公开(公告)号：US06866839B2

公开(公告)日：2005-03-15

申请号：US10457123

申请日：2003-06-09

Applicant: Gunnar Aberg ,  John Morley

Inventor： Gunnar Aberg ,  John Morley

IPC: A61K9/00 ,  A61K9/12 ,  A61K31/135 ,  A61K31/16 ,  A61K31/167 ,  A61K31/17 ,  A61K31/235 ,  A61K31/27 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/52 ,  A61L9/04

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.

公开(公告)号：US20040229921A1

公开(公告)日：2004-11-18

申请号：US10872491

申请日：2004-06-22

Applicant: Sepracor Inc.

Inventor： James W. Young

IPC: A61K031/455

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：US20040180952A1

公开(公告)日：2004-09-16

申请号：US10806423

申请日：2004-03-23

Applicant: Sepracor Inc.

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

IPC: A61K031/277

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：US20040058973A1

公开(公告)日：2004-03-25

申请号：US10665430

申请日：2003-09-22

Applicant: Sepracor Inc.

Inventor： Paul D. Rubin ,  Timothy J. Barberich

IPC: A61K031/4178

CPC classification number: A61K31/415 ,  A61K31/4178 ,  A61K31/00 ,  A61K2300/00

Abstract: Methods for the treatment, management, or prevention of apnea and apnea disorders, or symptoms thereof, using a therapeutically effective amount of substantially optically pure R(null) ondansetron, or a pharmaceutically acceptable salt thereof, substantially free of its S(null) stereoisomer

Abstract translation: 使用治疗有效量的基本上不含其S（ - ）立体异构体的基本上光学上纯的R（+）昂丹司琼或其药学上可接受的盐来治疗，管理或预防呼吸暂停和呼吸暂停障碍或其症状的方法

公开(公告)号：US20040019111A1

公开(公告)日：2004-01-29

申请号：US10620704

申请日：2003-07-17

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：US20030171440A1

公开(公告)日：2003-09-11

申请号：US10308878

申请日：2002-12-02

Applicant: SEPRACOR INC.

Inventor： Chris Hugh Senanayake ,  Thomas P. Jerussi ,  Paul T. Grover ,  Qun Kevin Fang ,  Mark Currie

IPC: A61K031/137 ,  A61K031/704 ,  A61K031/277 ,  C07D211/22 ,  A61K031/445 ,  A61K031/40

CPC classification number: C07C217/74 ,  C07C217/52 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14

Abstract: Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. 1 In formula I, R1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.

Abstract translation: 式I的化合物在治疗由阿片剂受体活性和/或单胺活性调节的病症中是有效的。 在式I中，R 1选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基; R 2选自氢，羟基，氰基，卤代烷基，糖基，SO 2 R 5和OR 5; R 3和R 4独立地选自氢和低级烷基，或R 3和R 4与氮一起形成五元或六元杂环或取代的杂环; R 5选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基。

公开(公告)号：US20030083343A1

公开(公告)日：2003-05-01

申请号：US10314269

申请日：2002-12-06

Applicant: Sepracor Inc.

Inventor： Paul D. Rubin

IPC: A61K031/445

CPC classification number: A61K45/06 ,  A61K31/445 ,  A61K31/47 ,  A61K31/475 ,  A61K31/41 ,  A61K31/405 ,  A61K31/40 ,  A61K2300/00

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

公开(公告)号：US20030078303A1

公开(公告)日：2003-04-24

申请号：US10295871

申请日：2002-11-18

Applicant: Sepracor, Inc.

Inventor： James W. Young ,  Thomas P. Jerussi

IPC: A61K031/137 ,  A61K031/728

CPC classification number: A61K45/06 ,  A61K31/135 ,  A61K2300/00 ,  A61K31/00

Abstract: This invention encompasses methods for the treatment and prevention of disorders that include, 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. The invention further encompasses pharmaceutical compositions and dosage forms which comprise optically pure (null) sibutramine, optionally in combination with a phosphodiesterase inhibitor or a lipase inhibitor.

Abstract translation: 本发明包括治疗和预防包括但不限于进食障碍的疾病的方法; 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。 本发明还包括药物组合物和剂型，其包含光学纯的（+）西布曲明，任选与磷酸二酯酶抑制剂或脂肪酶抑制剂组合。

公开(公告)号：US20030050328A1

公开(公告)日：2003-03-13

申请号：US10206878

申请日：2002-07-29

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：US20020132830A1

公开(公告)日：2002-09-19

申请号：US10095846

申请日：2002-03-12

Applicant: Sepracor Inc.

Inventor： John Morley

IPC: A61K031/4535

CPC classification number: A61K31/52 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/167 ,  A61K31/17 ,  A61K31/235 ,  A61K31/27 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K2300/00

Abstract: Improved use of selective null2 sympathomimetic bronchodilator drugs in the therapy of obstructive or inflammatory airways disease, e.g. asthma, comprises use in enantiomeric rather than conventional racemic form. The improved use reduces occurrence of side effect, e.g. exacerbation of basal disease status or compromise or deterioration of lung function.

Abstract translation: 改进使用选择性β2拟交感神经支气管扩张剂药物治疗阻塞性或炎性气道疾病，例如 哮喘包括以对映体而不是常规的外消旋形式使用。 改进的用途减少副作用的发生，例如。 基础疾病状况恶化或肺功能损害或恶化。