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    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    1.
    发明申请
    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 有权
    作为DOPAMINE D4受体拮抗剂的哌嗪衍生物 - 吡咯并吡啶衍生物，以及含有它们的药物组合物

    公开(公告)号：US20120209001A1

    公开(公告)日：2012-08-16

    申请号：US13454817

    申请日：2012-04-24

    申请人： Jae Yang KONG ,  Park Woo-Kyu ,  Heeyeong CHO ,  Daeyoung JEONG ,  Gildon CHOI ,  Hun Yeong KOH ,  Sang Hee KIM ,  Ae Nim PAE ,  Yong Seo CHO ,  Joo Hwan CHA ,  Hyunah CHOO ,  Sang Eun CHAE ,  Hee-Yoon LEE

    发明人： Jae Yang KONG ,  Park Woo-Kyu ,  Heeyeong CHO ,  Daeyoung JEONG ,  Gildon CHOI ,  Hun Yeong KOH ,  Sang Hee KIM ,  Ae Nim PAE ,  Yong Seo CHO ,  Joo Hwan CHA ,  Hyunah CHOO ,  Sang Eun CHAE ,  Hee-Yoon LEE

    IPC分类号： C07D403/10 ,  C07D401/14

    CPC分类号： C07D403/06

    摘要： The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

    摘要翻译： 本发明涉及一种新的哌嗪基 - 丙基 - 吡唑衍生物，其制备方法和包含其的药学上可接受的组合物。 本发明的新型哌嗪基 - 丙基 - 吡唑衍生物对多巴胺D4受体具有优异的选择性亲和力，可有效抑制阿扑吗啡诱导的精神病性行为（笼养），并在小鼠旋转试验中具有较低的不良反应。 因此，它可以被开发为用于治疗和预防中枢神经系统（CNS）障碍，特别是精神分裂症，注意缺陷多动障碍，抑郁症，压力疾病，恐慌症，恐惧症，强迫症，创伤后疼痛的治疗剂 压力障碍，认知障碍，阿尔茨海默病，帕金森病，焦虑症，过敏性反应，躁狂症，癫痫发作，人格障碍，偏头痛，药物成瘾，酒精成瘾，肥胖，进食障碍和睡眠障碍。

    CIS-2, 6-DISUBSTITUTED TETRAHYDROPYRAN DERIVATIVES AND PREPARATION METHOD THEREOF
    2.
    发明申请
    CIS-2, 6-DISUBSTITUTED TETRAHYDROPYRAN DERIVATIVES AND PREPARATION METHOD THEREOF 有权
    CIS-2,6,6-二取代衍生物衍生物及其制备方法

    公开(公告)号：US20090209770A1

    公开(公告)日：2009-08-20

    申请号：US12243244

    申请日：2008-10-01

    申请人： Yong Seo CHO ,  You Seung KIM ,  Jae Kyun LEE ,  Hyunah CHOO ,  Ae Nim PAE

    发明人： Yong Seo CHO ,  You Seung KIM ,  Jae Kyun LEE ,  Hyunah CHOO ,  Ae Nim PAE

    IPC分类号： C07D315/00

    CPC分类号： C07D309/06

    摘要： Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds. (wherein, R1, R2 and R3 are as defined in the specification.)

    摘要翻译： 公开了由化学式1表示的顺式-2,6-二取代四氢吡喃衍生物及其制备方法。 四氢吡喃衍生物可以通过Prins-在三甲基甲硅烷基三氟甲磺酸酯存在下将四氢吡喃衍生物与高官能醇衍生物反应来制备。 在四氢吡喃环的C2和C6位上具有顺式取代基的四氢​​吡喃衍生物可用作合成和开发治疗有效的天然存在的化合物的中间体。 （其中，R1，R2和R3如说明书中所定义）