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    베타-세크리테아제의 활성을 저해하는 아릴피페라진이 치환된 피페리딘 유도체 또는 이의 약제학적으로 허용 가능한 염 및 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 또는 치료용 조성물
    3.
    发明公开
    베타-세크리테아제의 활성을 저해하는 아릴피페라진이 치환된 피페리딘 유도체 또는 이의 약제학적으로 허용 가능한 염 및 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 또는 치료용 조성물 失效
    （4-ARYLPIPERAZIN-1-YL）哌啶衍生物抑制β-分泌酶活性或含有该组合物的药物组合物及其组合物，用于预防和治疗含有作为活性成分的神经损伤性疾病

    公开(公告)号：KR1020090035993A

    公开(公告)日：2009-04-13

    申请号：KR1020070101067

    申请日：2007-10-08

    Applicant: 한국화학연구원

    Inventor： 임희종 ,  정명희 ,  최일영 ,  박우규

    IPC: C07D401/04 ,  A61K31/497 ,  A61P25/28

    Abstract: A (4-arylpiperazin-1-yl)piperidine derivative is provided to inhibit activities of beta-secretase, thereby treating and preventing neurodegenerative diseases such as Alzheimer diseases and Downs syndrome. A pharmaceutical composition comprises piperidine derivative wherein arylpiperazin is substituted represented by the formula 1 and pharmaceutically allowable salts thereof. In the formula 1, R1 and R2 are independently -O-CO-R4 or the formula 1a, wherein R4 represents C6-C12 aryl group in which C6-C10-aryl-C1-C4 alkyl group, C6-C12 aryl group, C1-C5 aryloxy or C6-C12 aryloxy group is substituted; and R3 is hydrogen, -CO-NH-(CH2)m-R5 or -CO-NH-C(R6)(R7)-(CH2)m-COO-R8. In the formula 1a, Z is hydrogen, halogen, C1-C4 liner or branched alkyl group or C1-C5 alkoxy group, wherein R5 is C6-C12 aryl group in which one or two C1-C4 linear or branched alkyl, C1-C5 alkoxy or halogen; m is an integer of 0~2; R6 and R7 are independently hydrogen, C1-C4 linear or branched alkyl group or benzyl group; and R8 is C1-C4 linear or branched alkyl group.

    Abstract translation: 提供（4-芳基哌嗪-1-基）哌啶衍生物以抑制β-分泌酶的活性，从而治疗和预防神经变性疾病如阿尔茨海默病和唐氏综合征。 药物组合物包含哌啶衍生物，其中芳基哌嗪为取代基，由式1代表其药学上可允许的盐。 在式1中，R 1和R 2独立地为-O-CO-R 4或式1a，其中R 4表示C 6 -C 12芳基，其中C 6 -C 10 - 芳基-C 1 -C 4烷基，C 6 -C 12芳基，C 1 -C 5芳氧基或C6-C12芳氧基被取代; -CO-NH-（CH2）m -R5或-CO-NH-C（R6）（R7） - （CH2）m-COO-R8。 在式1a中，Z为氢，卤素，C1-C4内酰基或支链烷基或C1-C5烷氧基，其中R5为C6-C12芳基，其中一个或两个C1-C4直链或支链烷基C1-C5 烷氧基或卤素; m为0〜2的整数; R6和R7独立地是氢，C1-C4直链或支链烷基或苄基; R8为C1-C4直链或支链烷基。

    후퍼진-타크린 하이브리드와 이의 제조방법
    4.
    发明授权
    후퍼진-타크린 하이브리드와 이의 제조방법 失效
    石杉碱 - 他克林混合物及其制备方法

    公开(公告)号：KR100666756B1

    公开(公告)日：2007-01-15

    申请号：KR1020050031355

    申请日：2005-04-15

    Applicant: 한국화학연구원

    Inventor： 최일영 ,  변경희 ,  정명희 ,  임희종 ,  안미자 ,  박우규

    IPC: C07D401/12

    Abstract: 본 발명은 다음 화학식 1의 후퍼진-타크린 하이브리드(huperzine-tacrine hybrid) 유도체 및 이의 제조방법에 관한 것으로서, 본 발명의 후퍼진-타크린 하이브리드 유도체 는 치매치료에 효과가 있는 것으로 잘 알려져 있는 후퍼진 A 와 타크린 화합물의 혼합체로서 아세틸콜린에스트라제(AChE) 저해제로서의 활성을 보여준다.
    [화학식 1]

