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1. 发明申请

WO2008021932A2 MILNACIPRAN FOR THE TREATMENT OF COGNITIVE DYSFUNCTION ASSOCIATED WITH FIBROMYALGIA 审中-公开
标题翻译：治疗与纤维母细胞瘤相关的认知功能障碍的MILNACIPRAN
公开(公告)号：WO2008021932A2
公开(公告)日：2008-02-21
申请号：PCT/US2007075549
申请日：2007-08-09
申请人： CYPRESS BIOSCIENCE INC , GENDREAU MICHAEL R , KRANZLER JAY D , RAO SRINIVAS G
发明人： GENDREAU MICHAEL R , KRANZLER JAY D , RAO SRINIVAS G
IPC分类号： A61K31/165 , A61K31/195 , A61K31/197 , A61K31/4168 , A61K31/428 , A61K31/433 , A61K31/48 , A61K31/485
CPC分类号： A61K31/165 , A61K31/195 , A61K31/197 , A61K31/4168 , A61K31/428 , A61K31/433 , A61K31/48 , A61K31/485 , A61K45/06 , A61K2300/00
摘要： Methods for treating cognitive dysfunction associated with fibromyalgia by administering high-dose milnacipran to a patient suffering from such cognitive dysfunction are provided. Also provided are methods for the long-term treatment of cognitive dysfunction associate with FMS by administering milnacipran to a patient suffering from such cognitive dysfunction.
摘要翻译：提供了通过对患有这种认知功能障碍的患者施用高剂量米那普仑来治疗与纤维肌痛相关的认知功能障碍的方法。还提供了通过对患有这种认知功能障碍的患者施用米那普仑来长期治疗与FMS相关的认知功能障碍的方法。

2. 发明申请

WO2008019388A2 MILNACIPRAN FOR THE TREATMENT OF FATIGUE ASSOCIATED WITH FIBROMYALGIA SYNDROME 审中-公开
标题翻译：米非司酮用于治疗与纤维化综合征相关的疲劳
公开(公告)号：WO2008019388A2
公开(公告)日：2008-02-14
申请号：PCT/US2007075555
申请日：2007-08-09
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , GENDREAU MICHAEL R , KRANZLER JAY D
发明人： RAO SRINIVAS G , GENDREAU MICHAEL R , KRANZLER JAY D
IPC分类号： A61K31/165 , A61K31/195 , A61K31/197 , A61K31/4168 , A61K31/428 , A61K31/433 , A61K31/48 , A61K31/485 , A61K31/496
CPC分类号： A61K31/165 , A61K31/195 , A61K31/197 , A61K31/4168 , A61K31/428 , A61K31/433 , A61K31/48 , A61K31/485 , A61K31/496
摘要： Methods for treating fatigue associated with fibromyalgia by administering high- dose milnacipran to a patient suffering from such fatigue are provided. Also provided are methods for the long-term treatment of fatigue associated with FMS by administering milnacipran to a patient suffering from such fatigue.
摘要翻译：提供了通过向患有这种疲劳的患者施用高剂量米那普仑来治疗与纤维肌痛有关的疲劳的方法。还提供了通过给患有这种疲劳的患者施用米那普仑来长期治疗与FMS相关的疲劳的方法。

