US1992010631

申请日：1992-12-01

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  YOUNG, James, W. ,  BRANDT, Steven

IPC: A61K31/50

CPC classification number: A61K31/495

Abstract: Methods and compositions are disclosed utilizing the optically pure (+) isomer of zopiclone. This compound is a potent drug for the treatment of sleep disorders, such as insomnia, and convulsive disorders, such as epilepsy. Similarly, these novel compositions and methods are useful for the treatment of sleep disorders and convulsive disorders while avoiding the concomitant liability of adverse effects associated with the racemic mixture of zopiclone. The optically pure (+) isomer of zopiclone is also useful for treating disorders that are affected by the binding of agonists to central nervous system or peripheral benzodiazepine receptors. Also described are methods and compositions for treating disorders that are affected by binding of agonists to central nervous system or peripheral benzodiazepine receptors while avoiding the adverse effects associated with the administration of the racemic mixture of zopiclone.

Abstract translation: 公开了使用佐匹克隆的光学纯（+）异构体的方法和组合物。 该化合物是治疗睡眠障碍（例如失眠）和惊厥性疾病如癫痫的有效药物。 类似地，这些新的组合物和方法可用于治疗睡眠障碍和惊厥性疾病，同时避免与佐匹克隆的外消旋混合物相关的副作用的伴随的责任。 佐匹克隆的光学纯（+）异构体也可用于治疗受激动剂与中枢神经系统或外周苯并二氮杂受体结合影响的疾病。 还描述了用于治疗受激动剂与中枢神经系统或外周苯并二氮杂受体的结合影响的疾病的方法和组合物，同时避免与佐匹克隆的外消旋混合物的施用相关的不利影响。

公开(公告)号：WO1993000074A1

公开(公告)日：1993-01-07

申请号：PCT/US1992005376

申请日：1992-06-25

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  YOUNG, James, W.

IPC: A61K09/48

CPC classification number: A61K31/4178 ,  A61K31/415 ,  Y10S514/872

Abstract: Methods and compositions are disclosed utilizing the optically pure R(+) isomer of ondansetron. This compound is a potent drug for the treatment of nausea and vomiting associated with chemotherapy and radiation therapy, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. The R(+) isomer of ondansetron is also useful for the treatment of behavioral disorders such as mood anxiety and schizophrenia, and such other conditions as may be related to R(+) ondansetron's activity as a competitive antagonist of serotonin receptor subtype 5-HT3 such as disorders of gastrointestinal motility, depression, migraine, and as an aid for alcohol withdrawal, nicotine withdrawal, and drug (benzodiazepine et al.) withdrawal, without the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. Furthermore, the R(+) isomer of ondansetron is also useful for the treatment of cognitive disorders such as dementia or age-associated memory impairment, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron.

Abstract translation: 公开了使用昂丹司琼的光学纯的R（+）异构体的方法和组合物。 该化合物是用于治疗与化疗和放射治疗相关的恶心和呕吐的有效药物，同时避免与昂丹司琼外消旋混合物相关的副作用的伴随责任。 昂丹司琼的R（+）异构体也可用于治疗诸如情绪焦虑和精神分裂症等行为障碍，以及可能与R（+）昂丹司琼活性作为5-羟色胺受体亚型5-HT3的竞争性拮抗剂相关的其他条件 例如消化道运动障碍，抑郁症，偏头痛，以及用于酒精戒断，尼古丁戒断和药物（苯并二氮杂类等）撤离的辅助，而不伴随昂丹司琼外消旋混合物的不良反应。 此外，昂丹司琼的R（+）异构体也可用于治疗诸如痴呆或年龄相关记忆障碍的认知障碍，同时避免与昂丹司琼外消旋混合物相关的副作用的伴随责任。

公开(公告)号：WO1991014706A2

公开(公告)日：1991-10-03

申请号：PCT/US1991001578

申请日：1991-03-08

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  HOLTON, Oscar, Dile ,  FOURON, Yves

IPC: C07K17/08

CPC classification number: B01D67/0093 ,  B01D61/00 ,  B01D69/141 ,  B01J20/28033 ,  C07K1/22 ,  C07K14/53 ,  C07K16/065

Abstract: This invention relates to lectin affinity membranes and methods for carrying out affinity separations of glycosylated proteins using them. The method utilizes a membrane-bound lectin ligand first to capture and separate a glycosylated protein from a fluid mixture and subsequently to release said protein in purified form. The present affinity membrane methods recover high-purity glycosylated proteins. The invention has particular relevance to the recovery and purification of glycosylated proteins from mixtures of biological origin.

Abstract translation: 本发明涉及凝集素亲和膜和使用它们进行糖基化蛋白质的亲和分离的方法。 该方法首先利用膜结合的凝集素配体从流体混合物中捕获和分离糖基化的蛋白质，然后以纯化的形式释放所述蛋白质。 本发明的亲和膜方法回收高纯度糖基化蛋白质。 本发明与从生物来源的混合物中回收和纯化糖基化蛋白质特别相关。

公开(公告)号：WO1991007175A1

公开(公告)日：1991-05-30

申请号：PCT/US1990006824

申请日：1990-11-21

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  BARBERICH, Timothy, J. ,  BRATZLER, Robert, L. ,  YOUNG, James, W. ,  LOUIS, William, J.

