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公开(公告)号：KR1020050058587A
公开(公告)日：2005-06-17
申请号：KR1020030090518
申请日：2003-12-12
Applicant: 한국과학기술연구원
CPC classification number: C07K14/705 , C12N2503/02
Abstract: 본 발명은 레트로바이러스 발현 시스템을 이용하여 α
1G T-형 칼슘 채널이 안정적으로 발현되는 HEK293 세포를 인간 Kir2.1 유전자로 형질전환시킨 세포주에 관한 것이다. 본 발명의 HEK293 세포주는 Kir2.1 (칼륨 내부 정류 채널 (potassium inwardly-rectifying channel))을 영구적으로 추가 발현함으로써 세포 막전압을 과분극쪽으로 더 낮추어 안정적인 막전압을 발현하고, 따라서 전기생리학적 방법 이외에도 고농도의 KCl에 의하여 α
1G 가 활성화된다.-
42.发明公开진세노사이드 Ｒｇ３ 또는 진세노사이드 Ｒｈ２를포함하는 글루타메이트 매개 신경독성 억제 조성물 无效用于抑制含有GINSENOSIDE RG3或GINSENOSIDE RH2的谷氨酸介导的神经毒性的组合物
公开(公告)号：KR1020040036451A
公开(公告)日：2004-04-30
申请号：KR1020020065648
申请日：2002-10-26
Applicant: 한국과학기술연구원
IPC: A61K31/704
CPC classification number: A61K31/7048 , A61K2300/00
Abstract: PURPOSE: Provided is a composition for inhibiting glutamate-mediated neurotoxicity comprising ginsenoside Rg3 or ginsenoside Rh2. The composition has excellent neurotoxicity inhibiting effect or nerve cells protection effect, and is thus effective for treatment of brain diseases, such as Alzheimer's disease, Huntington's disease, epilepsy, stroke, cerebral paralysis and the like. CONSTITUTION: A composition for inhibiting glutamate-mediated neurotoxicity is characterized by containing 20(S)- ginsenosideRg3 or its metabolite, 20(S)-ginsenoside Rh2 which have excellent inhibition effect on an NMDA receptor. Therefore, it is used for treatment of brain diseases, such as Alzheimer's disease, Huntington's disease, epilepsy, stroke, cerebral paralysis and the like.
Abstract translation: 目的：提供一种抑制谷氨酸介导的神经毒性的组合物，包括人参皂甙Rg3或人参皂甙Rh2。 该组合物具有优异的神经毒性抑制作用或神经细胞保护作用，因此有效治疗诸如阿尔茨海默病，亨廷顿病，癫痫，中风，脑麻痹等脑疾病。 构成：用于抑制谷氨酸介导的神经毒性的组合物的特征在于含有对NMDA受体具有优异抑制作用的20（S） - 人参皂苷Rg3或其代谢物，20（S） - 人参皂甙Rh2。 因此，其用于治疗脑疾病，例如阿尔茨海默病，亨廷顿病，癫痫，中风，脑麻痹等。
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公开(公告)号：KR101822046B1
公开(公告)日：2018-01-25
申请号：KR1020160096119
申请日：2016-07-28
Applicant: 한국과학기술연구원
CPC classification number: A61B5/4064 , A61M2025/0007 , A61M2210/0693
Abstract: 뇌신경계의표적부위의판별및 약물주입을동시에수행하기위한약물주입장치및 이를이용한약물주입방법을이용하면표적부위로추정되는부위의전기생리신호를측정하여미세한표적부위를판별해내고, 동시에그 위치에약물을주입할수 있어효율적으로약물을전달할수 있다. 또한, 약물을전달한후에도표적부위로부터전기생리신호를측정할수 있으므로, 약물에대한표적부위의반응을관찰할수 있다.
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公开(公告)号：KR1020120096842A
公开(公告)日：2012-08-31
申请号：KR1020110016203
申请日：2011-02-23
Applicant: 한국과학기술연구원
Inventor： 추현아 , 배애님 , 조용서 , 이효선 , 이지은 , 조경희 , 임혜원 , 서선희 , 송치만 , 정혜진 , 남길수 , 금교창 , 김동진 , 최경일 , 최기현 , 이재균 , 강용구 , 박웅서 , 이주현 , 신선미 , 아미드,압둘와히드 , 김영수 , 민선준
IPC: C07D413/12 , A61K31/496 , A61P25/00 , A61P9/00
CPC classification number: C07D413/12
Abstract: PURPOSE: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is provided to have excellent activity as an antagonist of T- type calcium ion channel. CONSTITUTION: A 5-(substituted alkylaminomethyl)isoxazole based compound as T-type calcium channel blocker is represented by chemical formula 1. The encephalopathy therapy and for prevention agent selected from epilepsy, depression, Parkinson's disease, dementia, sleep disorder, an agent for cancer treatment and prevention, an agent for heart disease treatment and prevention selected from hypertensive, cardiac arrhythmia, angina, myocardial infarction, congestive heart failure, pharmaceutical composition for alleviating pain selected from neuropathic pain and chronic and acute pain includes a compound represented by chemical formula 1.
