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    1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel
    1.
    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。

    1,3-DIOXOISOINDOLE DERIVATIVES HAVING SELECTIVE ANTAGONISM OF T-TYPE CALCIUM CHANNEL
    2.
    发明申请
    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剂的1,3-二氧化物衍生物

    公开(公告)号：US20070259867A1

    公开(公告)日：2007-11-08

    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 ,  A61K31/4035 ,  C07D413/02 ,  C07D403/02

    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烷氧基，C 1 -C 6 - 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。

    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    4.
    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。

    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
    10.
    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：US08236806B2

    公开(公告)日：2012-08-07

    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： 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。