칼슘 채널에 활성을 지닌 신규 피라조일 피페라진 화합물
    42.
    发明公开
    칼슘 채널에 활성을 지닌 신규 피라조일 피페라진 화합물 有权
    吡唑基哌嗪化合物作为钙通道拮抗剂

    公开(公告)号:KR1020120125098A

    公开(公告)日:2012-11-14

    申请号:KR1020110043180

    申请日:2011-05-06

    Abstract: PURPOSE: A pyrazolyl piperazine compound with a pharmaceutical activity to a calcium channel and a pharmaceutical composition containing the same are provided to be used as a pharmaceutical composition for preventing or treating diseases of brain diseases, heart diseases, cancer, and pain. CONSTITUTION: A pyrazolyl piperazine compound is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by binding piperazine compounds of chemical formula 2 and chloride compounds of chemical formula 3 under the presence of a base at 20-30 Deg. C. The base includes an organic base such as an amine-based base and an inorganic base. The reaction solvent is dichloromethane, tetrahydrofurane(THF), dimethyl formamide(DMF), dimethyl aceteamide(DMAC), and dioxane. A pharmaceutical composition for preventing brain diseases, cancer, heart diseases, or pain contains the compound of chemical formula 1.

    Abstract translation: 目的:提供对钙通道具有药学活性的吡唑基哌嗪化合物和含有该通道的药物组合物作为预防或治疗脑疾病,心脏病,癌症和疼痛疾病的药物组合物。 构成:化学式1表示吡唑基哌嗪化合物。化学式1的化合物是通过在20-30度的碱存在下将化学式2的哌嗪化合物和化学式3的氯化合物结合而制备的。 C.碱包括有机碱如胺基和无机碱。 反应溶剂为二氯甲烷,四氢呋喃(THF),二甲基甲酰胺(DMF),二甲基乙酰胺(DMAC)和二恶烷。 用于预防脑疾病,癌症,心脏病或疼痛的药物组合物含有化学式1的化合物。

    T-형 칼슘 채널에 활성을 지닌 신규 다이페닐프로판노일 화합물
    45.
    发明公开
    T-형 칼슘 채널에 활성을 지닌 신규 다이페닐프로판노일 화합물 有权
    具有T型钙通道活性的新型二苯基丙烯酸酯化合物

    公开(公告)号:KR1020110119045A

    公开(公告)日:2011-11-02

    申请号:KR1020100038514

    申请日:2010-04-26

    CPC classification number: Y02P20/55

    Abstract: PURPOSE: A diphenylpropanoyl compound having T-type calcium channel activity is provided to ensure antagonism to a T-type calcium channel and to be used as a therapeutic agent and anticancer agent. CONSTITUTION: A diphenylpropanoyl is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating hypertension, angina, chronic pain, neurogenic pain or cancer contains a compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of binding a compound of chemical formula 2 with a compound of chemical formula 3.

    Abstract translation: 目的:提供具有T型钙通道活性的二苯基丙酰基化合物,以确保对T型钙通道的拮抗作用,并用作治疗剂和抗癌剂。 构成:二苯基丙酰基由化学式1表示。用于预防和治疗高血压,心绞痛,慢性疼痛,神经源性疼痛或癌症的药物组合物含有化学式1化合物作为活性成分。 制备化学式1的化合物的方法包括将化学式2的化合物与化学式3的化合物结合的步骤。

    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법
    47.
    发明公开
    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법 失效
    新型咪唑啉酮衍生物作为钙通道调节剂及其制备方法