Abstract translation: 目的：提供作为T型钙通道阻滞剂的5-（取代的烷基氨基甲基）异恶唑基化合物作为T-型钙离子通道的拮抗剂具有优异的活性。 构成：以化学式1表示作为T型钙通道阻断剂的5-（取代烷基氨基甲基）异恶唑类化合物。脑病治疗和预防药物选自癫痫，抑郁症，帕金森病，痴呆，睡眠障碍， 癌症治疗和预防，选自高血压，心律失常，心绞痛，心肌梗塞，充血性心力衰竭，减轻选自神经性疼痛和慢性和急性疼痛的疼痛的药物组合物的心脏病治疗和预防剂，包括由化学式 1。
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公开(公告)号：KR1020120088398A
公开(公告)日：2012-08-08
申请号：KR1020110009730
申请日：2011-01-31
Applicant: 한국과학기술연구원
IPC: C07D413/06 , C07D413/12 , A61K31/496 , A61P9/00
Abstract: PURPOSE: A pharmaceutical composition containing pentagonal heteroaromatic compound, a pharmaceutically acceptable salt thereof having a pharmaceutical activity to T-type calcium channel is provided to treat heart disease, brain diseases, stroma, chronic pain, neuropathic pain, and cancer. CONSTITUTION: A pentagonal heteroaromtaic compound with T-type calcium channel is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating stroma, hypertension, angina, chronic pain, neuropathic pain, and cancer contains the compound as an active ingredient. A method for preparing the compound comprises a step of binding carbochloride compound of chemical formula 3a and heterocyclic amine compounds of chemical formula 2a under the presence of an alkyl amine base.
Abstract translation: 目的：提供含有对T型钙通道具有药学活性的五价杂芳族化合物及其药学上可接受的盐的药物组合物，用于治疗心脏病，脑疾病，基质，慢性疼痛，神经性疼痛和癌症。 构成：用化学式1表示具有T型钙通道的五价杂合化合物。用于预防和治疗基质，高血压，心绞痛，慢性疼痛，神经性疼痛和癌症的药物组合物含有该化合物作为活性成分。 制备该化合物的方法包括在烷基胺基的存在下结合化学式3a的氯化碳化合物和化学式2a的杂环胺化合物的步骤。
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Patent Agency Ranking46.发明公开세로토닌 6 수용체와 Ｇ―ｐｒｏｔｅｉｎ α15가 동시에 안정적으로 발현하는 ＨＥＬＡ 세포주 및 상기 세포주와 칼슘 영상화를 이용하여 세라토닌 6 수용체의 선택적 리간드의 고효율 스크리닝 방법 有权细胞系稳定表达5-HT6R和G蛋白α15基因，并且可以通过使用钙成像直接成像科学荧光技术和选择性配体的高通量筛选方法
公开(公告)号：KR1020120021467A
公开(公告)日：2012-03-09
申请号：KR1020100074669
申请日：2010-08-02
Applicant: 한국과학기술연구원
Abstract: PURPOSE: A cell line which is prepared by permanently transfecting serotonin 6 receptor gene and permanently transforming G-protein alpha 15 gene is provided to detect human serotonin 6 receptor-specific ligand. CONSTITUTION: A cell line in which GPCR(G-protein coupled receptor) gene and G-protein alpha 15 gene are simultaneously expressed is prepared by transduction of a vector expressing GPCR gene and G-protein alpha15 gene. A method for screening GPCR-specific ligand comprises: a step of treating a test compound to the cell line; a step of measuring receptor activity of the cell line; and a step of comparing the result with the activity with untreated cell line.
Abstract translation: 目的：提供通过永久转染血清素6受体基因和永久转化G蛋白α15基因制备的细胞系，以检测人血清素6受体特异性配体。 构成：通过转导表达GPCR基因和G蛋白α15基因的载体，制备GPCR（G蛋白偶联受体）基因和G蛋白α15基因同时表达的细胞系。 用于筛选GPCR特异性配体的方法包括：将测试化合物处理至细胞系的步骤; 测量细胞系受体活性的步骤; 以及将结果与未处理细胞系的活性进行比较的步骤。
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47.发明公开
公开(公告)号：KR1020110115374A
公开(公告)日：2011-10-21
申请号：KR1020100034846
申请日：2010-04-15
Applicant: 한국과학기술연구원
IPC: C07D243/08 , C07D243/06 , A61P9/12
Abstract: 본 발명은 T-형 칼슘 채널에 대한 활성을 갖는 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물, 상기 화합물의 제조방법, 그리고 상기 화합물을 유효성분으로 포함하는 약학조성물에 관한 것이다. 본 발명의 신규 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물 또는 약학적으로 허용 가능한 이의 염은 T-형 칼슘 채널에 대한 길항작용을 가지므로 간질, 고혈압 등의 뇌질환 치료제, 협심증 등의 심장질환 치료제, 만성 통증, 신경성 통증 등의 통증질환 치료제, 또는 항암제로 유용하다.
