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公开(公告)号：KR1020120035684A
公开(公告)日：2012-04-16
申请号：KR1020100097362
申请日：2010-10-06
Applicant: 한국과학기술연구원
IPC: C07D277/24 , C07D417/06 , A61K31/427 , A61P19/02
Abstract: PURPOSE: A thiazolidinone compound with IKK-beta suppression and a pharmaceutical composition containing the same are provided to prevent and treat rheumatoid arthritis, degenerative arthritis, asthma, and cancer. CONSTITUTION: A thiazolidine-4-one derivative is denoted by chemical formula 1. A pharmaceutical composition for treating inflammatory diseases or cancer contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, degenerative arthritis, asthma, or chronic obstructive lung diseases. A method for preparing the thiazolidione compound comprises: a step of cyclizing aryl thiourea compound of chemical formula 2 with ethyl 2-chloroacetate or prepare 2-arylimino-thiazolidine-4-one compound of chemical formula 3 or 4; a step of condensing the compound of chemical formula 3 or 4 with aryl aldehyde compound of chemical formula 5.
Abstract translation: 目的：提供具有IKK-β抑制的噻唑烷酮化合物和含有它们的药物组合物以预防和治疗类风湿性关节炎，退行性关节炎，哮喘和癌症。 构成：噻唑烷-4-酮衍生物由化学式1表示。用于治疗炎性疾病或癌症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，退行性关节炎，哮喘或慢性阻塞性肺疾病。 制备噻唑烷二酮化合物的方法包括：用2-氯乙酸乙酯环化化学式2的芳基硫脲化合物或制备化学式3或4的2-芳基亚氨基 - 噻唑烷-4-酮化合物的步骤; 将化学式3或4的化合物与化学式5的芳基醛化合物缩合的步骤。
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公开(公告)号：KR101049935B1
公开(公告)日：2011-07-15
申请号：KR1020080121802
申请日：2008-12-03
Applicant: 한국과학기술연구원
Inventor： 한호규 , 신동윤 , 남기달 , 한민수 , 서선희 , 정혜진 , 김윤지 , 송치만 , 마혜덕 , 백이연 , 최기현 , 신계정 , 노은주 , 배애님 , 신희섭 , 김동진 , 최경일 , 임혜원 , 남길수 , 조용서 , 추현아 , 강순방 , 정찬성 , 김은경 , 정혜선 , 김기선 , 금교창 , 이철주 , 민선준 , 이재균 , 강용구 , 박웅서 , 김영수
IPC: C07D277/28 , A61P25/00 , A61P9/00 , A61P35/00
Abstract: 본 발명은 아래의 화학식 1의 구조를 갖는 티아졸린계 화합물 및 이를 포함하는 T-형 칼슘 채널 저해제에 관한 것이다. 본 발명의 T-형 칼슘 채널 저해제는 T-형 칼슘 채널의 과다 발현과 관련된 질병의 치료제로서 유용하다.