3. 发明申请

WO2004105690A3 TREATMENT OF CHRONIC PAIN ASSOCIATED WITH DRUG OR RADIATION THERAPY 审中-公开
标题翻译：治疗与药物或放射治疗相关的慢性疼痛
公开(公告)号：WO2004105690A3
公开(公告)日：2005-03-10
申请号：PCT/US2004016101
申请日：2004-05-20
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , KRANZLER JAY D
发明人： RAO SRINIVAS G , KRANZLER JAY D
IPC分类号： A61K20060101 , A61K31/137 , A61K31/22 , A61K31/55
CPC分类号： A61K31/22
摘要： Methods for treating chronic widespread pain associated with drug therapy or radiation therapy are described. The method generally involves administering a therapeutically effective amount of a dual or tri reuptake inhibitor of a specific type or a pharmaceutically acceptable salt thereof. Preferably the compound is a non-tricyclic dual reuptake inhibitor. The most preferred compound is milnacipran or a bioequivalent or pharmaceutically acceptable salt thereof. Other preferred compounds are duloxetine and venlafaxine or a bioequivalent or pharmaceutically acceptable salt thereof. In yet another embodiment, a therapeutically effective amount of a non-tricyclic triple reuptake inhibitor ("TRI") compound of a specific type, or a pharmaceutically acceptable salt thereof, is administered. The TRI compounds are characterized by their ability to block the reuptake (and, hence, increase central concentrations of) the three primary brain monoamines: serotonin, noradrenaline, and dopamine.
摘要翻译：描述了治疗与药物治疗或放射治疗相关的慢性广泛疼痛的方法。该方法通常涉及给予治疗有效量的特异型或其可药用盐的双重或三次再摄取抑制剂。优选地，该化合物是非三环双重再摄取抑制剂。最优选的化合物是米那普仑或其生物等效或药学上可接受的盐。其他优选的化合物是度洛西汀和文拉法辛或其生物等效或药学上可接受的盐。在另一个实施方案中，施用治疗有效量的特定类型的非三环三重再摄取抑制剂（“TRI”）化合物或其药学上可接受的盐。 TRI化合物的特征在于其阻断三种主要脑单胺（5-羟色胺，去甲肾上腺素和多巴胺）的再摄取（并因此增加中心浓度）的能力。

4. 发明申请

WO2006023702A3 METHOD FOR TREATING SLEEP RELATED BREATHING DISORDERS WITH SETIPTILINE 审中-公开
标题翻译：用SETIPTILINE治疗睡眠相关呼吸系统疾病的方法
公开(公告)号：WO2006023702A3
公开(公告)日：2007-02-15
申请号：PCT/US2005029502
申请日：2005-08-19
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , KRANZLER JAY D , ANDERSON JEFFERY J
发明人： RAO SRINIVAS G , KRANZLER JAY D , ANDERSON JEFFERY J
IPC分类号： A01N43/80 , A61K31/42
CPC分类号： A61K31/506 , A61K31/42 , A61K31/551 , A61K31/7008 , A61K45/06 , A61K2300/00
摘要： Compositions and methods for the treatment of sleep related breathing disorders are provided. Compositions include setiptiline in combination with other active pharmaceutical ingredients, such as zonisamide, topiramate or modafinil. The treated sleep related breathing disorders include sleep apnea and sleep hypopnea. In some embodiments, the pharmaceutical compounds are used as adjuvant therapy with positive airway pressure (PAP) therapy, thereby lowering the pressure required to maintain airway patency during PAP therapy.
摘要翻译：提供了治疗睡眠相关呼吸障碍的组合物和方法。组合物包括与其他活性药物成分组合的setiptiline，如唑尼沙胺，托吡酯或莫达非尼。经治疗的睡眠相关呼吸障碍包括睡眠呼吸暂停和睡眠呼吸不足。在一些实施方案中，药物化合物用作具有气道正压（PAP）治疗的辅助治疗，从而降低在PAP治疗期间维持气道通畅所需的压力。

5. 发明申请

WO2007038620A2 MILNACIPRAN FOR THE LONG-TERM TREATMENT OF FIBROMYALGIA SYNDROME 审中-公开
标题翻译：米非司酮用于长期治疗纤维化综合征
公开(公告)号：WO2007038620A2
公开(公告)日：2007-04-05
申请号：PCT/US2006037714
申请日：2006-09-27
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , GENDREAU MICHAEL , KRANZLER JAY D
发明人： RAO SRINIVAS G , GENDREAU MICHAEL , KRANZLER JAY D
IPC分类号： A61K31/165
CPC分类号： A61K31/165 , A61K31/197 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to methods for providing long-term treatment of fibromyalgia syndrome (FMS) by administering a dual re-uptake inhibitor to a patient with FMS. More particularly, the present invention is directed to the long-term treatment of FMS by administering a norepinephrine-serotonin reuptake inhibitor (NSRI) to a patient with FMS.
摘要翻译：本发明涉及通过向患有FMS的患者施用双重再摄取抑制剂来提供纤维肌痛综合征（FMS）的长期治疗的方法。更具体地说，本发明涉及通过向患有FMS的患者施用去甲肾上腺素 - 血清素再摄取抑制剂（NSRI）来长期治疗FMS。

