세로토닌 5-HT6 저해 활성을 갖는 5-설포닐아미노-5,6-다이하이드로-1H-피라졸로[3,4-c]피리딘-7(4H)-온 화합물
    11.
    发明公开
    세로토닌 5-HT6 저해 활성을 갖는 5-설포닐아미노-5,6-다이하이드로-1H-피라졸로[3,4-c]피리딘-7(4H)-온 화합물 有权
    新型5-磺酰氨基-5,6-二氢-1H-吡唑并[3,4-C]吡啶-7(4H) - 酮化合物,其具有丝氨酸5-HT6的抑制活性

    公开(公告)号:KR1020140118141A

    公开(公告)日:2014-10-08

    申请号:KR1020130033552

    申请日:2013-03-28

    Abstract: The present invention relates to a novel 5-sulfonylamino-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one compound having an inhibitory activity for 5-HT6, which is one of serotonin subtypes, and a pharmaceutical composition comprising the compound as an active ingredient. Since the novel compound of the present invention has 5-HT6 inhibitory activities, the compound can be used for diagnosing, preventing, and treating central nervous system (CNS) diseases such as Alzheimer′s disease (AD), attention deficit disorder (ADHD), epilepsy, depression, obesity, schizophrenia, sleep disorders, and pain disorders.

    Abstract translation: 本发明涉及对5-HT6具有抑制活性的新的5-磺酰基氨基-5,6-二氢-1H-吡唑并[3,4-c]吡啶-7(4H) - 酮化合物,其为5-羟色胺 亚型和包含该化合物作为活性成分的药物组合物。 由于本发明的新化合物具有5-HT 6抑制活性,所以该化合物可用于诊断,预防和治疗中枢神经系统(CNS)疾病如阿尔茨海默病(AD),注意缺陷障碍(ADHD) ,癫痫,抑郁症,肥胖,精神分裂症,睡眠障碍和疼痛障碍。

    5―HT7 수용체에 작용하는 바이페닐 아마이드 유도체
    14.
    发明公开
    5―HT7 수용체에 작용하는 바이페닐 아마이드 유도체 有权
    在5-HT7受体上起作用的联苯胺衍生物

    公开(公告)号:KR1020130102828A

    公开(公告)日:2013-09-23

    申请号:KR1020120023966

    申请日:2012-03-08

    Inventor: 추현아 김영재

    Abstract: PURPOSE: A biphenyl amide derivative is provided to show superior activity as a neuroprotective agent which functions on mitochondria and to be used as an effective agent for preventing and treating central nervous system disorders. CONSTITUTION: A biphenyl amide derivative is denoted by chemical formula 1. A method for preparing the derivative comprises the steps of bonding a compound of chemical formula 2 and a compound of chemical formula 3. A pharmaceutical composition which functions on 5-HT_7 receptor contains the biphenyl compound of chemical formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的:提供联苯酰胺衍生物作为在线粒体上起作用并用作预防和治疗中枢神经系统疾病的有效药物的神经保护剂的优异活性。 组成:联苯酰胺衍生物由化学式1表示。制备衍生物的方法包括将化学式2的化合物和化学式3的化合物键合的步骤。在5-HT_7受体上起作用的药物组合物含有 化学式1的联苯化合物或其药学上可接受的盐作为活性成分。

    항암활성을 지닌 카르보아졸계 화합물
    16.
    发明公开
    항암활성을 지닌 카르보아졸계 화합물 有权
    具有抗癌活性的新型咔唑类化合物

    公开(公告)号:KR1020120056684A

    公开(公告)日:2012-06-04

    申请号:KR1020100118341

    申请日:2010-11-25

    Abstract: PURPOSE: A carboazole-based compounds with an anticancer activity and a method for preparing the same are provided to prevent and treat cancer. CONSTITUTION: A carboazole-based compound with an anticancer activity is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the carboazole-based compounds of chemical formula 1. A method for preparing the carboazole-based compounds comprises: a step of reacting amidation of heterocyclic compounds of chemical formula III with 4-haloazole compounds of chemical formula IV to prepare a 4-halocaboazole-based compound of chemical formula V; and a step of performing Suzuki coupling of the compound of chemical formula V with a boronic acid compound of chemical formula VI.