(화학식 1)Abstract translation: 本发明涉及具有由下式（1）表示的结构的噻唑啉类化合物和含有其的T型钙通道抑制剂。 本发明的T型钙通道抑制剂可用作与T型钙通道过表达有关的疾病的治疗剂。
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公开(公告)号：KR1020100001288A
公开(公告)日：2010-01-06
申请号：KR1020080061148
申请日：2008-06-26
Applicant: 한국과학기술연구원
Inventor： 최경일 , 남길수 , 김혜란 , 임혜원 , 서선희 , 백이연 , 김윤지 , 신희섭 , 김동진 , 배애님 , 정혜진 , 조용서 , 추현아 , 노은주 , 강순방 , 신계정 , 한호규 , 신동윤 , 정찬성 , 남기달 , 강용구 , 이재균 , 박웅서 , 김영수 , 김은경 , 김기선 , 정혜선 , 금교창 , 이철주 , 최기현
IPC: C07D233/61
CPC classification number: C07D233/60 , C07D209/48 , C07D233/54 , C07D233/61 , C07D403/06
Abstract: PURPOSE: A novel imidazolylalkylcarbonyl derivative which is effective as calcium ion channel regulator is provided to effectively block T-type calcium ion channel, prevent and treat brain diseases, heart diseases and pain. CONSTITUTION: An imidazolylalkylcarbonyl derivative is denoted by chemical formula 1. The imidazolylalkylcarbonyl derivative of chemical formula 1 is prepared by performing amide bond of piperazine derivative of chemical formula 3 with imidazolylalkylcarboxylic acid of chemical formula 2. The amide bond is performed using binder selected from phosphonium system, ammonium system, carbodiimide system, imidazolinium, and organic phosphine system. A method for preparing the imidazolylalkylcarboxylic acid of chemical formula 2 comprises: a step of performing hetero-michael addition reaction of ethy alkenoate with imidazole compound under the presence of KF/Al2O3 catalyst to produce ethoxycarbonylalkylimidazole compound of chemical formula 2a; and a step of hydrolyzing the ethoxycarbonylalkylimidazole compound of chemical formula 2a to prepare imidazolylalkylcarboxylic acid of chemical formula 2.
Abstract translation: 目的：提供一种有效阻断T型钙离子通道，预防和治疗脑疾病，心脏病和疼痛的新型咪唑烷基羰基衍生物，作为钙离子通道调节剂有效。 构成：化学式1表示咪唑烷基羰基衍生物。化学式1的咪唑烷基羰基衍生物通过化学式3的哌嗪衍生物与化学式2的咪唑基烷基羧酸的酰胺键进行制备。酰胺键使用选自鏻 系统，铵系统，碳二亚胺系统，咪唑啉鎓和有机膦系统。 制备化学式2的咪唑基烷基羧酸的方法包括：在KF / Al 2 O 3催化剂存在下，进行异丁烯酸乙酯与咪唑化合物的异迈克尔加成反应，生成化学式2a的乙氧基羰基烷基咪唑化合物的步骤; 以及水解化学式2a的乙氧基羰基烷基咪唑化合物以制备化学式2的咪唑基烷基羧酸的步骤。
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公开(公告)号：KR100917037B1
公开(公告)日：2009-09-10
申请号：KR1020070111220
申请日：2007-11-01
Applicant: 한국과학기술연구원
IPC: C07D401/12 , C07D401/14
Abstract: 본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제-
公开(公告)号：KR1020090084150A
公开(公告)日：2009-08-05
申请号：KR1020080010156
申请日：2008-01-31
Applicant: 한국과학기술연구원
IPC: A61K31/522 , A61P9/10 , A61P13/10 , A61P25/00
CPC classification number: A61K31/522
Abstract: A composition for suppressing an inositol 1,4,5-triphosphate receptor subtype III is provided to prevent and treat diseases which is related to calcium ion release. An agent for suppressing a subtype III of inositol-1,4,5-triphosphate receptor comprises one or more among a group of caffeine, 7-isopropyl theophylline, 7-(beta-hydroxyethyl)theophyline, xanthenes, theophyline, 1,7-dimethyl-3-isobutyl xantene and their pharmaceutically allowable salt as active ingredient. A composition for preventing and treating diseases which is related to calcium ion excessive release comprises one or more among caffeine, 7-isopropyl theophyline, 7-(beta-hydroxyethyl)theopyline, xanthene, theophyline, 1,7-dimethyl-3-isobutyl xanthenes and their pharmaceutically allowable salt as active ingredient. The diseases related to calcium ion excessive release is one of stroke, anxiety, hyper sensitive bladder salt, inflammatory bowel disease, irritable colon syndrome, interstitial colitis, head injury, migraine, chronic, the neuropathy nature or the acute pain, the stress disorder after drug or the alcoholism, the neurological failure, psychosis, somnopathy, phobia, compulsion, debit, and the depression, stroma, diabetes, cancer, the male sterilization, hypertension, pulmonary hypertension, cardiac arrhythmia, congestive heart failure, angina, the polycystic kidney disease [autosomal dominant polycystic kidney] and Duchenne muscular dystrophy (DMD).