6. 发明申请

WO03039598A8 SELECTIVE NOREPINEPHRINE SEROTONIN REUPTAKE INHIBITORS FOR TREATING FIBROMYALGIA SYNDROME, CHRONIC FATIQUE SYNDROME AND PAIN 审中-公开
标题翻译：选择性肾上腺素硒激酶抑制剂治疗纤维瘤综合征，慢性疲劳综合征和疼痛
公开(公告)号：WO03039598A8
公开(公告)日：2004-06-03
申请号：PCT/US0235396
申请日：2002-11-05
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , KRANZLER JAY D
发明人： RAO SRINIVAS G , KRANZLER JAY D
IPC分类号： A61K31/00 , A61K31/135 , A61K31/165 , A61P25/00 , A61K45/00
CPC分类号： A61K31/135 , A61K31/00 , A61K31/165 , A61K2300/00
摘要： The present invention provides a method of treating, in a mammal, chronic fatigue syndrome (CFS), chronic fatigue syndrome (CFS) that is associated with depression, a combination of chronic fatigue syndrome (CFS) and fibromyalgia syndrome (FMS), fibromyalgia syndrome (FMS) associated with depression, pain and pain associated with depression. The method includes administering a therapeutically effective amount of a dual serotonin norepinepbrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了一种在哺乳动物中治疗慢性疲劳综合征（CFS），与抑郁症相关的慢性疲劳综合征（CFS），慢性疲劳综合征（CFS）和纤维肌痛综合征（FMS）的组合，纤维肌痛综合征（FMS）与抑郁症相关的疼痛和疼痛相关。该方法包括施用治疗有效量的双重5-羟色胺去甲肾上腺素再摄取抑制剂化合物或其药学上可接受的盐。

7. 发明申请

WO2006023703A3 METHOD FOR TREATING SLEEP RELATED BREATHING DISORDERS 审中-公开
标题翻译：治疗睡眠相关呼吸系统疾病的方法
公开(公告)号：WO2006023703A3
公开(公告)日：2007-04-19
申请号：PCT/US2005029504
申请日：2005-08-19
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , KRANZLER JAY D , ANDERSON JEFFERY J
发明人： RAO SRINIVAS G , KRANZLER JAY D , ANDERSON JEFFERY J
IPC分类号： A61K31/42
CPC分类号： A61K31/506 , A61K31/42 , A61K31/551 , A61K31/7008 , A61K45/06 , A61K2300/00
摘要： Compositions and methods for the treatment of sleep related breathing disorders are provided. Compositions include mirtazapine in combination with other active pharmaceutical ingredients, such as zonisamide, topiramate or modafinil. The treated sleep related breathing disorders include sleep apnea and sleep hypopnea. In some embodiments, the pharmaceutical compounds are used as adjuvant therapy with positive airway pressure (PAP) therapy, thereby lowering the pressure required to maintain airway patency during PAP therapy.
摘要翻译：提供了治疗睡眠相关呼吸障碍的组合物和方法。组合物包括米氮平与其它活性药物成分如唑尼沙胺，托吡酯或莫达非尼组合。经治疗的睡眠相关呼吸障碍包括睡眠呼吸暂停和睡眠呼吸不足。在一些实施方案中，药物化合物用作具有气道正压（PAP）治疗的辅助治疗，从而降低在PAP治疗期间维持气道通畅所需的压力。

