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    1,2,3,6-테트라하이드로피리디닐-벤즈이미다졸 유도체의제조방법
    1.
    发明公开
    1,2,3,6-테트라하이드로피리디닐-벤즈이미다졸 유도체의제조방법 无效
    制备1,2,3,6-四氢吡啶并苯并咪唑衍生物的方法，其可用于治疗作为具有改善的药物的肌钙蛋白受体激动剂的DEMENTIA

    公开(公告)号：KR1020050012503A

    公开(公告)日：2005-02-02

    申请号：KR1020030051485

    申请日：2003-07-25

    Applicant: 주식회사 코오롱 ,  한국화학연구원

    Inventor： 남궁미애 ,  정명희 ,  박정미 ,  최일영 ,  안미자 ,  박우규 ,  정용준 ,  김윤철

    IPC: C07D401/04

    Abstract: PURPOSE: A process for preparing 1,2,3,6-tetrahydropyridinyl-benzimidazole derivatives is provided, thereby preparing the 1,2,3,6-tetrahydropyridinyl-benzimidazole derivatives which are useful for treatment of dementia as a muscarinic receptor agonist with improved yield. CONSTITUTION: The process for preparing 1,2,3,6-tetrahydropyridinyl-benzimidazole derivatives represented by formula (1) and pharmaceutically acceptable salts thereof comprises the steps of: (a) reacting 4-pyridinecarboxalaldehyde of formula (2) with a compound of formula (3) and iodibenzene diacetate(IBD) in solvent to prepare a compound of formula (4); (b) reacting the compound of formula (4) with KOH/CH3I to prepare a 5/6-substituent isomer compound of formula (5); (c) reacting the compound of formula (5) with CH3I to prepare a compound of formula (7); and (d) reacting the compound of formula (7) with NaBH4, and treating a reaction product with acid, wherein X is NH or NCH3; R is H, NH2, Cl, NO2 or OCH3; and HA is an organic or inorganic salt selected from HCl, oxalic acid, p-toluenesulfonate, tartaric acid and fumaric acid.

    Abstract translation: 目的：提供制备1,2,3,6-四氢吡啶基 - 苯并咪唑衍生物的方法，从而制备可用于治疗痴呆作为毒蕈碱受体激动剂的1,2,3,6-四氢吡啶基 - 苯并咪唑衍生物，其具有改进的 产量。 构成：由式（1）表示的1,2,3,6-四氢吡啶基 - 苯并咪唑衍生物及其药学上可接受的盐的制备方法包括以下步骤：（a）使式（2）的4-吡啶甲醛与式 式（3）和二苯乙酮（IBD）在溶剂中制备式（4）化合物; （b）使式（4）的化合物与KOH / CH 3 I反应以制备式（5）的5 / 6-取代的异构体化合物; （c）使式（5）的化合物与CH 3 I反应以制备式（7）的化合物; 和（d）使式（7）的化合物与NaBH 4反应，并用酸处理反应产物，其中X是NH或NCH 3; R是H，NH2，Cl，NO2或OCH3; 并且HA是选自HCl，草酸，对甲苯磺酸盐，酒石酸和富马酸的有机或无机盐。

    1,2,5,6/1,2,3,6-테트라히드로피리디닐테트라히드로사이클로펜타/-헥사이속사졸 유도체 및 그 제조방법
    4.
    发明公开
    1,2,5,6/1,2,3,6-테트라히드로피리디닐테트라히드로사이클로펜타/-헥사이속사졸 유도체 및 그 제조방법 无效
    1,2,5,6 / 1,2,3,6-四氢吡啶并吡咯并环庚酮衍生物及其制备方法

    公开(公告)号：KR1020040021992A

    公开(公告)日：2004-03-11

    申请号：KR1020020053796

    申请日：2002-09-06

    Applicant: 주식회사 코오롱 ,  한국화학연구원

    Inventor： 정명희 ,  안미자 ,  박정미 ,  최일영 ,  정대영 ,  정용준 ,  김윤철 ,  박호진

    IPC: C07D413/04

    Abstract: PURPOSE: 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/-hexaisoxazole derivatives and a method for preparing the same are provided. The compounds are useful for treatment of dementia and brain disease as muscarinic receptor agonist and operated as tetrahydropyridine bioisostere. CONSTITUTION: 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/ -hexaisoxazole derivatives are represented by the formula(1), wherein X is CH2, O or S; n is an integer of 1 or 2; HA is inorganic or organic salt selected from HCl, oxalic acid, p-toluenesulfonic acid, tartaric acid and fumaric acid. A method for preparing the 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/-hexaisoxazole derivatives comprises the steps of: (a) adding NaOCl to 3/4-pyridinealdoxime of the formula(2) and cyclopentene/-hexene derivatives in a solvent and cyclizing them to prepare a compound of the formula(4); (b) reacting the compound of the formula(4) with CH3I to prepare 3/4-substituent isomer of the formula(5); and (c) reducing the compound of the formula(5) and adding inorganic and organic acids into the reduced compound.

