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    • 1. 发明申请
    • MPZP: A SMALL MOLECULE CORTICOTROPIN-RELEASING FACTOR TYPE 1 RECEPTOR (CRF1) ANTAGONIST
    • MPZP:小分子释放促凋亡因子1型受体(CRF1)拮抗剂
    • WO2009036340A3
    • 2009-12-30
    • PCT/US2008076257
    • 2008-09-12
    • SCRIPPS RESEARCH INSTKOOB GEORGE FZORRILA ERIC PMASON BARBARAJANDA KIMWIRSCHING PETER
    • KOOB GEORGE FZORRILA ERIC PMASON BARBARAJANDA KIMWIRSCHING PETER
    • C07D417/14A61K31/513
    • A61K31/519
    • A method for treating or preventing a host mammal that exhibits aversive signs and symptoms present during protracted abstinence or extended discontinuation syndromes as seen after cessation of compulsive activity, behaviors, or substance use is disclosed. That method comprises administering to a host mammal in need a pharmaceutical composition containing an aversive sign and symptom lessening amount a compound of Formula I or a pharmaceutically acceptable salt thereof dissolved or dispersed in a physiologically acceptable diluent, and repeating the administration as needed, wherein W, X, Y and Z, R1 and Ar are defined within. Data are provided in rats as host mammals using behavioral models dependent on the CRFi system: defensive burying, alcohol dependence, cocaine dependence and nicotine dependence. A contemplated method also is useful for inhibiting relapse of such a behavior. A contemplated method also is useful for treating substance -related or substance- induced psychiatric disorders that include aversive signs and symptoms.
    • 公开了一种用于治疗或预防宿主哺乳动物的方法,所述宿主哺乳动物在停止强迫活动,行为或物质使用之后看到的在持续禁欲或延长中断综合征期间呈现厌恶症状和症状。 该方法包括向需要的宿主哺乳动物施用含有厌恶症状和症状减轻量的药物组合物,溶解或分散于生理上可接受的稀释剂中的式I化合物或其药学上可接受的盐,并且根据需要重复施用,其中W ,X,Y和Z,R1和Ar定义在其中。 使用依赖于CRFI系统的行为模型:大鼠作为宿主哺乳动物提供数据:防御性掩埋,酒精依赖,可卡因依赖和尼古丁依赖。 预期的方法也可用于抑制这种行为的复发。 所考虑的方法也可用于治疗包括厌恶症状和症状的物质相关的或物质诱导的精神病症。
    • 2. 发明申请
    • MPZP: A SMALL MOLECULE CORTICOTROPIN-RELEASING FACTOR TYPE 1 RECEPTOR (CRF1) ANTAGONIST
    • MPZP:小分子CORTICOTROPIN释放因子1型受体(CRF1)ANTAGONIST
    • WO2009036340A2
    • 2009-03-19
    • PCT/US2008/076257
    • 2008-09-12
    • THE SCRIPPS RESEARCH INSTITUTEKOOB, George, F.ZORRILA, Eric, P.MASON, BarbaraJANDA, KimWIRSCHING, Peter
    • KOOB, George, F.ZORRILA, Eric, P.MASON, BarbaraJANDA, KimWIRSCHING, Peter
    • E05G1/024
    • A61K31/519
    • A method for treating or preventing a host mammal that exhibits aversive signs and symptoms present during protracted abstinence or extended discontinuation syndromes as seen after cessation of compulsive activity, behaviors, or substance use is disclosed. That method comprises administering to a host mammal in need a pharmaceutical composition containing an aversive sign and symptom lessening amount a compound of Formula I or a pharmaceutically acceptable salt thereof dissolved or dispersed in a physiologically acceptable diluent, and repeating the administration as needed, wherein W, X, Y and Z, R1 and Ar are defined within. Data are provided in rats as host mammals using behavioral models dependent on the CRFi system: defensive burying, alcohol dependence, cocaine dependence and nicotine dependence. A contemplated method also is useful for inhibiting relapse of such a behavior. A contemplated method also is useful for treating substance -related or substance- induced psychiatric disorders that include aversive signs and symptoms.
    • 公开了一种用于治疗或预防在停止强迫性活动,行为或物质使用过程中看到的延长禁欲或延长不连续综合征期间出现厌恶症状和症状的宿主哺乳动物的方法。 该方法包括向需要的宿主哺乳动物施用药物组合物,所述药物组合物含有溶解或分散在生理上可接受的稀释剂中的式I化合物或其药学上可接受的盐的反义征候和症状减轻量,并根据需要重复给药,其中W ,X,Y和Z,R1和Ar定义在其中。 使用依赖于CRFi系统的行为模型作为宿主哺乳动物提供数据:防御性掩埋,酒精依赖,可卡因依赖和尼古丁依赖。 预期的方法也可用于抑制这种行为的复发。 预期的方法也可用于治疗包括厌食症状和体征的物质相关或物质诱导的精神障碍。