베타형 및 감마형 퀴나크리돈의 새로운 제조방법
    42.
    发明授权
    베타형 및 감마형 퀴나크리돈의 새로운 제조방법 失效
    制备β-和γ-型喹吖啶酮的新方法

    公开(公告)号:KR1019930010504B1

    公开(公告)日:1993-10-25

    申请号:KR1019900015553

    申请日:1990-09-28

    Abstract: The beta- or gamma-quinacridone is produced by (a) reacting a diethyl 1,4-dicyclohexanedione-2,5-dicarboxylate of formula (II) with an aniline in the presence of a solvent (toluene or xylene) having a low b.p. and a trifluoro acetic acid catalyst to obtain a diethyl 2,5-dianilino-3,6-dihydroterephthalate of formula (III), (b) reacting the cpd. of (III) in the presence of a xylene solvent at 310-320 deg.C for 1 hr in the high pressure reactor to obtain a beta- 6,13- dihydroquinacridone of formula (IV), and (c) reacting a lower alcohol (methanol or ethanol), a sodium hydroxide soln. and a meta-sodium nitrobenzene sulfonate with the cpd. of (IV).

    Abstract translation: 通过(a)使式(II)的1,4-二环己烷二酮-2,5-二羧酸二乙酯与苯胺在溶剂(甲苯或二甲苯)存在下反应生成β-或γ-喹吖啶酮,所述溶剂(甲苯或二甲苯)具有低的沸点。 和三氟乙酸催化剂,得到式(III)的2,5-二苯胺基-3,6-二氢对苯二甲酸二乙酯,(b)使cpd反应。 的(III)在二甲苯溶剂存在下,在310-320℃下在高压反应器中反应1小时,得到式(IV)的β-6,13-​​二氢喹吖啶酮,和(c)使低级醇 (甲醇或乙醇),氢氧化钠溶胶。 和具有cpd的硝基苯磺酸钠。 的(Ⅳ)。

    알파-아미노아미드 유도체 화합물 및 이를 포함하는 약학적 조성물
    45.
    发明授权
    알파-아미노아미드 유도체 화합물 및 이를 포함하는 약학적 조성물 有权
    α-氨基酰胺衍生物和包含其的药物组合物

    公开(公告)号:KR101679568B1

    公开(公告)日:2016-11-28

    申请号:KR1020140132983

    申请日:2014-10-02

    Abstract: 발명은알파-아미노아미드유도체화합물및 이를포함하는약학적조성물에관한것이다. 본발명의여러구현예에따르면, MAO-B 저해제로사용되는기존약물의단점을극복할수 있으며, 구체적으로는 MAO-B와공유결합을통해비가역적으로작용하여치료효과를나타내는기존약물의부작용을완화혹은없앨수 있도록비공유결합을통해가역적으로 MAO-B를억제하는치료제를제공할수 있다. 특히기존의가역적 MAO-B 저해제보다뛰어난안정성및 효능을갖는새로운화합물을제공할수 있다.

    Abstract translation: 本发明涉及α-氨基酰胺衍生物化合物和包含其的药物组合物。 根据本发明的各种实施方案,药物组合物可以克服用作MAO-B抑制剂的常规药物的缺点。 更具体地说,药物组合物通过非共价键可逆地抑制MAO-B,从而可以通过共价键与MAO-B不可逆地作用而减轻或消除显示出治疗功效的常规药物的副作用。 特别地,与常规的可逆MAO-B抑制剂相比,本发明的新化合物具有显着的稳定性和有效性。 α-氨基酰胺衍生物化合物由化学式1表示。

    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법
    50.
    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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