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公开(公告)号：KR1020040026462A
公开(公告)日：2004-03-31
申请号：KR1020020057933
申请日：2002-09-24
Applicant: 한국과학기술연구원
IPC: C07D487/04
Abstract: PURPOSE: A pyrazolopyrimidine derivative as a cyclin-dependent kinase inhibitor and a process for preparing the same are provided. The compound inhibits cyclin-dependent kinase(CDK) regulating cell division cycle and has low toxicity. Therefore, it can be useful for prevention and treatment of liver cancer, breast cancer, stomach cancer, colon cancer or rectal cancer caused by activation of CDK. CONSTITUTION: A pyrazolopyrimidine derivative is represented by the formula(1), wherein R1 comprises ortho, meta, or para substituent, and is bromo, chloro, fluoro, methoxy, hydrogen, nitro or amino; R2 is hydrogen or C3 or less of lower alkyl; R3 is hydrogen or C3 or less of lower alkyl, or hydroxyethyl; and n is an integer of 0 or 1. A method for preparing the pyrazolopyrimidine derivative represented by the formula(1) comprises the steps of: reacting 6-methylmercaptopyrazolopyrimidine of the formula(IV) with meta-chloroperbenzoic acid in the presence of an organic solvent such as chloroform or dichloromethane at -10 to 10 deg. C for 2 to 5 hours and at room temperature for 3 to 12 hours to prepare 6-methylsulfonylpyrazolopyrimidine of the formula(II); and nucleophilic substitution reaction of 6-methylsulfonylpyrazolopyrimidine of the formula(II) with hydroxyethylamine in the presence of a mixed organic solvent of isopropanol or n-butanol and dimethylsulfoxide or dimethylformamide at 70 to 100 deg. C for 1 to 6 hours.
Abstract translation: 目的：提供作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶衍生物及其制备方法。 该化合物抑制细胞周期蛋白依赖性激酶（CDK）调节细胞分裂周期，毒性低。 因此，可用于预防和治疗由CDK激活引起的肝癌，乳腺癌，胃癌，结肠癌或直肠癌。 构型：吡唑并嘧啶衍生物由式（1）表示，其中R 1包括邻，间或对位取代基，并且是溴，氯，氟，甲氧基，氢，硝基或氨基; R2是氢或C3以下的低级烷基; R3是氢或C3以下的低级烷基或羟乙基; 并且n是0或1的整数。由式（1）表示的吡唑并嘧啶衍生物的制备方法包括以下步骤：使式（Ⅳ）的6-甲基巯基吡唑并嘧啶与间氯过苯甲酸在有机 溶剂如氯仿或二氯甲烷在-10至10℃。 C化2〜5小时，在室温下反应3〜12小时，得到式（II）的6-甲基磺酰基吡唑并嘧啶; 和式（II）的6-甲基磺酰基吡唑并嘧啶与异丙醇或正丁醇和二甲基亚砜或二甲基甲酰胺的混合有机溶剂在70-100℃下与羟乙基胺的亲核取代反应。 C 1〜6小时。
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公开(公告)号：KR1020020003789A
公开(公告)日：2002-01-15
申请号：KR1020000038284
申请日：2000-07-05
Applicant: 한국과학기술연구원
IPC: C07D477/10
CPC classification number: C07D477/20 , C07D413/06 , C07D417/06
Abstract: PURPOSE: Provided are novel 1 β-Methylcarbapenem derivatives and their preparation process, which derivatives show stability to dihydropeptidase-I, and have antibacterial effects on both gram positive and gram negative bacteria. Thus, they are used as antibacterial agents. CONSTITUTION: Novel 1 β-Methylcarbapenem derivatives have substituted 5-(2-isoxazolyl ethenyl)pyrrolidine-3-thio or 5-(2-isothiazolyl ethenyl)pyrrolidine-3-thio group as a main functional group at 1-beta methylcarbapenem represented by the formula(1). A pharmaceutical composition for an antibacterial agent contains the 1 β-Methylcarbapenem derivatives, as active ingredients. In the formula(1), R is described as in the description and has cis- or trans stereomer, X is hydrogen, methoxycarbonyl, hydroxymethyl, methylaminomethyl, C1-C4 alkoxy or halogen atom, and Y is hydrogen or halogen atom.
