公开(公告)号：US20040087661A1

公开(公告)日：2004-05-06

申请号：US10662997

申请日：2003-09-16

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Qun Kevin Fang ,  Mark G. Currie

IPC: A61K031/135

CPC classification number: C07C211/42 ,  A61K31/135 ,  A61K45/06 ,  C07C209/50 ,  C07C231/12 ,  C07C313/06 ,  C07C2601/14 ,  C07C2602/10 ,  C07C233/14

Abstract: Treatment of central nervous system disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine and with (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine is also disclosed.

Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺处理中枢神经系统疾病，用（1S，4R） 披露了4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺的方法。

公开(公告)号：US20030203970A1

公开(公告)日：2003-10-30

申请号：US10457123

申请日：2003-06-09

Applicant: Sepracor Inc.

Inventor： Gunnar Aberg ,  John Morley

IPC: A61K031/16 ,  A61L009/04

CPC classification number: A61K9/2018 ,  A61K9/008 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/135 ,  A61K31/16 ,  A61K31/167 ,  A61K31/17 ,  A61K31/235 ,  A61K31/27 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/52 ,  Y10S514/826 ,  A61K2300/00

Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, a low incidence of the development of tolerance and an increased duration of action, as compared to racemic formoterol.

Abstract translation: 公开了使用福莫特罗的纯（R，R）异构体的方法和组合物，其与外消旋福莫特罗相比，其是有效的支气管扩张剂，其副作用降低，耐受性发展的低发生率和作用持续时间增加。

公开(公告)号：US20030162825A1

公开(公告)日：2003-08-28

申请号：US10292368

申请日：2002-11-12

Applicant: SEPRACOR INC.

Inventor： Donald L. Heefner ,  Mark G. Currie ,  Richard Filip Rossi JR. ,  Charles M. Zepp

IPC: A61K031/473 ,  A61K031/404 ,  A61K031/401 ,  A61K031/34

CPC classification number: A61K31/34 ,  A61K31/401 ,  A61K31/404 ,  A61K31/405 ,  A61K31/473

Abstract: Methods and pharmaceutical compositions which inhibit the activity of D-amino acid oxidase (DAO) are disclosed. Inhibition of DAO improves memory, learning and cognition in individuals suffering from neurodegenerative diseases such as Alzheimer's, Huntington's or Parkinson's diseases; the methods and pharmaceutical compositions which inhibit the activity of DAO also improve cognitive dysfunctions associated with aging and improve catatonic schizophrenia. Several genera of heterocycle-2-carboxylic acids are disclosed as DAO inhibitors.

Abstract translation: 公开了抑制D-氨基酸氧化酶（DAO）活性的方法和药物组合物。 抑制DAO改善患有阿尔茨海默病，亨廷顿病或帕金森病等神经退行性疾病的个体的记忆，学习和认知; 抑制DAO活性的方法和药物组合物也改善与老化相关的认知功能障碍并改善紧张型精神分裂症。 公开了几种杂环-2-羧酸作为DAO抑制剂。

公开(公告)号：US20030096792A1

公开(公告)日：2003-05-22

申请号：US10278097

申请日：2002-10-23

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Qun K. Fang

IPC: A61K031/519 ,  A61K031/40 ,  A61K031/137

CPC classification number: A61K31/50 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/11 ,  A61K31/135 ,  A61K31/137 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/475 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions such as, but are not limited to: eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence. Pharmaceutical compositions and dosage forms are also disclosed which comprise a racemic or optically pure sibutramine metabolite and an optional additional pharmacologically active compound.

Abstract translation: 公开了用于治疗和预防疾病和病症的方法，例如但不限于：进食障碍; 体重增加; 肥胖; 过敏性肠综合征; 强迫症; 血小板粘附; 呼吸暂停 情感障碍，如注意力缺陷障碍，抑郁症和焦虑症; 男性和女性性功能障碍; 不安腿综合征 骨关节炎 药物滥用，包括尼古丁和可卡因成瘾; 发作性睡病 疼痛如神经性疼痛，糖尿病性神经病和慢性疼痛; 偏头痛 脑功能障碍; 慢性疾病如经前期综合征; 和失禁。 还公开了药物组合物和剂型，其包含外消旋或光学纯的西布曲明代谢物和任选的另外的药理活性化合物。

公开(公告)号：US20030086968A1

公开(公告)日：2003-05-08

申请号：US10256518

申请日：2002-09-26

Applicant: SEPRACOR INC.

Inventor： Nancy M. Gray

IPC: A61K031/4439

CPC classification number: A61K31/4439 ,  A61K31/44

Abstract: Methods and compositions are disclosed utilizing optically pure (null) 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 (null) isomer is also useful for the treatment of gastroesophageal reflux. (null) Pantoprazole 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（ - ）泮托拉唑用于治疗人类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：US20020183281A1

公开(公告)日：2002-12-05

申请号：US10160033

申请日：2002-06-04

Applicant: Sepracor Inc.