    公开(公告)号:KR1020100001288A

    公开(公告)日:2010-01-06

    申请号:KR1020080061148

    申请日:2008-06-26

    Abstract: PURPOSE: A novel imidazolylalkylcarbonyl derivative which is effective as calcium ion channel regulator is provided to effectively block T-type calcium ion channel, prevent and treat brain diseases, heart diseases and pain. CONSTITUTION: An imidazolylalkylcarbonyl derivative is denoted by chemical formula 1. The imidazolylalkylcarbonyl derivative of chemical formula 1 is prepared by performing amide bond of piperazine derivative of chemical formula 3 with imidazolylalkylcarboxylic acid of chemical formula 2. The amide bond is performed using binder selected from phosphonium system, ammonium system, carbodiimide system, imidazolinium, and organic phosphine system. A method for preparing the imidazolylalkylcarboxylic acid of chemical formula 2 comprises: a step of performing hetero-michael addition reaction of ethy alkenoate with imidazole compound under the presence of KF/Al2O3 catalyst to produce ethoxycarbonylalkylimidazole compound of chemical formula 2a; and a step of hydrolyzing the ethoxycarbonylalkylimidazole compound of chemical formula 2a to prepare imidazolylalkylcarboxylic acid of chemical formula 2.

    Abstract translation: 目的:提供一种有效阻断T型钙离子通道,预防和治疗脑疾病,心脏病和疼痛的新型咪唑烷基羰基衍生物,作为钙离子通道调节剂有效。 构成:化学式1表示咪唑烷基羰基衍生物。化学式1的咪唑烷基羰基衍生物通过化学式3的哌嗪衍生物与化学式2的咪唑基烷基羧酸的酰胺键进行制备。酰胺键使用选自鏻 系统,铵系统,碳二亚胺系统,咪唑啉鎓和有机膦系统。 制备化学式2的咪唑基烷基羧酸的方法包括:在KF / Al 2 O 3催化剂存在下,进行异丁烯酸乙酯与咪唑化合物的异迈克尔加成反应,生成化学式2a的乙氧基羰基烷基咪唑化合物的步骤; 以及水解化学式2a的乙氧基羰基烷基咪唑化合物以制备化学式2的咪唑基烷基羧酸的步骤。

    치자 추출물 및 치자로부터 분리된 신규 화합물 및 그 용도
    49.
    发明授权
    치자 추출물 및 치자로부터 분리된 신규 화합물 및 그 용도 失效
    栀子提取物及其分离的化合物及其用途

    公开(公告)号:KR100543897B1

    公开(公告)日:2006-01-23

    申请号:KR1020030036482

    申请日:2003-06-05

    Abstract: 본 발명은 활성산소 소거활성 및 항바이러스활성을 가지는 치자 추출물, 그로부터 분리된 신규한 화합물 및 그 용도에 관한 것이다. 보다 상세하게는 물 또는 유기용매로 추출되며, 유효성분으로 메틸 5-
    O -카페오일-4-
    O -시나포일퀴네이트, 메틸 3,5-
    O -디카페오일-4-
    O -(3-히드록시-3-메틸)글루타로일퀴네이트, 에틸 5-
    O -카페오일-4-
    O -시나포일퀴네이트, 메틸 3-
    O -카페오일-5-
    O -시나포일퀴네이트, 에틸 3-
    O -카페오일-5-
    O -시나포일퀴네이트, 3,5-
    O - 디카페오일퀴닉산 및 4,5-
    O -디카페오일퀴닉산을 포함하는 활성산소소거활성 및 항바이러스활성을 나타내는 치자추출물. 그로부터 분리된 신규 화합물에 관한 것이다.
    본 발명에 의한 치자 추출물 및 분리된 신규화합물들은 DPPH 자유라디칼, 슈퍼옥사이드 음이온 라디칼 등의 활성산소 소거활성이 우수하여 활성 산소에 의한 질병을 치료 및 예방하는데 뛰어난 효과가 있으며, 인간면역결핍바이러스의 인티그라제에 대한 저해 활성 및 항바이러스활성도 높아 AIDS 등 바이러스성 질환의 치료에 응용될 수 있다.
    치자, 활성산소 소거활성, 인티그라제(integrase), 항바이러스활성, AIDS,

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