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公开(公告)号：KR1020050036366A
公开(公告)日：2005-04-20
申请号：KR1020030072022
申请日：2003-10-16
Applicant: 한국화학연구원 , 크리스탈지노믹스(주)
IPC: C07C235/42
Abstract: 본 발명은 하기 화학식 1의 벤즈히드록시아미드 유도체, 이의 제조방법 및 이를 함유하는 항암 조성물에 관한 것으로, 본 발명의 벤즈히드록시아미드 유도체는 히스톤 디아세틸라제의 효소활성을 효과적으로 억제하여 종양세포의 증식을 억제할 수 있다.
상기 식에서,
R
1 은 히드록시, 할로겐, 알킬옥시, 알킬, 아미노, 알킬아미노, 카르복실, 니트로, 아미드 및 술폰으로 이루어진 군으로부터 선택된 하나 이상의 치환체로 치환되거나 치환되지 않은, C
3 -C
8 사이클로알킬, 아릴 또는 헤테로아릴; 또는 히드록시, 할로겐, 알킬옥시, 알킬, 아미노, 알킬아미노, 카르복실, 니트로 또는 아미드로 치환되거나 치환되지 않은 아릴 또는 헤테로아릴로 치환된 C
3 -C
8 사이클로알킬이고; 상기 헤테로아릴은 고리 중에 질소, 황 또는 산소를 하나 이상 포함하며;
Q는 비닐, 에틸, 2-프로페닐 또는 2-프로필이다.-
公开(公告)号：KR1020050023107A
公开(公告)日：2005-03-09
申请号：KR1020030060178
申请日：2003-08-29
Applicant: 한국화학연구원 , 크리스탈지노믹스(주)
IPC: C07D241/44
Abstract: PURPOSE: Quinoxaline derivatives and a preparation method thereof are provided, which derivatives have inhibitory activity against histone deacetylase, which removes an acetyl group from the lysine tail in the N-terminal of histone, by selectively inducing the terminal differentiation of the tumor cells, and thus by inhibiting the growth of tumor cells. CONSTITUTION: The quinoxaline derivatives represented by formula (1) are provided, wherein R1 is aryl, heteroaryl or C3-C8 cycloalkyl which is optionally substituted by one or more substituents selected from hydroxy, halogen, alkyloxy, alkyl, amino, alkylamino, carboxyl, nitro, amide and sulfone in which the heteroaryl contains one or more elements selected from nitrogen, sulfur and oxygen in a ring; R2 is hydrogen or arylalkyl; A is O, S, CH2, sulfone(SO2), sulfoxide(SO), CONH, NHCO, NX or NXSO2 in which X is hydrogen, C1-5 alkyl or independently the same as R1; and n is 0, 1, 2 or 3. The method for preparing a compound of formula (2) comprises the steps of: (a) acylation of 2-bromo arylalkyl carboxylic acid of formula (6) with 3,4-diamino benzoic ester of formula (7) in an aprotic solvent to prepare a compound of formula (8); (b) cyclization of the compounds of formula (8) in the presence of inorganic salts to prepare quinoxaline ester of formula (9); (c) treating the quinoxaline ester of formula (9) with hydroxide salts to prepare an organic acid of formula (10); and (d) acylation of the organic acid of formula (10) with the protected hydroxyl amine and hydrogenating the reaction product in the presence of palladium, wherein Y is O, S, CH2, SO2, SO or NX.
Abstract translation: 目的：提供喹喔啉衍生物及其制备方法，该衍生物通过选择性诱导肿瘤细胞的末端分化而对组蛋白脱乙酰酶具有抑制活性，其通过选择性诱导肿瘤细胞的末端分化而从组蛋白的N末端的赖氨酸尾部除去乙酰基， 从而通过抑制肿瘤细胞的生长。 组成：提供由式（1）表示的喹喔啉衍生物，其中R 1是芳基，杂芳基或任选被一个或多个选自羟基，卤素，烷氧基，烷基，氨基，烷基氨基，羧基， 硝基，酰胺和砜，其中杂芳基在环中含有一个或多个选自氮，硫和氧的元素; R2是氢或芳基烷基; A是O，S，CH2，砜（SO2），亚砜（SO），CONH，NHCO，NX或NXSO2，其中X是氢，C1-5烷基或与R1独立地相同; 制备式（2）化合物的方法包括以下步骤：（a）将式（6）的2-溴芳基烷基羧酸与3,4-二氨基苯甲酸 （7）的酯在非质子溶剂中制备式（8）的化合物; （b）在无机盐存在下环化式（8）化合物以制备式（9）的喹喔啉酯; （c）用氢氧化物盐处理式（9）的喹喔啉酯以制备式（10）的有机酸; 和（d）用保护的羟基胺酰化式（10）的有机酸，并在钯存在下氢化反应产物，其中Y是O，S，CH 2，SO 2，SO或NX。
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公开(公告)号：KR100446432B1
公开(公告)日：2004-08-30
申请号：KR1020010048742
申请日：2001-08-13
Applicant: 한국화학연구원
IPC: C07D417/14
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided are 2-benzothiazole carbapenem derivatives represented by the formula 1, a preparation method thereof and the composition containing the same. The composition has an excellent antibiotic property and is effective against resistant bacteria such as methicillin resistant Staphylococcus Aureus, MRSA and ofloxacin resistant Staphylococcus Aureus(QRSA). CONSTITUTION: In the carbapenem derivatives represented by the formula 1, M is hydrogen or a pair ion forming pharmaceutically allowed salts. The synthetic rout comprises reacting a compound of the formula 2 with a compound of the formula 3 to make a compound of the formula 4, and eliminating the carboxy protecting group from it. In the formula 4, R1 is a hydroxy protecting group such as tert-butyl silyl or triethylsilyl group; R2 is a carboxy protecting group such as p-nitrobenzyl, aryl or p-methoxybenzyl; R3 is an amine protecting group such as aryloxy carbonyl or p-nitrobenzyloxy carbonyl.