    Abstract translation: 目的:提供具有抗癌活性的基于咔唑的化合物及其制备方法,以预防和治疗癌症。 构成:具有抗癌活性的基于唑的化合物由化学式1表示。用于抗癌的药物组合物含有化学式1的咔唑类化合物。一种制备该类咔唑类化合物的方法包括:使酰胺化反应 的化学式III的4-卤唑化合物的化学式III的杂环化合物,以制备化学式V的4-卤代咔唑类化合物; 以及化学式V化合物与化学式VI的硼酸化合物的Suzuki偶联的步骤。

    GSK-3 억제활성을 보이는 1H-인다졸 화합물
    17.
    发明公开
    GSK-3 억제활성을 보이는 1H-인다졸 화합물 有权
    具有GSK-3抑制活性的1H-吲唑化合物

    公开(公告)号:KR1020120038033A

    公开(公告)日:2012-04-23

    申请号:KR1020100097910

    申请日:2010-10-07

    Abstract: PURPOSE: A 1H-indazole compound with GSK3 inhibition and pharmaceutically acceptable salt thereof are provided to be used as a therapeutic agent for treating diseases caused by GSK-3 activation. CONSTITUTION: A 1H-indazole compounds is denoted by chemical formula 1. A method for preparing the compound comprises: a step of performing amidation of 3-amino-1H-indazole compounds of chemical formula 2 and a substituted carboxylic acid compound of chemical formula 3 under the presence of pyridine base and 1-ethyl-3-(3'-dimethyl aminopropyl)carbodiimide hydrochloride(EDCI).

    Abstract translation: 目的:提供具有GSK3抑制的1H-吲唑化合物及其药学上可接受的盐作为治疗由GSK-3激活引起的疾病的治疗剂。 构成:1H-吲唑化合物由化学式1表示。一种制备化合物的方法包括:进行化学式2的3-氨基-1H-吲唑化合物和化学式3的取代的羧酸化合物的酰胺化步骤 在吡啶碱和1-乙基-3-(3'-二甲基氨基丙基)碳二亚胺盐酸盐(EDCI)的存在下。

    옥사스파이로 화합 및 이 화합물의 제조방법
    20.
    发明公开
    옥사스파이로 화합 및 이 화합물의 제조방법 有权
    OXASPIRO化合物及其制备方法

    公开(公告)号:KR1020100090979A

    公开(公告)日:2010-08-18

    申请号:KR1020090010234

    申请日:2009-02-09

    Abstract: PURPOSE: An oxaspiro compound and a method for preparing the same are provided to be used as an intermediate in a natural product or novel drug synthesis. CONSTITUTION: An oxaspiro compound is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are hydrogen, alkyl group of C1-C6, halogen, nitro, alkyl of C1-C6, or substituted or non-substituted phenyl group as a substituent of C1-C6 alkoxy. The oxaspiro compound of chemical formula 1 is prepared by reacting a carbo compound of chemical formula 3 with methylene cycloalkandiol of chemical formula 2 under the presence of lewis acid. The reaction solvent is dichloro methane. Trimethylsilyl trifluoromethansulfonate(TMSOTf) is used as the lewis acid.

    Abstract translation: 目的:提供氧杂螺环化合物及其制备方法,用作天然产物或新药合成中的中间体。 化学式1中,R1和R2为氢,C1-C6烷基,卤素,硝基,C1-C6烷基或取代或未取代的苯基,为 C1-C6烷氧基的取代基。 化学式1的氧杂螺环化合物通过在路易斯酸存在下使化学式3的碳化合物与化学式2的亚甲基环二醇反应来制备。 反应溶剂是二氯甲烷。 三氯甲磺酸三甲基甲硅烷基酯(TMSOTf)用作路易斯酸。

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