Abstract translation: 提供抑制肌醇1,4,5-三磷酸受体亚型III的组合物，以预防和治疗与钙离子释放有关的疾病。 用于抑制肌醇-1,4,5-三磷酸受体亚型III的药剂包括一组咖啡因，7-异丙基茶碱，7-（β-羟乙基）茶碱，呫吨酮，茶碱， 二甲基-3-异丁基呫吨及其药学上允许的盐作为活性成分。 用于预防和治疗与钙离子过度释放有关的疾病的组合物包括咖啡因，7-异丙基茶碱，7-（β-羟乙基）麻黄碱，呫吨，茶碱，1,7-二甲基-3-异丁基呫吨的一种或多种 及其药学上可允许的盐作为活性成分。 与钙离子过度释放相关的疾病是中风，焦虑，超敏性膀胱盐，炎性肠病，肠易激综合征，间质性结肠炎，头部损伤，偏头痛，慢性，神经病变或急性疼痛，紧张性疾病 药物或酒精中毒，神经系统衰竭，精神病，睡眠障碍，恐惧症，强迫性，借贷和抑郁症，基质，糖尿病，癌症，男性绝育，高血压，肺动脉高压，心律失常，充血性心力衰竭，心绞痛，多囊肾 疾病[常染色体显性多囊肾]和杜氏肌营养不良症（DMD）。
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Patent Agency Ranking86.发明授权이미다졸리움염에 고정화된 오스뮴 촉매와 키랄 리간드를 이용한 이웃한 키랄 다이올 화합물의 제조 방법 및 촉매회수 방법 失效使用锇催化剂和固定在咪唑鎓盐上的手性配体制备邻位手性二醇化合物的方法，并回收锇催化剂和手性配体
公开(公告)号：KR100528175B1
公开(公告)日：2005-11-15
申请号：KR1020030024334
申请日：2003-04-17
Applicant: 한국과학기술연구원
IPC: C07C29/74
CPC classification number: Y02P20/584
Abstract: 본 발명은 오스뮴 촉매를 사용하는 비대칭 다이히드록시화반응 (asymmetric dihydroxylation, AD라 약칭함)을 이용하여 올레핀 화합물로부터 이웃한 키랄 다이올(vicinal chiral diol)화합물을 제조하는 방법에 관한 것으로서, 1) 용매에 하기 화학식 1 또는 화학식 2의 키랄 리간드, 하기 화학식 3의 이미다졸리움염, 오스뮴 촉매를 넣고 교반한 후 여기에 보조산화제와 올레핀 화합물을 가하고 교반하는 단계(단계 1); 2) 모든 휘발성 물질을 감압하에서 제거하는 단계(단계 2); 3) 휘발성 물질이 제거된 잔류물을 유기용매로 추출하는 단계(단계 3); 및 4) 추출된 유기 용매층으로부터 이웃한 키랄 다이올 화합물을 분리하는 단계(단계 4)로 이루어지는 오스뮴 촉매를 이용하여 올레핀 화합물로부터 이웃한 키랄 다이올 화합물을 제조하는 방법에 관한 것이다. 본 발명은 오스뮴 촉매와 키랄 리간드를 이미다졸리움염에 고정시킴으로써 고가의 오스뮴 촉매 및 키랄 리간드를 용이하게 회수하고 재사용할 수 있어 매우 경제적이고 유용하며, 광학 순도가 높은 광학활성을 지닌 이웃한 키랄 다이올 화합물을 고수율로 제조할 수 있다.