8. 发明申请

WO2004045718A2 TREATMENT OF COGNITIVE DYSFUNCTIONS' 审中-公开
标题翻译：治疗精神功能障碍“
公开(公告)号：WO2004045718A2
公开(公告)日：2004-06-03
申请号：PCT/US0336813
申请日：2003-11-18
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS G , KRANZLER JAY D
发明人： RAO SRINIVAS G , KRANZLER JAY D
IPC分类号： A61K31/00 , A61K45/06 , A61K47/00 , A61P20060101 , A61P1/00 , A61P
CPC分类号： A61K45/06 , A61K31/00 , A61K2300/00
摘要： Cognitive dysfunction can be treated by administering to a mammal an effective amount of a compound that is an N-methyl-D-aspartate (NMDA) receptor antagonist and a selective norepinephrine (NE) serotonin (5-HT) reuptake inhibitor (NSRI), most preferably between 1:1 and 20:1 NE:5-HT reuptake. In a preferred embodiment the composition includes a pharmaceutically acceptable carrier and an effective cognition-enhancing amount of milnacipran, most preferably about 25 mg/day to about 250 mg/day. The composition may further include at least one of Ginkgo biloba, Huperzine A, Phosphatidylserine, Vitamin E, Tacrine, Donepezil, Rivastigmine, and Galantamine. The composition can also include at least one of sibutramine, an aminocyclopropane derivative, venlafaxine, duloxetine, desipramine, nortriptyline, protriptyline, amitriptyline, clomipramine, doxepine, imipramine, and trimipramine.
摘要翻译：可以通过向哺乳动物施用有效量的N-甲基-D-天冬氨酸（NMDA）受体拮抗剂和选择性去甲肾上腺素（NE）5-羟色胺（5-HT）再摄取抑制剂（NSRI）的化合物来治疗认知功能障碍，最优选1：1至20：1 NE：5-HT再摄取。在优选的实施方案中，组合物包含药学上可接受的载体和有效认知增强量的米那普仑，最优选约25mg /天至约250mg /天。组合物还可以包括银杏，石杉碱甲，磷脂酰丝氨酸，维生素E，他克林，多奈哌齐，利斯的明和加兰他敏中的至少一种。该组合物还可以包括西布曲明，氨基环丙烷衍生物，文拉法辛，度洛西汀，地昔帕明，去甲替林，依替西林，阿米替林，氯米帕明，多塞平，丙咪嗪和米帕明中的至少一种。

