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公开(公告)号：WO2013081420A2
公开(公告)日：2013-06-06
申请号：PCT/KR2012/010322
申请日：2012-11-30
Applicant: 한국과학기술연구원
IPC: C07D403/06 , A61K31/496 , A61P25/00
CPC classification number: C07D295/15 , C07D211/22 , C07D211/38 , C07D211/52 , C07D211/58 , C07D231/40 , C07D233/64 , C07D295/088 , C12N5/0686 , C12N2501/999
Abstract: 본 발명은 신규한 페녹시프로판올 유도체, 이의 T-형 칼슘 채널 및/또는 TREK 채널 저해 용도, 및 T-형 칼슘 채널 및/또는 TREK 채널 관련 질환의 예방 및/또는 치료 용도에 관한 것이다.
Abstract translation: 本发明涉及一种新的苯氧基丙醇衍生物，以及其在阻断T型钙通道和/或TREK通道中的用途，以及用于预防和/或治疗涉及T型钙通道和/或TREK通道的疾病。
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公开(公告)号：KR101319593B1
公开(公告)日：2013-10-16
申请号：KR1020110071653
申请日：2011-07-19
Applicant: 한국과학기술연구원
IPC: C07D417/10 , C07D417/12 , C07D277/36 , A61K31/427
Abstract: 본 발명은 메틸리덴-헤테로싸이클릭 화합물과 이의 약학적으로 허용 가능한 염, 이 화합물의 제조방법 및 이 화합물을 유효성분으로 함유하는 약제조성물에 관한 것이다.
본 발명의 화합물은 NF-κB의 활성 과정에 관여하는 IκB 키나제-b (IKK-b)에 대해 강한 저해활성을 가지고 있으므로 류마티스 관절염(rheumatoid arthritis), 유년기 관절염(juvenile arthritis), 천식(asthma), 척추성 관절염(spondyloarthopathies), 통풍(gout), 골관절염(osteoarthritis), 알러지성 비염, 아토피성 피부염, 담마진, 전신 홍반성 루푸스(systemic lupuserythematosus), 건선, 궤양성 대장염, 전신성 염증반응증후군, 폐혈증, 다발성근염, 결절다발성동맥염을 포함하는 각종 염증질환 치료를 위한 약제로써 유용하다.-
公开(公告)号：KR101476379B1
公开(公告)日：2014-12-29
申请号：KR1020110127053
申请日：2011-11-30
Applicant: 한국과학기술연구원
IPC: C07D403/06 , A61K31/496 , A61P25/00
CPC classification number: C07D295/15 , C07D211/22 , C07D211/38 , C07D211/52 , C07D211/58 , C07D231/40 , C07D233/64 , C07D295/088 , C12N5/0686 , C12N2501/999
Abstract: 본발명은신규한페녹시프로판올유도체, 이의 T-형칼슘채널및/또는 TREK 채널저해용도, 및 T-형칼슘채널및/또는 TREK 채널관련질환의예방및/또는치료용도에관한것이다.
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Patent Agency Ranking4.发明公开Ｔ형 칼슘 채널 저해작용을 가지는 신규 1-(4-할로페닐 옥소 또는 싸이오)-3-(4-치환피페라진-1-일)프로판-2올 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 약학적 조성물 无效新型1-（4-戊烯基氧基或硫代）-3-（4-取代的哌嗪-1-基）丙烷-2-醇衍生物，其具有T型钙通道抑制活性或药物可接受的盐，其制备方法和药物组合物包含 同样作为活跃成分
公开(公告)号：KR1020120066699A
公开(公告)日：2012-06-25
申请号：KR1020100093304
申请日：2010-09-27
Applicant: 한국과학기술연구원
IPC: C07D295/033 , A61K31/495 , A61P25/08 , A61P9/12
Abstract: PURPOSE: A pharmaceutical composition containing a novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propane-2-ol derivative is provided to effectively suppress T type calcium channel activation and to prevent or treat hypertension, cancer, epilepsy, and neurogenic pain. CONSTITUTION: A novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propan-2-ol derivative is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 comprises: a step of reacting a compound of chemical formula 2 with chiral epichlorohydrin under the presence of a base and solvent to prepare an epoxy compound of chemical formula 3; and a step of reacting the epoxy compound of chemical formula 3 with piperazine derivative of chemical formula 4. The base is potassium carbonate, sodium carbonate or pyridine. A pharmaceutical composition for preventing or treating diseases caused by overactivation of T type calcium channel contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.
