Abstract:
본 발명은 신규한 벤조아릴우레이도 화합물, 및 이의 퇴행성 뇌질환 예방 또는 치료에 있어서의 용도에 관한 것으로, 보다 상세하게는, 화학식 1의 구조를 갖는 벤조아릴우레이도 화합물, 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 예방 또는 치료용 조성물에 관한 것이다. 상기 퇴행성 뇌질환은 알츠하이머, 치매, 파킨슨병, 뇌졸중, 아밀로이드증, 픽 질환 (Pick's disease), 루게릭병, 헌팅턴병, 크로이츠펠트-야콥(Creutzfeld-Jakob)병 등일 수 있다. [화학식 1]
Abstract:
본 발명은 칼슘이온 채널 조절제로서 유효한 신규 이미다졸릴알킬카르보닐 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다. 이미다졸릴알킬카르보닐 유도체, 칼슘이온 채널 조절제, 뉴런, 탈분극화, 급성통증, 만성통증, 신경병증성 통증, 고혈압치료제.
Abstract:
PURPOSE: A novel benzoarylureido compound is provided to prevent the degeneration and damage of brain cells caused by beta-amyloid and to prevent or treat a neurodegenerative disorder. CONSTITUTION: A novel benzoarylureido compound has a structure of chemical formula 1. A composition for preventing or treating a neurodegenerative disorder contains a compound of chemical formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient. The composition is used in the form of a tablet, injection, capsule, or pill. A health food for preventing or treating a neurodegenerative disorder contains a compound of chemical formula 1 or a pharmaceutically acceptable salt as an active ingredient.
Abstract:
PURPOSE: The FADD-DD mutant proteins and genes encoding for the same are provided, thereby the FADD-DD mutant proteins capable of selectively transferring the cell death signal of Fas or TNF-alpha(tumor necrosis factor-alpha) can be prepared and the proteins can be effectively used in study on chemical therapy and cell death by stress. CONSTITUTION: The FADD-DD(Fas-associated death domain protein-death domain) mutant protein has the amino acid sequence of which 110th amino acid is substituted with an amino acid selected from glycine, alanine, valine, leucine and isoleucine. The FADD-DD mutant protein R110A, wherein 110th amino acid of the FADD-DD protein is substituted with alanine, has the amino acid sequence of SEQ ID NO: 11. A gene encoding for the FADD-DD mutant protein R110A has the nucleotide sequence of SEQ ID NO: 5. The FADD-DD mutant protein has the amino acid sequence of which 117th amino acid is substituted with an amino acid selected from glycine, alanine, valine, leucine and isoleucine. The FADD-DD mutant protein R117A, wherein 117th amino acid of the FADD-DD protein is substituted with alanine, has the amino acid sequence of SEQ ID NO: 12. A gene encoding for the FADD-DD mutant protein R117A has the nucleotide sequence of SEQ ID NO: 7.
Abstract translation:目的:提供FADD-DD突变蛋白和编码其的基因,从而可以制备能够选择性转移Fas或TNF-α(肿瘤坏死因子-α)细胞死亡信号的FADD-DD突变蛋白, 蛋白质可以有效地用于化学治疗和细胞死亡应激的研究。 构成:FADD-DD(Fas相关的死亡域蛋白 - 死亡域)突变蛋白具有氨基酸序列,其第110位氨基酸被选自甘氨酸,丙氨酸,缬氨酸,亮氨酸和异亮氨酸的氨基酸取代。 FADD-DD突变蛋白R110A,其中FADD-DD蛋白质的第110位氨基酸被丙氨酸取代,具有SEQ ID NO:11的氨基酸序列。编码FADD-DD突变蛋白R110A的基因具有核苷酸序列 的FADD-DD突变蛋白具有第117位氨基酸被选自甘氨酸,丙氨酸,缬氨酸,亮氨酸和异亮氨酸的氨基酸取代的氨基酸序列。 FADD-DD突变蛋白R117A,其中FADD-DD蛋白的第117位氨基酸被丙氨酸取代,具有SEQ ID NO:12的氨基酸序列。编码FADD-DD突变蛋白R117A的基因具有核苷酸序列 的SEQ ID NO:7。
Abstract:
본 발명은 칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체 및 이의 약제학적으로 허용 가능한 염, 이들 화합물의 제조방법, 그리고 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다. 피라졸릴메틸아민-피페라진 유도체, 칼슘이온 채널 조절제, 뉴런, 탈분극화, 급성통증, 만성통증, 신경병증성 통증, 고혈압치료제
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:
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。