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公开(公告)号：KR1020120097288A
公开(公告)日：2012-09-03
申请号：KR1020110016788
申请日：2011-02-24
Applicant: 한국과학기술연구원
IPC: C07D403/12 , C07D403/14 , A61K31/551 , A61P25/00
Abstract: PURPOSE: A pharmaceutical composition containing 1,4-diazepane pyrazole compound and a pharmaceutically acceptable salt thereof is provided to be used as an agent for preventing or treating brain diseases, heart diseases, cancer, epilepsy, and pain. CONSTITUTION: A 1,4-diazepane pyrazole compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases such as epilepsy, depression, Parkinson's diseases, dementia, sleep disorders, or heart diseases such as hypertension, cardiac arrhythmia, or myocardial infarction, or pain contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of reacting pyrazolemethyl amine of chemical formula 2 with chloroacetyl chloride.
Abstract translation: 目的：提供含有1,4-二氮杂环庚烷吡唑化合物及其药学上可接受的盐的药物组合物，用作预防或治疗脑疾病，心脏病，癌症，癫痫和疼痛的药剂。 构成：1,4-二氮杂环庚烷吡唑化合物由化学式1表示。用于预防和治疗脑疾病如癫痫，抑郁症，帕金森病，痴呆，睡眠障碍或心脏病如高血压，心律失常， 或心肌梗塞，或疼痛含有化学式1的化合物作为活性成分。 制备化学式1的化合物的方法包括使化学式2的吡唑甲胺与氯乙酰氯反应的步骤。
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公开(公告)号：KR1020120097287A
公开(公告)日：2012-09-03
申请号：KR1020110016787
申请日：2011-02-24
Applicant: 한국과학기술연구원
IPC: C07D401/12 , A61K31/454 , A61P25/00
Abstract: PURPOSE: A pharmaceutical composition containing pyrazoyl piperidine compounds and pharmaceutically acceptable salt thereof is provided to prevent or treat brain diseases, heard diseases, cancer, and pain. CONSTITUTION: A pyrazoyl piperidine compound is denoted by chemical formula 1. A pharmaceutical composition for treating cerebral diseases, cardiac diseases, cancer, or pain contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound comprises: a step of reacting piperidine acetate of chemical formula 2 and pyrazole methyl amine of chemical formula 3 of a step of reacting piperidine compound of chemical formula 4 with an aldehyde compound of chemical formula 5 by reduction-amination. [Reference numerals] (AA) Reductive amination
Abstract translation: 目的：提供含有吡唑基哌啶化合物及其药学上可接受的盐的药物组合物，以预防或治疗脑疾病，听到疾病，癌症和疼痛。 构成：化学式1表示吡唑基哌啶化合物。用于治疗脑疾病，心脏病，癌症或疼痛的药物组合物含有化学式1的化合物作为活性成分。 制备该化合物的方法包括：使化学式2的哌啶乙酸酯与化学式3的吡唑甲胺与化学式4的哌啶化合物与化学式5的醛化合物的还原胺化反应的步骤。 （参考号）（AA）还原胺化
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公开(公告)号：KR101152659B1
公开(公告)日：2012-06-15
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: 본 발명은 세로토닌 수용체 억제 작용과 세로토닌 트랜스포터 (Serotonin transporter)에 대한 억제 작용을 동시에 가지는 설폰아마이드 화합물과 이의 약제학적으로 허용 가능한 염에 관한 것이다.
본 발명이 특징으로 하는 설폰아마이드 화합물은 세로토닌 5-HT
2A 수용체 길항 작용과 세로토닌 트랜스포터 억제 작용을 가지므로 우울증, 비만, 정신병(psychosis), 정신분열증, 자살성향(suicidal tendency), 불안증(anxiety), 강박노이로제, 편두통, 식욕부진(appetite disorders), 수면장애(sleep disorders), 발작, 약물남용에 의한 금단증상 등 중추신경계(CNS)에 관련된 질환의 예방 및 치료제로 유용하다.
설폰아마이드 화합물, 세로토닌, 5-HT2A/5-HT2C, SSRI, 중추신경계, 우울증, 비만-
公开(公告)号：KR101152657B1
公开(公告)日：2012-06-05
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: 본발명은 T-형칼슘채널에대한활성을갖는다이페닐프로판노일화합물, 상기화합물의제조방법, 그리고상기화합물을유효성분으로포함하는약학조성물에관한것이다. 본발명의다이페닐프로판노일화합물또는약학적으로허용가능한이의염은 T-형칼슘채널에대한길항작용을가지므로간질, 고혈압등의뇌질환치료제, 협심증등의심장질환치료제, 만성통증, 신경성통증등의통증질환치료제, 또는항암제로유용하다.
