Abstract:
PURPOSE: A phenylpyrazolyl methyl-2-(4-substituted piperidine-1-yl)acetamide derivative as a calcium ion channel modulator is provided to be used as an agent for preventing and treating heart diseases or pain. CONSTITUTION: A phenylpyrazolyl methyl-2-(4-substituted piperidine-1-yl)acetamide derivative is denoted by chemical formula 1. An agent for preventing and treating heart diseases or an agent for relieving chronic and acute pain contains the compound of chemical formula 1 as an active ingredient.
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:
본 발명은 T-형 칼슘 채널에 대한 활성을 갖는 1-(4-치환-1,4-디아제판-1-일)에탄온 화합물, 상기 화합물의 제조방법, 그리고 상기 화합물을 유효성분으로 포함하는 약학조성물에 관한 것이다. 본 발명의 신규 1-(4-치환-1,4-디아제판-1-일)에탄온 화합물 또는 약학적으로 허용 가능한 이의 염은 T-형 칼슘 채널에 대한 길항작용을 가지므로 간질, 고혈압 등의 뇌질환 치료제, 협심증 등의 심장질환 치료제, 만성 통증, 신경성 통증 등의 통증질환 치료제, 또는 항암제로 유용하다.
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:
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。
Abstract:
본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다. 피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제
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,