    (상기 화학식 1에서, X는 수소, 할로겐기 또는 C
    1 ~C
    6 의 알킬기이고, m은 1 내지 3이고, n은 1 또는 2이다.)
    후퍼진-타크린 하이브리드, 치매, 후퍼진, 타크린, 아세틸콜린에스테라제 저해제

    1,2,3,6-테트라하이드로피리디닐-벤즈이미다졸 유도체의제조방법
    5.
    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。

    살균효과를 가지는 옥사졸 유도체
    6.
    发明授权
    살균효과를 가지는 옥사졸 유도체 失效
    살균효과를가지는옥사졸유도체

    公开(公告)号：KR100392075B1

    公开(公告)日：2003-07-22

    申请号：KR1020000056264

    申请日：2000-09-25

    Applicant: 한국화학연구원

    Inventor： 최일영 ,  이재현 ,  박창식 ,  임희종 ,  김진철

    IPC: A01N43/76

    Abstract: PURPOSE: A new oxazole derivative obtained by using amide as a starting material is provided which has a strong antibacterial effect on plant pathogenic bacteria with a small amount, for example Pyricularia oryzae Cavera, Rhizoctonia SolaniAG-1, Botrytis cinerea KCI, Phytophthora infestans or the like. CONSTITUTION: An amid compound(formula II) is refluxed in a solvent of dichloroacetone and ethanol to give chloromethyl oxazole(formula III). A chlorine atom of the chloromethyl oxazole is substituted to an iodine atom by use of sodium iodide and then reacted with 2-(2-hydroxyphenyl)-3-methoxy acrylic acid methylester(formula IV)(in case of A=C) or 2-methoxyimino-(2-hydroxyphenyl)-acetic acid methylester(formula IV)(in case of A=N) to produce an oxazole derivative(formula I).

    Abstract translation: 目的：提供一种以酰胺为原料得到的新型恶唑衍生物，对植物病原菌有较强的抗菌作用，如Pyricularia oryzae Cavera，Rhizoctonia SolaniAG-1，Botrytis cinerea KCI，致病疫霉或 喜欢。 构成：将酰胺化合物（式II）在二氯丙酮和乙醇的溶剂中回流得到氯甲基恶唑（式III）。 氯甲基恶唑的氯原子通过使用碘化钠被取代为碘原子，然后与2-（2-羟基苯基）-3-甲氧基丙烯酸甲酯（式IV）（在A = C的情况下）或2 （2-羟基苯基） - 乙酸甲酯（式IV）（在A = N的情况下）反应以产生恶唑衍生物（式I）。

    피리돈 유도체의 제조방법
    7.
    发明公开
    피리돈 유도체의 제조방법 失效
    制备吡啶衍生物的方法

    公开(公告)号：KR1020020049492A

    公开(公告)日：2002-06-26

    申请号：KR1020000078674

    申请日：2000-12-19

    Applicant: 한국화학연구원

    Inventor： 최일영 ,  정명희 ,  양준연 ,  이효원

    IPC: C07D215/22

    Abstract: PURPOSE: Provided is a process for preparing pyridone derivative represented by the formula(1) and useful as a therapeutics of Alzheimer's disease(AD). CONSTITUTION: The process for preparing pyridione derivative of the formula(1) comprises the steps of; reacting 1,4-cyclohexanedione monoketal of the formula(2) with secondary amine under acid catalyst; then treating the resultant with propiolamide of the formula(3) to obtain the compound of the formula(1). In the formulae, R1 and R2 represent individually C1-C6 alkyl group or R1 and R2 bind together to form 5-8 membered hetero ring.

