公开(公告)号：WO1994014446A1

公开(公告)日：1994-07-07

申请号：PCT/US1993012327

申请日：1993-12-17

Applicant: SEPRACOR, INC. ,  GEORGETOWN UNIVERSITY

Inventor： SEPRACOR, INC. ,  GEORGETOWN UNIVERSITY ,  GRAY, Nancy, M. ,  WOOSLEY, Raymond, L.

IPC: A61K31/495

CPC classification number: A61K31/495

Abstract: Methods and compositions are disclosed utilizing the optically pure (+) isomer of ketoconazole. This compound is a potent drug for the treatment of local and systemic fungal, yeast, and dermatophyte infections, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ketoconazole.

Abstract translation: 利用酮康唑的旋光纯（+）异构体公开了方法和组合物。 该化合物是用于治疗局部和全身真菌，酵母和皮肤癣菌感染的有效药物，同时避免与酮康唑外消旋混合物相关的副作用的伴随责任。

公开(公告)号：WO1994009785A2

公开(公告)日：1994-05-11

申请号：PCT/US1993010503

申请日：1993-11-02

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  GRAY, Nancy, M.

IPC: A61K31/505

CPC classification number: A61K31/505

Abstract: Methods and compositions are disclosed utilizing the optically pure (+) isomer of doxazosin. This compound is a potent drug for the treatment of benign prostatic hyperplasia while avoiding the concomitant liability of hypotensive effects associated with the racemic mixture of doxazosin. The optically pure (+) isomer of doxazosin is also useful for the treatment and prevention of atherosclerosis and other conditions related to elevated serum LDL and cholesterol levels, such as coronary artery disease, without the concomitant liability of adverse effects associated with the racemic mixture of doxazosin.

Abstract translation: 公开利用多沙唑嗪的光学纯（+）异构体的方法和组合物。 该化合物是治疗良性前列腺增生的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的降压作用的伴随责任。 多沙唑嗪的光学纯（+）异构体也可用于治疗和预防与血清LDL和胆固醇水平升高相关的动脉粥样硬化和其他相关疾病，如冠状动脉疾病，而与外消旋混合物有关的副作用的伴随责任 多沙唑嗪。

公开(公告)号：WO1994009783A1

公开(公告)日：1994-05-11

申请号：PCT/US1993010577

申请日：1993-11-02

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  GRAY, Nancy, M.

IPC: A61K31/495

CPC classification number: A61K31/495

Abstract: Methods and compositions are disclosed utilizing the optically pure (-) isomer of doxazosin. This compound is a potent drug for the treatment of benign prostatic hyperplasia while avoiding the concomitant liability of hypotensive effects associated with the racemic mixture of doxazosin. The optically pure (-) isomer of doxazosin is also useful for the treatment and prevention of atherosclerosis and other conditions related to elevated serum LDL and cholesterol levels, such as coronary artery disease, without the concomitant liability of adverse effects associated with the racemic mixture of doxazosin.

Abstract translation: 利用多沙唑嗪的光学纯（ - ）异构体公开了方法和组合物。 该化合物是治疗良性前列腺增生的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的降压作用的伴随责任。 多沙唑嗪的光学纯（ - ）异构体也可用于治疗和预防与血清LDL和胆固醇水平升高相关的动脉粥样硬化和其他病症，例如冠状动脉疾病，而与外消旋混合物相关的不良反应的伴随责任 多沙唑嗪。

公开(公告)号：WO1994006429A1

公开(公告)日：1994-03-31

申请号：PCT/US1993008991

申请日：1993-09-22

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  GRAY, Nancy, M.

