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    5-(4-치환된-[1,2,5]티아디아졸-3-일)-3-메틸-1,2,3,4-테트라하이드로피리미딘 유도체와 이의 제조방법
    81.
    发明公开
    5-(4-치환된-[1,2,5]티아디아졸-3-일)-3-메틸-1,2,3,4-테트라하이드로피리미딘 유도체와 이의 제조방법 失效
    5-（4-取代-1,2,5-三唑-3-基）-3-甲基-1,2,3,4-四氢咪唑衍生物及其制备方法

    公开(公告)号：KR1020010018854A

    公开(公告)日：2001-03-15

    申请号：KR1019990034974

    申请日：1999-08-23

    Applicant: 한국화학연구원

    Inventor： 정명희 ,  박준규 ,  조귀웅 ,  이미정 ,  최승원 ,  공재양

    IPC: C07D401/04

    Abstract: PURPOSE: Provided is a method for manufacturing a 5-(4-substituted-£1,2,5|thiadiazol-3-il)-3-methyl-1,2,3,4-tetrahydropyrimidine derivative which is effective on improving memory and treating Alzheimer's disease. CONSTITUTION: A 5-(4-substituted-£1,2,5|thiadiazol-3-il)-3-methyl-1,2,3,4-tetrahydropyrimidine derivative represented by the formula (1) is manufactured by the following steps of: i) reacting 5-pyrimidine carboxylaldehyde of the formula (2) with KCN/HOAc to synthesize hydroxy-pyrimidine-5-il-acetonitrile of the formula (3); ii) reacting hydroxy-pyrimidine-5-il-acetonitrile of the formula (3) with ammonium chloride and ammonium hydroxide to obtain amino-pyrimidine-5-il-acetonitrile of the formula (4) and reacting again amino-pyrimidine-5-il-acetonitrile with S2CL2 to obtain 5-(4-chloro-£1,2,5|thiadiazol-3-il)pyrimidine of the formula (5); iii) reacting 5-(4-chloro-£1,2,5|thiadiazol-3-il)pyrimidine with NaSH and alkylhalide to obtain a compound of the formula (6a); iv) reacting the compound of the formula (6a) with CH3L or methylfluoromethansulfonate at room temperature to obtain 5-(4-substituted sulfanil-£1,2,5|thiadiazol-3-il)-3-methylpyrimidium iodide of the formula (7a); and v) reducing 5-(4-substituted sulfanil-£1,2,5|thiadiazol-3-il)-3-methylpyrimidium iodide with NaBH4 to obtain a 5-(4-substituted-£1,2,5|thiadiazol-3-il)-3-methyl-1,2,3,4-tetrahydropyrimidine derivative. In the formula (1), X is oxygen atom or sulfur atom; R is hydrogen atom, low alkyl group having 1-5 carbon, propargyl group, benzil group, 4-methylbenzil group, or 4-chlorobenzil group.

    Abstract translation: 目的：提供一种有效提高记忆力的5-（4-取代-1,2,5 |噻二唑-3-基）-3-甲基-1,2,3,4-四氢嘧啶衍生物的方法 并治疗阿尔茨海默病。 构成：由式（1）表示的5-（4-取代-1,2,5-二噻唑-3-基）-3-甲基-1,2,3,4-四氢嘧啶衍生物由以下制备 步骤：i）使式（2）的5-嘧啶羧醛与KCN / HOAc反应合成式（3）的羟基 - 嘧啶-5-基 - 乙腈; ii）将式（3）的羟基 - 嘧啶-5-基 - 乙腈与氯化铵和氢氧化铵反应，得到式（4）的氨基 - 嘧啶-5-基 - 乙腈，再次使氨基 - 嘧啶-5-基 - （2-氯苯基）乙腈与S2CL2反应，得到式（5）的5-（4-氯-1,2,5,5-thiadiazol-3-il）嘧啶; iii）使5-（4-氯-1,2,5-噻二唑-3-基）嘧啶与NaSH和烷基卤反应，得到式（6a）化合物; iv）在室温下使式（6a）化合物与CH 3 L或甲基氟代甲磺酸酯反应，得到式（5）的5-（4-取代的磺胺 - 1,2,5-二噻唑-3-基）-3-甲基嘧啶碘化物 图7a）; 和v）用NaBH 4还原5-（4-取代的磺胺 - 1,2,5 - 噻二唑-3-基）-3-甲基嘧啶碘化物，得到5-（4-取代的1,2,5-thiadiazol -3-i）-3-甲基-1,2,3,4-四氢嘧啶衍生物。 在式（1）中，X是氧原子或硫原子; R是氢原子，具有1-5个碳的低级烷基，炔丙基，苯偶酰基，4-甲基苯甲酰基或4-氯苯甲基。

