GSK-3 억제활성을 보이는 1H-인다졸 화합물
    21.
    发明公开
    GSK-3 억제활성을 보이는 1H-인다졸 화합물 有权
    具有GSK-3抑制活性的1H-吲唑化合物

    公开(公告)号:KR1020120038033A

    公开(公告)日:2012-04-23

    申请号:KR1020100097910

    申请日:2010-10-07

    Abstract: PURPOSE: A 1H-indazole compound with GSK3 inhibition and pharmaceutically acceptable salt thereof are provided to be used as a therapeutic agent for treating diseases caused by GSK-3 activation. CONSTITUTION: A 1H-indazole compounds is denoted by chemical formula 1. A method for preparing the compound comprises: a step of performing amidation of 3-amino-1H-indazole compounds of chemical formula 2 and a substituted carboxylic acid compound of chemical formula 3 under the presence of pyridine base and 1-ethyl-3-(3'-dimethyl aminopropyl)carbodiimide hydrochloride(EDCI).

    Abstract translation: 目的:提供具有GSK3抑制的1H-吲唑化合物及其药学上可接受的盐作为治疗由GSK-3激活引起的疾病的治疗剂。 构成:1H-吲唑化合物由化学式1表示。一种制备化合物的方法包括:进行化学式2的3-氨基-1H-吲唑化合物和化学式3的取代的羧酸化合物的酰胺化步骤 在吡啶碱和1-乙基-3-(3'-二甲基氨基丙基)碳二亚胺盐酸盐(EDCI)的存在下。

    옥사스파이로 화합 및 이 화합물의 제조방법
    24.
    发明公开
    옥사스파이로 화합 및 이 화합물의 제조방법 有权
    OXASPIRO化合物及其制备方法

    公开(公告)号:KR1020100090979A

    公开(公告)日:2010-08-18

    申请号:KR1020090010234

    申请日:2009-02-09

    Abstract: PURPOSE: An oxaspiro compound and a method for preparing the same are provided to be used as an intermediate in a natural product or novel drug synthesis. CONSTITUTION: An oxaspiro compound is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are hydrogen, alkyl group of C1-C6, halogen, nitro, alkyl of C1-C6, or substituted or non-substituted phenyl group as a substituent of C1-C6 alkoxy. The oxaspiro compound of chemical formula 1 is prepared by reacting a carbo compound of chemical formula 3 with methylene cycloalkandiol of chemical formula 2 under the presence of lewis acid. The reaction solvent is dichloro methane. Trimethylsilyl trifluoromethansulfonate(TMSOTf) is used as the lewis acid.

    Abstract translation: 目的:提供氧杂螺环化合物及其制备方法,用作天然产物或新药合成中的中间体。 化学式1中,R1和R2为氢,C1-C6烷基,卤素,硝基,C1-C6烷基或取代或未取代的苯基,为 C1-C6烷氧基的取代基。 化学式1的氧杂螺环化合物通过在路易斯酸存在下使化学式3的碳化合物与化学式2的亚甲基环二醇反应来制备。 反应溶剂是二氯甲烷。 三氯甲磺酸三甲基甲硅烷基酯(TMSOTf)用作路易斯酸。

    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법
    25.
    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。

    C2 및 C6 위치에 시스 치환기가 있는테트라하이드로파이란 유도체와 이의 제조방법
    26.
    发明公开
    C2 및 C6 위치에 시스 치환기가 있는테트라하이드로파이란 유도체와 이의 제조방법 失效
    CIS-2,6-衍生的四氢衍生物衍生物及其制备方法

    公开(公告)号:KR1020090090224A

    公开(公告)日:2009-08-25

    申请号:KR1020080015550

    申请日:2008-02-20

    CPC classification number: C07D309/06

    Abstract: A method for manufacturing a tetrahydropyran derivative is provided to produce an intermediate for synthesizing functional natural material using a homopropagylic alcohol derivative and aldehyde compound. A tetrahydropyran derivative having cis-substituent on C2 and C6 is denoted by the chemical formula 1. In the chemical formula 1, R1 and R2 are separately C1-C6 alkyl group, C6-C15 aryl C1-C6 alkyl group, or C6-C15 aryl group. A method for manufacturing the tetrahydropyran derivative comprises a step of performing prince reaction of aldehyde compound of the chemical formula 3 with homopropagylic alcohol derivative of the chemical formula 2 to produce dihydropyran-3-ilyden triplate compound of the chemical formula 1a.

    Abstract translation: 提供四氢吡喃衍生物的制造方法,以制备使用高分子量醇衍生物和醛化合物合成官能天然材料的中间体。 化学式1表示在C2和C6上具有顺式取代基的四氢​​吡喃衍生物。在化学式1中,R 1和R 2分别是C 1 -C 6烷基,C 6 -C 15芳基C 1 -C 6烷基或C 6 -C 15 芳基。 四氢吡喃衍生物的制造方法包括使化学式3的醛化合物与化学式2的异丙醇衍生物进行王子反应的步骤,得到化学式1a的二氢吡喃-3-基锂化合物。

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