9. 发明申请

WO2006055854A3 METHODS FOR REDUCING THE SIDE EFFECTS ASSOCIATED WITH MIRTAZAPINE TREATMENT 审中-公开
标题翻译：减少与米拉珠星治疗相关的副作用的方法
公开(公告)号：WO2006055854A3
公开(公告)日：2007-02-01
申请号：PCT/US2005042019
申请日：2005-11-17
申请人： CYPRESS BIOSCIENCE INC , RAO SRINIVAS , KRANZLER JAY D , ANDERSON JEFFERY J
发明人： RAO SRINIVAS , KRANZLER JAY D , ANDERSON JEFFERY J
IPC分类号： A61K31/55 , A61K9/20
CPC分类号： A61K31/13 , A61K31/137 , A61K31/42 , A61K31/425 , A61K31/551 , A61K31/7008 , A61K45/06 , A61K2300/00
摘要： Compositions, and methods of use thereof, are provided for the prevention or treatment of side effects associated with the use of drugs that act as 5HT2/5HT3 serotonin receptor antagonists and alpha-2 adrenergic receptor antagonists (5HT2/5HT3 antagonist/alpha-2 antagonist). The method involves using dopamine-releasing compounds, such as amantadine, anticonvulsants, such as zonisamide, or dopamine/norepinephrine reuptake inhibitors, such as bupropion, in combination with 5HT2/5HT3 antagonist/alpha-2 antagonists, such as mirtazapine, to reduce the excessive daytime drowsiness and/or weight gain associated with 5HT2/5HT3 antagonist/alpha-2 antagonist use for the treatment of disorders, such as, depression, schizophrenia, anxiety disorders, sleep-related breathing disorders, insomnia, migraine headache, chronic tension-type headache, hot flashes, lower back pain, neuropathic pain and functional somatic syndromes. Formulations of dopamine-releasing compounds or anticonvulsants with 5HT2/5HT3 antagonist/alpha-2 antagonists are provided. In particular embodiments, combination therapy with mirtazapine and zonisamide provides relief from chronic low back pain, while reducing or avoiding side effects associated with monotherapy with mirtazapine or zonisamide.
摘要翻译：提供组合物及其使用方法用于预防或治疗与使用作为5HT2 / 5HT3血清素受体拮抗剂和α-2肾上腺素能受体拮抗剂（5HT2 / 5HT3拮抗剂/α-2拮抗剂）的药物相关的副作用）。该方法包括使用多巴胺释放化合物，例如金刚烷胺，抗惊厥药如唑尼沙胺，或多巴胺/去甲肾上腺素再摄取抑制剂，例如安非他酮，与5HT2 / 5HT3拮抗剂/α-2拮抗剂如米氮平联合使用，以减少与5HT2 / 5HT3拮抗剂/α-2拮抗剂有关的过度白天嗜睡和/或体重增加用于治疗诸如抑郁症，精神分裂症，焦虑症，睡眠相关呼吸障碍，失眠，偏头痛头痛，慢性紧张症，类型头痛，潮热，下背痛，神经性疼痛和功能性体质综合征。提供了具有5HT2 / 5HT3拮抗剂/α-2拮抗剂的多巴胺释放化合物或抗惊厥药的制剂。在具体实施方案中，使用米氮平和唑尼沙胺的联合治疗可减轻慢性腰背痛，同时减少或避免与米氮平或唑尼沙胺进行单一疗法相关的副作用。

10. 发明申请

WO2004030633A3 DOSAGE ESCALATION AND DIVIDED DAILY DOSE OF ANTI-DEPRESSANTS TO TREAT NEUROLOGICAL DISORDERS 审中-公开
标题翻译：抗衰老药物治疗神经病变的剂量自然和分散日剂量
公开(公告)号：WO2004030633A3
公开(公告)日：2004-07-15
申请号：PCT/US0331622
申请日：2003-10-03
申请人： CYPRESS BIOSCIENCE INC
发明人： RAO SRINIVAS G , KRANZLER JAY D , GENDREAU MICHAEL R
IPC分类号： A61K31/00 , A61K31/165
CPC分类号： A61K31/00 , A61K31/165
摘要： The present invention provides a method to treat neurological disorders. The method includes, e.g., administering higher daily dosages of anti-depressant. The higher daily dosages result in an improved efficacy of the drug, the maintenance of a positive patient toleration, the maintenance of a positive patient safety profile (e.g., dose limiting toxicity), a suitable peak plasma concentration (Cmax) of drug, and/or a once-a-day (QD) as opposed to twice-a-day (BID) administration. Applicants have discovered that increased daily dosages anti-depressant that would normally evoke adverse effects can be administered without the negative patient tolerability (i.e., adverse reactions ) by escalating dosages over time. Such escalation dosages provide more efficacious amounts of anti-depressant than would otherwise be permitted. Similarly, higher levels of circulating drug are possible in patients by administering the compound in divided doses over the course of a day rather than once a day.
摘要翻译：本发明提供治疗神经障碍的方法。该方法包括例如施用更高剂量的抗抑郁剂。更高的日剂量导致药物的功效改善，维持阳性患者耐受性，维持阳性患者安全性特征（例如剂量限制性毒性），药物的合适的峰值血浆浓度（C max）和/ 或每天一次（QD），而不是每天两次（BID）管理。申请人已经发现，通常会引起不良反应的每日剂量增加的抗抑郁剂可以通过随着时间的不断升高的剂量而没有负面的患者耐受性（即不良反应）来施用。这种升级剂量比否则允许的提供更有效量的抗抑郁药。类似地，通过在一天的时间内分批施用化合物而不是每天一次，在患者中可以使用较高水平的循环药物。

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