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公开(公告)号：WO1990002118A1
公开(公告)日：1990-03-08
申请号：PCT/US1989003695
申请日：1989-08-25
Applicant: SEPRACOR, INC.
Inventor： SEPRACOR, INC. , ZEPP, Charles, M.
IPC: C07D205/04
CPC classification number: C07D205/04 , C07D207/16 , C07D211/60
Abstract: This invention relates to novel S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues, which derivatives are useful for the reasons 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. Consequently, this invention also relates to the novel precursors. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, methods for converting the derivatives to the resolved de-derivatized stereoisomeric species of the ACE inhibitor and its analogues are described.
Abstract translation: 本发明涉及血管紧张素转换酶（ACE）及其类似物的口服活性抑制剂的新型S-保护衍生物，其衍生物是有用的，原因是它们（1）容易由新型前体制备，（2）可分解 （3）转化成对应于药理学活性抑制剂及其类似物的非衍生的立体异构物质。 因此，本发明还涉及新颖的前体。 制备衍生物及其前体的新方法在本文中也被注明。 此外，描述了将衍生物转化成ACE抑制剂及其类似物的分解的去衍生的立体异构体物种的方法。
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32.发明申请
公开(公告)号：WO1998021175A1
公开(公告)日：1998-05-22
申请号：PCT/US1997020472
申请日：1997-11-07
Applicant: SEPRACOR, INC.
Inventor： SEPRACOR, INC. , GAO, Yun , HETT, Robert , FANG, Kevin, Q. , WALD, Stephen, A. , SENANAYAKE, Chris, H.
IPC: C07C231/18
CPC classification number: C07C233/25 , A61K9/0073 , C07B2200/07 , C07C59/255 , C07C201/12 , C07C205/37 , C07C205/45 , C07C213/02 , C07C217/86 , C07C231/02 , C07C231/18 , C07C233/43 , C07D303/36
Abstract: A method is disclosed for the preparation of optically pure isomes of formeterol, especially the (R,R)- and (S,S)-isomer, by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy- alpha -methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as is the novel L-tartrate salt of R,R-formoterol.
Abstract translation: 公开了通过光学纯的4-苄氧基-3-甲酰氨基苯氧基氧化物与光学纯的反应制备光学纯的异戊二烯异构体的方法，特别是（R，R） - 和（S，S） - 异构体 4-甲氧基-α-甲基-N-（苯基甲基）苯乙胺，然后脱苄基。 还公开了该方法中有用的中间体，以及R，R-福莫特罗的新型L-酒石酸盐。
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33.发明申请DEXTROROTATORY ISOMERS OF OXYBUTYNIN AND DESETHYLOXYBUTYNIN IN THE TREATMENT OF GASTROINTESTINAL HYPERACTIVITY 审中-公开氧自由基和脱乙酰壳多糖在胃肠道超微结构治疗中的诱导异构体
公开(公告)号：WO1998001125A2
公开(公告)日：1998-01-15
申请号：PCT/US1997012284
申请日：1997-07-09
Applicant: SEPRACOR, INC. , ABERG, Gunnar
Inventor： SEPRACOR, INC.
IPC: A61K31/215
CPC classification number: A61K31/216
Abstract: A method for treating gastrointestinal hyperactivity, irritable bowel syndrome and other motility disorders involving the gastrointestinal tract is disclosed. The method comprises administering a therapeutically effective amount of (S)-oxybutynin, (S)-desethyloxybutynin, or a pharmaceutically acceptable salt thereof, substantially free of the corresponding R enantiomer.
Abstract translation: 公开了一种治疗胃肠道多动症，肠易激综合征和涉及胃肠道的其他运动障碍的方法。 该方法包括施用治疗有效量的基本上不含相应的R对映体的（S） - 奥昔布宁，（S） - 乙氧基奥昔布宁或其药学上可接受的盐。
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34.发明申请TREATING URINARY INCONTINENCE USING (S)-OXYBUTYNIN AND (S)-DESETHYLOXYBUTYNIN 审中-公开使用（S）-OYYBUTYNIN和（S）-DESETHYLOXYBUTYNIN处理尿酸不良
公开(公告)号：WO1998000126A1
公开(公告)日：1998-01-08
申请号：PCT/US1997011570
申请日：1997-06-27
Applicant: SEPRACOR, INC.
Inventor： SEPRACOR, INC. , ABERG, Gunnar , McCULLOUGH, John, R.
IPC: A61K31/215
CPC classification number: A61K31/216
Abstract: A method for treating urinary incontinence while avoiding concomitant liability of adverse effects associated with racemic oxybutynin is disclosed. The method comprises administering from 100 mg to 1 000 mg/day of (S)-oxybutynin, (S)-desethyloxybutynin or a pharmaceutically acceptable salt thereof, substantially free of the corresponding R enantiomer. Pharmaceutical compositions in the form of tablets, soft elastic gelatin capsules and transdermal devices comprising an acceptable carrier and up to 500 mg of (S)-oxybutynin or (S)-desethyloxybutynin are also disclosed.