    Abstract translation: 目的：提供用于制备由式（1）表示的吡酮酮衍生物并用作阿尔茨海默病（AD）的治疗剂的方法。 构成：制备式（1）的吡啶酮衍生物的方法包括以下步骤： 在酸催化剂下使式（2）的1,4-环己二酮单钾与仲胺反应; 然后用式（3）的丙酰胺处理所得物，得到式（1）的化合物。 在该式中，R 1和R 2分别表示C 1 -C 6烷基或R 1和R 2结合在一起形成5-8元杂环。

    우수한 살균력을 가진 옥사지닐 유도체
    8.
    发明公开
    우수한 살균력을 가진 옥사지닐 유도체 无效
    具有超级活性活性的氧化衍生物

    公开(公告)号：KR1020000002286A

    公开(公告)日：2000-01-15

    申请号：KR1019980022959

    申请日：1998-06-18

    Applicant: 한국화학연구원

    Inventor： 이재현 ,  최일영 ,  지성기 ,  최경자

    IPC: C07D413/04

    Abstract: PURPOSE: Oxazinyl derivatives of the formula (I) wherein: R is H or methyl; X is H, Cl, trifluoromethyl, 2,4-dichlorophenyl, methoxy, or fluoro; Y is morpholine, piperidine, pyrrole, pyrrolidine, imidazole, or triazole; Z is phenyl, 2-fluorophenyl, 3-fluorophenyl, 2,4-chlorophenyl, or benzyl) which can be used as bactericide for agriculture and gardening are prepared. CONSTITUTION: The acetophenone derivatives of the formula (II) are provided in carbon disulfide and brome is added to the solution to give dibromoacetophenone derivatives, which is dissolved in methanol and hydroxyamine HCl salt is added to give oxime derivatives of the formula (III). The oxime of the formula (III) is dissolved in methylene chloride and cycled with arylether compound of the formula (IV) to give bromooxazine derivatives of the formula (V), which are dissolved in THF and reacted with morpholine, piperidine, pyrrole, pyrrolidine, imidazole, or triazole to give the compound of the formula (I).

    Abstract translation: 目的：式（I）的恶嗪基衍生物，其中：R为H或甲基; X是H，Cl，三氟甲基，2,4-二氯苯基，甲氧基或氟; Y是吗啉，哌啶，吡咯，吡咯烷，咪唑或三唑; Z是可用作农业和园艺杀菌剂的苯基，2-氟苯基，3-氟苯基，2,4-氯苯基或苄基）。 构成：将式（II）的苯乙酮衍生物提供在二硫化碳中，并将brome加入到溶液中，得到溶解在甲醇中的二溴苯乙酮衍生物，加入羟胺HCl盐，得到式（III）的肟衍生物。 将式（III）的肟溶解在二氯甲烷中，并与式（Ⅳ）的芳基醚化合物一起循环，得到式（Ⅴ）的溴恶嗪衍生物，它们溶于THF中，与吗啉，哌啶，吡咯，吡咯烷 ，咪唑或三唑，得到式（I）化合物。

    제초력이 있는 신규 이소옥사졸린 디페닐에테르 유도체
    9.
    发明授权
    제초력이 있는 신규 이소옥사졸린 디페닐에테르 유도체 失效
    ISOOXAZOLOLIN DIPHENYL ETHER

    公开(公告)号：KR1019930011487B1

    公开(公告)日：1993-12-08

    申请号：KR1019910009728

    申请日：1991-06-13

    Applicant: 한국화학연구원

    Inventor： 이재현 ,  최일영 ,  강철훈 ,  김현진 ,  유주현

    IPC: C07D213/30

    Abstract: A issoxazoline diphenyl ether derivative of formula (I) is prepd. for use as a herbicide. The (I) is prepd. by reacting a compound of formula (II) with hydroxyamine or its acid salt. In the formula; X is nitrogen or carbon; Y is hydrogen, halogen or nitro; Z is chloride or CF3; R is cyano, methyl, methyl ester, ethyl ester, t-butyl ester or methyl ketone; R1 is methyl, amino etc.; R2 is cyano, methyl ketone, methyl ester or ethyl ester.

    Abstract translation: 制备式（I）的异恶唑啉二苯醚衍生物。 用作除草剂。 （I）是prepd。 通过使式（II）的化合物与羟胺或其酸式盐反应。 在公式; X是氮或碳; Y是氢，卤素或硝基; Z是氯或CF 3; R是氰基，甲基，甲酯，乙酯，叔丁酯或甲基酮; R1是甲基，氨基等; R2是氰基，甲基酮，甲酯或乙酯。

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