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    • 3. 发明申请
    • COMPOSITIONS FOR AFFECTING WEIGHT LOSS
    • 影响重量损失的组合物
    • WO2007016108A1
    • 2007-02-08
    • PCT/US2006/028875
    • 2006-07-24
    • OREXIGEN THERAPEUTICS, INC.TOLLEFSON, GaryMCKINNEY, Anthony, A.HIGGIN, Michelle, S.MCCALL, John, M.
    • TOLLEFSON, GaryMCKINNEY, Anthony, A.HIGGIN, Michelle, S.MCCALL, John, M.
    • A61K45/06A61K31/485A61K31/137A61K31/138A61P3/04
    • A61K31/137A61K31/138A61K31/165A61K31/485A61K45/06A61K2300/00
    • Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a metabolite of naltrexone, such as 6-β-naltrexol or a prodrug of a naltrexone metabolite, and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) and/or a melanocortin 4 receptor (MC4-R), and/or increases the concentration of α-MSH in the central nervous system. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity with a metabolite of naltrexone, such as 6-β-naltrexol or a prodrug of a naltrexone metabolite, and treating that individual to enhance α-MSH activity, e.g., by administration of a second compound causes increased agonism of MC3-R and/or MC4-R, and/or increases the concentration of α-MSH in the central nervous system.
    • 公开了用于影响体重减轻的组合物,其包含第一化合物和第二化合物,其中第一化合物是纳曲酮的代谢物,例如6-β-纳曲醇或纳曲酮代谢物的前药,以及 第二化合物引起黑皮质素3受体(MC3-R)和/或黑皮质素4受体(MC4-R)的激动作用增加,和/或增加中枢神经系统中α-MSH的浓度。 还公开了影响体重减轻,增加能量消耗,增加个体饱腹感或抑制个体食欲的方法,包括鉴定需要其的个体并治疗该个体以拮抗纳曲酮代谢物的阿片样物质受体活性,例如 作为6-β-纳曲醇或纳曲酮代谢物的前药,并且治疗该个体以增强α-MSH活性,例如通过施用第二化合物引起MC3-R和/或MC4-R增加的激动作用,和/或 增加中枢神经系统中α-MSH的浓度。
    • 4. 发明申请
    • METHODS AND COMPOSITIONS FOR MANAGING PSYCHOTIC DISORDERS
    • 管理心理障碍的方法和组成
    • WO2006130522A2
    • 2006-12-07
    • PCT/US2006/020616
    • 2006-05-25
    • OREXIGEN THERAPEUTICS, INC.TOLLEFSON, Gary
    • TOLLEFSON, Gary
    • A61K31/496A61K31/551A61K31/519A61K31/423
    • A61K31/519A61K31/19A61K31/423A61K31/425A61K31/496A61K31/551A61K31/7008A61K31/7048A61K2300/00
    • Compositions for treating psychotic disorders comprise a first ingredient and a second ingredient, wherein the first ingredient comprises at least one antipsychotic agent selected from the group consisting of ziprasidone, olanzapine and risperidone and the second ingredient comprises at least one anticonvulsant selected from the group consisting of zonisamide and topiramate. Methods of treating psychotic disorders, symptoms associated with psychotic disorders, and side effects associated with antipsychotic agents, comprise administering a first ingredient and a second ingredient, wherein the first ingredient comprises at least one antipsychotic agent selected from the group consisting of ziprasidone, olanzapine and risperidone and the second ingredient comprises at least one anticonvulsant selected from the group consisting of zonisamide and topiramate. The second ingredient of the compositions and methods may further comprise an antidepressant. In various embodiments, the antipsychotic agent and the anticonvulsant act synergistically to alleviate symptoms and/or side effects associated with psychotic disorders and their treatment.
