세로토닌 5-HT6 저해 활성을 갖는 5,6,7,8-테트라하이드로퀴나졸린-2-아민 화합물

    公开(公告)号:KR101730790B1

    公开(公告)日:2017-04-28

    申请号:KR1020150186413

    申请日:2015-12-24

    Abstract: 본발명은세로토닌서브타입중하나인 5-HT수용체에대하여저해활성을가지는신규 5,6,7,8-테트라하이드로퀴나졸린-2-아민화합물과상기화합물이포함된중추신경계 (CNC) 질환의예방또는치료용약제조성물또는중추신경계 (CNC) 질환의진단시약에관한것이다. 본발명의신규화합물은 5-HT수용체에대한결합력및 저해활성을가지므로알쯔하이머(AD), 주의력결핍증(ADHD), 간질, 우울증(depression), 비만, 정신분열증, 수면장애, 통증불안증과같은중추신경계(CNS, central nervous system) 질환의진단, 예방및 치료를목적으로유용하게사용될수 있다.

    5-HT7 수용체에 작용하는 카바졸 유도체
    33.
    发明授权
    5-HT7 수용체에 작용하는 카바졸 유도체 有权
    作用于5-HT7受体的5-HT7咔唑衍生物

    公开(公告)号:KR101672943B1

    公开(公告)日:2016-11-04

    申请号:KR1020140048074

    申请日:2014-04-22

    Abstract: 본발명은 5-HT수용체에작용하는카바졸유도체및 이의약제학적으로허용가능한염에관한것으로, 5-HT세로토닌수용체에대하여우수한결합친화력과우수한길항활성을가져 5-HT길항활성이요구되는우울증, 편두통, 불안, 통증, 염증성통증, 신경병성통증, 체온조절장애, 생체리듬조절장애, 수면장애및 평활근관련질환등의중추신경계질환의치료및 예방제로유용하게적용할수 있다.

    Abstract translation: 本发明涉及作用于5-HT_7受体的咔唑衍生物及其药学上可接受的盐,其中5-HT_7受体具有优异的结合亲和力和优异的拮抗活性,因此可用于应用于治疗和预防中枢的药剂 神经系统疾病,如需要5-HT_7拮抗活性的重症抑郁障碍,偏头痛,焦虑症,疼痛,炎症性疼痛,神经性疼痛,温度调节障碍,昼夜节律调节障碍,睡眠障碍和平滑肌相关障碍等。

    퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물 및 이의 스크리닝 방법
    35.
    发明公开
    퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물 및 이의 스크리닝 방법 无效
    用于预防或治疗变应性脑病的药物组合物及其筛选方法

    公开(公告)号:KR1020140058480A

    公开(公告)日:2014-05-14

    申请号:KR1020140047606

    申请日:2014-04-21

    CPC classification number: A61K31/44 A61K31/437 A61K31/55

    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases, and a screening method thereof. According to an embodiment of the present invention, by applying the screening method which screens candidate substances for preventing or treating neurodegenerative diseases, a substance for preventing or treating neurodegenerative diseases can be effectively screened. The pharmaceutical composition for preventing or treating neurodegenerative diseases obtained by the screening method can effectively prevents or treats various neurodegenerative diseases.

    Abstract translation: 本发明涉及用于预防或治疗神经变性疾病的药物组合物及其筛选方法。 根据本发明的一个实施方案,通过应用筛选候选物质的预防或治疗神经变性疾病的筛选方法,可以有效地筛选用于预防或治疗神经变性疾病的物质。 用于预防或治疗通过筛选方法获得的神经变性疾病的药物组合物可以有效地预防或治疗各种神经变性疾病。

    메틸리덴-헤테로싸이클릭 화합물
    36.
    发明公开
    메틸리덴-헤테로싸이클릭 화합물 有权
    甲基 - 杂环化合物

    公开(公告)号:KR1020130010784A

    公开(公告)日:2013-01-29

    申请号:KR1020110071653

    申请日:2011-07-19

    Abstract: PURPOSE: A methylidene-heterocyclic compound and a pharmaceutical composition containing the same are provided to strongly suppress IkappaB kinase-b(IKK-b) and to treat various inflammatory diseases. CONSTITUTION: A methylidene-heterocyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating inflammatory diseases contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, juvenile arthritis, asthma, spondyloarthopathies, gout, osteoarthritis, allergic rhinitis, atopic dermatitis, systemic lupuserythematosus, psoriasis, ulcerative colitis, SIRS, sepsis, or polymyositis. A method for preparing the compound of chemical formula 1 comprises: a step of cyclizing an aniline compound of chemical formula 2 and preparing a 3-phenyl rhodanine compound of chemical formula 3; and a step of condensing the compound of chemical formula 3 with aldehyde compound of R2-C(O)H under an acidic condition. [Reference numerals] (AA) Step 1; (BB) Step 2