Abstract translation: 目的：提供新型1型β-甲基碳青霉烯衍生物及其制备方法，该衍生物显示对二氢肽酶-I的稳定性，对革兰氏阳性菌和革兰氏阴性菌均具有抗菌作用。 因此，它们被用作抗菌剂。 构成：新型1β-甲基碳青霉烯衍生物具有取代的5-（2-异恶唑基乙烯基）吡咯烷-3-硫基或5-（2-异噻唑基乙烯基）吡咯烷-3-硫基作为主要官能团，以1-β甲基碳青霉烯为代表 公式（1）。 作为抗菌剂的药物组合物含有作为活性成分的1β-甲基碳青霉烯衍生物。 在式（1）中，R如说明书所述，具有顺式或反式立体异构体，X为氢，甲氧基羰基，羟甲基，甲基氨基甲基，C1-C4烷氧基或卤原子，Y为氢或卤素原子。
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公开(公告)号：KR1019930010504B1
公开(公告)日：1993-10-25
申请号：KR1019900015553
申请日：1990-09-28
Applicant: 한국과학기술연구원
IPC: C09B48/00
Abstract: The beta- or gamma-quinacridone is produced by (a) reacting a diethyl 1,4-dicyclohexanedione-2,5-dicarboxylate of formula (II) with an aniline in the presence of a solvent (toluene or xylene) having a low b.p. and a trifluoro acetic acid catalyst to obtain a diethyl 2,5-dianilino-3,6-dihydroterephthalate of formula (III), (b) reacting the cpd. of (III) in the presence of a xylene solvent at 310-320 deg.C for 1 hr in the high pressure reactor to obtain a beta- 6,13- dihydroquinacridone of formula (IV), and (c) reacting a lower alcohol (methanol or ethanol), a sodium hydroxide soln. and a meta-sodium nitrobenzene sulfonate with the cpd. of (IV).
Abstract translation: 通过（a）使式（II）的1,4-二环己烷二酮-2,5-二羧酸二乙酯与苯胺在溶剂（甲苯或二甲苯）存在下反应生成β-或γ-喹吖啶酮，所述溶剂（甲苯或二甲苯）具有低的沸点。 和三氟乙酸催化剂，得到式（III）的2,5-二苯胺基-3,6-二氢对苯二甲酸二乙酯，（b）使cpd反应。 的（III）在二甲苯溶剂存在下，在310-320℃下在高压反应器中反应1小时，得到式（IV）的β-6,13-二氢喹吖啶酮，和（c）使低级醇 （甲醇或乙醇），氢氧化钠溶胶。 和具有cpd的硝基苯磺酸钠。 的（Ⅳ）。
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Patent Agency Ranking
公开(公告)号：KR102063155B1
公开(公告)日：2020-01-08
申请号：KR1020180042031
申请日：2018-04-11
Applicant: 한국과학기술연구원
IPC: C07D405/12 , A61K31/506 , C07D405/14 , A61P35/00 , A61P25/28 , A61P25/16 , A61P29/00
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67.发明公开
公开(公告)号：KR1020130111082A
公开(公告)日：2013-10-10
申请号：KR1020120033590
申请日：2012-03-30
Applicant: 한국과학기술연구원
IPC: C07D413/12 , C07D307/86 , A61K31/421 , A61P25/00
CPC classification number: C07D413/12 , C07D307/81 , C07D405/12
Abstract: PURPOSE: An aminostyrylbenzofuran compound and a pharmaceutical composition containing the same are provided to prevent and treat neurodegenerative diseases caused by beta-amyloid fibrillation. CONSTITUTION: A compound is selected among an aminostyrylbenzofuran compound of chemical formula 1 and a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof. A pharmaceutical composition which suppresses beta-fibrillation contains the compound as an active ingredient. A pharmaceutical composition for preventing or treating neurodegenerative diseases contains the compound as an active ingredient. The neurodegenerative diseases are senile dementia, stroke, Parkinson's disease, Huntington's disease, or bovine spongiform encephalopathy.