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35.发明公开
公开(公告)号：KR1020120056078A
公开(公告)日：2012-06-01
申请号：KR1020100117602
申请日：2010-11-24
Applicant: 한국과학기술연구원
IPC: C07D413/10 , A61K31/422 , A61P31/04
CPC classification number: Y02A50/473 , Y02A50/481
Abstract: PURPOSE: An antibacterial composition containing novel oxazolidinone derivative is provided to ensure antibacterial activity against gram positive bacteria. CONSTITUTION: A novel oxazolidinone derivative with antibacterial activity is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 or the salt thereof comprises: a step of reacting an amine group of a compound of chemical formula 2 with a compound of chemical formula 3 or 4; and a step of substituting a hydroxyl group of an oxazolidinone derivative or a pharmaceutically acceptable salt thereof with a halogen group or methoxy group. An antibacterial composition contains the oxazolidinone derivative of chemical formula 1 or a salt thereof as an active ingredient.
Abstract translation: 目的：提供含有新恶唑烷酮衍生物的抗菌组合物，以确保对革兰氏阳性菌的抗菌活性。 构成：具有抗菌活性的新型恶唑烷酮衍生物由化学式1表示。化学式1化合物或其盐的制备方法包括：使化学式2的化合物的胺基与 化学式3或4; 以及将恶唑烷酮衍生物或其药学上可接受的盐的羟基与卤素基或甲氧基取代的步骤。 抗菌组合物含有化学式1的恶唑烷酮衍生物或其盐作为活性成分。
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Patent Agency Ranking36.发明公开1,6-이치환-3-아미노-4,5,6,7-테트라하이드로-1Ｈ-피라졸로［3,4-ｃ］피리딘-7-온 화합물 및 이 화합물의 제조방법 有权新的1,6-二异丙基氨基-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备方法
公开(公告)号：KR1020110139988A
公开(公告)日：2011-12-30
申请号：KR1020100060138
申请日：2010-06-24
Applicant: 한국과학기술연구원
IPC: C07D471/04 , C07D403/02 , A61K31/437 , A61P35/00
CPC classification number: C07D471/04
Abstract: PURPOSE: A novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one is provided to suppress cancer cells. CONSTITUTION: A 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one compound is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of alkylating 3-amino compounds of chemical formula 2 with haloalkylcarbonyl piperazine of chemical formula 3 by alkylating.
Abstract translation: 目的：提供新颖的1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮以抑制癌细胞。 构成：1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物由化学式1表示。用于抗癌的药物组合物含有化合物 的化学式1或其药学上可接受的盐作为活性成分。 制备化学式1的化合物的方法包括通过烷基化将化学式2的3-氨基化合物与化学式3的卤代烷基羰基哌嗪烷基化的步骤。
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37.发明公开3,6-이치환-4,5,6,7-테트라하이드로-1Ｈ-피라졸로［3,4-ｃ］피리딘-7-온 화합물과 이 화합물의 제조방법 有权新的3,6-取代-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备方法
公开(公告)号：KR1020110121868A
公开(公告)日：2011-11-09
申请号：KR1020100041360
申请日：2010-05-03
Applicant: 한국과학기술연구원 , 서울대학교산학협력단
IPC: C07D471/02 , C07D487/04 , A61P35/00 , A61K31/437
Abstract: PURPOSE: A novel 3,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound is provided to suppress cancer cell and to be used as an anticancer agent. CONSTITUTION: A 3,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises: a step of performing acrylation of 3-amino compound of chemical formula 2 with acyl halide compound of chemical formula 3 to prepare 3-haloacylcarbamoyl compound of chemical formula 4; and a step of substituting 3-haloacylcarbamoyl compound of chemical formula 4 with amine compounds of chemical formula 5.
