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    1,2,3,6-테트라하이드로피리디닐-벤즈이미다졸 유도체의제조방법
    44.
    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。

    카스파제-3 저해제로서의 퀴놀린 유도체, 이의 제조방법및 이를 포함하는 약제학적 조성물
    45.
    发明公开
    카스파제-3 저해제로서의 퀴놀린 유도체, 이의 제조방법및 이를 포함하는 약제학적 조성물 失效
    喹啉衍生物作为CASPASE-3抑制剂，其制备方法和含有它的药物组合物

    公开(公告)号：KR1020030086417A

    公开(公告)日：2003-11-10

    申请号：KR1020030027872

    申请日：2003-04-30

    Applicant: 영진약품 주식회사 ,  한국화학연구원

    Inventor： 김성규 ,  정윤성 ,  공재양 ,  박우규

    IPC: C07D215/44

    CPC classification number: C07D409/12 ,  C07D215/42 ,  C07D215/44 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

    Abstract: PURPOSE: Quinoline derivatives as a caspase-3 inhibitor, a preparation process thereof and a pharmaceutical composition containing the same are provided. The compounds are useful for prevention and treatment of diseases associated with caspase-3. CONSTITUTION: Quinoline derivatives of the formula 1 or pharmaceutically acceptable salts thereof are provided, wherein R2 is H, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxyalkyl or C3-6 cycloalkyl; R1 is COYA, -CN or NHOSOn(H2C)R3; Y is O, N or S; A is H, C1-3 alkyl optionally substituted C3-6 alkenyl, C3-6 cycloalkyl, halogen, C1-6 alkyl or C1-6 alkoxy optionally substituted C6-14 aryl, C1-6 alkoxyalkyl, or C6-14 aryl or 5 to 15 membered ring heteroaryl optionally substituted C1-6 alkyl; R3 is H, halogen, optionally substituted amino, C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxyalkyl, or C3-6 cycloalkyl; n is 0, 1, 2 or 3; R is H, halogen, C1-6 alkyl, C1-6 alkoxy or amino optionally substituted C6-14 aryl, halogen, C1-6 alkyl, C1-6 alkoxy or amino optionally substituted 5 to 15 membered ring heterocyclic, or -(CH2)n-CHR4R5; R4 is H, C1-6 alkyl, C1-6 alkoxy, halogen, C1-6 alkyl, C1-6 halogenoalkyl, C1-6 alkoxy or amino optionally substituted C6-14 aryl, 5 to 15 membered ring heteroaryl, C3-6 cycloalkyl, C1-6 alkyl optionally substituted 5 to 15 membered ring heterocyclic, or 5 to 15 membered ring heterocyclic fused C6-14 aryl; and R5 is H, C1-6 alkyl, C1-6 alkoxy or C1-6 alkoxyalkyl.

    Abstract translation: 目的：提供作为半胱天冬酶-3抑制剂的喹啉衍生物及其制备方法和含有它们的药物组合物。 该化合物可用于预防和治疗与半胱天冬酶-3相关的疾病。 提供：式1的喹啉衍生物或其药学上可接受的盐，其中R 2是H，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基烷基或C 3-6环烷基; R1是COYA，-CN或NHOSOn（H2C）R3; Y为O，N或S; A是H，C 1-3烷基任选取代的C 3-6烯基，C 3-6环烷基，卤素，C 1-6烷基或C 1-6烷氧基任选取代的C 6-14芳基，C 1-6烷氧基烷基或C 6-14芳基或5 至15元环杂芳基任选取代的C 1-6烷基; R3是H，卤素，任选取代的氨基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基烷基或C 3-6环烷基; n为0,1,2或3; 或者 - （CH 2）2，其中R 1是H，卤素，C 1-6烷基，C 1-6烷氧基或氨基任意取代的C 6-14芳基，卤素，C 1-6烷基，C 1-6烷氧基或氨基任选取代的5至15元环杂环，或 - ）正CHR4R5; R 4是H，C 1-6烷基，C 1-6烷氧基，卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或氨基任选取代的C 6-14芳基，5至15元环杂芳基，C 3-6环烷基 任选取代的5至15元环杂环的C 1-6烷基或5至15元环杂环稠合的C 6-14芳基; R5是H，C1-6烷基，C1-6烷氧基或C1-6烷氧基烷基。

