T-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법
    32.
    发明公开
    T-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법 有权
    具有T型钙通道活性的新型奥氮唑 - 哌嗪化合物

    公开(公告)号:KR1020110020023A

    公开(公告)日:2011-03-02

    申请号:KR1020090077687

    申请日:2009-08-21

    Abstract: PURPOSE: An oxazole-piperazine compound having a pharmaceutical activity with respect to T-type calcium channel is provided to ensure excellent activity as an antagonist of the channel and to prevent and treat cancer, epilepsy, heart diseases, and pain. CONSTITUTION: An oxazole-piperazine compounds is denoted by chemical formula 1. A pharmaceutical composition for treating epilepsy, cancer, hypertension, myocardial infarction, neuropathic pain, and acute and chronic pain contains the oxazole-piperazine compound of chemical formula 1. The compound of chemical formula 1 is prepared by reacting piperazine-amine compound of chemical formula 2 and oxazole aldehyde compound of chemical formula 3 by reductive amination. The reductive amination is performed under the presence of molecules of 4-8 meshes and NaBH(OAc)_3, NaBH_3CN, or NaBH_4.

    Abstract translation: 目的:提供相对于T型钙通道具有药学活性的恶唑 - 哌嗪化合物,以确保作为通道拮抗剂的优异活性,并预防和治疗癌症,癫痫,心脏病和疼痛。 构成:化学式1表示恶唑 - 哌嗪化合物。用于治疗癫痫,癌症,高血压,心肌梗死,神经性疼痛和急性和慢性疼痛的药物组合物含有化学式1的恶唑 - 哌嗪化合物。 化学式1通过化学式2的哌嗪 - 胺化合物和化学式3的恶唑醛化合物通过还原胺化反应来制备。 还原胺化在4-8目和NaBH(OAc)3,NaBH 3 CN或NaBH 4的分子存在下进行。

    무스카린성 아세틸콜린 수용체에 작용하는테트라하이드로피리딘 유도체
    33.
    发明授权
    무스카린성 아세틸콜린 수용체에 작용하는테트라하이드로피리딘 유도체 失效
    무스카린성아세틸콜린수용체체에용하는테트라하이드로피리딘유도체

    公开(公告)号:KR100432283B1

    公开(公告)日:2004-05-22

    申请号:KR1020010066568

    申请日:2001-10-27

    CPC classification number: C07D401/06

    Abstract: The present invention relates to novel tetrahydropyridine derivatives of formula 1 having an appropriately substituted pyrrolidinone and oxime, wherein m is 0 or 1, n is 1 or 2, R1 is hydrogen, C1-4 alkyl, C2-4 alkynyl or aryl, R3 is C1-4 alkyl, which show high efficacy, low cholinergic adverse effects and high affinity for muscarinic acetylcholine receptor; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

    Abstract translation: 本发明涉及具有适当取代的吡咯烷酮和肟的式1的四氢吡啶衍生物,其中m为0或1,n为1或2,R 1为氢,C 1-4烷基,C 2-4炔基或芳基,R 3为 它表现出高效力,低胆碱能不良作用和对毒蕈碱乙酰胆碱受体的高亲和力; 和其药学上可接受的盐; 其制备方法; 和包含这些化合物或盐的药物组合物。

    인듐을 이용한 알킬 방향족 화합물의 제조방법
    34.
    发明公开
    인듐을 이용한 알킬 방향족 화합물의 제조방법 失效
    使用印花生产芳香族芳族化合物

    公开(公告)号:KR1020000065376A

    公开(公告)日:2000-11-15

    申请号:KR1019990011595

    申请日:1999-04-02

    Abstract: PURPOSE: A process for preparing the titled compound by reacting alkyl halide compounds with aromatic compounds using a catalyst in the presence of a solvent is provided which produces alkyl aromatic compounds useful as intermediates or final products of various industrial chemicals. CONSTITUTION: An aryl aromatic compound of formula (III) is prepared by alkylating aryl halides of formula (I) and aromatic compounds of formula (II) using a catalyst selected from metal indium alone, indium and a solid base, indium and a base and a 4A molecular sieve in the presence of a solvent or in its absence. In formula, R1 and R2 denote each H or straight or side chained C1 to C5 hydrocarbon substituted to carbon of the aryl group selected from methyl, ethyl, propyl, butyl and pentyl; X denotes Cl, Br, I or F; R3 and R4 denote each H, methyl, F, hydroxyl or methyl. The aryl halides of formula (I) and aromatic compounds of formula (II) are used in a molar ratio of 100 : 1 to 1 : 100.

    Abstract translation: 目的:提供了一种通过在溶剂存在下使用催化剂使烷基卤化合物与芳族化合物反应制备标题化合物的方法,其产生可用作各种工业化学品的中间体或最终产物的烷基芳族化合物。 构成:通过使用选自单独的金属铟,铟和固体碱,铟和碱的催化剂烷基化式(I)的芳基卤和式(II)的芳族化合物来制备式(III)的芳基芳族化合物, 4A分子筛在溶剂存在下或在其不存在下进行。 在式中,R 1和R 2表示被取代为选自甲基,乙基,丙基,丁基和戊基的芳基的碳的每个H或直链或侧链C1至C5烃基; X表示Cl,Br,I或F; R3和R4分别表示H,甲基,F,羟基或甲基。 式(I)的芳基卤化物和式(II)的芳族化合物以100:1至1:100的摩尔比使用。

    신규 퀴놀린 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
    37.
    发明授权
    신규 퀴놀린 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 有权
    用于预防或治疗新型喹啉化合物和含有它们的癌症的药物组合物

    公开(公告)号:KR101778938B1

    公开(公告)日:2017-09-18

    申请号:KR1020160075019

    申请日:2016-06-16

    Abstract: 본발명은암세포에대한우수한항 증식효능을나타내는퀴놀린화합물, 이의약학적으로허용가능한염, 또는수화물과, 이의제조방법및 이를유효성분으로함유하는암 질환의예방또는치료용의약조성물에관한것으로서, 상기본 발명에따른화합물, 이의약학적으로허용가능한염, 또는수화물은우수한암세포억제활성과단백질키나아제및 돌연변이키나아제의억제활성을나타내고있으므로, 부작용이적은새로운항암제로유용하게사용될수 있다.

    Abstract translation: 本发明涉及一种优良的抗 - 喹啉化合物为代表增殖作用,其药学上可接受的盐,或它们的水合物及它们的制备方法和预防或治疗的药物组合物含有与用于癌细胞的活性成分的癌症疾病, 因为这些化合物根据基本发明,其药学上可接受的盐,或水合物显示出优异的肿瘤抑制活性,并且所述蛋白激酶和所述突变体的激酶抑制活性,这种副作用可有利地具有小的新的抗癌药物使用。

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