[화학식 1]
[화학식 2]
(상기 화학식 1과 화학식 2는 각각 퀴니딘과 퀴닌의 히드록시기의 수소원자가 치환된 유도체로서 서로 유사 거울상 이성질체임)
[화학식 3]
(상기 식에서, R
1 , R
2 , R
3 , R
4 , R
5 , n 및 A는 명세서 내에서 정의한 바와 같음)-
公开(公告)号：KR1020050028392A
公开(公告)日：2005-03-23
申请号：KR1020030064579
申请日：2003-09-17
Applicant: 한국과학기술연구원
IPC: C07C2/22
Abstract: A process is provided to produce alkenylated aromatic compounds at a rapid velocity in a high selectivity and a high yield by a Friedel-Crafts alkenylation using a Lewis acid catalyst in the presence of an imidazolium salt. The used Lewis acid catalyst can be separated easily from the produced alkenylated aromatic compounds. The alkenylated aromatic compounds are represented by the formula 1 and are produced by the process containing the steps of: stirring an aromatic compound, an alkyne compound, the imidazolium salt represented by the formula 2, and the Lewis acid catalyst represented by the formula 3: M^n+(B^-)n; separating an organic layer containing the alkenylated aromatic compounds from the imidazolium salt layer containing the Lewis acid catalyst; separating the alkenylated aromatic compounds from the organic layer and refining. In the formula 1, each of R1 and R2 is hydrogen, an alkyl, an aryl and arene is an aromatic compound containing a heteroaromatic compound. In the formula 2, R1 is a C1-C18 alkyl, R2 to R5 are hydrogen or C1-C18 alkyl groups, n is an integer of 1-3, and A is a salt-formable anion. In the formula 3, M is a 3 group, 4 group, 11 group, 12 group, 13 group, 14 group, 15 group element or a lanthanide metal, n is an integer of 2-5, and B is X^-, R6O^- or R7R8N^-.
Abstract translation: 提供了一种通过使用路易斯酸催化剂在咪唑鎓盐存在下，通过Friedel-Crafts烯化反应以快速速度以高选择性和高产率制备烯基化芳族化合物的方法。 使用的路易斯酸催化剂可以容易地从所制备的链烯基芳族化合物中分离出来。 链烯基芳族化合物由式1表示，并通过包括以下步骤的方法制备：将芳族化合物，炔化合物，式2所示的咪唑盐和由式3表示的路易斯酸催化剂： M 1的n +（B ^ - ）n表示 从含有路易斯酸催化剂的咪唑盐层中分离含有烯基化芳族化合物的有机层; 将烯基化芳族化合物与有机层分离并精制。 在式1中，R 1和R 2各自为氢，烷基，芳基和芳烃为含有杂芳族化合物的芳族化合物。 在式2中，R 1为C 1 -C 18烷基，R 2至R 5为氢或C 1 -C 18烷基，n为1-3的整数，A为可成盐阴离子。 式3中，M为3组，4组，11组，12组，13组，14组，15组或镧系金属，n为2-5的整数，B为X ^ - ， R6O - 或R7R8N - 。
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公开(公告)号：KR100476584B1
公开(公告)日：2005-03-17
申请号：KR1020020038928
申请日：2002-07-05
Applicant: 한국과학기술연구원
IPC: C07D207/09
Abstract: 본 발명은 하기 화학식 1로 표시되는 고분자에 결합된 키랄 피롤리디닐(비스포스피노다이아미드) 유도체, 그의 제조방법 및 용도에 관한 것으로, 하기 화합물은 팔라듐과 킬레이트화 반응을 통하여 비대칭 알릴 치환반응 (asymmetric allylic substitution reaction)의 키랄 촉매로 사용되어 광학적 순도가 높은 화합물을 고수율로 제조할 수 있고, 반응 후 용이하게 회수가 가능한 특징이 있다.
