公开(公告)号：WO2005123071A1

公开(公告)日：2005-12-29

申请号：PCT/US2005/021171

申请日：2005-06-14

Applicant: SEPRACOR INC. ,  BARBERICH, Timothy, J.

Inventor： BARBERICH, Timothy, J.

IPC: A61K31/41

CPC classification number: A61K31/415 ,  A61K31/135 ,  A61K31/41 ,  A61K31/54 ,  A61K31/70 ,  A61K45/06 ,  A61K2300/00

Abstract: This invention related to methods of treating, preventing and managing various pulmonary or respiratory diseases or disorders using albuterol in combination with calcium activated potassium channel openers. Pharmaceuticals compositions comprising albuterol and calcium activated potassium channel openers are also disclosed.

Abstract translation: 本发明涉及使用沙丁胺醇与钙活化钾通道开放剂联合治疗，预防和治疗各种肺或呼吸系统疾病或病症的方法。 还公开了包含沙丁胺醇和钙活化的钾通道开放剂的药物组合物。

公开(公告)号：WO2005072715A1

公开(公告)日：2005-08-11

申请号：PCT/US2005/002785

申请日：2005-01-28

Applicant: SEPRACOR, INC. ,  BARBERICH, Timothy, J.

Inventor： BARBERICH, Timothy, J.

IPC: A61K31/137

CPC classification number: A61K31/137

Abstract: This invention relates, in part, to methods of treating, preventing and/or managing a sleep disorder using enantiomerically pure (S)-didesmethylsibutramine, or a pharmaceutically acceptable salt, hydrate, solvate, clathrate or prodrug thereof. Specific methods for treating, preventing and/or managing insomnia, wakefulness, circadian rhythm sleep disorders, shift work sleep disorder, and periodic limb movement disorder are also disclosed.

Abstract translation: 本发明部分地涉及使用对映异构纯的（S） - 二甲基西布曲明或其药学上可接受的盐，水合物，溶剂合物，包合物或前药治疗，预防和/或治疗睡眠障碍的方法。 还公开了治疗，预防和/或治疗失眠，觉醒，昼夜节律睡眠障碍，转移工作睡眠障碍和周期性肢体运动障碍的具体方法。

公开(公告)号：WO1993009769A1

公开(公告)日：1993-05-27

申请号：PCT/US1992000888

申请日：1992-02-05

Applicant: SEPRACOR, INC.

Inventor： SEPRACOR, INC. ,  YOUNG, James, W. ,  BARBERICH, Timothy, J.

IPC: A61K31/13

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is a potent antidepressant and appetite suppressant substantially free of unwanted, adverse toxic or psychological effects. In addition, methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is useful in treating migraine headaches, pain, in particular chronic pain, and obsessive-compulsive disorders. Further, methods and compositions for treating a condition alleviated or improved by inhibition of serotonin uptake in serotonergic neurons and platelets in a human using optically pure S(+) fluoxetine are disclosed.

Abstract translation: 公开了使用氟西汀的纯S（+）异构体的方法和组合物，其是有效的抗抑郁药和食欲抑制剂，其基本上不含有害的，不利的毒性或心理作用。 此外，利用氟西汀的纯S（+）异构体可用于治疗偏头痛，疼痛，特别是慢性疼痛和强迫症的方法和组合物被公开。 此外，公开了通过使用光学纯的S（+）氟西汀在人体中抑制5-羟色胺能神经元和血小板中5-羟色胺摄取而缓解或改善的病症的方法和组合物。

公开(公告)号：WO1992016197A1

公开(公告)日：1992-10-01

申请号：PCT/US1992001950

申请日：1992-03-10

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  YOUNG, James, W. ,  BARBERICH, Timothy, J.

IPC: A61K31/135

CPC classification number: A61K31/425 ,  A61K31/135 ,  A61K31/50 ,  A61K31/505 ,  C07C43/10 ,  C07C43/164 ,  C07C69/63 ,  C07C69/708 ,  C07C205/40 ,  C07C233/36 ,  C07C235/08 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  Y10S514/821 ,  Y10S514/929 ,  A61K2300/00

Abstract: Optically pure (S) metoprolol, which is substantially free of the (R) enantiomer, is a potent beta-blocker for treating myocardial infarction and for relieving the symptoms of angina pectoris, cardiac arrhythmia and hypertension in individuals. A method is disclosed utilizing the optically pure (S) configurational enantiomer of metoprolol for treating cardiovascular disorders while reducing undesirable side effects associated with the administration of beta-blockers.