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公开(公告)号：KR101064258B1
公开(公告)日：2011-09-14
申请号：KR1020080135519
申请日：2008-12-29
Applicant: 한국과학기술연구원
Inventor： 한호규 , 남기달 , 신동윤 , 박찬호 , 조성우 , 김은아 , 남길수 , 최경일 , 서선희 , 신희섭 , 김동진 , 배애님 , 정혜진 , 추현아 , 임혜원 , 조용서 , 노은주 , 금교창 , 최기현 , 신계정 , 정찬성 , 이재균 , 강용구 , 김영수 , 박웅서 , 김기선 , 정혜선 , 송치만 , 민선준 , 김은경 , 이철주 , 강순방
IPC: C07D277/82 , C07D263/58 , C07D235/30 , A61P25/28
CPC classification number: C07D277/82 , C07D235/22 , C07D263/58 , C07D327/04 , C07D333/06
Abstract: 본 발명은 신규한 벤조아릴우레이도 화합물, 및 이의 퇴행성 뇌질환 예방 또는 치료에 있어서의 용도에 관한 것으로, 보다 상세하게는, 화학식 1의 구조를 갖는 벤조아릴우레이도 화합물, 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 예방 또는 치료용 조성물에 관한 것이다. 상기 퇴행성 뇌질환은 알츠하이머, 치매, 파킨슨병, 뇌졸중, 아밀로이드증, 픽 질환 (Pick's disease), 루게릭병, 헌팅턴병, 크로이츠펠트-야콥(Creutzfeld-Jakob)병 등일 수 있다.
[화학식 1]-
公开(公告)号：KR1020110020023A
公开(公告)日：2011-03-02
申请号：KR1020090077687
申请日：2009-08-21
Applicant: 한국과학기술연구원
IPC: C07D413/12 , C07D413/10
Abstract: PURPOSE: An oxazole-piperazine compound having a pharmaceutical activity with respect to T-type calcium channel is provided to ensure excellent activity as an antagonist of the channel and to prevent and treat cancer, epilepsy, heart diseases, and pain. CONSTITUTION: An oxazole-piperazine compounds is denoted by chemical formula 1. A pharmaceutical composition for treating epilepsy, cancer, hypertension, myocardial infarction, neuropathic pain, and acute and chronic pain contains the oxazole-piperazine compound of chemical formula 1. The compound of chemical formula 1 is prepared by reacting piperazine-amine compound of chemical formula 2 and oxazole aldehyde compound of chemical formula 3 by reductive amination. The reductive amination is performed under the presence of molecules of 4-8 meshes and NaBH(OAc)_3, NaBH_3CN, or NaBH_4.
Abstract translation: 目的：提供相对于T型钙通道具有药学活性的恶唑 - 哌嗪化合物，以确保作为通道拮抗剂的优异活性，并预防和治疗癌症，癫痫，心脏病和疼痛。 构成：化学式1表示恶唑 - 哌嗪化合物。用于治疗癫痫，癌症，高血压，心肌梗死，神经性疼痛和急性和慢性疼痛的药物组合物含有化学式1的恶唑 - 哌嗪化合物。 化学式1通过化学式2的哌嗪 - 胺化合物和化学式3的恶唑醛化合物通过还原胺化反应来制备。 还原胺化在4-8目和NaBH（OAc）3，NaBH 3 CN或NaBH 4的分子存在下进行。
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公开(公告)号：KR1020100005476A
公开(公告)日：2010-01-15
申请号：KR1020080065522
申请日：2008-07-07
Applicant: 한국과학기술연구원
IPC: C07D403/12
CPC classification number: C07D401/12 , A61K31/454
Abstract: PURPOSE: An isoindolinone derivative having pharmaceutical activation to T-type calcium channel is provided to have antagonistic activity to T-type calcium channel and use as a therapeutic agent for hypertension, cancer, and neurogenic pain. CONSTITUTION: An isoindolinone derivative is denoted by chemical formula 1. In chemical formula 1, R1 is hydrogen atom, halogen atom, alkoxy group of C1-C6, haloalkyl group of C1-C6, nitro group, cyano group, or hydroxyl group. R2 is hydrogen atom, alkyl group of C1-C6, or aryl group. The isoindolinone derivative is obtained by reacting piperidinyl propylamine derivative of chemical formula 9 with isoindolinone carboxylic acid derivative of chemical formula 8 through amide reaction. A pharmaceutical composition for treating hypertension, cancer, epilepsy, and neurogenic pain contains the isoindolinone derivative and its pharmaceutically acceptable salt.
Abstract translation: 目的：提供具有T型钙通道药学活性的异吲哚啉酮衍生物，对T型钙通道具有拮抗作用，用作高血压，癌症和神经源性疼痛的治疗剂。 构成：异吲哚啉酮衍生物由化学式1表示。在化学式1中，R 1为氢原子，卤素原子，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，硝基，氰基或羟基。 R2是氢原子，C1-C6烷基或芳基。 异吲哚啉酮衍生物通过化学式9的哌啶基丙胺衍生物与化学式8的异吲哚酮羧酸衍生物反应而得到。 用于治疗高血压，癌症，癫痫和神经原性疼痛的药物组合物含有异吲哚啉酮衍生物及其药学上可接受的盐。
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