Abstract translation: 目的：提供新的3,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物以抑制癌细胞并用作抗癌剂 。 构成：3,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮由化学式1表示。用于抗癌的药物组合物含有 化学式1为活性成分。 制备化学式1化合物的方法包括：用化学式3的酰卤化合物进行化学式2的3-氨基化合物的丙烯酸化以制备化学式4的3-卤代酰基氨基甲酰基化合物的步骤; 和用化学式5的胺化合物代替化学式4的3-卤代酰基氨基甲酰基化合物的步骤。
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38.发明授权신규 페닐아세테이트 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 Ｔ-형 칼슘 이온 채널의 활성에 의해 유발되는 질환의 예방 또는 치료용 조성물 有权新苯乙酸衍生物或其药学上可接受的盐，它们的制备和组合物用于预防或治疗由含有作为活性成分的T-型钙通道的活性的疾病
公开(公告)号：KR101052620B1
公开(公告)日：2011-07-29
申请号：KR1020080084563
申请日：2008-08-28
Applicant: 한국과학기술연구원
Inventor： 신계정 , 이형국 , 노은주 , 배애님 , 서선희 , 백이연 , 김윤지 , 신희섭 , 김동진 , 최경일 , 임혜원 , 정혜진 , 남길수 , 조용서 , 추현아 , 한호규 , 강순방 , 신동윤 , 정찬성 , 김은경 , 정혜선 , 김기선 , 금교창 , 이철주 , 민선준 , 남기달 , 이재균 , 강용구 , 박웅서 , 김영수 , 최기현 , 송치만
IPC: C07D235/14 , C07D241/04
CPC classification number: C07D211/34 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D235/14 , C07D235/16 , C07D295/145 , C07D295/15
Abstract: 본 발명은 하기 화학식 1로 표시되는 신규 페닐아세테이트 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 T-형 칼슘 이온 채널의 활성에 의해 유발되는 질환의 예방 또는 치료용 조성물에 관한 것으로, 본 발명에 따른 페닐아세테이트 유도체를 함유하는 조성물은 T-형 칼슘 이온 채널 활성을 효과적으로 억제하므로 T-형 칼슘 이온 채널의 활성에 의해 유발되는 고혈압, 암, 간질, 신경성 통증 등의 질병의 예방 또는 치료제로서 유용하게 사용될 수 있다.
[화학식 1]
.
(상기 화학식 1에서, 상기 X, R
1 및 R
2 는 본 명세서에서 정의된 바와 같다.)
T-형 칼슘 채널 블로커, 페닐아세테이트 유도체, 통증치료제Abstract translation: 本发明的用于引起的新颖苯乙酸衍生物或其药学上可接受的盐，其含有与由下式表示的活性成分T-型钙离子通道的制备和活性的疾病的预防和治疗（1） 涉及一种组合物，含有本发明的苯基乙酸酯衍生物，例如组合物是T-型钙离子通道的活性，有效地抑制由T-型钙离子通道，高血压，癌症，癫痫，神经性疼痛的活化诱导这样 并且可以有用地用作疾病的预防或治疗剂。
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公开(公告)号：KR1020100134977A
公开(公告)日：2010-12-24
申请号：KR1020090053364
申请日：2009-06-16
Applicant: 한국과학기술연구원
IPC: C07D493/04 , C07D493/02
Abstract: PURPOSE: A method for preparing 1,6-dioxecane compound is provided to enlarge other ring by Diels-Alder reaction and to use as an intermediate. CONSTITUTION: A 1,6-Dioxecanes compound is denoted by chemical formula 1. The 1,6-Dioxecanes compound is prepared by Prins reaction of alcohol compound of chemical formula 2 and aldehyde compound of chemical formula 3. A tetrahydrofuran is used as a reaction catalyst. The reaction temperature is -78 to 30°C.
Abstract translation: 目的：提供1,1-二氧化合物的制备方法，以通过狄尔斯 - 阿尔德反应扩大其它环并用作中间体。 构成：1,6-二氧癸烷化合物由化学式1表示。1,6-二氧癸烷化合物通过化学式2的醇化合物与化学式3的醛化合物的Prins反应制备。使用四氢呋喃作为反应 催化剂。 反应温度为-78〜30℃。
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公开(公告)号：KR1020100063329A
公开(公告)日：2010-06-11
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: PURPOSE: A thiazoline compounds and a T-type calcium channel inhibitor containing the same are provided to treat diseases relating to T-type calcium channel overexpression. CONSTITUTION: A thiazoline compounds have a structure of chemical formula 1. A composition for preventing and treating diseases relating to T-type calcium channel overexpression contains the thiazoline compounds of chemical formula 1. The diseases are Parkinson's disease, Alzheimer, schizophrenia, somnopathy, pain, hypertension, arrhythmia, angina, cardiac insufficiency, myocardial infarction, or cancer.
Abstract translation: 目的：提供噻唑啉化合物和含有此类化合物的T型钙通道抑制剂，用于治疗与T型钙通道过度表达相关的疾病。 构成：噻唑啉化合物具有化学式1的结构。用于预防和治疗与T型钙通道过度表达有关的疾病的组合物含有化学式1的噻唑啉化合物。疾病为帕金森病，阿尔茨海默病，精神分裂症，睡眠障碍，疼痛 ，高血压，心律不齐，心绞痛，心功能不全，心肌梗塞或癌症。
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