Abstract translation: 目的：提供氨基苯乙烯基苯并呋喃化合物和含有它们的药物组合物，以预防和治疗由β-淀粉样蛋白原纤颤引起的神经变性疾病。 构成：化合物选自化学式1的氨基苯乙烯基苯并呋喃化合物及其药学上可接受的盐，异构体，水合物和溶剂合物。 抑制β-原纤维化的药物组合物含有作为活性成分的化合物。 用于预防或治疗神经变性疾病的药物组合物含有该化合物作为活性成分。 神经变性疾病是老年性痴呆，中风，帕金森病，亨廷顿氏病或牛海绵状脑病。
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公开(公告)号：KR101116756B1
公开(公告)日：2012-03-13
申请号：KR1020090102359
申请日：2009-10-27
Applicant: 한국과학기술연구원
IPC: C07D403/04 , C07D209/04 , A61K31/40 , A61P35/00
CPC classification number: C07D403/04 , A61K31/404 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
Abstract: 본 발명은 단백질 키나아제 저해활성을 갖는 1,6-치환된 인돌 화합물, 이의 약학적으로 허용 가능한 염, 그리고 이 화합물을 유효성분으로 함유하는 비정상 세포 성장으로 유발되는 종양질환의 예방 및 치료용 약학적 조성물에 관한 것이다.
본 발명의 신규 인돌 화합물은 성장 인자 신호 전달에 관여하는 다양한 단백질 키나아제에 대하여 우수한 억제 효과를 나타내므로, 이들 단백질 키나아제에 의해 유발되는 종양 질환의 예방 및 치료제로서 유용하다.
인돌, 단백질, 키나아제, 억제제, 비정상 세포 성장 질환-
公开(公告)号：KR101074025B1
公开(公告)日：2011-10-17
申请号：KR1020080094366
申请日：2008-09-25
Applicant: 한국과학기술연구원
IPC: C07D513/04
CPC classification number: C07D513/04 , C07D498/04
Abstract: 식중에서, A, R, R및 R은명세서중에정의한바와같다.
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70.发明授权
公开(公告)号：KR101068835B1
公开(公告)日：2011-09-30
申请号：KR1020070108420
申请日：2007-10-26
Applicant: 한국과학기술연구원
IPC: C07D209/48 , A61K31/4035 , A61P25/28
CPC classification number: C07D209/46 , C07D209/48
Abstract: 본 발명은 베타-아밀로이드 피브릴(
beta -amyloid fibril)에 우수한 결합 친화도를 나타내어 치매를 비롯한 퇴행성 뇌질환의 조기 진단과, 이들 질환의 예방 및 치료에 유용한 하기 화학식 1로 표시되는 이소인돌론(isoindolone) 화합물, 이의 제조 방법 및 이를 포함하는 약학적 조성물에 관한 것이다.
[화학식 1]
식 중에서, A는 C=O 또는 CH
2 기이고, R
1 은 H, OH, 불소, 염소, 브롬 및 요오드 중에서 선택되는 할로겐 원자, C
1 ∼C
8
알킬기, C
1 ∼C
8
알콕시기, 토실옥시-C
1 ∼C
8
알콕시기, 메실옥시-C
1 ∼C
8
알콕시기, 노실옥시-C
1 ∼C
8
알콕시기, 불소, 염소, 브롬 및 요오드 중에서 선택되는 할로겐 원자로 치환된 C
1 ∼C
8
알콕시기, 또는 C
1 ∼C
8
알킬아미노기이며, R
2 는 H, 불소, 염소, 브롬 및 요오드 중에서 선택되는 할로겐 원자 또는 C
1 ∼C
8
알킬기이며, R
3 및 R
4 는 각각 H, C
1 ∼C
8
알콕시기 또는 C
1 ∼C
8
알킬아미노기이다.
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