公开(公告)号：US20020147220A1

公开(公告)日：2002-10-10

申请号：US10075617

申请日：2002-02-15

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：US20020137768A1

公开(公告)日：2002-09-26

申请号：US10108294

申请日：2002-03-28

Applicant: Sepracor, Inc.

Inventor： Raymond L. Woosley ,  A. K. Gunnar Aberg

IPC: A61K031/454

CPC classification number: A61K31/454 ,  A61K31/445 ,  A61K2300/00

Abstract: Methods and compositions are disclosed utilizing metabolic derivatives of astemizole for the treatment of allergic disorders while avoiding the concomitant liability of adverse effects associated with the astemizole. The metabolic derivatives of astemizole are also useful for the treatment of retinopathy and other small vessel disorders associated with diabetes mellitus and such other conditions as may be related to the antihistamine activity of astemizole. For example, the metabolic derivatives of astemizole are useful for the treatment of asthma, motion sickness, and vertigo, without the concomitant liability of adverse effects associated with astemizole. Furthermore, the metabolic derivatives of astemizole, in combination with non-steroidal anti-inflammatory agents or other non-narcotic analgesics, or in combination with a decongestant, cough suppressant/antitussive or expectorant, are useful for the treatment of cough, cold, cold-like, and/or flu symptoms and the discomfort, headache, pain, fever, and general malaise associated therewith, without the concomitant liability of adverse effects associated with astemizole.

Abstract translation: 公开了利用阿司咪唑的代谢衍生物治疗过敏性疾病的方法和组合物，同时避免与阿司咪唑相关的副作用的伴随的责任。 阿司咪唑的代谢衍生物也可用于治疗与糖尿病相关的视网膜病变和其它小血管障碍以及可能与阿司咪唑的抗组织胺活性相关的其它病症。 例如，阿司咪唑的代谢衍生物可用于治疗哮喘，晕车和眩晕，而不伴随与阿司咪唑有关的不良反应。 此外，阿司咪唑的代谢衍生物与非甾体抗炎剂或其他非麻醉止痛剂组合，或与减充血剂，止咳剂/镇咳药或祛痰剂组合可用于治疗咳嗽，感冒，感冒 类似，和/或流感症状以及与之相关的不适，头痛，疼痛，发烧和全身不适，而不伴随与阿司咪唑有关的不良反应。

公开(公告)号：US20020086904A1

公开(公告)日：2002-07-04

申请号：US10014592

申请日：2001-12-14

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：US20020082245A1

公开(公告)日：2002-06-27

申请号：US10013142

申请日：2001-12-10

Applicant: Sepracor Inc.

Inventor： William E. Yelle

IPC: A61K031/675 ,  A61K031/519

CPC classification number: A61K31/505 ,  A61K31/51 ,  A61K31/675

Abstract: Methods and compositions utilizing compounds represented by Formula III, 1 or a pharmaceutically acceptable salt thereof, for the treatment and prevention of psychoses in humans are disclosed. Compounds of the present invention exhibit fewer side effects than risperidone, a lessened liability toward drug-drug interactions than risperidone and a more predictable dosing regimen than risperidone. Compounds of the invention are also useful for the treatment and prevention of emesis and withdrawal syndromes.

Abstract translation: 公开了利用式III表示的化合物或其药学上可接受的盐用于治疗和预防人类精神病的方法和组合物。 与利培酮相比，本发明的化合物表现出比利培酮更少的副作用，比利培酮减轻了药物相互作用的责任，而且比利培酮更可预测的给药方案。 本发明的化合物还可用于治疗和预防呕吐和戒断综合征。

公开(公告)号：US20020077326A1

公开(公告)日：2002-06-20

申请号：US09993130

申请日：2001-11-14

Applicant: SEPRACOR INC.

Inventor： Mark G. Currie ,  Thomas P. Jerussi ,  Paul D. Rubin

IPC: A61K031/496

CPC classification number: C07D249/12 ,  A61K31/496

Abstract: Treatment of psychoses with (S)-hydroxynefazodone is disclosed.

Abstract translation: 公开了用（S） - 羟基吗啡酮治疗精神病

公开(公告)号：US20020058675A1

公开(公告)日：2002-05-16

申请号：US09992197

申请日：2001-11-14

Applicant: SEPRACOR INC.

Inventor： Mark G. Currie ,  Thomas P. Jerussi ,  Paul D. Rubin

IPC: A61K031/4745

CPC classification number: A61K31/496 ,  C07D249/12

Abstract: Treatment of psychoses with (R)-hydroxynefazodone is disclosed.

Abstract translation: 公开了用（R） - 羟基吗唑酮治疗精神病

公开(公告)号：US20020042433A1

公开(公告)日：2002-04-11

申请号：US09981108

申请日：2001-10-17

Applicant: SEPRACOR INC.

Inventor： William E. Yelle ,  Timothy J. Barberich ,  Paul D. Rubin

IPC: A61K031/4439

CPC classification number: A61K31/4439

Abstract: Methods and compositions are disclosed utilizing optically pure (null) lansoprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of lansoprazole. The optically pure (null) isomer is also useful for the treatment of gastroesophageal reflux. (null) Lansoprazole 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（+）兰索拉唑治疗人类溃疡的方法和组合物，同时显着减少与兰索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。 （+）兰索拉唑是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：US20010029260A1

公开(公告)日：2001-10-11

申请号：US09840117

申请日：2001-04-24

Applicant: Sepracor Inc.

Inventor： James W. Young

IPC: A61K031/44

CPC classification number: A61K31/44 ,  Y10S514/866 ,  Y10S514/929

Abstract: Methods and compositions are disclosed utilizing the optically pure (null) isomer of amlodipine. 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 amlodipine. The (null) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (null) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

Abstract translation: 公开利用氨氯地平的光学纯（ - ）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，同时避免与氨氯地平外消旋混合物相关的副作用的伴随责任。 氨氯地平的（ - ）异构体也可用于治疗心绞痛和其他可能与（ - ）氨氯地平作为钙通道拮抗剂如脑缺血，脑障碍，心律失常，心脏肥大，冠状动脉 血管痉挛，心肌梗塞，肾功能衰竭和急性肾功能衰竭，无与氨氯地平外消旋混合物相关的副作用的伴随责任。

公开(公告)号：US20010012842A1

公开(公告)日：2001-08-09

申请号：US09794006

申请日：2001-02-28

Applicant: Sepracor Inc.

Inventor： James W. Young ,  A.K. Gunnar Aberg

IPC: A61K031/496

CPC classification number: A61K31/47 ,  A61K31/496 ,  Y02A50/475 ,  Y02A50/481

Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin to treat bacterial infection. In particular, this compound is a potent drug for the treatment of Mycobacteria infection.

Abstract translation: 公开了使用洛美沙星的光学纯（S） - 异构体来治疗细菌感染的方法和组合物。 特别地，该化合物是用于治疗分枝杆菌感染的有效药物。

公开(公告)号：US20010011103A1

公开(公告)日：2001-08-02

申请号：US09803956

申请日：2001-03-13

Applicant: Sepracor Inc.

Inventor： John R. McCullough ,  Paul D. Rubin

IPC: A61K031/135

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.

Abstract translation: 公开利用安非他酮的光学纯的（+）异构体来帮助戒烟，治疗吸烟和尼古丁成瘾以及治疗疼痛的方法和组合物，包括但不限于慢性疼痛，神经性疼痛和反射性交感神经营养不良 ，以及其他疾病如发作性睡病，慢性疲劳综合征，纤维肌痛，季节性情感障碍和经前期综合征，同时避免与外消旋安非他酮相关的不良影响。