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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：KR101084734B1
公开(公告)日：2011-11-22
申请号：KR1020090010234
申请日：2009-02-09
Applicant: 한국과학기술연구원
IPC: C07D307/90 , C07D307/93
Abstract: 본 발명은 옥사스파이로 화합물 및 이 화합물의 제조방법에 관한 것으로서, 더욱 상세하게는 메틸렌사이클로알칸다이올 유도체와 카르보 화합물을 출발물질로 사용하여 루이스산 존재하에서 프린스 고리화 반응 및 알킬 자리 옮김 반응을 동시에 수행하여 제조된 하기 화학식 1로 표시되는 신규 옥사스파이로 화합물과 이 화합물의 제조방법에 관한 것이다.
상기 화학식 1에서, R
1
및 R
2 는 각각 수소원자; C
1 -C
6 의 알킬기; 또는 할로겐, 니트로, C
1 -C
6 의 알킬, 및 C
1 -C
6 의 알콕시 중에서 선택된 1 내지 3개의 치환체로 치환 또는 비치환된 페닐기를 나타내고, 또한 R
1
및 R
2 는 서로 결합하여 5각형 내지 7각형의 지방족 또는 방향족 고리를 형성할 수 있고, n은 0, 1 또는 2를 나타낸다.
옥사스파이로 화합물, 프린스 반응, 알킬 자리 옮김 반응-
公开(公告)号：KR1020110119045A
公开(公告)日：2011-11-02
申请号：KR1020100038514
申请日：2010-04-26
Applicant: 한국과학기술연구원
IPC: C07D241/04 , A61K31/495 , A61P25/08 , A61P9/12
CPC classification number: Y02P20/55
Abstract: PURPOSE: A diphenylpropanoyl compound having T-type calcium channel activity is provided to ensure antagonism to a T-type calcium channel and to be used as a therapeutic agent and anticancer agent. CONSTITUTION: A diphenylpropanoyl is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating hypertension, angina, chronic pain, neurogenic pain or cancer contains a compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of binding a compound of chemical formula 2 with a compound of chemical formula 3.
Abstract translation: 目的：提供具有T型钙通道活性的二苯基丙酰基化合物，以确保对T型钙通道的拮抗作用，并用作治疗剂和抗癌剂。 构成：二苯基丙酰基由化学式1表示。用于预防和治疗高血压，心绞痛，慢性疼痛，神经源性疼痛或癌症的药物组合物含有化学式1化合物作为活性成分。 制备化学式1的化合物的方法包括将化学式2的化合物与化学式3的化合物结合的步骤。
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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：KR101035712B1
公开(公告)日：2011-05-19
申请号：KR1020090053364
申请日：2009-06-16
Applicant: 한국과학기술연구원
IPC: C07D493/04 , C07D493/02
Abstract: 본 발명은 1,6-디옥세케인 화합물과 이의 제조방법에 관한 것으로서, 더욱 상세하게는 알렌닐 알코올 또는 알릴 알코올 화합물을 알데하이드 화합물과 루이스산 존재하에서 프린스 고리화 반응을 수행하여 제조된 하기 화학식 1로 표시되는 1,6-디옥세케인 화합물과 이 화합물의 제조방법에 관한 것이다.
상기 화학식 1에서, R은 탄소수 5 내지 15의 아릴기, 또는 질소, 산소 및 황 원자 중에서 선택된 헤테로원자가 1 내지 3개 포함된 탄소수 5 내지 15의 헤테로아릴기를 나타내며; n은 0 또는 1을 나타낸다.
1,6-디옥세케인, 알렌닐 알코올, 알릴 알코올, 루이스산, 프린스반응-
Patent Agency Ranking
公开(公告)号：KR1020110038903A
公开(公告)日：2011-04-15
申请号：KR1020090096094
申请日：2009-10-09
Applicant: 한국과학기술연구원
IPC: C07D207/14 , C07D207/09 , A61K31/4985 , A61P25/24
CPC classification number: C07C311/18 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D211/14 , C07D295/13 , C07D409/12
Abstract: PURPOSE: A sulfonamide compound and pharmaceutically acceptable salt thereof are provided to be used as an agent for preventing and treating central nervous system(CNS)-related diseases. CONSTITUTION: A sulfonamide derivative is denoted by chemical formula 1. A pharmaceutical composition contains the sulfonamide derivative and pharmaceutically acceptable salt thereof as an active ingredient. The composition is used for treating depression, obesity, psychosis, suicidal tendency, anxiety, appetite disorders, or sleep disorders. A method for preparing the sulfonamide compounds comprises: a step of performing reductive amination of a carbonyl compound of chemical formula 2 with primary amine compound of chemical formula 3 to prepare a secondary amine compound of chemical formula 4; and a step of performing sulfonization of the secondary amine compound of chemical formula 4 with a sulfonyl halide compound of chemical formula 5 to prepare a sulfonamide compound of chemical formula 1.
