Abstract:
PURPOSE: A pyrazolylmethylamine-piperazine derivative which is effective as a calcium ion channel modulator is provided to ensure effective activation as an T-type calcium ion channel antagonist and to use as an agent for preventing and treating brain diseases, heart diseases and pain diseases. CONSTITUTION: A pyrazolylmethylamine-peperazine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases, heart diseases or pain diseases by T-type calcium ion channel antagonism contains the pyrazolylmethylamine-peperazine derivative of chemical formula 1 or its pharmaceutically acceptable salt an active ingredient. The brain disease is epilepsy, depression, Parkison's disease, dementia or somnipathy. The heart disease is hypertension, cardiac arrhythmia, myocardial infarction, or congestive failure. The pain disease is chronic pain, acute pain, or neurogenic pain. The pyrazolylmethylamine-peperazine derivative is prepared by binding pyrazolylmethylamine compound of chemical formula 3 with piperazine acetyl halide compound of chemical formula 2.
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, (a) p K a 값이 상이한 술폰아미드 스티렌계 또는 술폰아미드 아크릴계 단량체를 제공하고, (b) 열 응답성 폴리이소프로필아크릴아미드 또는 폴리메틸렌비스아크릴아미드를 제공하고, (c) 상기 (a) 단계는 합성된 단량체를 극성 또는 비극성 용매 중에서 조절/리빙 중합에 따라 폴리이소프로필아크릴아미드 또는 폴리메틸렌비스아크릴아미드와 공중합시킴으로써, 분자량이 조절되고 열 및 pH에 대한 이중 자극 응답성 (Dual Stimuli-Responsive)을 갖는 하이드로젤의 랜덤 및 블록 공중합체를 제조하는 방법에 관한 것이다.
Abstract:
PURPOSE: A plasmid for expressing protein containing thioredoxin as a fusion partner is provided to easily remove thioredoxin and to massively produce a target protein. CONSTITUTION: A pET-32-S(-) plasmid contains a multi-cloning site for inserting thioredoxin gene, thrombin recognition site, S-tag coding region, and a gene encoding a target protein. A method for producing the target protein comprises: a step of inserting the gene encoding target protein into a multi-cloning site of a plasmid; a step of transforming the plasmid to E.coli and culturing; and a step of treating thrombine.
Abstract:
본 발명은 인산기-선택적인 형광 프로브의 제조 방법에 관한 것으로서, 특히 특정 구조의 인산기 결합성 물질에 형광 물질을 공유 결합시킨 후, 생성 화합물을 금속 이온과 배위 결합시키는 것을 포함하는, 인산기-선택적인 형광 프로브의 제조 방법에 관한 것이다. 본 발명에 따라 제조된 인산기-선택적인 형광 프로브는 포스파타제 활성 측정 방법에 유용하게 이용될 수 있다. 포스파타제 (phosphatase), 탈인산화 반응 (dephosphorylation), CIP (calf intestinal alkaline phosphatase), 형광 편광도 (fluorescence polarization), 인산기-선택적인 프로브 (phosphate-specific probe).
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