    Abstract translation: 目的：提供1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊二烯并 - 己烯恶唑衍生物及其制备方法。 该化合物可用于治疗痴呆和脑疾病作为毒蕈碱受体激动剂，并作为四氢吡啶生物电子等离子体操作。 构成：1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊酯/ - 己烯恶唑衍生物由式（1）表示，其中X为CH 2，O或S; n为1或2的整数; HA是选自HCl，草酸，对甲苯磺酸，酒石酸和富马酸的无机或有机盐。 制备1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊二烯并 - 六氢异恶唑衍生物的方法包括以下步骤：（a）将NaOCl加入式（2）的3 / 4-吡啶醛肟和环戊烯 己烯衍生物在溶剂中并使其环化以制备式（4）的化合物; （b）使式（4）的化合物与CH 3 I反应制备式（5）的3 / 4-取代基异构体; 和（c）还原式（5）的化合物，并向还原的化合物中加入无机和有机酸。

    3-(치환-페닐티오)-4-하이드록시퀴놀린-2(1H)-온 유도체 및 그들의 제조방법
    5.
    发明授权
    3-(치환-페닐티오)-4-하이드록시퀴놀린-2(1H)-온 유도체 및 그들의 제조방법 失效

    公开(公告)号：KR100301129B1

    公开(公告)日：2001-11-30

    申请号：KR1019970058546

    申请日：1997-11-06

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정용준 ,  박우규 ,  이승호 ,  정영식 ,  이창우 ,  최진일 ,  최승원 ,  공재양

    IPC: C07D217/24

    Abstract: PURPOSE: Provided are 3-(substitution-phenylthio)-4-hydroxyquinoline-2(1H)-one derivative acting as an antagonist of excitoamino acid and useful to remedy or prevention of neurodegenerative disease, central nerve system disease and schizophrenia, and a method for preparation thereof. CONSTITUTION: 3-(substitution-phenylthio)-4-hydroxyquinoline-2(1H)-one is represented by the formula(1), wherein X is H, S, or NH; R1, R2, R3, and R4 is hydroxy, halogen, nitro, amino, haloalkyl, cyano, alkyl, alkenyl, alkinyl, azido, acylamino, substituted or nonsubstituted aryl, alkoxy, or substituted or nonsubstituted heterocyclic ring; and R5 and R6 is respectively, hydrogen, halogen, amino, carboxylate, thiol, haloalkyl, alkyl, alkenyl, alkinyl, azido, acylamino, sulfonyl, aminosulfonyl, substituted or nonsubstituted aryl, alkoxy, substituted or nonsubstituted heterocyclic ring, acyloxy, alkylthio, alkylcarboxylate, arylcarboxylate, aralkylcarboxlate, alkylester, arylester, aralkylester, urea, amidine, aralkyl, heteroarylalkyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, substituted(halo)-aralkylester, substituted(halo)-arylsulfonyl, heteroarylcarbonyl, aralkylthiourea, substituted(halo)-arylthiourea, alkoxycarbonyl, aminoalkyl or iminoaralkyl.

    3-(치환-페닐티오)-4-하이드록시퀴놀린-2(1H)-온 유도체 및 그들의 제조방법
    6.
    发明公开
    3-(치환-페닐티오)-4-하이드록시퀴놀린-2(1H)-온 유도체 및 그들의 제조방법 失效
    3-（取代的 - 苯硫基）-4-羟基喹啉-2（1H） - 酮衍生物及其制备方法

    公开(公告)号：KR1019990038717A

    公开(公告)日：1999-06-05

    申请号：KR1019970058546

    申请日：1997-11-06

    Applicant: 한국화학연구원

    Inventor： 박노상 ,  성철민 ,  정용준 ,  박우규 ,  이승호 ,  정영식 ,  이창우 ,  최진일 ,  최승원 ,  공재양

    IPC: C07D217/24

    Abstract: 본 발명은 하기 화학식 1의 3-(치환-페닐티오)-4-하이드록시퀴놀린-2(1H)-온 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 , R
    2 , R
    3 , R
    4 , R
    5 , R
    6 및 X 는 명세서에 기재된 바와 같다.)

    NMDA수용체길항제로작용하는4-(말단치환-알킬아미노)-퀴놀린-2-카복실산유도체
    9.
    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
    10.
    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.)

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