T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물
    35.
    发明公开
    T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물 有权
    5-(取代的烷基氨基甲酰基)异噻唑衍生物作为T型钙通道拮抗剂

    公开(公告)号:KR1020120096842A

    公开(公告)日:2012-08-31

    申请号:KR1020110016203

    申请日:2011-02-23

    CPC classification number: C07D413/12

    Abstract: PURPOSE: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is provided to have excellent activity as an antagonist of T- type calcium ion channel. CONSTITUTION: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is represented by chemical formula 1. The encephalopathy therapy and for prevention agent selected from epilepsy, depression, Parkinson's disease, dementia, sleep disorder, an agent for cancer treatment and prevention, an agent for heart disease treatment and prevention selected from hypertensive, cardiac arrhythmia, angina, myocardial infarction, congestive heart failure, pharmaceutical composition for alleviating pain selected from neuropathic pain and chronic and acute pain includes a compound represented by chemical formula 1.

    Abstract translation: 目的:提供作为T型钙通道阻滞剂的5-(取代的烷基氨基甲基)异恶唑基化合物作为T-型钙离子通道的拮抗剂具有优异的活性。 构成:以化学式1表示作为T型钙通道阻断剂的5-(取代烷基氨基甲基)异恶唑类化合物。脑病治疗和预防药物选自癫痫,抑郁症,帕金森病,痴呆,睡眠障碍, 癌症治疗和预防,选自高血压,心律失常,心绞痛,心肌梗塞,充血性心力衰竭,减轻选自神经性疼痛和慢性和急性疼痛的疼痛的药物组合物的心脏病治疗和预防剂,包括由化学式 1。

    T-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법
    36.
    发明公开
    T-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법 有权
    具有T型钙通道活性的新型奥氮唑 - 哌嗪化合物

    公开(公告)号:KR1020110020023A

    公开(公告)日:2011-03-02

    申请号:KR1020090077687

    申请日:2009-08-21

    Abstract: PURPOSE: An oxazole-piperazine compound having a pharmaceutical activity with respect to T-type calcium channel is provided to ensure excellent activity as an antagonist of the channel and to prevent and treat cancer, epilepsy, heart diseases, and pain. CONSTITUTION: An oxazole-piperazine compounds is denoted by chemical formula 1. A pharmaceutical composition for treating epilepsy, cancer, hypertension, myocardial infarction, neuropathic pain, and acute and chronic pain contains the oxazole-piperazine compound of chemical formula 1. The compound of chemical formula 1 is prepared by reacting piperazine-amine compound of chemical formula 2 and oxazole aldehyde compound of chemical formula 3 by reductive amination. The reductive amination is performed under the presence of molecules of 4-8 meshes and NaBH(OAc)_3, NaBH_3CN, or NaBH_4.

    Abstract translation: 目的:提供相对于T型钙通道具有药学活性的恶唑 - 哌嗪化合物,以确保作为通道拮抗剂的优异活性,并预防和治疗癌症,癫痫,心脏病和疼痛。 构成:化学式1表示恶唑 - 哌嗪化合物。用于治疗癫痫,癌症,高血压,心肌梗死,神经性疼痛和急性和慢性疼痛的药物组合物含有化学式1的恶唑 - 哌嗪化合物。 化学式1通过化学式2的哌嗪 - 胺化合物和化学式3的恶唑醛化合物通过还原胺化反应来制备。 还原胺化在4-8目和NaBH(OAc)3,NaBH 3 CN或NaBH 4的分子存在下进行。

    이소옥사졸 피페라진 계열의 화합물의 제조방법 및 그것에 의해 제조된 라이브러리
    37.
    发明授权
    이소옥사졸 피페라진 계열의 화합물의 제조방법 및 그것에 의해 제조된 라이브러리 失效
    用于制备具有异噻唑啉哌嗪类化合物及其文库的化合物的方法

    公开(公告)号:KR100343947B1

    公开(公告)日:2002-07-22

    申请号:KR1019990041613

    申请日:1999-09-28

    Abstract: 본발명은화학식 1을갖는이소옥사졸피페라진계열의화합물또는그 염의제조방법및 상기방법에의해만들어진라이브러리에관한것으로, 상기방법은화학식 2의화합물과화학식 3의화합물을염기및 염소화제의존재하에 1,3-쌍극자고리화첨가반응시켜화학식 1 또는그 염의화합물을제조하는것으로구성된다. 그화학식 1, 2, 3과반응식 1은다음과같다. 상기화학식 1, 2, 3과반응식 1에서, R및 R는페닐, 벤질, 할로겐화페닐, C-C의알킬기로치환된페닐, C-C의알콕시기로치환된페닐, (트리플루오로)메틸페닐, 피리딜등의페닐유도체를말하며, R-R는수소이며, X는질소이며,는이중결합또는삼중결합을의미하며,는이중결합또는단일결합을의미한다.

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