Abstract translation: 基本上不含（R）对映异构体的光学纯（S）美托洛尔是治疗心肌梗塞和缓解个体心绞痛，心律失常和高血压症状的有效β受体阻滞剂。 公开了利用美托洛尔的光学纯（S）构型对映异构体治疗心血管疾病同时减少与β-受体阻滞剂相关的不良副作用的方法。

公开(公告)号：WO2005097191A2

公开(公告)日：2005-10-20

申请号：PCT/US2005/009910

申请日：2005-03-25

Applicant: SEPRACOR INC. ,  BARBERICH, Timothy, J.

Inventor： BARBERICH, Timothy, J.

IPC: A61K45/00

CPC classification number: A61K45/06 ,  A61K31/44 ,  A61K2300/00

Abstract: One aspect of the present invention relates to pharmaceutical compositions comprising optically pure (S)-amlodipine and a HMG-CoA reductase inhibitor. In a preferred embodiment, the HMG-CoA reductase inhibitor is lovastatin. Another aspect of the present invention relates to a pharmaceutical composition comprising optically pure (S)-amlodipine and a cholesterol absorption inhibitor. In a prefered embodiment, the cholesterol absorption enhancer is ezetimibe. Another aspect of the present invention relates to a pharmaceutical composition comprising optically pure (S)-amlodipine, a HMG- CoA reductase inhibitor, and a cholesterol absorption inhibitor. Another aspect of the present invention relates to the aforementioned pharmaceutical compositions further comprising niacin. The invention also relates to methods for treating a patient suffering from hypertension, hyperlipidemia, or a cardiac disorder. The invention also relates to methods for the treatment of hypertension and hyperlipidemia.

Abstract translation: 本发明的一个方面涉及包含光学纯（S） - 氨氯地平和HMG-CoA还原酶抑制剂的药物组合物。 在一个优选的实施方案中，HMG-CoA还原酶抑制剂是洛伐他汀。 本发明的另一方面涉及包含光学纯（S） - 氨氯地平和胆固醇吸收抑制剂的药物组合物。 在一个优选的实施方案中，胆固醇吸收促进剂是依泽替米贝。 本发明的另一方面涉及包含光学纯（S） - 氨氯地平，HMG-CoA还原酶抑制剂和胆固醇吸收抑制剂的药物组合物。 本发明的另一方面涉及还包含烟酸的上述药物组合物。 本发明还涉及治疗患有高血压，高脂血症或心脏病的患者的方法。 本发明还涉及治疗高血压和高脂血症的方法。

公开(公告)号：WO2005097095A1

公开(公告)日：2005-10-20

申请号：PCT/US2005/011489

申请日：2005-04-05

Applicant: SEPRACOR INC. ,  BARBERICH, Timothy, J.

Inventor： BARBERICH, Timothy, J.

IPC: A61K31/167

CPC classification number: A61K31/167 ,  A61K31/404 ,  A61K31/47 ,  A61K45/06 ,  C07C2601/16 ,  A61K2300/00

Abstract: This invention related to methods of treating, preventing and managing various pulmonary diseases or disorders using stereomerically pure (R,R)-formoterol in combination with other pharmacological agents such as leukotriene inhibitors and neurokinin receptor antagonists. Pharmaceutical compositions comprising (R,R)-formoterol and other pharmacological agents are also disclosed.

Abstract translation: 本发明涉及使用立体纯的（R，R） - 福莫特罗与其他药理学试剂如白三烯抑制剂和神经激肽受体拮抗剂组合治疗，预防和治疗各种肺部疾病或病症的方法。 还公开了包含（R，R） - 福莫特罗和其他药理学试剂的药物组合物。

公开(公告)号：WO1995028152A1

公开(公告)日：1995-10-26

申请号：PCT/US1995004508

申请日：1995-04-10

Applicant: SEPRACOR INC.

Inventor： SEPRACOR INC. ,  YOUNG, James, W. ,  BARBERICH, Timothy, J.

IPC: A61K31/135

CPC classification number: A61K31/135

Abstract: Methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is a potent antidepressant and appetite suppressant substantially free of unwanted, adverse toxic or psychological effects. In addition, methods and compositions are disclosed utilizing the pure S(+) isomer of fluoxetine which is useful in treating migraine headaches, pain, in particular chronic pain, obsessive-compulsive disorders, sexual dysfunction and memory disorders. Further, methods and compositions for treating a condition alleviated or improved by inhibition of serotonin uptake in serotonergic neurons and platelets in a human using optically pure S(+) fluoxetine are disclosed.

Abstract translation: 公开了使用氟西汀的纯S（+）异构体的方法和组合物，其是有效的抗抑郁药和食欲抑制剂，其基本上不含有害的，不利的毒性或心理作用。 此外，公开了使用氟西汀的纯S（+）异构体的方法和组合物，其可用于治疗偏头痛，疼痛，特别是慢性疼痛，强迫症，性功能障碍和记忆障碍。 此外，公开了通过使用光学纯的S（+）氟西汀在人体中抑制5-羟色胺能神经元和血小板中5-羟色胺摄取而缓解或改善的病症的方法和组合物。

公开(公告)号：WO2005079851A2

公开(公告)日：2005-09-01

申请号：PCT/US2005/003937

申请日：2005-02-07

Applicant: SEPRACOR, INC. ,  BARBERICH, Timothy, J.

