변이형 FADD-DD 단백질 및 이를 암호화하는 염기서열
    4.
    发明公开
    변이형 FADD-DD 단백질 및 이를 암호화하는 염기서열 无效
    FADD-DD突变蛋白及其编码基因

    公开(公告)号:KR1020020042882A

    公开(公告)日:2002-06-08

    申请号:KR1020000072220

    申请日:2000-12-01

    CPC classification number: C07K14/4703

    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。

    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법
    7.
    发明公开
    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법 失效
    新型吡咯烷基胺化合物作为钙通道调节剂及其制备方法

    公开(公告)号:KR1020100042111A

    公开(公告)日:2010-04-23

    申请号:KR1020080101249

    申请日:2008-10-15

    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 translation: 目的:提供作为钙离子通道调节剂有效的吡唑基甲胺 - 哌嗪衍生物,以确保作为T型钙离子通道拮抗剂的有效活化,并用作预防和治疗脑疾病,心脏病和疼痛疾病的药剂。 构成:吡唑基甲胺 - 哌嗪衍生物由化学式1表示。用于通过T型钙离子通道拮抗作用预防和治疗脑疾病,心脏病或疼痛疾病的药物组合物含有化学式1的吡唑基甲基 - 哌嗪衍生物或其药学上可接受的盐 可接受的盐为活性成分。 脑疾病是癫痫,抑郁症,帕金森病,痴呆或嗜睡。 心脏病是高血压,心律失常,心肌梗死或充血性衰竭。 疼痛疾病是慢性疼痛,急性疼痛或神经源性疼痛。 通过将化学式3的吡唑基甲基胺化合物与化学式2的哌嗪乙酰卤化合物结合,制备吡唑基甲胺 - 哌嗪衍生物。

    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법
    10.
    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。

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