公开(公告)号：WO1998021205A1

公开(公告)日：1998-05-22

申请号：PCT/US1997020462

申请日：1997-11-12

Applicant: SEPRACOR, INC.

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

IPC: C07D405/14

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/12

Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl R,R-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.

Abstract translation: 公开了制备羟基特他康唑的光学纯异构体的方法，特别是仲丁基R，R-异构体及其磷酸盐和硫酸盐衍生物的两种顺式二氧戊环非对映异构体。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。

公开(公告)号：WO1998021204A1

公开(公告)日：1998-05-22

申请号：PCT/US1997020461

申请日：1997-11-12

Applicant: SEPRACOR, INC.

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

IPC: C07D405/14

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/12

Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.

Abstract translation: 公开了制备羟基特他康唑的光学纯异构体的方法，特别是仲丁基（S，S） - 异构体的两种顺式二氧戊环非对映异构体及其磷酸盐和硫酸盐衍生物。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。

公开(公告)号：WO1998000138A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011258

申请日：1997-06-27

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

Inventor： SEPRACOR, INC.

IPC: A61K31/435

CPC classification number: C07D453/02 ,  A61K31/439

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R)-clidinium. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R)-clidinium, or a pharmaceutically acceptable salt thereof, substantially free of the (S)-clidinium enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (R)-clidinium, 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（R） - idin啶治疗尿失禁的方法，例如由膀胱逼尿肌不稳定引起的失禁。 该方法包括施用基本上不含（S） - 脒对映异构体的治疗有效量的对映异构体富集的（R） - 哒啶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（R） - idin啶或其药学上可接受的盐和可接受的载体。

公开(公告)号：WO1993017680A1

公开(公告)日：1993-09-16

申请号：PCT/US1993002282

申请日：1993-03-12

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  YOUNG, James, W. ,  GRAY, Nancy, M. ,  WECHTER, William, J.

IPC: A61K31/40

CPC classification number: A61K31/40

Abstract: Methods and compositions are disclosed utilizing optically pure R(-) etodolac for the treatment of pain, including but not limited to pain associated with toothaches, headaches, sprains, joint pain and surgical pain, for example dental pain and ophthalmic pain, while substantially reducing adverse effects which are associated with the administration of the racemic mixture of etodolac. The optically pure R(-) etodolac is also useful in treating pyrexia while substantially reducing the adverse effects associated with the administration of the racemic mixture of etodolac.

Abstract translation: 公开了使用光学纯的R（ - ）依托度酸治疗疼痛的方法和组合物，所述方法和组合物用于治疗疼痛，包括但不限于与牙痛，头痛，扭伤，关节疼痛和手术疼痛相关的疼痛，例如牙痛和眼痛，同时基本上减少 与服用依托度酸的外消旋混合物有关的不良反应。 光学纯的R（ - ）依托度酸也可用于治疗发热，同时显着减少与依托度酸的外消旋混合物的给药相关的不良反应。

公开(公告)号：WO1993017677A1

公开(公告)日：1993-09-16

申请号：PCT/US1993002126

申请日：1993-03-08

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  YOUNG, James, W. ,  GRAY, Nancy, M. ,  WECHTER, William, J.

IPC: A61K31/19

CPC classification number: A61K31/19

Abstract: Methods and compositions are disclosed utilizing optically pure R(-) ketoprofen for the treatment of pain including, but not limited to, pain associated with toothaches, headaches, sprains, joint pain and post-surgical pain, for example dental pain and ophthalmic pain, while substantially reducing adverse effects including, but not limited to, gastrointestinal, renal and hepatic toxicities, and leukopenia, which are associated with the administration of racemic ketoprofen. Optically pure R(-) ketoprofen is also useful in treating pyrexia while substantially reducing the adverse effects associated with the administration of racemic ketoprofen.

Abstract translation: 公开了使用光学纯的R（ - ）酮洛芬用于治疗疼痛的方法和组合物，包括但不限于与牙痛，头痛，扭伤，关节疼痛和手术后疼痛相关的疼痛，例如牙痛和眼痛， 同时显着降低与外消旋酮洛芬的施用相关的不良反应，包括但不限于胃肠道，肾脏和肝脏毒性以及白细胞减少。 光学纯的R（ - ）酮洛芬也可用于治疗发热，同时显着减少与外消旋酮洛芬的给药相关的不良反应。

公开(公告)号：WO1993010785A1

公开(公告)日：1993-06-10

申请号：PCT/US1992010142

申请日：1992-11-25

Applicant: SEPRACOR, INC.

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

IPC: A61K31/495

CPC classification number: A61K31/495

Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin. This compound is a potent drug for the treatment of infection or other diseases requiring antibiotics while avoiding the concomitant liability of adverse effects that are associated with the racemic mixture of lomefloxacin.