    • 用于治疗精神病的组合物包含第一成分和第二成分,其中第一成分包含至少一种选自齐拉西酮,奥氮平和利培酮的抗精神病药,第二成分包含至少一种选自以下的抗惊厥药: 唑尼沙胺和托吡酯。 治疗精神病,与精神病性症状相关的症状以及与抗精神病药相关的副作用的方法包括施用第一成分和第二成分,其中第一成分包含至少一种抗精神病药,其选自齐拉西酮,奥氮平和 利培酮和第二成分包含至少一种选自唑尼沙胺和托吡酯的抗惊厥药。 组合物和方法的第二成分可以进一步包含抗抑郁药。 在各种实施方案中,抗精神病药和抗惊厥剂协同作用以缓解与精神病性疾病及其治疗相关的症状和/或副作用。
    • 5. 发明申请
    • COMPOSITIONS AND METHODS FOR REDUCING MAJOR ADVERSE CARDIOVASCULAR EVENTS
    • 用于减少主要不良心血管事件的组合物和方法
    • WO2015085044A1
    • 2015-06-11
    • PCT/US2014/068527
    • 2014-12-04
    • OREXIGEN THERAPEUTICS, INC.
    • KLASSEN, PrestonTAYLOR, Kristin
    • A61K31/485A61K31/137A61P3/04
    • A61K31/485A61K31/137A61K2300/00
    • The present application relates to compositions, kits, uses, systems and methods of using naltrexone and bupropion, or pharmaceutically acceptable salts thereof, for reducing the risk of adverse cardiovascular outcomes or events, including Major Adverse Cardiovascular Events (MACE) in subjects, preferably those at increased risk of adverse cardiovascular outcomes or MACE, that may be overweight or obese. The present application also relates to compositions, kits, uses, systems and methods of using naltrexone and bupropion or pharmaceutically acceptable salts thereof for treatment of overweight or obesity in subjects, preferably at increased risk of adverse cardiovascular outcomes or MACE, wherein the treatment reduces the risk of MACE.
    • 本申请涉及使用纳曲酮和安非他酮或其药学上可接受的盐的组合物,试剂盒,用途,系统和方法,用于降低不良心血管结局或事件的风险,包括受试者中的主要不良心血管事件(MACE),优选那些 心血管事件不良或MACE的风险增加,可能超重或肥胖。 本申请还涉及将纳曲酮和安非他酮或其药学上可接受的盐用于治疗受试者的超重或肥胖的组合物,试剂盒,用途,系统和方法,优选地具有不良心血管结局或MACE的增加的风险,其中治疗减少 MACE的风险。
    • 7. 发明申请
    • METHODS FOR TREATING HYPERTENSION IN OVERWEIGHT AND OBESE INDIVIDUALS
    • 治疗高血压和肥胖个体的方法
    • WO2007047351A3
    • 2007-11-01
    • PCT/US2006039862
    • 2006-10-13
    • OREXIGEN THERAPEUTICS INCGADDE KISHORE MKRISHNAN K RANGA RMCKINNEY ANTHONY
    • GADDE KISHORE MKRISHNAN K RANGA RMCKINNEY ANTHONY
    • C07D235/02C07D403/02
    • A61K31/485A61K45/06A61K2300/00
    • Disclosed are novel compositions for treating hypertension and conditions associated with hypertension comprising a first ingredient and a second ingredient, wherein the first ingredient comprises at least one anti-hypertensive agent and the second ingredient comprises at least one anti-obesity agent. Also disclosed are methods of treating hypertension and conditions associated with hypertension comprising administering a first ingredient and a second ingredient, wherein the first ingredient comprises at least one anti-hypertensive agent and the second ingredient comprises at least one anti-obesity agent. In various embodiments, the combinations act synergistically to alleviate symptoms and/or risk factors associated with hypertension. In preferred embodiments, the anti-obesity agent does not substantially affect blood pressure, and thereby decreases the risk and/or unpredictability associated with concurrent administration of the anti-hypertensive agent.
    • 公开了用于治疗高血压和与高血压相关的病症的新型组合物,其包含第一成分和第二成分,其中第一成分包含至少一种抗高血压药,第二成分包含至少一种抗肥胖剂。 还公开了治疗高血压和与高血压相关的病症的方法,包括施用第一成分和第二成分,其中第一成分包含至少一种抗高血压药,第二成分包含至少一种抗肥胖剂。 在各种实施方案中,组合起协同作用以缓解与高血压相关的症状和/或危险因素。 在优选的实施方案中,抗肥胖剂基本上不影响血压,从而降低与同时施用抗高血压剂相关的风险和/或不可预测性。