公开(公告)号：WO2005097132A3

公开(公告)日：2006-02-16

申请号：PCT/US2005011593

申请日：2005-04-05

Applicant: SEPRACOR INC ,  WESSEL THOMAS ,  CARON JUDY

Inventor： WESSEL THOMAS ,  CARON JUDY

IPC: A61K31/4985 ,  A61P9/10 ,  A61P15/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P25/28 ,  A61P29/00

CPC classification number: A61K31/4985

Abstract: The invention relates to the use of eszopiclone for the treatment of symptoms accompanying perimenopause or menopause, autism, aphasia, jet lag, low-level chronic pain, and fatigue associated with pain.

Abstract translation: 本发明涉及依曲普洛酮用于治疗伴有围绝经期或绝经期，自闭症，失语症，时差，低水平慢性疼痛和与疼痛有关的疲劳的症状。

公开(公告)号：WO2005097191A3

公开(公告)日：2005-12-08

申请号：PCT/US2005009910

申请日：2005-03-25

Applicant: SEPRACOR INC ,  BARBERICH TIMOTHY J

Inventor： BARBERICH TIMOTHY J

IPC: A61K31/44 ,  A61P9/00

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旋光纯（S） - 氨氯地平和HMG-CoA还原酶抑制剂的药物组合物。 在优选的实施方案中，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。 在优选的实施方案中，胆固醇吸收增强剂是依泽替米贝。 本发明的另一方面涉及包含光学纯的（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进一步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，高脂血症或心脏病症的患者的方法。 本发明还涉及治疗高血压和高脂血症的方法。

公开(公告)号：WO2005066143A3

公开(公告)日：2005-10-20

申请号：PCT/US2004043547

申请日：2004-12-28

Applicant: SEPRACOR INC ,  FANG Q KEVIN ,  HOPKINS SETH ,  JONES STEVEN

Inventor： FANG Q KEVIN ,  HOPKINS SETH ,  JONES STEVEN

IPC: A61K31/42 ,  C07D261/20 ,  A61K31/423 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D261/20

Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: I wherein Z1 is N or CR3; Z2 is N or CR4; Z3 is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.

Abstract translation: 增加D-丝氨酸氧化的毒性产物的D-丝氨酸浓度和浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛或预防神经元功能丧失 神经变性疾病的特征包括向需要治疗的受试者施用治疗量的式I化合物或其药学上可接受的盐或溶剂化物：其中Z 1是N或CR 3; Z2是N或CR4; Z3是O或S; A是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌或其混合物; R 1，R 2，R 3和R 4独立地选自氢，烷基，羟基烷氧基，芳基，酰基，卤素，氰基，卤代烷基，NHCOOR 5和SO 2 NH 2; R5是芳基，芳基烷基，杂芳基或杂芳基烷基; R1，R2，R3和R4中的至少一个不是氢; 并且Z1和Z2中的至少一个不是N.

公开(公告)号：WO2005066135A3

公开(公告)日：2005-10-06

申请号：PCT/US2004043791

申请日：2004-12-28

Applicant: SEPRACOR INC ,  FANG Q KEVIN ,  HOPKINS SETH ,  JONES STEVEN

Inventor： FANG Q KEVIN ,  HOPKINS SETH ,  JONES STEVEN

IPC: A61K31/401 ,  A61K31/405 ,  A61K31/415 ,  A61K31/416 ,  C07D207/34 ,  C07D209/42 ,  C07D209/44 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D231/56 ,  C07D491/04 ,  A61K31/403 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D231/56 ,  C07D207/34 ,  C07D209/42 ,  C07D209/44 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D491/04

Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof: (I) wherein R and R are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR ; or R and R , taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR R )n; R is hydrogen, alkyl or M ; M is aluminum, calcium, lithium, magnesium, potassium , sodium , zinc ion or a mixture thereof; Z is N or CR ; R is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR ; R is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R and R are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R , R and R is other than hydrogen; and at least one of X and Y is (CR R )n. D-serine or cycloserine may be coadministered along with the compound of formula (I).

Abstract translation: 用于提高D-丝氨酸氧化的毒性产物的D-丝氨酸浓度和降低浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛或预防神经元功能丧失特征 神经变性疾病包括向需要治疗的受试者施用治疗有效量的式（I）化合物或其药学上可接受的盐或溶剂化物：（I）其中R 1和R 2独立地选自 由氢，卤素，硝基，烷基，酰基，烷基芳基和XYR 5组成; 或者R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R 3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或其混合物; Z是N或CR 4; R 4选自氢，卤素，硝基，烷基，烷基芳基和XYR 5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R 6和R 7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可与式（I）化合物一起共同施用。

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：WO2005066143A2

公开(公告)日：2005-07-21

申请号：PCT/US2004/043547

申请日：2004-12-28

Applicant: SEPRACOR INC. ,  FANG, Q. Kevin ,  HOPKINS, Seth ,  JONES, Steven

Inventor： FANG, Q. Kevin ,  HOPKINS, Seth ,  JONES, Steven

IPC: C07D263/00

CPC classification number: C07D261/20

Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: I wherein Z1 is N or CR3; Z2 is N or CR4; Z3 is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.

