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    항산화 활성을 갖는 페닐아미딘 유도체 및 이를 포함하는약학적 조성물
    23.
    发明公开
    항산화 활성을 갖는 페닐아미딘 유도체 및 이를 포함하는약학적 조성물 失效
    具有抗氧化活性的苯甲酰胺衍生物和含有其的药物组合物

    公开(公告)号：KR1020040008856A

    公开(公告)日：2004-01-31

    申请号：KR1020020042579

    申请日：2002-07-19

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  정영식 ,  성철민 ,  임희종 ,  윤중호 ,  공재양 ,  박우규

    IPC: C07D409/12

    Abstract: PURPOSE: Phenylamidine derivatives having anti-oxidant activity and a pharmaceutical composition containing the same are provided. The compounds have improved anti-oxidant activity and lower toxicity. CONSTITUTION: Phenylamidine derivatives are characterized by the formula 1, wherein X1 and X2 are independently hydrogen, or linear or branched chain alkyl having C1-C9 saturated or unsaturated carbon; Y is CH2 or CH=CH(C=O); and Ar is phenyl, thiopen or pyrrole. An anti-oxidant is characterized by containing the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof. The pharmaceutical composition for prevention of aging and treatment of cancer, diabetes, epilepsy, apoplexy, Parkinson's disease, Huntington's disease and dementia contains the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof.

    Abstract translation: 目的：提供具有抗氧化活性的苯脒衍生物和含有它们的药物组合物。 该化合物具有改善的抗氧化活性和较低的毒性。 构成：苯基脒衍生物的特征在于式1，其中X 1和X 2独立地是氢，或具有C 1 -C 9饱和或不饱和碳的直链或支链烷基; Y是CH 2或CH = CH（C = O）; 和Ar是苯基，噻吩或吡咯。 抗氧化剂的特征在于含有式1的苯基脒衍生物及其药学上可接受的盐。 用于预防癌症，糖尿病，癫痫，中风，帕金森病，亨廷顿病和痴呆的衰老和治疗的药物组合物含有式1的苯基脒衍生物及其药学上可接受的盐。

    항산화 활성을 갖는 4-히드록시 신남아미드 유도체, 그의제조방법 및 이를 포함하는 약학적 조성물
    24.
    发明公开
    항산화 활성을 갖는 4-히드록시 신남아미드 유도체, 그의제조방법 및 이를 포함하는 약학적 조성물 失效
    具有抗氧化活性的4-羟基喹啉衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：KR1020030042586A

    公开(公告)日：2003-06-02

    申请号：KR1020010073301

    申请日：2001-11-23

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  정영식 ,  성철민 ,  임희종 ,  조향옥 ,  공재양 ,  박우규

    IPC: C07C237/20

    Abstract: PURPOSE: A 4-hydroxycinnamamide derivative, pharmaceutically acceptable salt thereof and preparation thereof are provided. A pharmaceutical composition containing them as an active ingredient for use in anti-aging, and treating cancers, diabetes, epilepsy and neurodegenerative diseases is also provided. CONSTITUTION: The 4-hydroxycinnamamide derivative has the formula 1, wherein each of X1 and X2 is independently hydrogen or a C1-C15 saturated or unsaturated, linear or branched alkyl group; each of Y1, Y2, Y3 and Y4 is independently hydrogen, halogen, hydroxy group, amino group, phenyl group, C1-C8 alkyl group or C1-C8 alkoxy group; and n is an integer between 0 and 9. The 4-hydroxycinnamamide derivative and pharmaceutically acceptable salt thereof have excellent anti-oxidant activity and low toxicity compared to other conventional anti-oxidants.

    Abstract translation: 目的：提供4-羟基肉桂酰胺衍生物，其药学上可接受的盐及其制备方法。 还提供含有它们作为用于抗衰老的活性成分以及治疗癌症，糖尿病，癫痫和神经变性疾病的药物组合物。 构成：4-羟基肉桂酰胺衍生物具有式1，其中X1和X2各自独立地为氢或C1-C15饱和或不饱和的直链或支链烷基; Y1，Y2，Y3和Y4各自独立地为氢，卤素，羟基，氨基，苯基，C1-C8烷基或C1-C8烷氧基; n为0〜9的整数。与其它常规抗氧化剂相比，4-羟基肉桂酰胺衍生物及其药学上可接受的盐具有优异的抗氧化活性和低毒性。

    NMDA수용체길항제로작용하는4-(3-치환-프로필옥시)-퀴놀린-2-카복실산유도체
    25.
    发明授权
    NMDA수용체길항제로작용하는4-(3-치환-프로필옥시)-퀴놀린-2-카복실산유도체 失效
    作为NMDA受体拮抗剂的4-（3-取代的丙氧基） - 喹啉-2-羧酸衍生物

