T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물
    12.
    发明公开
    T-형 칼슘 채널 길항제로서의 5-(치환된알킬아미노메틸)아이속사졸계 화합물 有权
    5-(取代的烷基氨基甲酰基)异噻唑衍生物作为T型钙通道拮抗剂

    公开(公告)号:KR1020120096842A

    公开(公告)日:2012-08-31

    申请号:KR1020110016203

    申请日:2011-02-23

    CPC classification number: C07D413/12

    Abstract: PURPOSE: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is provided to have excellent activity as an antagonist of T- type calcium ion channel. CONSTITUTION: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is represented by chemical formula 1. The encephalopathy therapy and for prevention agent selected from epilepsy, depression, Parkinson's disease, dementia, sleep disorder, an agent for cancer treatment and prevention, an agent for heart disease treatment and prevention selected from hypertensive, cardiac arrhythmia, angina, myocardial infarction, congestive heart failure, pharmaceutical composition for alleviating pain selected from neuropathic pain and chronic and acute pain includes a compound represented by chemical formula 1.

    Abstract translation: 目的:提供作为T型钙通道阻滞剂的5-(取代的烷基氨基甲基)异恶唑基化合物作为T-型钙离子通道的拮抗剂具有优异的活性。 构成:以化学式1表示作为T型钙通道阻断剂的5-(取代烷基氨基甲基)异恶唑类化合物。脑病治疗和预防药物选自癫痫,抑郁症,帕金森病,痴呆,睡眠障碍, 癌症治疗和预防,选自高血压,心律失常,心绞痛,心肌梗塞,充血性心力衰竭,减轻选自神经性疼痛和慢性和急性疼痛的疼痛的药物组合物的心脏病治疗和预防剂,包括由化学式 1。

    새로운 알파형 퀴나크리돈계 유도체 및 그 제조방법
    14.
    发明授权
    새로운 알파형 퀴나크리돈계 유도체 및 그 제조방법 失效
    新的α-型喹吖啶酮衍生物及其制备方法

    公开(公告)号:KR1019930010503B1

    公开(公告)日:1993-10-25

    申请号:KR1019900015291

    申请日:1990-09-26

    CPC classification number: C09B67/0027 C09B48/00

    Abstract: Quinacridone derivatives of formula (I) are prepd. by (a) reacting diethyl 1,4-dicyclohexadione-2,5-dicarboxylate with aromatic amine derivatives such as 5-aminoindane, 3,4-(methylenedioxy) aniline, 2-aminofluorene, 3- amino-9-ethylcarbazole in the presence of trifluoroacetic acid to obtain diethyl 2,5-dianilino-3,6-dihydroterephthalate (II), (b) reacting (II) in a mixed solvent of biphenyl and diphenylether at 250-270 deg.C for 1 hr to obtain 6,13-dihydroquinacridone (II), and (c) oxidn. of (III) with m-nitrobenzene sulfonic acid sodium salt in ethanol, water and NaOH solution. In formula (I), A= cyclopentyl, methylenedioxy, indanyl or N-ethyl indolyl.

    Abstract translation: 式(I)的喹吖啶酮衍生物是制备的。 通过(a)使1,4-二环己酮-2,5-二羧酸二乙酯与芳族胺衍生物如5-氨基茚满,3,4-(亚甲二氧基)苯胺,2-氨基芴,3-氨基-9-乙基咔唑的存在 的三氟乙酸,得到2,5-二苯胺基-3,6-二氢对苯二甲酸二乙酯(II),(b)在联苯和二苯基醚的混合溶剂中于250-270℃反应1小时,得到6, (II)和(c)氧化物。 的(III)与间硝基苯磺酸钠盐在乙醇,水和NaOH溶液中。 在式(I)中,A =环戊基,亚甲二氧基,茚满基或N-乙基吲哚基。

    프롤린 화합물의 제조방법
    16.
    发明授权
    프롤린 화합물의 제조방법 无效
    制备脯氨酸化合物的方法

    公开(公告)号:KR1019900002050B1

    公开(公告)日:1990-03-31

    申请号:KR1019870006734

    申请日:1987-06-30

    Abstract: The method for preparing proline compounds of formula (I), used as the inhibitor against angiotensin and antihypertensive agent, is presented. Thus, 4.1g of N-(2-bromopropionyl)-proline benzylester is dissolved in 200 ml of chloroform and the above mixture is cooled in water-ice bath. Then, 1.7g of 2-bromopropionyl chloride is dropped slowly to the 15ml of chloroform solution containing the proline ester. The above mixture is stirred at 25≦̸C for 24 hrs and the obtained chloroform layer is washed with water three times, evaporated and purified using chromatograhy. In (I), R1 and R7 are each H, C1-10 lower alkyl or aryl; R2, R3, R5 and R6 are each H, C1-10 lower alkyl, aryl, amine or cyano ; R4 is H or C1-10 lower alkyl.

    Abstract translation: 提出了制备用于抑制血管紧张素和抗高血压药的式(I)脯氨酸化合物的制备方法。 因此,将4.1g N-(2-溴丙酰基) - 脯氨酸苄基酯溶于200ml氯仿中,将上述混合物在水 - 冰浴中冷却。 然后,将1.7g 2-溴丙酰氯缓慢滴加到15ml含脯氨酸酯的氯仿溶液中。 将上述混合物在25℃下搅拌24小时,所得氯仿层用水洗涤三次,蒸发并用色谱纯化。 在(I)中,R 1和R 7各自为H,C 1-10为低级烷基或芳基; R2,R3,R5和R6各自为H,C1-10低级烷基,芳基,胺或氰基; R4是H或C1-10低级烷基。

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