Abstract translation: 公开了一种治疗尿失禁的方法，同时避免与外消旋奥昔布宁相关的副作用的伴随责任。 该方法包括施用100mg至1000mg /天的（S） - 奥昔布宁，（S） - 乙氧基奥昔布宁或其药学上可接受的盐，基本上不含相应的R对映异构体。 还公开了片剂形式的药物组合物，软弹性明胶胶囊和包含可接受载体和至多500mg（S） - 奥昔布宁或（S） - 乙氧基丁基宁的透皮装置。
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35.发明申请METHODS AND COMPOSITIONS FOR TREATING URINARY INCONTINENCE USING ENANTIOMERICALLY ENRICHED (R)-TRIDIHEXETHYL 审中-公开使用完全强化（R） - 四氢呋喃的方法和组合物治疗尿毒症
公开(公告)号：WO1998000011A1
公开(公告)日：1998-01-08
申请号：PCT/US1997011647
申请日：1997-06-27
Applicant: SEPRACOR, INC. , FABIANO, Vincent, L. , McCULLOUGH, John, R.
Inventor： SEPRACOR, INC.
IPC: A01N33/18
CPC classification number: A61K31/14
Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R)-tridihexethyl. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R)-tridihexethyl or a pharmaceutically acceptable salt thereof, substantially free of the (S)-tridihexethyl enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (R)-tridihexethyl, 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） - 二乙基己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。 该方法包括施用基本上不含（S） - 十二乙基对映异构体的治疗有效量的对映异构体富集的（R） - 二乙基己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（R） - 二乙基己基或其药学上可接受的盐和可接受的载体。
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Patent Agency Ranking36.发明申请METHODS AND COMPOSITIONS FOR TREATING ALLERGIC RHINITIS AND OTHER DISORDERS USING DESCARBOETHOXYLORATADINE 审中-公开使用脱乙酰壳多糖处理过敏性RHINITIS和其他疾病的方法和组合物
公开(公告)号：WO1996020708A1
公开(公告)日：1996-07-11
申请号：PCT/US1995015995
申请日：1995-12-11
Applicant: SEPRACOR, INC.
Inventor： SEPRACOR, INC. , ABERG, A., K., Gunnar , MCCULLOUGH, John, R. , SMITH, Emil, R.
IPC: A61K31/44
CPC classification number: A61K31/4545 , A61K31/451 , A61K45/06 , Y10S514/826 , A61K2300/00
Abstract: Methods are disclosed utilizing DCL, a metabolic derivative of loratadine, for the treatment of allergic rhinitis, and other disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines.
Abstract translation: 公开了使用氯雷他定的代谢衍生物DCL用于治疗过敏性鼻炎和其他疾病的方法，同时避免与其他非镇静抗组胺剂相关的副作用的伴随的责任。
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37.发明申请METHOD FOR TREATING URINARY INCONTINENCE USING OPTICALLY PURE S-TERODILINE 审中-公开使用光学纯S-TERODILINE治疗尿毒症的方法
公开(公告)号：WO1995010270A1
公开(公告)日：1995-04-20
申请号：PCT/US1994011420
申请日：1994-10-07
Applicant: SEPRACOR, INC.
Inventor： SEPRACOR, INC. , GRAY, Nancy, M. , YOUNG, James, W.
IPC: A61K31/135
CPC classification number: A61K31/135
Abstract: Methods and compositions are disclosed utilizing the optically pure S-isomers of terodiline or of the hydroxylated derivatives of terodiline. These compounds are potent drugs for the treatment of urinary incontinence, obstructive pulmonary disease and such other conditions as are related to the compounds' activity as anticholinergic agents. Furthermore, the optically pure S-isomers of terodiline or of the hydroxylated derivatives of terodiline are useful for the treatment of angina and such other conditions as may be related to the compounds' activity as calcium antagonists.
Abstract translation: 公开的方法和组合物利用光学纯的异噻吩的S-异构体或三苯胺的羟基化衍生物。 这些化合物是用于治疗尿失禁，阻塞性肺疾病和与化合物作为抗胆碱能药物的活性相关的其它病症的有效药物。 此外，泰乐兰的光学纯S-异构体或泰乐灵的羟基化衍生物可用于治疗心绞痛和其它与化合物作为钙拮抗剂的活性相关的其它病症。
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38.发明申请METHODS AND COMPOSITIONS OF (2S,4R) ITRACONAZOLE FOR TREATING FUNGAL YEAST AND DERMATOPHYTE INFECTIONS 审中-公开（2S，4R）异噻唑酮用于治疗真菌和感染的方法和组合物
公开(公告)号：WO1994016701A1
公开(公告)日：1994-08-04
申请号：PCT/US1994001006
申请日：1994-01-27
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 uitlizing the optically pure (2S, 4R) isomer of itraconazole. 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 itraconazole.
Abstract translation: 公开了将伊曲康唑的光学纯（2S，4R）异构体取代的方法和组合物。 该化合物是治疗局部和全身真菌，酵母和皮肤癣菌感染的有效药物，同时避免与伊曲康唑外消旋混合物相关的副作用的伴随责任。
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39.发明申请METHODS AND COMPOSITIONS OF (+) DOXAZOSIN FOR THE TREATMENT OF HYPERTENSION 审中-公开（+）多西紫杉醇治疗高血压的方法和组合
公开(公告)号：WO1994009786A1
公开(公告)日：1994-05-11
申请号：PCT/US1993010648
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 hypertension while avoiding 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。 该化合物是治疗高血压的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的副作用的伴随责任。
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40.发明申请METHODS AND COMPOSITIONS OF (-) DOXAZOSIN FOR THE TREATMENT OF HYPERTENSION 审中-公开（ - ）多西紫杉醇治疗高血压的方法和组成
公开(公告)号：WO1994009782A1
公开(公告)日：1994-05-11
申请号：PCT/US1993010504
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 hypertension while avoiding 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。 该化合物是治疗高血压的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的副作用的伴随责任。
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