Abstract translation: 目的：提供含有新型1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物的药物组合物，以有效抑制T型钙通道激活和预防 或治疗高血压，癌症，癫痫和神经源性疼痛。 构成：化学式1表示新的1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物。一种制备化学式1化合物的方法 包括：在碱和溶剂的存在下使化学式2的化合物与手性表氯醇反应以制备化学式3的环氧化合物的步骤; 和使化学式3的环氧化合物与化学式4的哌嗪衍生物反应的步骤。碱是碳酸钾，碳酸钠或吡啶。 用于预防或治疗由T型钙通道过度活化引起的疾病的药物组合物含有其衍生物或药学上可接受的盐作为活性成分。
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公开(公告)号：KR101331186B1
公开(公告)日：2013-11-22
申请号：KR1020130092770
申请日：2013-08-05
Applicant: 한국과학기술연구원
IPC: C07D403/06 , C07D403/12 , A61K31/497 , A61P25/00
Abstract: 본 발명은 신규한 페녹시프로판올 유도체, 이의 T-형 칼슘 채널 및/또는 TREK 채널 저해 용도, 및 T-형 칼슘 채널 및/또는 TREK 채널 관련 질환의 예방 및/또는 치료 용도에 관한 것이다.
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公开(公告)号：KR1020130010784A
公开(公告)日：2013-01-29
申请号：KR1020110071653
申请日：2011-07-19
Applicant: 한국과학기술연구원
IPC: C07D417/10 , C07D417/12 , C07D277/36 , A61K31/427
Abstract: PURPOSE: A methylidene-heterocyclic compound and a pharmaceutical composition containing the same are provided to strongly suppress IkappaB kinase-b(IKK-b) and to treat various inflammatory diseases. CONSTITUTION: A methylidene-heterocyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating inflammatory diseases contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, juvenile arthritis, asthma, spondyloarthopathies, gout, osteoarthritis, allergic rhinitis, atopic dermatitis, systemic lupuserythematosus, psoriasis, ulcerative colitis, SIRS, sepsis, or polymyositis. A method for preparing the compound of chemical formula 1 comprises: a step of cyclizing an aniline compound of chemical formula 2 and preparing a 3-phenyl rhodanine compound of chemical formula 3; and a step of condensing the compound of chemical formula 3 with aldehyde compound of R2-C(O)H under an acidic condition. [Reference numerals] (AA) Step 1; (BB) Step 2
Abstract translation: 目的：提供亚甲基杂环化合物和含有它们的药物组合物以强烈抑制IkappaB激酶b（IKK-b）并治疗各种炎性疾病。 构成：亚甲基杂环化合物由化学式1表示。用于预防和治疗炎性疾病的药物组合物含有化学式1的化合物作为活性成分。 炎性疾病包括类风湿性关节炎，青少年关节炎，哮喘，脊椎动物病痛，痛风，骨关节炎，过敏性鼻炎，特应性皮炎，系统性红斑狼疮，牛皮癣，溃疡性结肠炎，SIRS，败血症或多发性肌炎。 制备化学式1的化合物的方法包括：使化学式2的苯胺化合物环化并制备化学式3的3-苯基绕丹宁化合物的步骤; 和在酸性条件下将化学式3的化合物与R2-C（O）H的醛化合物缩合的步骤。 （附图标记）（AA）步骤1; （BB）步骤2
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公开(公告)号：KR1020130103461A
公开(公告)日：2013-09-23
申请号：KR1020130092770
申请日：2013-08-05
Applicant: 한국과학기술연구원
IPC: C07D403/06 , C07D403/12 , A61K31/497 , A61P25/00
Abstract: PURPOSE: A phenoxypropanol derivative is provided to effectively suppress T-type calcium channel or TWIK-related K+ (TREK)-1 channel, thereby treating various diseases caused by the activation of the channels. CONSTITUTION: A phenoxypropanol derivative of chemical formula I or a racemic body, a pharmaceutically acceptable salt, a solvate, or a hydrate thereof is provided. A pharmaceutical composition for preventing or treating diseases related to T-type calcium channel or TREK-1 channel, selected among Parkinson's disease, Alzheimer's disease, schizophrenia, sleep disorder, epilepsy, pain, hypertension, arrhythmia, ventricular hypertrophy, angina pectoris, heart failure, myocardial infarction, cancer, hypoxia, cerebral ischemia, alkalemia, and depression contains the phenoxypropanol derivative, the racemic body, the pharmaceutically acceptable salt, the solvate, or the hydrate as an active ingredient. A method for suppressing T-type calcium channel or TREK-1 channel comprises the steps of: preparing a biological sample from an organ; and applying the phenoxypropanol derivative, the racemic body, the pharmaceutically acceptable salt, the solvate, or the hydrate to the biological sample.
