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公开(公告)号：KR1020130115696A
公开(公告)日：2013-10-22
申请号：KR1020120038239
申请日：2012-04-13
Applicant: 한국과학기술연구원
IPC: C07D211/42 , C07D241/28 , A61K31/44 , A61P25/00
Abstract: PURPOSE: A urea derivative is provided to selectively suppress the action of mPTP in the brain, thereby being used as a neuroprotective agent which improves the action of the mitochondria. CONSTITUTION: A urea derivative is denoted by chemical formula 1. A method for preparing the urea derivative comprises the steps of making a compound of chemical formula 2 react with isocyanate compounds or isothiocyanate compounds. The compound of chemical formula 2 is prepared by making a compound of chemical formula 3 react with benzyl halide compounds. A pharmaceutical composition for suppressing the action of mPTP contains the urea derivative or a pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for treating nervous diseases contains the urea derivative or a pharmaceutically acceptable salt thereof as an active ingredient.
Abstract translation: 目的：提供尿素衍生物以选择性抑制脑中mPTP的作用，从而用作改善线粒体作用的神经保护剂。 构成：以化学式1表示脲衍生物。制备尿素衍生物的方法包括使化学式2的化合物与异氰酸酯化合物或异硫氰酸酯化合物反应的步骤。 通过使化学式3的化合物与苄基卤化合物反应来制备化学式2的化合物。 用于抑制mPTP作用的药物组合物含有尿素衍生物或其药学上可接受的盐作为活性成分。 用于治疗神经疾病的药物组合物含有尿素衍生物或其药学上可接受的盐作为活性成分。
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公开(公告)号：KR1020130058225A
公开(公告)日：2013-06-04
申请号：KR1020110124122
申请日：2011-11-25
Applicant: 한국과학기술연구원
IPC: C07D241/04 , A61K31/496 , A61K31/495 , A61K31/065
Abstract: PURPOSE: A biphenyl derivative or a pharmaceutically acceptable salt thereof is provided to ensure excellent activity to 5-HT7 serotonin receptor and to be used as a preventive and therapeutic agent for depression, migraine, anxiety, pain especially inflammatory pain and neuropathy pain, bio rhythm, sleep, smooth muscle related diseases. CONSTITUTION: A biphenyl derivative is denoted by chemical formula 2. The biphenyl derivative has a structure of chemical formula 4 or 5. A pharmaceutical composition for preventing or treating diseases contains the biphenyl derivative or a pharmaceutically acceptable salt thereof. A method for preparing the biphenyl derivative of chemical formula 2 comprises: a step of performing Suzuki coupling of aryl boronic acid of chemical formula 6 and bromobenzene aldehyde of chemical formula 7 to prepare a biphenyl aldehyde intermediate of chemical formula 8; and a step of performing reductive amination of the biphenyl aldehyde intermediate with arylpiperazine of chemical formula 9.
Abstract translation: 目的：提供联苯衍生物或其药学上可接受的盐，以确保对5-HT7血清素受体的优异活性，并用作抑郁症，偏头痛，焦虑症，疼痛，特别是炎性疼痛和神经病疼痛，生物节律的预防和治疗剂 ，睡眠，平滑肌相关疾病。 构成：联苯衍生物由化学式2表示。联苯衍生物具有化学式4或5的结构。用于预防或治疗疾病的药物组合物含有联苯衍生物或其药学上可接受的盐。 制备化学式2的联苯衍生物的方法包括：进行化学式6的芳基硼酸和化学式7的溴苯醛的Suzuki偶联以制备化学式8的联苯醛中间体的步骤; 以及用化学式9的芳基哌嗪进行联苯醛中间体的还原胺化的步骤。
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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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85.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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Patent Agency Ranking
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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公开(公告)号：KR100879636B1
公开(公告)日：2009-01-21
申请号：KR1020070084322
申请日：2007-08-22
Applicant: 한국과학기술연구원
IPC: A61K31/517 , A61P25/00
CPC classification number: A61K31/517 , A61K31/5377
Abstract: A pharmaceutical composition for preventing and treating the disease related to the central nervous system, and a food composition are provided to obtain the effect on emesis, nausea, alcoholism, drugs abuse, depression, compulsion neurosis, anxiety, etc. A pharmaceutical composition for preventing and treating the disease related to the central nervous system comprises a quinoline derivative compound represented by the formula 1 or its pharmaceutically acceptable salt as an active ingredient, wherein R1 is H, a C1-C6 alkyl group, a phenyl group or a benzyl group; R2 is a heterocyclic group selected from morpholine, pyrrolidine and piperidine; the phenyl group or the benzyl group can be substituted with a substituent selected from a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group; and n is an integer of 1-6.
Abstract translation: 提供了用于预防和治疗与中枢神经系统有关的疾病的药物组合物和食物组合物，以获得对呕吐，恶心，酒精中毒，药物滥用，抑郁，强迫性神经症，焦虑等的作用。 并且治疗与中枢神经系统相关的疾病包括由式1表示的喹啉衍生物化合物或其药学上可接受的盐作为活性成分，其中R1是H，C1-C6烷基，苯基或苄基; R2是选自吗啉，吡咯烷和哌啶的杂环基; 苯基或苄基可以被选自卤素原子，C1-C6烷基和C1-C6烷氧基的取代基取代; n为1-6的整数。
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