公开(公告)号：WO1998000132A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011257

申请日：1997-06-27

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

Inventor： SEPRACOR, INC.

IPC: A61K31/40

CPC classification number: C07D207/12

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R,S)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R,S)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (S,R)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treatment of urinary incontinence comprising enantiomerically enriched (R,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（R，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（S，R） - 甘氨酸酯对映异构体的对映异构体富集的（R，S） - 乙酰丙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（R，S） - 乙酰丙酸酯，或其药学上可接受的盐和可接受的载体。

公开(公告)号：WO1998000016A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011644

申请日：1997-06-27

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

Inventor： SEPRACOR, INC.

IPC: A01N43/38

CPC classification number: A61K31/40

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R, R)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R, R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (S, S)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treament of urinary incontinence comprising enantiomerically enriched (R, R)-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的（R，R） - 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（S，S） - 乙酰丙酸酰对映异构体的对映异构体富集的（R，R） - 乙酰丙酸酯或其药学上可接受的盐。 还公开了包含对映异构体富集的（R，R） - 乙酰丙酸酯或其药学上可接受的盐和可接受的载体的用于尿失禁治疗的药物组合物。

公开(公告)号：WO1997018819A1

公开(公告)日：1997-05-29

申请号：PCT/US1996018695

申请日：1996-11-19

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

Inventor： SEPRACOR, INC.

IPC: A61K31/66

CPC classification number: A61K31/662

Abstract: Methods and compositions are disclosed utilizing optically pure (-)-fotemustine for the treatment of various malignancies, while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of fotemustine.

Abstract translation: 公开了使用旋光纯（ - ） - 莫司汀治疗各种恶性肿瘤的方法和组合物，同时显着降低伴随着与莫曲汀的外消旋混合物相关的副作用的伴随的责任。

公开(公告)号：WO1997018818A1

公开(公告)日：1997-05-29

申请号：PCT/US1996018488

申请日：1996-11-19

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

Inventor： SEPRACOR, INC.

IPC: A61K31/66

CPC classification number: A61K31/662

Abstract: Methods and compositions are disclosed utilizing optically pure (+)-fotemustine for the treatment of various malignancies, while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of fotemustine.

Abstract translation: 公开了使用光学纯的（+） - 莫司汀治疗各种恶性肿瘤的方法和组合物，同时显着减少与莫曲汀的外消旋混合物相关的副作用的伴随的责任。

公开(公告)号：WO1996023492A1

公开(公告)日：1996-08-08

申请号：PCT/US1996001053

申请日：1996-01-25

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  ABERG, Gunnar ,  MC CULLOUGH, John, R. ,  FANG, Yue

IPC: A61K31/215

CPC classification number: A61K31/216 ,  Y10S514/946

Abstract: A method for treating urinary incontinence while avoiding concomitant liability of adverse effects associated with racemic oxybutynin 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. Pharmaceutical compositions in the form of tablets and transdermal devices comprising (S)-oxybutynin or (S)-desethyloxybutynin and an acceptable carrier are also disclosed, as is a synthesis of desethyloxybutynin.

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有关的副作用的伴随责任。 该方法包括施用治疗有效量的基本上不含相应R对映异构体的（S） - 奥昔布宁，（S） - 乙氧基奥昔布宁或其药学上可接受的盐。 还公开了包含（S） - 奥昔布宁或（S） - 乙氧基丁炔宁和可接受的载体的片剂和透皮装置形式的药物组合物，以及去乙氧基丁炔的合成。

公开(公告)号：WO1995031982A1

公开(公告)日：1995-11-30

申请号：PCT/US1995006445

申请日：1995-05-22

Applicant: SEPRACOR, INC.

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

IPC: A61K31/415

CPC classification number: A61K31/4184

Abstract: Methods and compositions are disclosed utilizing optically pure (-)-liarozole for the treatment of conditions supported by estrogen or caused by elevated estrogen levels such as estrogen-dependent breast cancer, gynecomastia, systemic lupus erythematosus and premature labor while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of liarozole. Methods and compositions are also disclosed utilizing optically pure (-)-liarozole for the treatment of conditions supported by or caused by elevated testosterone levels, such as hormone dependent prostate cancer. Further disclosed are methods and compositions utilizing pure (-)-liarozole in combination with retinoic acid for enhancing therapy with retinoic acid, such as in the treatment of neuroectodermal and neuroepithelial malignancies, including glioma, promyelocytic leukemia and hormone-independent prostate cancer.

