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    Methods of treating and preventing depression using didesmethylsibutramine
    1.
    发明申请
    Methods of treating and preventing depression using didesmethylsibutramine 审中-公开
    使用二甲基西布曲明治疗和预防抑郁症的方法

    公开(公告)号：US20040092481A1

    公开(公告)日：2004-05-13

    申请号：US10693980

    申请日：2003-10-28

    申请人： Sepracor, Inc.

    发明人： Thomas P. Jerussi

    IPC分类号： A61K031/724 ,  A61K031/137 ,  A61K031/519

    CPC分类号： 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

    摘要： 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.

    摘要翻译： 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。

    Methods of treating or preventing erectile dysfunction
    2.
    发明申请
    Methods of treating or preventing erectile dysfunction 失效
    治疗或预防勃起功能障碍的方法

    公开(公告)号：US20030195261A1

    公开(公告)日：2003-10-16

    申请号：US10395298

    申请日：2003-03-25

    申请人： Sepracor Inc.

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

    IPC分类号： A61K031/137

    CPC分类号： A61K45/06 ,  A61K31/11 ,  A61K31/135 ,  A61K31/137 ,  A61K2300/00

    摘要： Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutrarnine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3 antagonists.

    摘要翻译： 公开了用于治疗和预防疾病和病症的方法，包括但不限于勃起功能障碍，情感障碍，体重增加，脑功能障碍，疼痛，强迫症，药物滥用，慢性障碍，焦虑，进食障碍 ，偏头痛和失禁。 所述方法包括施用多巴胺再摄取抑制剂和任选的另外的药理活性化合物。 还公开了包含多巴胺再摄取抑制剂和任选的另外的药理学活性化合物的药物组合物和剂型。 优选的多巴胺再摄取抑制剂是外消旋或光学纯的西布睾胺代谢物及其药学上可接受的盐，溶剂化物和包合物。 优选的另外的药理活性化合物包括影响中枢神经系统的药物，例如5-HT <3> 拮抗剂。

    Compositions of optically pure (+) norcisapride
    5.
    发明申请
    Compositions of optically pure (+) norcisapride 失效
    光学纯（+）诺西沙必利组合物

    公开(公告)号：US20010020031A1

    公开(公告)日：2001-09-06

    申请号：US09809165

    申请日：2001-03-16

    申请人： Sepracor Inc.

    发明人： John R. McCullough ,  Thomas P. Jerussi

    IPC分类号： A61K031/445

    CPC分类号： A61K31/495 ,  A61K31/4468 ,  A61K2300/00

    摘要： Compositons employing and methods utilizing the optically pure (null) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (null) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (null) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

    摘要翻译： 公开了使用诺西西滨的旋光纯（+）异构体的复合物和方法。 令人惊讶地发现，该化合物是用于治疗中枢神经系统疾病的有效药物。 化合物（+）诺西沙必利还被发现是一种有效的止吐剂。 最后，诺西沙必利的（+）异构体也避免了某些不良副作用和某些不良药物相互作用。

    Antiemetic compositions of optically pure (+) norcisapride
    6.
    发明申请
    Antiemetic compositions of optically pure (+) norcisapride 审中-公开
    光学纯（+）诺西沙必利的止吐组合物

    公开(公告)号：US20040044039A1

    公开(公告)日：2004-03-04

    申请号：US10653072

    申请日：2003-09-03

    申请人： Sepracor Inc.

    发明人： John R. McCullough ,  Thomas P. Jerussi

    IPC分类号： A61K031/445

    CPC分类号： A61K31/495 ,  A61K31/4468 ,  A61K2300/00

    摘要： Compositons employing and methods utilizing the optically pure (null) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (null) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (null) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

    摘要翻译： 公开了使用诺西西滨的旋光纯（+）异构体的复合物和方法。 令人惊讶地发现，该化合物是用于治疗中枢神经系统疾病的有效药物。 化合物（+）诺西沙必利还被发现是一种有效的止吐剂。 最后，诺西沙必利的（+）异构体也避免了某些不良副作用和某些不良药物相互作用。

    Methods of treating or preventing weight gain, obesity, and related disorders
    7.
    发明申请
    Methods of treating or preventing weight gain, obesity, and related disorders 有权
    治疗或预防体重增加，肥胖和相关疾病的方法

    公开(公告)号：US20020188029A1

    公开(公告)日：2002-12-12

    申请号：US10000806

    申请日：2001-12-04

    申请人： Sepracor Inc.

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

    IPC分类号： A61K031/137

    CPC分类号： A61K45/06 ,  A61K31/11 ,  A61K31/135 ,  A61K31/137 ,  A61K2300/00

    摘要： Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3 antagonists.

    摘要翻译： 公开了用于治疗和预防疾病和病症的方法，包括但不限于勃起功能障碍，情感障碍，体重增加，脑功能障碍，疼痛，强迫症，药物滥用，慢性障碍，焦虑，进食障碍 ，偏头痛和失禁。 所述方法包括施用多巴胺再摄取抑制剂和任选的另外的药理活性化合物。 还公开了包含多巴胺再摄取抑制剂和任选的另外的药理学活性化合物的药物组合物和剂型。 优选的多巴胺再摄取抑制剂是外消旋或光学纯的西布曲明代谢物及其药学上可接受的盐，溶剂化物和包合物。 优选的额外的药理活性化合物包括影响中枢神经系统的药物，例如5-HT 3拮抗剂。

    Derivatives of (-)- and (+)-venlafaxine and methods of preparing and using the same
    8.
    发明申请
    Derivatives of (-)- and (+)-venlafaxine and methods of preparing and using the same 审中-公开
    （ - ） - 和（+） - 文拉法辛的衍生物及其制备和使用方法

    公开(公告)号：US20040180952A1

    公开(公告)日：2004-09-16

    申请号：US10806423

    申请日：2004-03-23

    申请人： Sepracor Inc.

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

    IPC分类号： A61K031/277

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

    摘要： 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.

    摘要翻译： 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。

    Tramadol analogs and uses thereof
    10.
    发明申请
    Tramadol analogs and uses thereof 有权
    曲马多类似物及其用途

    公开(公告)号：US20030171440A1

    公开(公告)日：2003-09-11

    申请号：US10308878

    申请日：2002-12-02

    申请人： SEPRACOR INC.

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

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

    CPC分类号： C07C217/74 ,  C07C217/52 ,  C07C255/59 ,  C07C2601/02 ,  C07C2601/14

    摘要： 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.

    摘要翻译： 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。