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    Cis-2, 6-disubstituted tetrahydropyran derivatives and preparation method thereof
    1.
    发明授权
    Cis-2, 6-disubstituted tetrahydropyran derivatives and preparation method thereof 有权
    顺-2,6-二取代四氢吡喃衍生物及其制备方法

    公开(公告)号：US08115019B2

    公开(公告)日：2012-02-14

    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： C07D309/06 ,  C07D309/22

    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）。

    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    7.
    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：US20100063286A1

    公开(公告)日：2010-03-11

    申请号：US12530312

    申请日：2007-07-13

    申请人： Jae Yang Kong ,  Woo-Kyu Park ,  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 ,  Woo-Kyu Park ,  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： C07D403/06

    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。

    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
    8.
    发明授权
    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same 有权
    哌嗪基 - 丙基 - 吡唑衍生物作为多巴胺D4受体拮抗剂，以及含有它们的药物组合物

    公开(公告)号：US08372844B2

    公开(公告)日：2013-02-12

    申请号：US13454817

    申请日：2012-04-24

    申请人： Jae Yang Kong ,  Woo-Kyu Park ,  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 ,  Woo-Kyu Park ,  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： A61K31/496 ,  C07D231/12 ,  C07D401/04 ,  C07D409/04

    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。

    PYRAZOLOPYRIMIDINE DERIVATIVES HAVING BIOLOGICAL ACTIVITY ON SEROTONIN RECEPTOR 5-HT2c
    9.
    发明申请
    PYRAZOLOPYRIMIDINE DERIVATIVES HAVING BIOLOGICAL ACTIVITY ON SEROTONIN RECEPTOR 5-HT2c 有权
    对SEROTONIN受体5-HT2c具有生物活性的吡唑并嘧啶衍生物

    公开(公告)号：US20100298563A1

    公开(公告)日：2010-11-25

    申请号：US12575235

    申请日：2009-10-07

    申请人： Ae Nim PAE ,  Hyunah Choo ,  Yong Seo Cho ,  Ahmed Asif ,  Woo-Kyu Park

    发明人： Ae Nim PAE ,  Hyunah Choo ,  Yong Seo Cho ,  Ahmed Asif ,  Woo-Kyu Park

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to a novel medicinal use of pyrazolopyrimidine compounds having superior effect as serotonin 5-HT2C receptor ligand thus being useful for the prevention and treatment of central nervous system (CNS) diseases. Accordingly, the pharmaceutical composition comprising pyrazolopyrimidine compounds and their pharmaceutically acceptable salts as active ingredients are useful for the prevention and treatment of serotonin 5-HT2C-related central nervous system diseases such as obesity, depression, anxiety and withdrawal symptoms due to drug abuse.

    摘要翻译： 本发明涉及作为5-羟色胺5-HT 2C受体配体具有优越作用的吡唑并嘧啶化合物的新药用，因此可用于预防和治疗中枢神经系统（CNS）疾病。 因此，包含吡唑并嘧啶化合物及其药学上可接受的盐作为活性成分的药物组合物可用于预防和治疗5-羟色胺5-HT2C相关的中枢神经系统疾病如肥胖症，抑郁症，由药物滥用导致的焦虑和戒断症状。

    1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel
    10.
    发明授权
    1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel 失效
    具有T型钙通道选择性拮抗作用的1,3-二氧代异吲哚衍生物

    公开(公告)号：US07319098B2

    公开(公告)日：2008-01-15

    申请号：US11600391

    申请日：2006-11-16

    申请人： Yong Seo Cho ,  Hyunah Choo ,  Ae Nim Pae ,  Joo Hwan Cha ,  Hun Yeong Koh ,  Hwa-Sil Kim ,  Hyewhon Rhim ,  Seon Hee Seo

    发明人： Yong Seo Cho ,  Hyunah Choo ,  Ae Nim Pae ,  Joo Hwan Cha ,  Hun Yeong Koh ,  Hwa-Sil Kim ,  Hyewhon Rhim ,  Seon Hee Seo

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4025 ,  C07D413/12 ,  C07D403/12 ,  C07D401/12 ,  C07D207/06

    CPC分类号： C07D209/48

    摘要： The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.

    摘要翻译： 本发明涉及式（1）的1,3-二氧代异吲哚衍生物或其药学上可接受的盐，其制备方法及其作为T型钙通道拮抗剂的用途，基于以下事实： 式（1）表示对T型钙通道的选择性拮抗活性，因此有效治疗脑疾病，心脏病和神经源性疼痛：其中R 1是苯基或苄基，任选被 选自卤素原子，C 1 -C 6烷氧基，C 1 -C 6烷基的部分 烷基和氰基; R 2是选自哌啶基，吡咯烷基，吗啉基和哌嗪基的杂环基，其中杂环基任选被C 1 -C 6烷基取代， C 1-6烷基; n为1或2。