Abstract translation: 公开了使用光学纯的（ - ） - 利罗唑用于治疗由雌激素支持或由升高的雌激素水平引起的病症，例如雌激素依赖性乳腺癌，男子乳腺发育症，系统性红斑狼疮和早产，同时显着减少伴随的责任 与利咯唑的外消旋混合物有关的不良反应。 还公开了使用光学纯的（ - ） - 利罗唑用于治疗由升高的睾酮水平如激素依赖性前列腺癌支持或由升高的睾酮水平引起的病症的方法和组合物。 进一步公开的是使用纯（ - ） - 利唑唑与视黄酸组合以增强用视黄酸治疗的方法和组合，例如治疗神经外胚层和神经上皮性恶性肿瘤，包括胶质瘤，早幼粒细胞白血病和不依赖激素的前列腺癌。

公开(公告)号：WO1994026269A1

公开(公告)日：1994-11-24

申请号：PCT/US1994005192

申请日：1994-05-10

Applicant: SEPRACOR, INC.

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

IPC: A61K31/38

CPC classification number: A61K31/38 ,  A61K31/381

Abstract: Methods and compositions are disclosed utilizing optically pure (-)-zileuton for the treatment of asthma, rheumatoid arthritis and ulcerative colitis in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of zileuton. (-)-Zileuton is an inhibitor of 5-lipoxygenase and is therefore useful in the treatment of other conditions related to elevated leukotriene levels. (-)-Zileuton is also an antioxidant and is therefore useful in treating or preventing atherosclerosis.

Abstract translation: 公开了使用光学纯的（ - ） - 齐鲁汤用于治疗人类的哮喘，类风湿性关节炎和溃疡性结肠炎的方法和组合物，同时显着降低与齐鲁汤的外消旋混合物相关的副作用的伴随责任。 （ - ） - Zileuton是5-脂氧合酶的抑制剂，因此可用于治疗与升高的白三烯水平相关的其他病症。 （ - ） - Zileuton也是抗氧化剂，因此可用于治疗或预防动脉粥样硬化。

公开(公告)号：WO1994025028A1

公开(公告)日：1994-11-10

申请号：PCT/US1994004575

申请日：1994-04-25

Applicant: SEPRACOR, INC.

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

IPC: A61K31/44

CPC classification number: A61K31/44

Abstract: Methods and compositions are disclosed utilizing optically pure (+) pantoprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of pantoprazole. The optically pure (+) isomer is also useful for the treatment of gastroesophageal reflux. (+) Pantoprazole is an inhibitor of H release and is therefore useful in the treatment of other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

Abstract translation: 公开了使用光学纯的（+）泮托拉唑用于治疗人体溃疡的方法和组合物，同时显着降低与泮托拉唑的外消旋混合物相关的副作用的伴随的责任。 光学纯的（+）异构体也可用于治疗胃食管反流。 （+）泮托拉唑是H +释放的抑制剂，因此可用于治疗与胃分泌异常有关的其他病症，如Zollinger-Ellison综合征。

公开(公告)号：WO1994020635A1

公开(公告)日：1994-09-15

申请号：PCT/US1994002505

申请日：1994-03-08

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  HEEFNER, Donald, L. ,  ZEPP, Charles, M.

IPC: C12P41/00

CPC classification number: C12P13/00 ,  C12P7/40 ,  C12P41/004 ,  Y10S435/911

Abstract: A process for producing substantially pure R-ketoprofen by the enantioselective hydrolysis of racemic ketoprofen choline ester is disclosed. The process utilizes either intact Beauveria bassiana hyphae or an R-specific ester hydrolase isolated therefrom. The ester hydrolase has an approximate molecular weight of 17,800 daltons and an N-terminal sequence of Ala-Pro-Asp-W-Ile-Ile-Gln-Gly-Leu-Ser-Arg-Ala-X-Asp-Gly-Gln-Asp.

Abstract translation: 公开了通过外消旋酮洛芬胆碱酯的对映选择性水解制备基本上纯的R-酮洛芬的方法。 该方法利用完整的白僵菌菌丝体或与其分离的R-特异性酯水解酶。 酯水解酶具有17,800道尔顿的近似分子量和Ala-Pro-Asp-W-Ile-Ile-Gln-Gly-Leu-Ser-Arg-Ala-X-Asp-Gly-Gln- 天冬氨酸。

公开(公告)号：WO1994010334A1

公开(公告)日：1994-05-11

申请号：PCT/US1993010179

申请日：1993-10-25

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  ROSSI, Richard, Filip ,  HEEFNER, Donald, Lee ,  ZEPP, Charles, Melvyn

IPC: C12P41/00

CPC classification number: C12P41/002 ,  C12P7/40

Abstract: A process for enantioselectively converting an aldehyde, a bisulfite adduct of an aldehyde or a glycidate to a chiral carboxylic acid is disclosed. The process utilizes a microorganism or an enzyme preparation from a microorganism and is particularly useful for producing NSAIDs of the profen class from readily available precursors. Bacteria, yeasts and fungi are exemplified as capable of transforming precursors to profens.

Abstract translation: 公开了将醛，醛或缩水甘油酸的亚硫酸氢盐加合物对映选择性转化成手性羧酸的方法。 该方法利用来自微生物的微生物或酶制剂，并且特别可用于从容易获得的前体产生等级的NSAID。 细菌，酵母菌和真菌被证明能够将前体转化为特征。