公开(公告)号：US20030158229A1

公开(公告)日：2003-08-21

申请号：US10372875

申请日：2003-02-26

Applicant: SEPRACOR INC.

Inventor： Paul D. Rubin ,  Timothy J. Barberich

IPC: A61K031/445

CPC classification number: A61K31/445 ,  A61K31/4468

Abstract: Methods for the prevention, treatment, or management of apnea, apnea disorders, bulimia nervosa, irritable bowel syndrome, urinary incontinence, bradycardia, bradyarrhythmia, syncope, other disorders, or symptoms thereof using (null) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (null) stereoisomer.

Abstract translation: 使用（ - ）诺西沙必利或其药学上可接受的盐的预防，治疗或治疗呼吸暂停，呼吸暂停障碍，贪食症，肠易激综合征，尿失禁，心动过缓，缓慢性心律失常，晕厥，其他障碍或其症状的方法， 基本上不含（+）立体异构体。

公开(公告)号：US20030130321A1

公开(公告)日：2003-07-10

申请号：US10325686

申请日：2002-12-20

Applicant: Sepracor, Inc.

Inventor： Chris H. Senanayake ,  Gerald J. Tanoury ,  Harold S. Wilkinson ,  Roger P. Bakale ,  Andrei A. Zlota

IPC: C07D213/46 ,  C07D211/82 ,  A01N043/40

CPC classification number: C07D211/90

Abstract: The invention relates to methods of resolving racemic amlodipine into enantiomerically enriched compositions by precipitation with tartaric acid in the presence of a non-aqueous solvent, such as N,Nnull-dimethylacetamide. The molar ratio of tartaric acid:amlodipine is preferably less than 0.25:1.0 or greater than 0.75:1.0.

Abstract translation: 本发明涉及通过在非水溶剂如N，N'-二甲基乙酰胺的存在下用酒石酸沉淀来将外消旋氨氯地平拆分成对映异构体富集的组合物的方法。 酒石酸：氨氯地平的摩尔比优选小于0.25:1.0或大于0.75:1.0。

公开(公告)号：US20030119841A1

公开(公告)日：2003-06-26

申请号：US10259851

申请日：2002-09-30

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Paul D. Rubin ,  Yaping Hong ,  Roger A. Bakale ,  Tingjian Xiang ,  Fran A. McConville

IPC: A61K031/498

CPC classification number: A61K31/4985 ,  A61K31/498 ,  C07B2200/07 ,  C07D487/04

Abstract: The invention is directed to compositions comprising, and methods of using, racemic N-desmethylzopiclone, optically pure (null)-N-desmethylzopiclone, and optically pure (null)-N-desmethylzopiclone in the treatment and prevention of diseases and conditions in mammals. The invention is further directed to novel methods of preparing N-desmethylzopiclone, optically pure (null)-N-desmethylzopiclone, and optically pure (null)-N-desmethylzopiclone.

Abstract translation: 本发明涉及包含外消旋的N-去甲基佐氮克隆，光学纯的（+） - N-去甲基佐匹克隆和光学纯的（ - ） - N-去甲基佐匹克隆的组合物，其用于治疗和预防哺乳动物的疾病和病症。 本发明进一步涉及制备N-去甲基异佐匹克隆，光学纯的（+） - N-去甲基佐匹克隆和光学纯的（ - ） - N-去甲基异佐匹克隆的新方法。

公开(公告)号：US20030109540A1

公开(公告)日：2003-06-12

申请号：US10269871

申请日：2002-10-15

Applicant: Sepracor Inc.

Inventor： Dean A. Handley ,  Paul D. Rubin

IPC: A61K031/473

CPC classification number: A61K45/06 ,  A61K31/445 ,  A61K31/4545 ,  Y10S514/826 ,  Y10S514/864

Abstract: Methods utilizing descarboethoxyloratadine (nullDCLnull) for the treatment of allergic disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. Also included are methods for the treatment of allergic asthma using DCL and either a decongestant or a leukotriene inhibitor, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. The invention also encompasses the administration of DCL in a nasal or oral spray.

Abstract translation: 利用去甲氧基吡咯烷（“DCL”）治疗过敏性疾病的方法，同时避免与其他非镇静抗组胺药相关的副作用的伴随责任。 还包括使用DCL和减充血剂或白三烯抑制剂治疗过敏性哮喘的方法，同时避免与其它非镇静性抗组胺药相关的副作用的伴随的责任。 本发明还包括以鼻腔或口腔喷雾剂施用DCL。

公开(公告)号：US20030096873A1

公开(公告)日：2003-05-22

申请号：US10277905

申请日：2002-10-23

Applicant: Sepracor Inc.

