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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

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。

3. 发明申请

WO2008157094A1 IMPROVING THE TOLERABILITY OF MIRTAZAPINE AND A SECOND ACTIVE BY USING THEM IN COMBINATION 审中-公开
标题翻译：改善米他芝的耐受性和使用它们在组合中的第二活性
公开(公告)号：WO2008157094A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/066206
申请日：2008-06-06
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
CPC分类号： A61K31/4402 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： A reduction in the side effects of treating with an agent having combined 5HT2/5HT3and alpha-2 antagonistic activity is obtained by administering an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. A combined dosage form comprising an agent having 5HT2/5HT3and a1pha-2 antagonistic activity and an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity is presented. Some embodiments of the combined dosage form comprise an immediate release component comprising an agent having 5HT2/5HT3and alpha-2 antagonistic activity and a delayed release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine HI agonist activity. Some embodiments of the combined dosage form comprise a delayed release component comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and an immediate release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine H1 agonist activity. Methods of treatment and kits for administration are also provided
摘要翻译：通过施用具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的药物，可以减少用具有组合的5HT2 / 5HT3和α-2拮抗活性的药物治疗的副作用。提供了包含具有5HT2 / 5HT3和α1-2拮抗活性的药剂和具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的药剂的组合剂型。组合剂型的一些实施方案包括包含具有5HT2 / 5HT3和α-2拮抗活性的试剂的立即释放组分和包含具有选择性去甲肾上腺素再摄取抑制剂或组胺HI激动剂活性的试剂的延迟释放组分。组合剂型的一些实施方案包括包含具有5HT 2 / 5HT 3和α-2拮抗活性的试剂的延迟释放组分和包含具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的试剂的速释组分。还提供了治疗方法和用于给药的试剂盒

4. 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。

5. 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。

6. 发明申请

WO2006023702A2 METHOD FOR TREATING SLEEP RELATED BREATHING DISORDERS WITH SETIPTILINE 审中-公开
标题翻译：用SETIPTILINE治疗睡眠相关呼吸道疾病的方法
公开(公告)号：WO2006023702A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/029502
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： A61K31/7008 , A61K31/551 , A61K31/506 , A61L9/04 , 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。组合物包括与其它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。

7. 发明申请

WO2004105690A2 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：WO2004105690A2
公开(公告)日：2004-12-09
申请号：PCT/US2004/016101
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： A61K
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重再摄取抑制剂。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。

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

WO2008128116A1 TREATMENT OF DOWN SYNDROME WITH BENZODIAZEPINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：用苯二氮卓类受体拮抗剂治疗下调综合征
公开(公告)号：WO2008128116A1
公开(公告)日：2008-10-23
申请号：PCT/US2008/060133
申请日：2008-04-11
申请人： CYPRESS BIOSCIENCES, INC. , RAO, Srinivas , ANDERSON, Jeffery, J. , KRANZLER, Jay, D.
发明人： RAO, Srinivas , ANDERSON, Jeffery, J. , KRANZLER, Jay, D.
IPC分类号： A01N43/58
CPC分类号： A61K31/00 , A61K9/006 , A61K31/5517
摘要： Pharmaceutical compositions and methods of treating Down Syndrome, mental retardation or both are provided. The pharmaceutical compositions comprise one or more benzodiazepine receptor antagonists, such as flumazenil.
摘要翻译：提供治疗唐氏综合征，精神发育迟滞或两者的药物组合物和方法。药物组合物包含一种或多种苯并二氮杂受体拮抗剂，例如氟马西尼。

10. 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。

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