    Abstract translation: 目的:提供亚甲基杂环化合物和含有它们的药物组合物以强烈抑制IkappaB激酶b(IKK-b)并治疗各种炎性疾病。 构成:亚甲基杂环化合物由化学式1表示。用于预防和治疗炎性疾病的药物组合物含有化学式1的化合物作为活性成分。 炎性疾病包括类风湿性关节炎,青少年关节炎,哮喘,脊椎动物病痛,痛风,骨关节炎,过敏性鼻炎,特应性皮炎,系统性红斑狼疮,牛皮癣,溃疡性结肠炎,SIRS,败血症或多发性肌炎。 制备化学式1的化合物的方法包括:使化学式2的苯胺化合物环化并制备化学式3的3-苯基绕丹宁化合物的步骤; 和在酸性条件下将化学式3的化合物与R2-C(O)H的醛化合物缩合的步骤。 (附图标记)(AA)步骤1; (BB)步骤2

    1,6-이치환-3-아미노-4,5,6,7-테트라하이드로-1H-피라졸로[3,4-c]피리딘-7-온 화합물 및 이 화합물의 제조방법
    39.
    发明公开
    1,6-이치환-3-아미노-4,5,6,7-테트라하이드로-1H-피라졸로[3,4-c]피리딘-7-온 화합물 및 이 화합물의 제조방법 有权
    新的1,6-二异丙基氨基-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备方法

    公开(公告)号:KR1020110139988A

    公开(公告)日:2011-12-30

    申请号:KR1020100060138

    申请日:2010-06-24

    CPC classification number: C07D471/04

    Abstract: PURPOSE: A novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one is provided to suppress cancer cells. CONSTITUTION: A 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one compound is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of alkylating 3-amino compounds of chemical formula 2 with haloalkylcarbonyl piperazine of chemical formula 3 by alkylating.

    Abstract translation: 目的:提供新颖的1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮以抑制癌细胞。 构成:1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物由化学式1表示。用于抗癌的药物组合物含有化合物 的化学式1或其药学上可接受的盐作为活性成分。 制备化学式1的化合物的方法包括通过烷基化将化学式2的3-氨基化合物与化学式3的卤代烷基羰基哌嗪烷基化的步骤。

    3,6-이치환-4,5,6,7-테트라하이드로-1H-피라졸로[3,4-c]피리딘-7-온 화합물과 이 화합물의 제조방법
    40.
    发明公开
    3,6-이치환-4,5,6,7-테트라하이드로-1H-피라졸로[3,4-c]피리딘-7-온 화합물과 이 화합물의 제조방법 有权
    新的3,6-取代-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备方法

    公开(公告)号:KR1020110121868A

    公开(公告)日:2011-11-09

    申请号:KR1020100041360

    申请日:2010-05-03

    Abstract: PURPOSE: A novel 3,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound is provided to suppress cancer cell and to be used as an anticancer agent. CONSTITUTION: A 3,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises: a step of performing acrylation of 3-amino compound of chemical formula 2 with acyl halide compound of chemical formula 3 to prepare 3-haloacylcarbamoyl compound of chemical formula 4; and a step of substituting 3-haloacylcarbamoyl compound of chemical formula 4 with amine compounds of chemical formula 5.

    Abstract translation: 目的:提供新的3,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物以抑制癌细胞并用作抗癌剂 。 构成:3,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮由化学式1表示。用于抗癌的药物组合物含有 化学式1为活性成分。 制备化学式1化合物的方法包括:用化学式3的酰卤化合物进行化学式2的3-氨基化合物的丙烯酸化以制备化学式4的3-卤代酰基氨基甲酰基化合物的步骤; 和用化学式5的胺化合物代替化学式4的3-卤代酰基氨基甲酰基化合物的步骤。

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