화학식 1
(상기식에서,
ⓟ는 모두 명세서내 기재된 바와 같으며, 수소원자(1)과 수소원자(2)는 서로 트랜스의 위치에 있다.)-
公开(公告)号：KR1020040004861A
公开(公告)日：2004-01-16
申请号：KR1020020038928
申请日：2002-07-05
Applicant: 한국과학기술연구원
IPC: C07D207/09
Abstract: PURPOSE: A chiral pyrolidinyl(bisphosphinodiamide) derivative useful for asymmetric allylic substitution reaction is provided. The compound is used as a chiral catalyst in asymmetric allylic substitution reaction to produce a high optical purity compound in higher yield and is easily recovered after the reaction. CONSTITUTION: A chiral pyrolidinyl(bisphosphinodiamide) derivative of the formula(1) useful for asymmetric allylic substitution reaction is provided, wherein P is polystyrene, JANDAJEL(TM) polymer; hydrogen(1) and hydrogen(2) are positioned at a trans position each other; and the compound of the formula(1) comprises mirror image isomers represented by formulas(1a and 1b). A method for preparing the chiral pyrolidinyl(bisphosphinodiamide) derivative of the formula(1) comprises reacting a compound of the formula(2) with a compound of the formula(3), wherein Z is halogen.
Abstract translation: 目的：提供可用于不对称烯丙基取代反应的手性吡咯烷基（二膦基二酰胺）衍生物。 该化合物用作不对称烯丙基取代反应中的手性催化剂以产生更高收率的高光学纯度化合物，并且在反应后容易回收。 构成：提供了可用于不对称烯丙基取代反应的式（1）的手性吡咯烷基（二膦基二酰胺）衍生物，其中P是聚苯乙烯，JANDAJEL TM聚合物; 氢（1）和氢（2）彼此位于反位; 并且式（1）的化合物包括由式（1a和1b）表示的镜像异构体。 制备式（1）的手性吡咯烷基（二膦基二酰胺）衍生物的方法包括使式（2）的化合物与式（3）的化合物反应，其中Z是卤素。
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公开(公告)号：KR100275785B1
公开(公告)日：2001-02-01
申请号：KR1019980003408
申请日：1998-02-06
Applicant: 한국과학기술연구원
IPC: C07D205/08
Abstract: PURPOSE: Provided are a preparation method of (3R,4S)-hydroxy-4-phenylazetidine-2-one and its intermediate, represented by formula(1), wherein the intermediate is a vital intermediate in the synthesis of taxane based anti-cancer agents. The method provides optically pure compound of the formula(1) in high yield. CONSTITUTION: The method of preparation comprises: reacting trans-cinnamamide derivatives(formula 5) with unsymmetric dihydroxy catalyst to obtain (2R,2S)-2,3-dihydroxy-3-phenylpropionamide derivative(formula 6); halocarboxylating the above compound(formula 6) to prepare (2R,2S)-2-carboxy-3-halo-3-phenylpropionamide derivative(formula 8); reacting the above compound(formula 8) with base in a non protonic solvent to manufacture (3R,4S)-3-carboxy-4-phenylazetidine-2-one derivative(formula 10); reacting the above compound(formula 10) with oxidant in the organic solvent to manufacture (3R,4S)-3-carboxy-4-phenylazetidine-2-one derivative(formula 11); and hydrolyzing number 3 carbon atom of the above compound(formula 11) to manufacture the title compound(formula 1).
Abstract translation: 目的：提供式（1）表示的（3R，4S） - 羟基-4-苯基氮杂环丁烷-2-酮及其中间体的制备方法，其中中间体是合成基于紫杉烷的抗癌药物中的重要中间体 代理商。 该方法以高产率提供式（1）的光学纯的化合物。 构成：制备方法包括：使反式肉桂酰胺衍生物（式5）与不对称二羟基催化剂反应，得到（2R，2S）-2,3-二羟基-3-苯基丙酰胺衍生物（式6）; 卤代羧化上述化合物（式6）以制备（2R，2S）-2-羧基-3-卤代-3-苯基丙酰胺衍生物（式8）; 使上述化合物（式8）与非质子溶剂中的碱反应制备（3R，4S）-3-羧基-4-苯基氮杂环丁烷-2-酮衍生物（式10）。 将上述化合物（式10）与氧化剂在有机溶剂中反应制备（3R，4S）-3-羧基-4-苯基氮杂环丁烷-2-酮衍生物（式11）; 并水解上述化合物（式11）的3个碳原子以制备标题化合物（式1）。
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