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    Oxazolidinone derivative and medical composition containing same
    5.
    发明授权
    Oxazolidinone derivative and medical composition containing same 有权
    恶唑烷酮衍生物和含有它们的医药组合物

    公开(公告)号：US08846669B2

    公开(公告)日：2014-09-30

    申请号：US14008702

    申请日：2012-03-29

    申请人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Hye Jin Heo ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Hye Jin Heo ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D413/14 ,  A61K31/53 ,  A61K31/5355

    CPC分类号： C07D413/14

    摘要： Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group.In Formula 1, R and Q are the same as defined in the detailed description.In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.

    摘要翻译： 公开了上述通式1所示的新型恶唑烷酮衍生物，特别是具有环状偕胺肟或环状氨基腙基的新型恶唑烷酮化合物。 在式1中，R和Q与详细描述中定义相同。 此外，公开了一种抗生素的药物组合物，其包含式1的新型恶唑烷酮衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为活性成分。 新型恶唑烷酮衍生物，其前体药剂，其水合物，其溶剂合物，其异构体及其药学上可接受的盐具有抗抗性细菌的抗菌谱，对革兰氏阳性和革兰氏阴性菌具有低毒性和强抗菌作用 因此可以有效地用作抗生素。

    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：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。

    Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof
    8.
    发明授权
    Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof 有权
    具有环偕胺肟或环状氨基腙的恶唑烷酮衍生物其药物组合物

    公开(公告)号：US08242113B2

    公开(公告)日：2012-08-14

    申请号：US13120568

    申请日：2009-09-22

    申请人： Young Lag Cho ,  Sang Eun Chae ,  Sung Yoon Baek ,  Yeon Ok Kim ,  Seong Jin Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sang Eun Chae ,  Sung Yoon Baek ,  Yeon Ok Kim ,  Seong Jin Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D403/08 ,  A61K31/5377

    CPC分类号： C07D403/08

    摘要： Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.

    摘要翻译： 公开了一种新的恶唑烷酮衍生物，特别是具有环偕胺肟或环状氨基腙基团的新型恶唑烷酮化合物。 还公开了包含新的恶唑烷酮衍生物，其体内可水解的酯，其体内可水解的磷酸酯，其异构体或其药学上可接受的盐作为有效成分的药物抗生素组合物。 因为新的恶唑烷酮衍生物，其体内可水解的酯，其体内可水解的磷酸酯，其异构体或其药学上可接受的盐，表现出对抗细菌的抗菌谱广，毒性低，抗革兰氏阳性 和革兰阴性菌，可以有效地用作抗生素。

    PIPERAZINYL-PROPYL-PYRAZOLE DERIVATIVES AS DOPAMINE D4 RECEPTOR ANTAGONISTS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    10.
    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。