Inventor： BARBERICH, Timothy, J.

IPC: A61K45/06

CPC classification number: A61K45/06 ,  A61K31/137 ,  A61K31/425 ,  A61K31/4985 ,  A61K2300/00

Abstract: The present invention generally to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)-N-desmethylzoplicone. In a preferred embodiment, the dopanime agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)-N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders. In addition, the present invention relates to a method of treating a patient suffering from restless-leg syndrome, periodic-limb-movement disorder, a sleep abnormality, or insomnia comprising coadministering a therapeutically effective amount of a dopamine agonist and a therapeutically effective amount of a sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S). N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)-N-desmethylzopiclone.

Abstract translation: 本发明一般涉及包含多巴胺激动剂和镇静剂的药物组合物。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基叠氮基。 在优选的实施方案中，所述多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 本发明的药物组合物可用于治疗不宁腿综合征和周期性肢体运动障碍以及各种睡眠障碍。 此外，本发明涉及治疗患有不宁腿综合征，周期性肢体运动障碍，睡眠异常或失眠的患者的方法，其包括共同施用治疗有效量的多巴胺激动剂和治疗有效量的 镇静剂。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）。 N-二desmethylzopiclone。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。

公开(公告)号：WO2005063248A1

公开(公告)日：2005-07-14

申请号：PCT/US2004/042938

申请日：2004-12-21

Applicant: SEPRACOR INC. ,  LALJI, Karim ,  BARBERICH, Timothy, J.

Inventor： LALJI, Karim ,  BARBERICH, Timothy, J.

IPC: A61K31/495

CPC classification number: A61K45/06 ,  A61K31/165 ,  A61K31/195 ,  A61K31/4164 ,  A61K31/495 ,  A61K31/7008 ,  A61K31/724 ,  A61K2300/00

Abstract: One aspect of the present invention relates to pharmaceutical compositions comprising a compound that modulates the orexin system and a sedative agent. In a preferred embodiment, the compound that modulates the orexin system is modafinil and the sedative agent is ( S )-zopiclone. The pharmaceutical compositions of the invention are useful in the treatment of various sleep disorders. In addition, the present invention relates to a method of treating a patient suffering from a sleep abnormality or insomnia comprising administering a therapeutically effective amount of a pharmaceutical composition of the invention.

Abstract translation: 本发明的一个方面涉及包含调节食欲素系统的化合物和镇静剂的药物组合物。 在优选的实施方案中，调节食欲素系统的化合物是莫达非尼，镇静剂是（S） - 佐匹克隆。 本发明的药物组合物可用于治疗各种睡眠障碍。 此外，本发明涉及治疗患有睡眠异常或失眠的患者的方法，包括给予治疗有效量的本发明的药物组合物。

公开(公告)号：WO2005060968A1

公开(公告)日：2005-07-07

申请号：PCT/US2004/040962

申请日：2004-12-08

Applicant: SEPRACOR INC. ,  LALJI, Karim ,  BARBERICH, Timothy, J. ,  CARON, Judy ,  WESSEL, Thomas

Inventor： LALJI, Karim ,  BARBERICH, Timothy, J. ,  CARON, Judy ,  WESSEL, Thomas

IPC: A61K31/4985

CPC classification number: A61K31/4985 ,  A61K31/137 ,  A61K31/138 ,  A61K31/495 ,  A61K31/724 ,  A61K45/06 ,  A61K2300/00

Abstract: One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT 2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT 2A modulator or DRI.

Abstract translation: 本发明的一个方面涉及含有两种或更多种活性剂的药物组合物，当它们一起被用于治疗，例如失眠和/或抑郁症时。 药物组合物的第一组分是调节GABA受体的化合物。 药物组合物的第二组分是5-羟色胺再摄取抑制剂，去甲肾上腺素再摄取抑制剂，5-HT2A调节剂或多巴胺再摄取抑制剂。 在某些实施方案中，药物组合物包含依佐匹克。 在优选的实施方案中，药物组合物包含依佐匹克和氟西汀。 本发明还涉及一种治疗睡眠异常，治疗失眠，治疗抑郁症，增强抗抑郁药治疗，引发剂量保留作用，减少抑郁症复发，改善抗抑郁治疗疗效或提高抗抑郁治疗耐受性的方法，包括 向有需要的患者共同施用GABA受体调节化合物; 和SRI，NRI，5-HT2A调节剂或DRI。