IPC: A61K31/495

CPC classification number: A61K31/495

Abstract: Methods and compositions are disclosed utilizing optically pure (-) cetirizine for the treatment of seasonal and perennial allergic rhinitis in humans while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cetirizine. The optically pure (-) isomer is also useful for the treatment of allergic asthma and chronic and physical urticaria. (-) Cetirizine is an inhibitor of eosinophil chemotaxis and is therefore useful in the treatment of other conditions related to eosinophilia such as allergic asthma, seasonal allergic rhinitis, atopic dermatitis, some parasitic diseases, some chronic obstructive lung diseases and certain gastrointestinal and genitourinary disorders.

Abstract translation: 公开利用旋光纯（ - ）西替利嗪治疗人类季节性和常年性过敏性鼻炎的方法和组合物，同时避免与西替利嗪的外消旋混合物相关的副作用的伴随责任。 光学纯的（ - ）异构体也可用于治疗过敏性哮喘和慢性和身体性荨麻疹。 （ - ）西替利嗪是嗜酸粒细胞趋化性的抑制剂，因此可用于治疗与嗜酸性粒细胞增多有关的其他病症，如过敏性哮喘，季节性过敏性鼻炎，特应性皮炎，一些寄生虫病，一些慢性阻塞性肺疾病和某些胃肠道和泌尿生殖器疾病 。

公开(公告)号：WO1993010788A1

公开(公告)日：1993-06-10

申请号：PCT/US1992010705

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: 公开利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：WO1993009769A1

公开(公告)日：1993-05-27

申请号：PCT/US1992000888

申请日：1992-02-05

Applicant: SEPRACOR, INC.

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

IPC: A61K31/13

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is a potent antidepressant and appetite suppressant substantially free of unwanted, adverse toxic or psychological effects. In addition, methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is useful in treating migraine headaches, pain, in particular chronic pain, and obsessive-compulsive disorders. Further, methods and compositions for treating a condition alleviated or improved by inhibition of serotonin uptake in serotonergic neurons and platelets in a human using optically pure S(+) fluoxetine are disclosed.

Abstract translation: 公开了使用氟西汀的纯S（+）异构体的方法和组合物，其是有效的抗抑郁药和食欲抑制剂，其基本上不含有害的，不利的毒性或心理作用。 此外，利用氟西汀的纯S（+）异构体可用于治疗偏头痛，疼痛，特别是慢性疼痛和强迫症的方法和组合物被公开。 此外，公开了通过使用光学纯的S（+）氟西汀在人体中抑制5-羟色胺能神经元和血小板中5-羟色胺摄取而缓解或改善的病症的方法和组合物。

公开(公告)号：WO1992016173A1

公开(公告)日：1992-10-01

申请号：PCT/US1992002342

申请日：1992-03-18

Applicant: SEPRACOR, INC.

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

IPC: A61F13/00

CPC classification number: A61K31/135

Abstract: A method and composition are disclosed utilizing the pure (-) isomer of terbutaline, which is a potent bronchodilator with reduced adverse effects, has a low incident of the development of tolerance and has increased bronchial distribution when administered by inhalation.

Abstract translation: 公开了使用特布他林的纯（ - ）异构体的方法和组合物，特布他林是一种有效的支气管扩张剂，其副作用降低，耐受性发展低，并且通过吸入给药时支气管分布增加。

公开(公告)号：WO1991002512A1

公开(公告)日：1991-03-07

申请号：PCT/US1990004623

申请日：1990-08-16

Applicant: SEPRACOR, INC.

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

IPC: A61K07/16

CPC classification number: A61K8/365 ,  A61K8/36 ,  A61K31/19 ,  A61Q11/00

Abstract: A composition for the treatment of disorders associated with periodontal disease affecting soft tissue and bone of the oral cavity, and a composition useful in the method. The method comprises applying to buccal membranes a therapeutically effective quantity of at least one S enantiomer, generally an S(+) enantiomer, of a nonsteroidal anti-inflammatory drug, such as S(+) flurbiprofen or S(+) ketoprofen. The composition is a formulation which is a toothpaste or which is a mouthwash.

