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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
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。
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12.发明公开
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
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。
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公开(公告)号：KR1020020040160A
公开(公告)日：2002-05-30
申请号：KR1020000070105
申请日：2000-11-23
Applicant: 한국화학연구원
IPC: C07C50/26
Abstract: PURPOSE: Provided is a quinone compound having excellent antioxidant activity, which can be used for preventing aging and curing cancer, diabetes, epilepsy, imbecility, Parkinson's disease, and etc. CONSTITUTION: The quinone compound is represented by the formula 1 and produced from a compound represented by the formula 3, wherein R1 and R2 are independently methyl or methoxy or R1 and R2 are connectively -CH=CH-CH=CH-, R3 is -NH-(CH2)m-R5, -CO2R6, -OH, and etc., R5 is methyl, phenyl, benzyl, and etc., R6 is hydrogen atom or C1-C4 alkyl, X is CH2 or C=O, and n and m are each 0 or an integer of 1-10.
Abstract translation: 目的：提供具有优异抗氧化活性的醌化合物，其可用于预防老化和治愈癌症，糖尿病，癫痫，不育，帕金森病等。构成：醌化合物由式1表示并由 由式3表示的化合物，其中R 1和R 2独立地是甲基或甲氧基或R 1和R 2连接地是-CH = CH-CH = CH-，R 3是-NH-（CH 2）m -R 5，-CO 2 R 6，-OH， R 5是甲基，苯基，苄基等，R 6是氢原子或C 1 -C 4烷基，X是CH 2或C = O，n和m各自为0或1-10的整数。
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公开(公告)号：KR102253950B1
公开(公告)日：2021-05-20
申请号：KR1020190089266
申请日：2019-07-24
IPC: C07D233/56 , A61K31/4164 , A61P25/04
Abstract: 본발명은 1H-이미다졸-4-카바알데하이드와 1-브로모-2,3-디메틸벤젠으로부터메데토미딘을제조하는방법에관한것이다.
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15.发明授权베타-세크리테아제 활성을 억제하는 4-(아릴유레이도)피롤리딘 유도체 및 이를 유효성분으로 함유하는 약제학적 조성물 有权- 4- 4-芳基吡咯烷衍生物抑制β-分泌酶的活性和含有与活性成分相同的药物组合物
公开(公告)号：KR101569341B1
公开(公告)日：2015-11-16
申请号：KR1020130165453
申请日：2013-12-27
Applicant: 한국화학연구원
IPC: C07D207/10 , A61K31/4015 , A61P25/00
Abstract: 본발명은하기화학식 1로표시되는 4-(아릴유레이도)피롤리딘유도체또는이의약제학적으로허용가능한염, 이를유효성분으로함유하는신경퇴행성질환의예방및 치료용약제학적조성물및 이를유효성분으로함유하는베타-세크리테아제(BACE)의활성억제제조성물에관한것이다. [화학식 1]본발명에따른 4-(아릴유레이도)피롤리딘유도체는베타-세크리테아제(BACE)의활성을억제하여신경세포를손상시키는베타-아밀로이드단백질의생성을억제함으로써알츠하이머, 다운증후군등의신경퇴행성질환을치료하거나예방하는데효과적으로사용될수 있다.
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Patent Agency Ranking16.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
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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公开(公告)号：KR100838645B1
公开(公告)日：2008-06-16
申请号：KR1020060095156
申请日：2006-09-28
Applicant: 한국화학연구원
IPC: C07D211/56 , A61K31/4406
Abstract: 본 발명은 하기 화학식 Ⅰ로 표시되는 (3R)-아미노-(4R)-아릴피페리딘 화합물 또는 이의 약제학적으로 허용 가능한 염에 관한 것이고, 또한 상기 3R)-아미노-(4R)-아릴피페리딘 화합물 또는 이의 약제학적으로 허용 가능한 염을 유효성분으로 함유하는 알쯔하이머 또는 다운증후군의 예방 또는 치료용 조성물, 또는 베타-세크리테아제(BACE)의 활성 억제제 조성물에 관한 발명이다.
[화학식 Ⅰ]
본 발명에 따른 3R)-아미노-(4R)-아릴피페리딘 화합물은 베타-세크리테아제(BACE)의 활성을 억제하여 신경세포를 손상시키는 베타-아밀로이드 단백질의 생성을 억제함으로써 알츠하이머 질환을 치료하거나 예방하는데 효과적으로 사용될 수 있다.
알츠하이머 질환, 피페리딘 화합물, 베타-세크리테아제, 노화, 신경퇴행성 질환, 베타-아밀로이드-
公开(公告)号：KR100808685B1
公开(公告)日：2008-02-29
申请号：KR1020060101544
申请日：2006-10-18
Applicant: 한국화학연구원
IPC: C07D401/08 , C07D417/08 , C07D413/08
Abstract: A novel piperazine derivative is provided to show excellent antagonism against a dopamine receptor D4, thereby being effective as a therapeutic agent for schizophrenia. A piperazine derivative having a cycloalkyl bicyclic heterocycle group is represented by a formula(1), where R1 is a group represented by the structural formula(1) or (2); X is H, halogen, nitro, cyano, C1-6 alkyl, or C1-6 alkoxy; Y is NH, S or O; R2 is phenyl or pyridine, which may be substituted or unsubstituted by a substituent selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, and cyano; n is an integer from 1 to 3. A method for preparing a piperazine compound represented by the formula(1b) comprises the steps of: (a) subjecting cyclopentanone carboxylic acid coupled to a Wang resin and represented by the formula(3) with a piperazine to a reducing amination to obtain a compound represented by the formula(3a); and (b) applying microwave to the compound of the formula(3a) with an amine compound represented by the formula(3b) to synthesize the compound of the formula(1b), where R2, X, Y, and n are the same as defined above, and A is Wang resin. A therapeutic agent for schizophrenia comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof.