Inventor： John R. McCullough ,  Paul D. Rubin

IPC: A61K031/137

CPC classification number: A61K31/137 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/135

Abstract: Methods and compositions are disclosed utilizing the optically pure (null)-isomer of bupropion to assist in smoking cessation, for treating smoking and nicotine addiction, and for treating pain, including, but not limited to, chronic pain, neuropathetic pain and reflex sympathetic dystrophy, and other disorders such as narcolepsy, chronic fatigue syndrome, fibromyalgia, seasonal affective disorder and premenstrual syndrome, while avoiding adverse affects associated with racemic bupropion.

公开(公告)号：US20030069280A1

公开(公告)日：2003-04-10

申请号：US10263558

申请日：2002-10-02

Applicant: SEPRACOR INC.

Inventor： Patrick Koch ,  Paul D. Rubin ,  William E. Yelle

IPC: A61K031/4439

CPC classification number: A61K31/4439 ,  A61K31/00

Abstract: Methods and compositions are disclosed utilizing optically pure S(null)rabeprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of rabeprazole. The optically pure S(null) isomer is also useful for the treatment of gastroesophageal reflux. S(null)rabeprazole is an inhibitor of Hnull 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S（ - ）雷贝拉唑治疗人体溃疡的方法和组合物，同时显着减少与雷贝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S（ - ）异构体也可用于治疗胃食管反流。 S（ - ）雷贝拉唑是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：US20030036500A1

公开(公告)日：2003-02-20

申请号：US10233580

申请日：2002-09-04

Applicant: SEPRACOR, INC.

Inventor： Paul D. Rubin ,  Timothy Barberich

IPC: A61K031/00

CPC classification number: A61K31/135 ,  A61K31/415 ,  A61K31/445 ,  A61K38/16 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.

公开(公告)号：US20030018083A1

公开(公告)日：2003-01-23

申请号：US10222815

申请日：2002-08-19

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Nandkumar N. Bhongle

IPC: A61K031/137

CPC classification number: C07C217/74 ,  A61K31/137 ,  A61K31/277 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/02 ,  C07C215/64 ,  C07C2601/14

Abstract: Methods of preparing, and compositions comprising, derivatives of (null)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract translation: 公开了制备方法和包含（ - ） - 文拉法辛的衍生物的组合物。 还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和 体重增加，失禁，痴呆和相关疾病。

公开(公告)号：US20020183241A1

公开(公告)日：2002-12-05

申请号：US10146415

申请日：2002-05-16

Applicant: Sepracor Inc.

Inventor： John R. McCullough

IPC: A61K031/00

CPC classification number: A61K31/4545

Abstract: Methods for treating urinary incontinence, vertigo and motion sickness comprising administering a therapeutically effective amount of descarboethoxyloratadine, or a pharmaceutically acceptable salt thereof.

Abstract translation: 用于治疗尿失禁，眩晕和晕车的方法，包括给予治疗有效量的去甲氧基乙酰基吗啡胺或其药学上可接受的盐。

公开(公告)号：US20020151543A1

公开(公告)日：2002-10-17

申请号：US10158886

申请日：2002-06-03

Applicant: Sepracor Inc.

Inventor： Timothy J. Barberich ,  Paul D. Rubin ,  Dean A. Handley

IPC: A61K031/5513 ,  A61K031/137

CPC classification number: A61K31/495 ,  A61K31/445 ,  A61K31/505 ,  A61K31/55 ,  A61K2300/00

Abstract: Pharmaceutical compositions which comprises R(null) fluoxetine and one or more other biologically active compounds are disclosed. Methods of treating or preventing a disease or disorder, especially a psychotic or psychiatric disease or disorder, using the above pharmaceutical composition or by administering a R(null) fluoxetine in combination with one or more other biologically active compounds are also disclosed. Methods of treating patients having or at risk of having AIDS or HIV infection, cancer, cardiac disorder, post-myocardial depression and posttraumatic stress disorder using optically pure R(null) fluoxetine in combination with one or more other biologically active compounds are further disclosed.

Abstract translation: 公开了包含R（ - ）氟西汀和一种或多种其它生物活性化合物的药物组合物。 还公开了使用上述药物组合物或通过与一种或多种其它生物活性化合物组合施用R（ - ）氟西汀来治疗或预防疾病或障碍，特别是精神病或精神疾病或病症的方法。 进一步公开了使用光学纯的R（ - ）氟西汀与一种或多种其它生物活性化合物组合治疗患有AIDS或HIV感染或有风险患有癌症，心脏病，心肌后抑郁症和创伤后应激障碍的患者的方法。