    NMDA수용체길항제로작용하는4-(말단치환-알킬아미노)-퀴놀린-2-카복실산유도체
    82.
    发明授权
    NMDA수용체길항제로작용하는4-(말단치환-알킬아미노)-퀴놀린-2-카복실산유도체 失效
    作为NMDA受体拮抗剂起作用的4-（端羟基亚氨基） - 喹啉-2-羧酸衍生物

    公开(公告)号：KR100274005B1

    公开(公告)日：2000-12-15

    申请号：KR1019980006276

    申请日：1998-02-26

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정영식 ,  정용준 ,  김란희 ,  최진일 ,  공재양

    IPC: C07D215/42

    Abstract: PURPOSE: Provided are the novel NMDA receptor antagonists, 4-(end-substituted-alkylamine)-quinoline-2-carboxylic acid derivatives and the preparation method thereof. CONSTITUTION: The novel derivatives are represented by the chemical formula 1, where n is 0-10, Nu is either appropriately substituted or unsubstituted arylthio, alkylphosphonate, arylsulfonyl, thiourea, non-aromatic thio, heterocyclic thio, arylphosphonate, heterocycle, alkyl, aryl, cyano, hydroxyl, halogen, arylphosphonate alkylsulfonyl, arylsulfonyl, carbamate, amide, urea, acylurea, sulfonylurea, acylthiourea, sulfonylthiourea, thiocarbamate, amidine, guanidine, imidate, thioimidate, phosphorylamide, sulfonamide or amine groups. The synthetic process contains the following steps: alkylating 5,7-dichlorokynurenic acid methylester with 1,3-dibromopropane; eliminating N-tosyl group with sulfuric acid and substitution of the bromine with NaN3 to make azidomine; reducing with Pd/C to amine compound; converting to the corresponding thioisocyanate and finally hydrolysing the ester group to make the compound of formula 1. The synthetic process of the compound of formula 1, where Nu is substituted arylthio or alkyphosphonate group, comprises the steps of: alkylating 5,7-dichlorokynurenic acid methylester with 1,3-dibromopropane; treating the resultant bromine compound either with arylthio compound to make sulfides or with alkylphosphonates to obtain phosphonate compound; treating these compounds with sulfuric acid to eliminate N-tosyl group and finally hydrolysing them with base to obtain the compound of formula 1. They are effective in the treatment and prevention of the chronic neurodegenerative disease such as epilepsy, Alzheimer's disease, Huntington's and Parkinson's disease and also effective as an analgesic, tranquilizer, treatment agents for depression and psychotic diseases.

    Abstract translation: 目的：提供新型NMDA受体拮抗剂4-（末端取代烷基胺） - 喹啉-2-羧酸衍生物及其制备方法。 构成：新型衍生物由化学式1表示，其中n为0-10，Nu为适当取代或未取代的芳硫基，烷基膦酸酯，芳基磺酰基，硫脲，非芳族硫代，杂环硫基，芳基膦酸酯，杂环，烷基，芳基 氰基，羟基，卤素，芳基膦酸酯烷基磺酰基，芳基磺酰基，氨基甲酸酯，酰胺，脲，酰基脲，磺酰脲，酰基硫脲，磺酰基硫脲，硫代氨基甲酸酯，脒，胍，亚氨酸酯，硫代亚氨酸酯，磷酰胺，磺酰胺或胺基。 合成方法包括以下步骤：用1,3-二溴丙烷将5,7-二氯喹诺酮酸甲酯烷基化; 用硫酸除去N-甲苯磺酰基，用NaN 3取代溴，得到叠氮基; 用Pd / C还原为胺化合物; 转化为相应的硫代异氰酸酯，最后水解酯基以制备式1的化合物。其中Nu为取代的芳硫基或亚膦酸酯基团的式1化合物的合成方法包括以下步骤：将5,7-二氯喹诺酮酸 甲基酯与1,3-二溴丙烷; 用芳硫基化合物处理所得溴化合物以制备硫化物或与烷基膦酸酯反应得到膦酸酯化合物; 用硫酸处理这些化合物以消除N-甲苯磺酰基，最后用碱水解它们，得到式1化合物。它们有效治疗和预防慢性神经变性疾病如癫痫，阿尔茨海默病，亨廷顿病和帕金森病 并且作为抑郁和精神病的止痛剂，镇定剂，治疗剂也是有效的。