Abstract translation: 用于治疗与影响口腔软组织和骨的牙周病相关的病症的组合物，以及用于该方法的组合物。 该方法包括向颊膜施用治疗有效量的非甾体抗炎药物如S（+）氟比洛芬或S（+）酮洛芬的至少一种S对映异构体，通常为S（+）对映异构体。 组合物是一种制剂，其是牙膏或漱口剂。

公开(公告)号：WO1990004609A1

公开(公告)日：1990-05-03

申请号：PCT/US1989004620

申请日：1989-10-16

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  AZAD, A., R., M. ,  GOFFE, Randal, A.

IPC: C08F08/00

CPC classification number: C08F8/00 ,  Y10S436/824 ,  Y10S530/815 ,  Y10S530/816

Abstract: The covalent modification of a hydrophobic polymer surface by a process which utilizes the functionalizable chain ends of the hydrophobic polymer is disclosed. The process of the invention is conveniently carried out under heterogeneous conditions, allowing the practitioner to take full advantage of the general processability, strength, and other desirable characteristics of a hydrophobic polymer used in the production of a manufactured article. The invention is most advantageously applied to the surface modification of microporous membranes, allowing the practitioner to choose from a vast range of possible surface macromolecular species which may be covalently bound to the membrane polymer chain ends. The process of the invention proceeds without a significant reduction in the pore dimensions or hydraulic permeability of the original unmodified membrane. This invention also discloses a four-component dope composition which exhibits surprising and useful thermal phase separation characteristics which can be exploited in a manufacturing process disclosed herein. A spinnerette assembly which greatly facilitates the efficiency and versatility of said process is also described.

Abstract translation: 公开了通过利用疏水性聚合物的官能化链端的方法对疏水聚合物表面的共价修饰。 本发明的方法方便地在异质条件下进行，使得从业者能够充分利用用于制造制品的疏水性聚合物的一般加工性，强度和其它所需特性。 本发明最有利地应用于微孔膜的表面改性，允许从业者从可能共价结合到膜聚合物链端的广泛范围的可能的表面大分子物质中进行选择。 本发明的方法不会显着降低原始未改性膜的孔尺寸或水力渗透性。 本发明还公开了四组分涂料组合物，其显示出令人惊奇且有用的热相分离特性，其可以在本文公开的制造方法中使用。 还描述了大大促进所述方法的效率和多功能性的喷丝组件。

公开(公告)号：WO1990002732A1

公开(公告)日：1990-03-22

申请号：PCT/US1989003960

申请日：1989-09-12

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  ZEPP, Charles, M.

IPC: C07D205/04

CPC classification number: C07D207/16 ,  C07D205/04 ,  C07D211/60

Abstract: This invention relates to novel methods for converting a diastereomeric mixture of S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues into its separate optically resolved diastereomeric components. Specifically the invention relates to methods for the preparation of optically purified captopril and its analogs from racemic precursors. This resolution process is achieved through the fractional crystallization of S-protected derivatives of captopril and its precursors, which derivatives are useful for the reason that they are (1) easily prepared from novel precursors, (2) resolvable to their optically purified stereoisomeric species and (3) convertible to non-derivatized stereoisomeric species which correspond to the pharmacologically active inhibitor and its analogues. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, the novel derivatives and their precursors are also described herein.

Abstract translation: 本发明涉及将血管紧张素转换酶（ACE）的口服活性抑制剂的S-保护衍生物与其类似物的非对映异构体混合物转化成其单独的光学拆分的非对映体组分的新方法。 具体地说，本发明涉及从外消旋前体制备光学纯化的卡托普利及其类似物的方法。 该解决方法通过卡托普利及其前体的S-保护衍生物的分级结晶实现，该衍生物由于它们（1）容易地由新型前体制备，（2）可分解成其光学纯化的立体异构物质和 （3）可转化成对应于药理活性抑制剂及其类似物的非衍生化立体异构体。 本文还注意到制备衍生物及其前体的新方法。 此外，本文还描述了新的衍生物及其前体。