Abstract translation: 公开利用洛美沙星的光学纯（S） - 异构体的方法和组合物。 该化合物是治疗需要抗生素的感染或其他疾病的有效药物，同时避免与洛美沙星的外消旋混合物相关的副作用的伴随责任。

公开(公告)号：WO1993000090A1

公开(公告)日：1993-01-07

申请号：PCT/US1992005378

申请日：1992-06-25

Applicant: SEPRACOR, INC.

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

IPC: A61K31/44

CPC classification number: A61K31/44

Abstract: A method and composition are disclosed utilizing the pure (+) isomer of pirbuterol, which is a potent bronchodilator and a potent cardiovascular stimulant with reduced adverse effects, having a low incidence of the development of tolerance and having increased bronchial distribution when administered by inhalation.

Abstract translation: 公开了使用吡布特罗的纯（+）异构体的方法和组合物，其是有效的支气管扩张剂和具有降低的副作用的有效的心血管兴奋剂，其通过吸入施用时具有低耐受性的发生率并且具有增加的支气管分布。

公开(公告)号：WO1993000075A1

公开(公告)日：1993-01-07

申请号：PCT/US1992005377

申请日：1992-06-25

Applicant: SEPRACOR, INC.

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

IPC: A61K09/48

CPC classification number: A61K31/415

Abstract: Methods and compositions are disclosed utilizing the optically pure S(-) 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 S(-) 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 S(-) 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 liability of adverse effects associated with the racemic mixture of ondansetron. Furthermore, the S(-) 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S（ - ）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的外消旋混合物相关的副作用的伴随责任。 昂丹司琼的S（ - ）异构体也可用于治疗诸如情绪焦虑和精神分裂症的行为障碍，以及可能与S（ - ）昂丹司琼活性相关的其他条件，作为5-羟色胺受体亚型5-HT3的竞争性拮抗剂 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（苯二氮卓等）撤离的辅助，而不伴随昂丹司琼外消旋混合物不良反应的不利责任的责任。 此外，昂丹司琼的S（ - ）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：WO1992021350A1

公开(公告)日：1992-12-10

申请号：PCT/US1992004461

申请日：1992-05-29

Applicant: SEPRACOR, INC. ,  WECHTER, William, J.

Inventor： SEPRACOR, INC.

IPC: A61K31/557

CPC classification number: A61K31/557 ,  A61K31/54 ,  A61K31/415 ,  A61K31/405 ,  A61K31/40 ,  A61K31/19 ,  A61K2300/00

Abstract: A combination of a non-steroidal anti-inflammatory drug and a prostaglandin of the E series is administered to individuals to treat inflammatory diseases or to reduce or prevent chronic bone demineralization or to promote bone remineralization. This drug combination is used to treat rheumatoid arthritis or other inflammatory diseases or to treat osteoporosis, bone loss associated with periodontal disease or repair of fractures. The administered amounts of the non-steroidal anti-inflammatory drug or prostaglandin are less than the typical amount of either drug that is given when that drug is individually used to achieve a desired effect. This administration feature minimizes the adverse side effects associated with these drugs.

Abstract translation: 向个体施用非甾体抗炎药和E系列前列腺素的组合以治疗炎性疾病或减少或预防慢性骨脱矿质或促进骨再矿化。 这种药物组合用于治疗类风湿关节炎或其他炎性疾病或治疗骨质疏松症，与牙周病相关的骨丢失或骨折修复。 非甾体抗炎药物或前列腺素的给药量小于当单独使用该药物达到期望效果时给予的任一药物的典型量。 这种给药特征使与这些药物相关的副作用最小化。

公开(公告)号：WO1990008183A1

公开(公告)日：1990-07-26

申请号：PCT/US1990000227

申请日：1990-01-11

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  LEE, Eric, K. ,  KALYANI, Vinay, J. ,  MATSON, Stephen, L.

IPC: C12G03/10

CPC classification number: C12G3/085 ,  B01D61/362 ,  B01D2313/243 ,  B01D2313/46 ,  B01D2313/90

Abstract: The method and apparatus of the present invention has general applicability to the manipulation of the concentration, by partial depletion or enrichment, of one or more volatile components in a given liquid such as ethanol content in alcoholic beverages while leaving the other volatile components in the liquid in a substantially undisturbed or unadulterated state.

Abstract translation: 本发明的方法和装置通常适用于通过部分消耗或富集在给定液体中的一种或多种挥发性组分（例如酒精饮料中的乙醇含量）而将其它挥发性组分留在液体中的操作 在基本上不受干扰或未掺杂的状态。