Abstract translation: 提供了一种新的哌嗪衍生物，以显示对多巴胺受体D4的极好的拮抗作用，从而作为精神分裂症的治疗剂是有效的。 具有环烷基双环杂环基的哌嗪衍生物由式（1）表示，其中R 1是由结构式（1）或（2）表示的基团。 X是H，卤素，硝基，氰基，C 1-6烷基或C 1-6烷氧基; Y是NH，S或O; R2是苯基或吡啶，其可以被选自卤素，C 1-6烷基，C 1-6烷氧基和氰基的取代基取代或未取代。 n为1〜3的整数。由式（1b）表示的哌嗪化合物的制备方法包括以下步骤：（a）将与式（3）表示的Wang树脂偶联的环戊酮羧酸与 哌嗪还原胺化得到式（3a）表示的化合物; 和（b）用式（3b）表示的胺化合物向式（3a）化合物施加微波以合成式（1b）化合物，其中R 2，X，Y和n与 A为王树脂。 精神分裂症的治疗剂包括式（1）的化合物或其药学上可接受的盐。
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公开(公告)号：KR1020060109085A
公开(公告)日：2006-10-19
申请号：KR1020050031355
申请日：2005-04-15
Applicant: 한국화학연구원
IPC: C07D401/12
Abstract: Huperzine-tacrine hybrids and preparing process thereof is provided to improve inhibiting activity of acetylcholine esterase(AChE) associated with occurrence of neurodegenerative disease, and enhance their production yield. The huperzine-tacrine hybrid derivatives represented by the formula(1) having neurodegenerative disease-treating effect are provided, wherein X is hydrogen, halogen group or C1-C6 alkyl group, m is 1 to 3 and n is 1 or 2; and the neurodegenerative disease is dementia. The precursors of the huperzine-tacrine hybrid derivatives represented by the formula(6) are provided. The process for preparing the huperzine-tacrine hybrid derivatives comprises the steps of: (1) treating chloro acrydine represented by the formula(2) with hydroxylamine to prepare hydroxy compounds represented by the formula(3); (2) oxidizing the compounds of the formula(3) with an oxidizing agent selected from pyridinium chlorochromate(PCC), pyridinium dichromate(PDC), Jone's reagent and manganese dioxide to prepare aldehyde compounds represented by the formula(4); (3) condensing the aldehyde compounds of the formula(4) with pyridineamine represented by the formula(5) by using a molecular sieve to prepare immine, and reducing it to prepare compounds represented by the formula(6); and (4) deprotecting the compounds of the formula(6) by using trimethylsilyl iodide(TMSI).
Abstract translation: 提供石杉碱混合物及其制备方法，以改善与神经退行性疾病发生相关的乙酰胆碱酯酶（AChE）的抑制活性，提高其产量。 提供了具有神经变性疾病治疗效果的由式（1）表示的石杉碱 - 他克林杂合衍生物，其中X为氢，卤素基或C 1 -C 6烷基，m为1至3，n为1或2; 神经变性疾病是痴呆。 提供了由式（6）表示的石杉碱 - 他克林杂合衍生物的前体。 制备石杉木混合衍生物的方法包括以下步骤：（1）用羟胺处理由式（2）表示的氯丙酸，制备由式（3）表示的羟基化合物; （2）用选自氯铬酸吡啶鎓（PCC），重铬酸吡啶鎓（PDC），琼氏试剂和二氧化锰的氧化剂氧化式（3）的化合物，制备由式（4）表示的醛化合物。 （3）通过使用分子筛将式（4）的醛化合物与式（5）所示的吡啶胺缩合以制备赖氨酸，并将其还原以制备由式（6）表示的化合物; 和（4）通过使用三甲基甲硅烷基碘（TMSI）使式（6）的化合物脱保护。
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公开(公告)号：KR100574435B1
公开(公告)日：2006-04-27
申请号：KR1020040025267
申请日：2004-04-13
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: 본 발명은 다음 화학식 1로 표시되는 후퍼진(huperzine) B 유도체와 이의 제조방법에 관한 것으로서, 더욱 상세하게는 다음 화학식 2로 표시되는 카르복실산 화합물을 출발물질로 사용하고, C5 위치의 카르복실기를 아민화 및
N -알켄일화하여 다음 화학식 4로 표시되는 화합물을 반응 중간체로 합성한 후에, 이 중간체 화합물을 복분해반응(Ring Closing Metathesis, RCM)한 후에 메틸보호기를 제거하는 일련의 제조과정을 거쳐 합성하게 되는, 다음 화학식 1로 표시되는 후퍼진 B 유도체와 이의 제조방법에 관한 것이다. 본 발명에 따른 상기 화학식 1로 표시되는 화합물은 치매치료 효과가 있는 것으로 잘 알려져 있는 후퍼진 B 화합물의 유도체로서 화합물 그 자체의 의약적 활성이 기대된다.
후퍼진 B, 치매 치료, N-알켄일화, 복분해(Ring Closing Metathesis, RCM)
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