Abstract translation: 提高D-丝氨酸浓度和降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能丧失的方法 神经变性疾病的特征包括向需要治疗的受试者施用治疗量的式I化合物或其药学上可接受的盐或溶剂化物：其中Z 1是N或CR 3; Z2为N或CR4; Z3为O或S; A为氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌或它们的混合物; R 1，R 2，R 3和R 4独立地选自氢，烷基，羟基烷氧基，芳基，酰基，卤素，氰基，卤代烷基，NHCOOR 5和SO 2 NH 2; R5是芳基，芳基烷基，杂芳基或杂芳基烷基; R 1，R 2，R 3和R 4中的至少一个不是氢; 并且Z1和Z2中的至少一个不是N.

公开(公告)号：WO2005066135A2

公开(公告)日：2005-07-21

申请号：PCT/US2004/043791

申请日：2004-12-28

Applicant: SEPRACOR INC. ,  FANG, Q., Kevin ,  HOPKINS, Seth ,  JONES, Steven

Inventor： FANG, Q., Kevin ,  HOPKINS, Seth ,  JONES, Steven

IPC: C07D231/00

CPC classification number: C07D231/56 ,  C07D207/34 ,  C07D209/42 ,  C07D209/44 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D491/04

Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof: (I) wherein R 1 and R 2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR 5 ; or R 1 and R 2 , taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR 6 R 7 ) n ; R 3 is hydrogen, alkyl or M + ; M is aluminum, calcium, lithium, magnesium, potassium , sodium , zinc ion or a mixture thereof; Z is N or CR 4 ; R 4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR 5 ; R 5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R 6 and R 7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R 1 , R 2 and R 4 is other than hydrogen; and at least one of X and Y is (CR 6 R 7 ) n . D-serine or cycloserine may be coadministered along with the compound of formula (I).

Abstract translation: 提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失 的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式（I）化合物或其药学上可接受的盐或溶剂化物：（I）其中R 1和R 2独立地选自 从氢，卤素，硝基，烷基，酰基，烷基芳基和XYR 5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R 3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR 4; R 4选自氢，卤素，硝基，烷基，烷基芳基和XYR 5; R 5选自芳基，取代芳基，杂芳基和取代的杂芳基; R 6和R 7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式（I）化合物一起共同施用。

公开(公告)号：WO2004043447A3

公开(公告)日：2005-01-27

申请号：PCT/US0336269

申请日：2003-11-13

Applicant: SEPRACOR INC ,  CURRIE MARK G ,  HEEFNER DONALD L ,  RUBIN PAUL ,  ZEPP CHARLES M

Inventor： CURRIE MARK G ,  HEEFNER DONALD L ,  RUBIN PAUL ,  ZEPP CHARLES M

IPC: A61K31/17 ,  A61K31/495 ,  A61P27/16

CPC classification number: A61K31/17 ,  A61K31/495

Abstract: Ototoxic side-effects have either limited the application of an important group of antibiotics, aminoglycoside antibiotics, or have added further burden to those who have to resort to platinum-containing antineoplastic agents to treat life-threatening tumors. The present invention discloses pharmaceutical compositions that prevent or treat the ototoxic side-effects of aminoglycoside antibiotics and platinum-containing antineoplastic agents. The otoprotective compositions disclosed herein can also be used to treat noise induced hearing loss.

Abstract translation: 耳毒性副作用限制了一组重要的抗生素，氨基糖苷类抗生素的应用，或者为那些不得不使用含铂抗肿瘤剂治疗危及生命的肿瘤的人增加了进一步的负担。 本发明公开了预防或治疗氨基糖苷类抗生素和含铂抗肿瘤剂的耳毒性副作用的药物组合物。 本文公开的保护性组合物也可用于治疗噪声引起的听力损失。

公开(公告)号：WO2004047845A1

公开(公告)日：2004-06-10

申请号：PCT/US2003/024732

申请日：2003-08-07

Applicant: SEPRACOR INC.

Inventor： CURRIE, Mark, G. ,  JONES, Steve ,  GROVER, Paul ,  SENANAYAKE, Chris, H. ,  FANG, Kevin, Q.

IPC: A61K31/573

CPC classification number: A61K45/06 ,  A61K31/137 ,  A61K31/56 ,  A61K31/573 ,  A61K31/58 ,  Y10S514/87 ,  A61K2300/00

Abstract: Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula (I) are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.

Abstract translation: 公开了含有β2肾上腺素能激动剂与式（I）的碳酸酯和氨基甲酸酯组合的组合物。 该组合物可用于治疗支气管痉挛，用于诱发支气管扩张和治疗鼻炎，哮喘和慢性阻塞性肺病（COPD）和炎性疾病，特别是通过吸入治疗。

公开(公告)号：WO2003086393A1

公开(公告)日：2003-10-23

申请号：PCT/US2003/009399

申请日：2003-03-27

Applicant: SEPRACOR, INC.

Inventor： HAUSKE, James, R. ,  HOLLAND, Joanne, M. ,  RADEKE, Heiki

IPC: A61K31/435

CPC classification number: C07D221/04 ,  A61K31/495 ,  C07D221/16 ,  C07D295/13 ,  C07D487/04

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine receptors. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, and senile dementia.

Abstract translation: 本发明的一个方面涉及新的杂环化合物。 本发明的第二方面涉及新型杂环化合物作为各种细胞受体（包括血清素受体和多巴胺受体）的配体的用途。 本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病， 止痛，精神分裂症，帕金森病，不宁腿综合征，睡眠障碍，注意缺陷多动障碍，肠易激综合征，早泄，月经性烦躁综合症，尿失禁，炎性疼痛，神经性疼痛，莱氏阴道炎，威尔逊病，图雷特综合征， 精神障碍，中风和老年痴呆。