    NMDA수용체길항제로작용하는4-(말단치환-알킬아미노)-퀴놀린-2-카복실산유도체
    83.
    发明公开
    NMDA수용체길항제로작용하는4-(말단치환-알킬아미노)-퀴놀린-2-카복실산유도체 失效
    用作NMDA受体拮抗剂的4-（末端取代的 - 烷基氨基） - 喹啉-2-羧酸衍生物

    公开(公告)号：KR1019990071057A

    公开(公告)日：1999-09-15

    申请号：KR1019980006276

    申请日：1998-02-26

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정영식 ,  정용준 ,  김란희 ,  최진일 ,  공재양

    IPC: C07D215/42

    Abstract: 본 발명은 하기 화학식 1의 4-(말단치환-알킬아미노)-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 식에서 Nu 은 명세서에 정의된 바와 같다.)

    신규한 1-페닐-카르복실산 에스테르 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를유효성분으로 함유하는 무스카린 수용체 길항제 또는유기인 화합물 중독에 의한 신경계 질환 예방 및 치료용약학적 조성물
    90.
    发明公开
    신규한 1-페닐-카르복실산 에스테르 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를유효성분으로 함유하는 무스카린 수용체 길항제 또는유기인 화합물 중독에 의한 신경계 질환 예방 및 치료용약학적 조성물 有权
    新型1-苯基 - 羧酸酯衍生物或药物可接受的盐，其制备方法和药物受体拮抗剂或药物组合物，用于预防和治疗由含有作为活性成分的有机磷酸盐化合物的神经系统疾病

    公开(公告)号：KR1020090116053A

    公开(公告)日：2009-11-11

    申请号：KR1020080041736

    申请日：2008-05-06

    Applicant: 한국화학연구원

    Inventor： 정영식 ,  박노상 ,  박우규 ,  공재양

    IPC: C07D207/08 ,  A61P39/02 ,  A61P25/00

    Abstract: PURPOSE: A pharmaceutical composition for preventing and treating nervous system disease caused by organophosphate compound or mucarine receptor antagonist is provided to prevent and treat nerve system diseases such as convulsion, Parkison's disease, and epilepsy. CONSTITUTION: A novel 1-phenyl-carboxylic acid ester derivative is denoted by the chemical formula 1. In the chemical formula 1, X is hydrogen, halogen, amino, nitro, straight or branched alkyl of C1-C5 or alkoxy of C1-C5. A method for producing 1-phenyl-carboxylic acid ester derivative comprises: a step of reacting thionyl chloride with carboxylic acid of the chemical formula 2 to obtain a compound of the chemical formula 3; and a step of performing esterification of a compound of the chemical formula 3 and a compound of the chemical formula 4 to obtain a derivative of the chemical formula 1.

    Abstract translation: 目的：提供一种用于预防和治疗由有机磷酸盐化合物或粘蛋白受体拮抗剂引起的神经系统疾病的药物组合物，用于预防和治疗诸如惊厥，帕金森氏病和癫痫的神经系统疾病。 构成：化学式1表示新的1-苯基 - 羧酸酯衍生物。在化学式1中，X是C1-C5的C1-C5或C1-C5的烷氧基的氢，卤素，氨基，硝基，直链或支链烷基 。 1-苯基 - 羧酸酯衍生物的制造方法包括：使亚硫酰氯与化学式2的羧酸反应，得到化学式3的化合物的工序; 以及化学式3的化合物和化学式4的化合物进行酯化以获得化学式1的衍生物的步骤。

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