    NMDA 수용체 길항제로 작용하는 4-치환-퀴놀린-2-카복실산 유도체
    46.
    发明授权
    NMDA 수용체 길항제로 작용하는 4-치환-퀴놀린-2-카복실산 유도체 失效
    作为NMDA受体拮抗剂的4-取代的喹啉-2-羧酸衍生物

    公开(公告)号：KR100267707B1

    公开(公告)日：2000-10-16

    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: PURPOSE: Provided is 4-substituted-quinoline-2-carboxylic acid derivative which acts as an antagonist of NMDA receptor. And its pharmaceutically acceptable salt is provided. CONSTITUTION: 4-substituted-quinoline-2-carboxylic acid derivative is represented from the formula (1), wherein R1 can be sulfonamide, amide or alkylthio, (3-(4-benzyl-piperazine-1-yl)-propyl)-(toluene-4-sulfonyl)-amino group or (2-(4-benzyl-piperazin-1-yl)-ethyl)-(toluene-4-sulfonyl)-amino group.

    Abstract translation: 目的：提供作为NMDA受体拮抗剂的4-取代喹啉-2-羧酸衍生物。 并提供其药学上可接受的盐。 组成：4-取代 - 喹啉-2-羧酸衍生物由式（1）表示，其中R 1可以是磺酰胺，酰胺或烷硫基，（3-（4-苄基 - 哌嗪-1-基） - 丙基） - （甲苯-4-磺酰基） - 氨基或（2-（4-苄基 - 哌嗪-1-基） - 乙基） - （甲苯-4-磺酰基） - 氨基。

    베타-세크리테아제 활성을 억제하는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물
    50.
    发明授权
    베타-세크리테아제 활성을 억제하는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물 有权
    抑制β-分泌酶活性的4-（苯并咪唑-2-基氨基）吡咯烷衍生物和含有其作为活性成分的药物组合物

    公开(公告)号：KR101383239B1

    公开(公告)日：2014-04-10

    申请号：KR1020120045621

    申请日：2012-04-30

    Applicant: 한국화학연구원

    Inventor： 임희종 ,  이계형 ,  박우규 ,  조희영

    IPC: C07D403/12 ,  C07D235/14 ,  A61K31/4178 ,  A61P25/00

    Abstract: 본 발명은 하기 화학식 1로 표시되는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 또는 이의 약제학적으로 허용 가능한 염, 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 및 치료용 약제학적 조성물 및 이를 유효성분으로 함유하는 베타-세크리테아제(BACE)의 활성 억제제 조성물에 관한 것이다.
    [화학식 1]

    본 발명에 따른 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체는 베타-세크리테아제(BACE)의 활성을 억제하여 신경세포를 손상시키는 베타-아밀로이드 단백질의 생성을 억제함으로써 알츠하이머, 다운증후군 등의 신경퇴행성 질환을 치료하거나 예방하는데 효과적으로 사용될 수 있다.

    Abstract translation: 本发明涉及化学式1的4-（苯并咪唑-2-基氨基）吡咯烷衍生物或其药学上可接受的盐; 含有与用于预防和治疗神经变性疾病的活性成分相同的药物组合物; 以及含有与活性成分相同的β-分泌酶（BACE）活化的抑制剂组合物。 根据本发明的4-（苯并咪唑-2-基氨基）吡咯烷衍生物抑制BACE的活化和产生引起神经细胞损伤的β-淀粉样蛋白，从而有效地预防或治疗神经变性疾病如阿尔茨海默氏病和 唐氏综合症。

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