IPC: A61K31/165

CPC classification number: A61K31/165

Abstract: Optically pure S(-) atenolol, which is substantially free of the R(+) enantiomer, is a potent beta-blocker for controlling heartbeat, relieving the symptoms of angina pectoris and reducing blood pressure in individuals. A method is disclosed utilizing the optically pure S(-) enantiomer of atenolol for treating cardiovascular disorders while reducing undesirable side effects associated with beta-blockers.

Abstract translation: 基本上不含R（+）对映异构体的光学纯的S（ - ）阿替洛尔是用于控制心跳，缓解心绞痛症状和降低个体血压的有效β-受体阻滞剂。 公开了利用阿替洛尔的光学纯的S（ - ）对映异构体治疗心血管疾病同时减少与β-受体阻滞剂相关的不良副作用的方法。

公开(公告)号：WO1989009765A1

公开(公告)日：1989-10-19

申请号：PCT/US1989001429

申请日：1989-04-06

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  MATSON, Stephen, L. ,  WALD, Stephen, A. ,  ZEPP, Charles, M. ,  DODDS, David, R.

IPC: C07C69/76

CPC classification number: C12P41/005 ,  B01J19/2475 ,  B01J2219/00159 ,  B01J2219/00162 ,  B01J2219/00177 ,  C07C219/10 ,  C07C305/04 ,  C07C305/10 ,  C07C309/65 ,  C07C309/66 ,  C07C327/32 ,  C07F9/091 ,  C12N11/02 ,  C12P1/00 ,  C12P7/40 ,  C12P41/00

Abstract: This invention relates to novel compositions of matter and their methods of preparation, which compositions are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with this invention's novel enzymatic resolving methods which are mediated in an aqueous environment.

Abstract translation: 本发明涉及新颖的物质组合物及其制备方法，该组合物是具有增强的水溶性的酯，用于这些酯的外消旋混合物的水性酶拆分反应中。 外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。 对于本发明的水溶性酯具有特别意义的是，它们用增强其水溶性的基团衍生化，并且它们与在水性环境中介导的本发明的新型酶拆分方法的反应性衍生化。

公开(公告)号：WO1987002380A1

公开(公告)日：1987-04-23

申请号：PCT/US1986002088

申请日：1986-10-08

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  MATSON, Stephen, L.

IPC: C12G03/08

CPC classification number: C12G3/085 ,  B01D3/322 ,  B01D11/0415 ,  B01D61/00 ,  B01D61/005 ,  B01D61/246 ,  B01D61/38 ,  B01D63/02

Abstract: Low-ethanol wines and other alcoholic beverages are produced by treating ordinary alcoholic beverages with novel membrane extraction methods. Semipermeable membranes and extraction fluids comprised either of a non-toxic, water-immiscible organic solvent or an aqueous solution of a low-molecular-weight but membrane-impermeable solute are used under mild conditions to selectively extract ethanol from alcoholic beverages, while leaving substantially intact the complement of other organic constituents that contribute to the color, aroma, and taste of the beverage. The methods disclosed may be adapted to continuous processing of alcohol-containing beverages, in which an ethanol-rich product is continuously recovered from the organic or aqueous extraction fluid and the latter is continuously regenerated and subsequently recycled to the membrane extraction unit.

公开(公告)号：WO1998021213A3

公开(公告)日：1998-05-22

申请号：PCT/US1997020729

申请日：1997-11-12

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  MCCULLOUGH, John, R. ,  SENANAYAKE, Chris, H. ,  TANOURY, Gerald, J. ,  HONG, Yaping ,  KOCH, Patrick

IPC: C07D405/14

公开(公告)号：WO1998000141A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011643

申请日：1997-06-27

Applicant: SEPRACOR, INC. ,  FABIANO, Vincent, L. ,  McCULLOUGH, John, R.

Inventor： SEPRACOR, INC.

IPC: A61K31/445

CPC classification number: C07D295/092 ,  A61K31/00 ,  A61K31/4453 ,  C07B2200/07 ,  Y10S514/878 ,  Y10S514/906

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (S)-trihexyphenidyl. The method comprises administering a therapeutically effective amount of enantiomerically enriched (S)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, substantially free of the (R)-trihexyphenidyl enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (S)-trihexyphenidyl, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract translation: 使用对映异构体富集的（S） - 己烯苯基酯治疗尿失禁的方法，例如由膀胱逼尿肌不稳定引起的失禁。 该方法包括施用治疗有效量的基本上不含（R） - 己烯缩苯基
对映异构体的对映异构体富集的（S） - 己烯缩水甘油基或其药学上可接受的盐。 还公开了用于治疗尿失禁的药物组合物，其包含对映异构体富集的（S） - 三己菲基，或其药学上可接受的盐和可接受的载体。

公开(公告)号：WO1998000133A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011645

申请日：1997-06-27

Applicant: SEPRACOR, INC. ,  FABIANO, Vincent, L. ,  McCULLOUGH, John, R.

Inventor： SEPRACOR, INC.

IPC: A61K31/40

CPC classification number: A61K31/40

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (S,S)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (S,S)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (R,R)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (S,S)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract translation: 使用对映异构体富集（S，S） - 乙酰丙酸酯治疗尿失禁的方法，例如由膀胱逼尿肌不稳定引起的失禁。 该方法包括施用治疗有效量的基本上不含（R，R） - 乙酰丙酸酰对映异构体的对映异构体富集的（S，S） - 乙酰基吡咯烷酸酯或其药学上可接受的盐。 还公开了用于治疗尿失禁的药物组合物，其包含对映异构体富集的（S，S） - 乙酰丙酸酯或其药学上可接受的盐和可接受的载体。