Abstract translation: 目的：提供磺酰胺化合物及其药学上可接受的盐作为预防和治疗中枢神经系统（CNS）相关疾病的药物。 构成：磺酰胺衍生物由化学式1表示。药物组合物含有磺酰胺衍生物及其药学上可接受的盐作为活性成分。 该组合物用于治疗抑郁症，肥胖症，精神病，自杀倾向，焦虑症，食欲障碍或睡眠障碍。 制备磺酰胺化合物的方法包括：用化学式3的伯胺化合物进行化学式2的羰基化合物的还原胺化以制备化学式4的仲胺化合物的步骤; 用化学式5的磺酰卤化合物对化学式4的仲胺化合物进行磺化以制备化学式1的磺酰胺化合物的步骤。
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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：KR1020090087732A
公开(公告)日：2009-08-18
申请号：KR1020080013153
申请日：2008-02-13
Applicant: 한국과학기술연구원
IPC: C07D311/26 , C07D311/22 , C07D311/28
Abstract: A method for producing a 1-(2-hydroxyphenyl)buta-2-en-1-one or cromene-4-one derivative is provided to simply synthesize and use as an intermediate of novel medicine. A 1-(2-hydroxyphenyl)buta-2-en-1-one derivative of the chemical formula 1 or cromene-4-one derivative of the chemical formula 2 is produced by reacting derivative of the chemical formula 3 and aldehyde derivative of the chemical formula 4 under the presence of lewis acid catalyst. In the chemical formulas, R1 is hydrogen atom, C1-C10 alkyl group, C5-C15 aryl group or C1-C10 alkyl silyl group, R2 is hydrogen atom, C1-C10 alkyl group or C5-C15 aryl group.
Abstract translation: 提供1-（2-羟基苯基）丁-2-烯-1-酮或色烯-4-酮衍生物的制备方法，简单地合成并用作新药的中间体。 化学式1的1-（2-羟基苯基）丁-2-烯-1-酮衍生物或化学式2的色烯-4-酮衍生物通过使化学式3的衍生物与 化学式4在路易威酸催化剂存在下。 在化学式中，R 1是氢原子，C 1 -C 10烷基，C 5 -C 15芳基或C 1 -C 10烷基甲硅烷基，R 2是氢原子，C 1 -C 10烷基或C 5 -C 15芳基。
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200.发明授权세로토닌 수용체 5-ＨＴ2ａ 또는 5-ＨＴ2ｃ의 길항제로활성을 갖는 1,2-다이하이드로-1-옥소프탈라지닐 피페라진화합물 및 이의 제조방법 失效具有生物活性的新的1,2-二氢-1-氧代乙酰胆碱衍生物对硒酸受体5-HT2A和5-HT2C的生物活性及其制备
公开(公告)号：KR100843352B1
公开(公告)日：2008-07-03
申请号：KR1020070009627
申请日：2007-01-30
Applicant: 한국과학기술연구원 , 주식회사 디비하이텍
IPC: C07D401/12 , A61K31/502
CPC classification number: C07D237/32
Abstract: A 1,2-dihydro-1-oxophthalazinyl piperazine derivative is provided to show selective antagonistic activity on serotonin 5-HT2a or 5-HT2c receptor, thereby being used for a pharmaceutical composition for treating and preventing central nervous system diseases. A 1,2-dihydro-1-oxophthalazinyl piperazine derivative is represented by a formula(1) and is prepared by reacting an amine compound represented by a formula(2) with a carboxylic acid compound represented by a formula(3). In the formulae, R1 is H, halogen, C1-10 alkyl, C1-10 alkoxy, phenyl, pyridyl or pyrimidyl; R2 is aryl selected from the group consisting of phenyl, pyridyl and pyrimidyl which may be substituted or unsubstituted by a substituent selected from the group consisting of halogen, nitro, C1-10 alkyl, C1-10 haloalkyl, C1-10 alkoxy, C1-10 haloalkoxy, and C1-6 acyl; and n is an integer from 0 to 5. A pharmaceutical composition for treating and preventing diseases such as anxiety, depression, stroke, obsessive neurosis, psychosis, schizophrenia, suicidal tendency, sleep disorders, appetite disorders, withdrawal symptoms caused by drug abuse, and migraine comprises the 1,2-dihydro-1-oxophthalazinyl piperazine derivative represented by the formula(1) or a pharmaceutically acceptable salt thereof.
Abstract translation: 提供1,2-二氢-1-氧酞嗪哌嗪衍生物以显示对5-羟色胺5-HT2a或5-HT2c受体的选择性拮抗活性，从而用于治疗和预防中枢神经系统疾病的药物组合物。 1,2-二氢-1-氧代吖嗪基哌嗪衍生物由式（1）表示，通过使由式（2）表示的胺化合物与由式（3）表示的羧酸化合物反应制备。 式中，R 1为H，卤素，C 1-10烷基，C 1-10烷氧基，苯基，吡啶基或嘧啶基; R 2是选自苯基，吡啶基和嘧啶基的芳基，其可以被选自卤素，硝基，C 1-10烷基，C 1-10卤代烷基，C 1-10烷氧基，C 1-10烷氧基， 10个卤代烷氧基和C1-6酰基; n为0〜5的整数。用于治疗和预防焦虑，抑郁，中风，强迫神经症，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍，药物滥用引起的戒断症状的药物组合物，以及 偏头痛包含由式（1）表示的1,2-二氢-1-氧代嗪嗪哌嗪衍生物或其药学上可接受的盐。
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