Inventor： Chrisantha Hugh Senanayake ,  Qun Kevin Fang ,  Zhengxu Han ,  Dhileepkumar Krishnamurthy

IPC: C08B037/16 ,  C07C249/02 ,  A61K031/724 ,  A61K031/13

CPC classification number: C07C251/18 ,  A61K31/11 ,  A61K31/135 ,  A61K45/06 ,  C07B2200/07 ,  C07C45/44 ,  C07C47/457 ,  C07C211/29 ,  C07C2601/04 ,  A61K2300/00 ,  A61K31/137

Abstract: Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.

Abstract translation: 公开了制备和使用西布曲明的外消旋和光学纯的代谢物及其药学上可接受的盐，溶剂合物和笼形物的方法。 还公开了药物组合物和剂型，其包含多巴胺再摄取抑制剂，例如外消旋或光学纯的西布曲明代谢物，以及任选的另外的药理活性化合物。

公开(公告)号：US20020147238A1

公开(公告)日：2002-10-10

申请号：US10062766

申请日：2002-02-05

Applicant: Sepracor, Inc.

Inventor： Thomas P. Jerussi ,  Paul D. Rubin

IPC: A61K031/192

CPC classification number: A61K31/137 ,  A61K31/00 ,  A61K31/165 ,  A61K31/192 ,  A61K31/415 ,  A61K31/43 ,  A61K31/435 ,  A61K31/46 ,  A61K31/465 ,  C07B2200/07 ,  C07C49/84 ,  C07D265/32 ,  A61K2300/00

Abstract: Methods of treating neuropathic pain, tinnitus, and related disorders are disclosed. These methods comprise the administration of optically pure R(null)-ketoprofen. Also disclosed are pharmaceutical compositions useful in the treatment of neuropathic pain and tinnitus which comprise optically pure R(null)-ketoprofen.

Abstract translation: 公开了治疗神经性疼痛，耳鸣和相关疾病的方法。 这些方法包括给予光学纯的R（ - ） - 酮洛芬。 还公开了可用于治疗包含光学纯的R（ - ） - 酮洛芬的神经性疼痛和耳鸣的药物组合物。

公开(公告)号：US20020115726A1

公开(公告)日：2002-08-22

申请号：US10076645

申请日：2002-02-19

Applicant: Sepracor, Inc.

Inventor： James W. Young

IPC: A61K031/137

CPC classification number: A61K31/137 ,  A61K31/135

Abstract: Methods and compositions are disclosed utilizing the optically pure (null)-isomer of bupropion, which is a potent drug for treating depression, Parkinson's disease, obesity, weight gain and other disorders.

Abstract translation: 公开利用安非他酮的光学纯（ - ） - 异构体的方法和组合物，其是用于治疗抑郁症，帕金森病，肥胖，体重增加和其它障碍的有效药物。

公开(公告)号：US20020099079A1

公开(公告)日：2002-07-25

申请号：US10046464

申请日：2001-10-19

Applicant: SEPRACOR INC.

Inventor： William E. Yelle

IPC: A61K031/4439

CPC classification number: A61K31/4439

Abstract: Methods and compositions are disclosed utilizing hydroxylansoprazole for the treatment of ulcers in humans. Hydroxylansoprazole exhibits a lessened liability toward drug-drug interactions than lansoprazole and a more predictable dosing regimen than lansoprazole. Hydroxylansoprazole is also useful for the treatment of gastroesophageal reflux and other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

Abstract translation: 公开了利用羟基索非唑来治疗人类溃疡的方法和组合物。 羟考兰唑与兰索拉唑相比显着降低药物相互作用的责任，比兰索拉唑更可预测的给药方案。 羟基索非唑还可用于治疗胃食管反流和其他与胃分泌过多相关的病症，例如Zollinger-Ellison综合征。

公开(公告)号：US20020086854A1

公开(公告)日：2002-07-04

申请号：US10084250

申请日：2002-02-28

Applicant: Sepracor, Inc.

Inventor： Paul D. Rubin

IPC: A61K031/454 ,  A61K031/415

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

Abstract: Methods and pharmaceutical compositions employing norastemizole and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma or the symptoms thereof. Also included are methods and compositions employing norastemizole and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma or the symptoms thereof.

Abstract translation: 使用诺尔阿司咪唑和白三烯抑制剂用于治疗或预防炎症或过敏性疾病如哮喘或其症状的方法和药物组合物。 还包括使用诺尔阿司咪唑和减充血剂用于治疗或预防炎症或过敏性疾病如哮喘或其症状的方法和组合物。