    公开(公告)号：KR100274004B1

    公开(公告)日：2000-12-15

    申请号：KR1019980006274

    申请日：1998-02-26

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정영식 ,  이창우 ,  민충식 ,  이종철 ,  공재양 ,  박우규

    IPC: C07D215/233

    Abstract: PURPOSE: Provided are the novel NMDA receptor antagonist, 4-(3-substituted-propyloxy)-quinoline-2-carboxylic acid derivatives and the preparation method thereof. CONSTITUTION: The derivatives are represented as shown in the chemical formula 1, where A represents carbamate, amide, thiourea, sulfonylurea, acylthiourea, thiocarbamate, amidine, guanidine, imidate, thioimidate, phosphorylamide, sulfonamide, sulfonthiourea or amines and R represents alkyl (C1¯C20), aryl (C6¯C12), aralkyl, heterocycles, carbocycles (C3¯C14), fused bicyclic, hydrogen or cyano groups. The synthetic process comprises the steps of alkylating 5,7-dichlorokynurenic acid methylester with 1,3-dibromopropane; substitution of the bromine with NaN3 to make azidomine; reducing the resultant to amine compound with Pd-catalyst; converting to amide with the corresponding isocyanate, thioisocyanate or acid chloride and finally hydrolysing the ester group in the parent moiety to make the compound of formula 1. They are strong and unique antagonist acting on the coupling position of the strychnine non-susceptive glycine in the NMDA receptor complex and penetrate effectively into central nervous system. They are effective in the treatment of neurodegeneration, especially useful for the CNS damages effected by the diseases such as heart attack, low blood sugar, local anemia and heart beat halt arising from the low oxygen concentration caused by the external wounds or anemia.

    Abstract translation: 目的：提供新型NMDA受体拮抗剂4-（3-取代 - 丙氧基） - 喹啉-2-羧酸衍生物及其制备方法。 构成：衍生物如化学式1所示，其中A表示氨基甲酸酯，酰胺，硫脲，磺酰脲，酰基硫脲，硫代氨基甲酸酯，脒，胍，亚氨酸酯，硫代亚氨酸酯，磷酰胺，磺酰胺，磺酰硫脲或胺，R代表烷基 C 20），芳基（C 6 -C 12），芳烷基，杂环，碳环（C 3 -C 14），稠合双环，氢或氰基。 该合成方法包括使5,7-二氯喹诺酮酸甲酯与1,3-二溴丙烷烷基化的步骤; 用NaN3取代溴以制备叠氮胺; 用Pd催化剂将产物还原成胺化合物; 用相应的异氰酸酯，硫代异氰酸酯或酰氯转化成酰胺，最后水解母体部分中的酯基以制备式1的化合物。它们是强力和独特的拮抗剂作用于士的宁非感受性甘氨酸的偶联位置 NMDA受体复合物并有效渗入中枢神经系统。 它们有效治疗神经变性，特别适用于由外部伤口或贫血引起的低氧浓度引起的心脏病，低血糖，局部贫血和心跳停止等疾病所致的CNS损伤。

    NMDA 수용체 길항제로 작용하는 4-치환-퀴놀린-2-카복실산 유도체
    27.
    发明公开
    NMDA 수용체 길항제로 작용하는 4-치환-퀴놀린-2-카복실산 유도체 失效
    作为NMDA受体拮抗剂的4-取代 - 喹啉-2-羧酸衍生物

    公开(公告)号：KR1019990071056A

    公开(公告)日：1999-09-15

    申请号：KR1019980006275

    申请日：1998-02-26

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  박우규 ,  정영식 ,  최승원 ,  최진일 ,  이창우

    IPC: C07D401/12 ,  A61K31/47 ,  C07D215/02 ,  C07D417/12

    Abstract: 본 발명은 하기 화학식 1의 4-치환-퀴놀린-2-카복실산 유도체, 그 제조방법 및 NMDA 수용체 복합체에 있는 스트리키닌 (strychinine) 비감수성 글리신 결합자리에 작용하는 강력하면서 특이성을 갖는 길항제 (antagonist)로서의 용도에 관한 것이다. 본 발명의 화합물은 신경퇴행성 질환의 치료 및 예방에 유용하다. 특히, 본 발명의 화합물은 뇌졸증, 저혈당증, 국소빈혈, 심장박동정지, 외상과 같은 빈혈이나 저산소증의 결과로서 야기되는 중추신경계의 손상을 줄이는데 유용하다. 또한, 본 발명의 화합물은 간질, 알츠하이머병, 헌팅톤병 및 파킨슨씨병을 포함하는 만성 신경퇴행성 질환의 예방 및 치료에 유용하다. 또한, 본 발명의 화합물은 항경련제, 진통제, 항우울증 치료제, 항불안 치료제 및 항정신분열증 치료제로 사용된다.


    (상기 R
    1 및 R
    2 는 명세서에 정의한 바와 같다.)

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