Abstract translation: 目的：提供苯氧基丙醇衍生物，有效抑制T型钙通道或TWIK相关K +（TREK）-1通道，从而治疗由通道激活引起的各种疾病。 构成：提供化学式I的苯氧基丙醇衍生物或外消旋体，其药学上可接受的盐，溶剂化物或其水合物。 用于预防或治疗与帕金森病，阿尔茨海默病，精神分裂症，睡眠障碍，癫痫，疼痛，高血压，心律失常，心室肥大，心绞痛，心力衰竭有关的T型钙通道或TREK-1通道相关疾病的药物组合物 ，心肌梗死，癌症，缺氧，脑缺血，碱血症和抑郁症含有苯氧基丙醇衍生物，外消旋体，药学上可接受的盐，溶剂合物或水合物作为活性成分。 抑制T型钙通道或TREK-1通道的方法包括以下步骤：从器官制备生物样品; 以及将所述苯氧基丙醇衍生物，外消旋体，药学上可接受的盐，溶剂合物或水合物施用于生物样品。
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公开(公告)号：KR1020130060799A
公开(公告)日：2013-06-10
申请号：KR1020110127053
申请日：2011-11-30
Applicant: 한국과학기술연구원
IPC: C07D403/06 , A61K31/496 , A61P25/00
CPC classification number: C07D295/15 , C07D211/22 , C07D211/38 , C07D211/52 , C07D211/58 , C07D231/40 , C07D233/64 , C07D295/088 , C12N5/0686 , C12N2501/999
Abstract: PURPOSE: A phenoxy propanol derivative is provided to effectively suppress T-type calcium channel or TREK(TWIK-related K+)-1 channel and to treat various diseases. CONSTITUTION: A pharmaceutical composition for preventing or treating diseases related to T-type calcium channel or TREK-1 channel contains a phenoxy propanol derivative with a structure of chemical formula I or a racemic body, a pharmaceutically acceptable salt, solvent, or hydrate thereof as an active ingredient. A method for suppressing the T-type calcium channel or TREK-1 channel comprises: a step of preparing a biological sample from organism; and a step of applying the phenoxy propanol derivative, or a racemic body, a pharmaceutically acceptable salt, solvate, or hydrate thereof.
Abstract translation: 目的：提供苯氧丙醇衍生物，有效抑制T型钙通道或TREK（TWIK相关K +）-1通道，治疗各种疾病。 构成：用于预防或治疗与T型钙通道或TREK-1通道有关的疾病的药物组合物含有具有化学式I结构的苯氧基丙醇衍生物或其外消旋体，其药学上可接受的盐，溶剂或水合物作为 活性成分。 抑制T型钙通道或TREK-1通道的方法包括：从生物体制备生物样品的步骤; 以及施用苯氧基丙醇衍生物或外消旋体，其药学上可接受的盐，溶剂合物或水合物的步骤。
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