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28 条记录 (耗时 0.022 秒)

    Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same
    2.
    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。

    Synthesis of 7-membered carbocyclic compound having diexomethylene groups
    3.
    发明授权
    Synthesis of 7-membered carbocyclic compound having diexomethylene groups 失效
    具有阴离子亚甲基的7-元碳环化合物的合成

    公开(公告)号：US07094913B2

    公开(公告)日：2006-08-22

    申请号：US10823707

    申请日：2004-04-14

    申请人： Yong Seo Cho ,  Moon Ho Chang ,  Hun Yeong Koh ,  Ae Nim Pae ,  Hyun Jung Kang

    发明人： Yong Seo Cho ,  Moon Ho Chang ,  Hun Yeong Koh ,  Ae Nim Pae ,  Hyun Jung Kang

    IPC分类号： C07D313/04

    CPC分类号： C07D493/08

    摘要： The present invention relates to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 7-membered carbocyclic compound is a useful intermediate for synthesis of other multicyclic compounds. In Chemical Formula 1, R1 is a C1 to C6 alkyl group, and R2 and R3 is respectively a hydrogen atom, or R1, R2 and R3 may be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

    摘要翻译： 本发明涉及具有阴离子亚甲基的7-元碳环化合物的合成，更具体地说，涉及具有下式化学式1所示结构的新化合物，具有三亚甲基硅烷基甲基的三元碳环化合物 通过使用路易斯酸的分子内Prins环化形成的α-烯醇衍生物。 7元碳环化合物是合成其他多环化合物的有用中间体。 在化学式1中，R 1是C 1 -C 6烷基，R 2和R 2是C 1 -C 6烷基， 分别为氢原子或R 1，R 2，R 3和R 3可以与相邻的取代基连接 以形成5至10元脂族或芳族环。

    Method of preparing tetrabenazine and dihydrotetrabenazine
    5.
    发明授权
    Method of preparing tetrabenazine and dihydrotetrabenazine 有权
    制备丁苯那嗪和二氢丁苯那嗪的方法

    公开(公告)号：US08993766B2

    公开(公告)日：2015-03-31

    申请号：US13617357

    申请日：2012-09-14

    申请人： Sun Joon Min ,  Yong Seo Cho ,  Jae Kyun Lee ,  Ae Nim Pae ,  Young Wook Son

    发明人： Sun Joon Min ,  Yong Seo Cho ,  Jae Kyun Lee ,  Ae Nim Pae ,  Young Wook Son

    IPC分类号： C07D455/06 ,  C07F7/08

    CPC分类号： C07D455/06 ,  C07F7/0812

    摘要： The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.

    摘要翻译： 本发明涉及一种制备丁苯那嗪（TBZ）和二氢丁苯那嗪（DTBZ）的方法，更具体地涉及通过使用6,7-二甲氧基苯并咪唑的简单且短的反应方法制备丁苯那嗪（TBZ）和二氢丁苯那嗪（DTBZ）的方法 -1,2,3,4-四氢异喹啉和4-甲基-2-（3-（三甲基甲硅烷基）丙-1-烯-2-基）戊烷作为起始原料，以顺序进行烷基化反应，Aza-Prins环化反应 在氧化剂和氧化反应的存在下。

    Pyrazolopyrimidine derivatives having biological activity on serotonin receptor 5-HT2c
    7.
    发明授权
    Pyrazolopyrimidine derivatives having biological activity on serotonin receptor 5-HT2c 有权
    对5-羟色胺受体5-HT2c具有生物活性的吡唑并嘧啶衍生物

    公开(公告)号：US08232279B2

    公开(公告)日：2012-07-31

    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： A01N43/90 ,  A61K31/519 ,  C07D487/00

    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。

    CIS-2, 6-DISUBSTITUTED TETRAHYDROPYRAN DERIVATIVES AND PREPARATION METHOD THEREOF
    9.
    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）

    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method
    10.
    发明授权
    Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method 失效
    具有顺式取代基的四氢​​呋喃衍生物及其制备方法

    公开(公告)号：US07388101B1

    公开(公告)日：2008-06-17

    申请号：US11732602

    申请日：2007-04-04

    申请人： Yong Seo Cho ,  Hyunah Choo ,  Joo Hwan Cha ,  Ae Nim Pae ,  Satish N. Chavre ,  Kyung Il Choi

    发明人： Yong Seo Cho ,  Hyunah Choo ,  Joo Hwan Cha ,  Ae Nim Pae ,  Satish N. Chavre ,  Kyung Il Choi

    IPC分类号： C07D307/02

    CPC分类号： C07D307/12

    摘要： The present invention relates to a tetrahydrofuran compound having cis substituents, the derivatives thereof and a process for preparing the same, and in particular relates to a dihydrofuran-3-ylidene triflate compound having cis substituents at C2 and C5 positions prepared through Prins-type cyclization using a homopropargylic alcohol derivative as a starting material in the presence of Lewis acid catalyst, a tetrahydrofuran compound having cis substituents at C2, C3 and C5 positions prepared through the hydrolysis of triflate group in the derivatives of the dihydrofuran-3-ylidene triflate compound, and a preparation method thereof.The derivatives and the target tetrahydrofuran compound prepared according to the present invention are hydrofuran compounds with novel structures having cis substituents at C2, C3 and/or C5 positions, which are useful as a derivative for synthesizing drugs such as an antagonist for neurokinin receptor.

    摘要翻译： 本发明涉及具有顺式取代基的四氢​​呋喃化合物及其衍生物及其制备方法，特别涉及在C 2上具有顺式取代基的二氢呋喃-3-亚基三氟甲磺酸酯化合物和 在路易斯酸催化剂存在下，使用均二炔醇衍生物作为起始原料，在C 2 N 2上具有顺式取代基的四氢​​呋喃化合物，通过Prins-型环化制备的C 5 H 3位， 通过在二氢呋喃-3-亚基三氟甲磺酸酯化合物的衍生物中水解三氟甲磺酸酯基制备的C 3和C 5 H 3位及其制备方法。 根据本发明制备的衍生物和目标四氢呋喃化合物是具有在C 2，C 3和/或C 5上具有顺式取代基的新结构的氢呋喃化合物 其可用作合成药物的衍生物，例如用于神经激肽受体的拮抗剂。