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：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：WO1994003170A1

公开(公告)日：1994-02-17

申请号：PCT/US1993007260

申请日：1993-08-03

Applicant: SEPRACOR INC. ,  GEORGETOWN UNIVERSITY

Inventor： SEPRACOR INC. ,  GEORGETOWN UNIVERSITY ,  YOUNG, James, W. ,  GRAY, Nancy, M. ,  WOOSLEY, Raymond, L. ,  CHEN, Yiwang

IPC: A61K31/445

CPC classification number: A61K45/06 ,  A61K31/445 ,  A61K2300/00

Abstract: A pharmaceutical composition comprising a compound of formula (I): wherein Z is COOH, COOCH3 or CH2OH, or a pharmaceutically acceptable salt thereof, for use in an anti-histaminic treatment which does not induce any significant cardiac arrhythmia, comprising administering a therapeutically effective amount of a compound of formula (I) to a human patient.

Abstract translation: 一种药物组合物，其包含式（I）化合物：其中Z为COOH，COOCH 3或CH 2 OH或其药学上可接受的盐，用于不引起任何明显心律不齐的抗组胺治疗，包括给予治疗有效的 式（I）化合物与人类患者的量。

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。

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。

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。

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。