Abstract translation: 目的：提供由式1表示的2-苯并噻唑碳青霉烯衍生物，其制备方法和含有其的组合物。 该组合物具有优异的抗生素性质，并且对抵抗性细菌例如耐甲氧西林金黄色葡萄球菌，MRSA和耐氧氟沙星金黄色葡萄球菌（QRSA）是有效的。 构成：在由式1表示的碳代青霉烯衍生物中，M为氢或形成药学允许盐的一对离子。 合成路线包括将式2的化合物与式3的化合物反应以制备式4的化合物，并从其中除去羧基保护基。 式4中，R 1为羟基保护基，例如叔丁基甲硅烷基或三乙基甲硅烷基; R2是羧基保护基，如对硝基苄基，芳基或对甲氧基苄基; R3是胺保护基团，如芳氧基羰基或对硝基苄氧基羰基。
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公开(公告)号：KR100385364B1
公开(公告)日：2003-05-27
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为可用于制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 它可用作制备β-甲基碳青霉烯类抗生素的中间体，并通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酰胺化合物反应制备。
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35.发明授权C-2에서 락탐이 히드록시메틸에 연결된 1-베타메틸카르바페넴카르복실산 에스테르유도체 및 그의 제조방법 失效其中内酰胺在C-2上与羟甲基连接的1- Betamethylcarbapenem羧酸酯衍生物及其制备方法
公开(公告)号：KR100286381B1
公开(公告)日：2001-04-16
申请号：KR1019980011976
申请日：1998-04-04
IPC: C07D477/14 , C07D205/02 , C07D487/04
Abstract: PURPOSE: Provided is a 1-βmethylcarbapenemcarboxylic acid ester derivative wherein lactam is linked to hydroxymethyl at C-2, which has high antibiotic effects on both gram positive and negative bacteria except for Pseudomonas aeruginosa. Also, its preparation method is provided. CONSTITUTION: 1-βmethylcarbaphenemcarboxylic acid ester derivative is represented by the formula(1), wherein R1 is hydrogen atom or cyclic or noncyclic low alkyl having C1-C4; R2 is pivaloyloxyalkyl, low alkoxycarbonyloxyalkyl or alkyldioxoleneonalkyl having C1-C6; and n is 1-3. It is prepared by reacting 1-βmethylvcarbephenem derivative represented by the formula(2), wherein R1, R2 and n is as described above; R is hydrogen or anion induced from organic or inorganic salt; and X is halogen with halide represented by the formula(3) of X-R2 or sulfonate compound.
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Patent Agency Ranking
公开(公告)号：KR1019950029264A
公开(公告)日：1995-11-22
申请号：KR1019940006998
申请日：1994-04-02
Applicant: 한국화학연구원
IPC: C07D413/06 , C07D417/06 , C07D487/04
Abstract: 본 발명은 베타메칠아제티디논 유도체의 제조방법으로서, 더욱 상세하게는 다음 구조식(Ⅰ)로 표시되는 1-베타메칠카르바페넴 항생제의 제조시 중간체로 사용되는 다음구조식(Ⅱ)의 베타메칠아제티디논 유도체, 즉(3S, 4S)-3 (1R)-1〔(t-부틸디메칠실릴)옥시〕에칠｝-4｛〔(1R)-1-메칠-(4, 4-디알킬-2-치옥소-1, 3-옥사 또는 치아졸리딘)-3-일〕메칠｝아제티딘-2-온의 제조방법에 관한 것이다.
상기 식에서, R은 항생작용을 지닌 활성잔기를 나타내며, R
1 은 히드록시보호기중 t-부칠디메칠실릴기를 나타내고, R
2 는 수소 또는 저급알킬기를 나타내고, X
1 및 X
2 는 산소 또는 황원자를 나타낸다.
본 발명에 의하면 상기 구조식(Ⅱ)의 베타메칠아제티디논 유도체가 높은 입체선택성으로 고수율로 얻어지며, 어키랄 옥시러리를 사용하여 간단한 제조방법을 제공한다.-
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公开(公告)号：KR101745741B1
公开(公告)日：2017-06-12
申请号：KR1020120088577
申请日：2012-08-13
IPC: C07D487/04 , C07D403/14 , A61K31/4985 , A61K31/506 , A61K31/5377
Abstract: 본발명은신규한트리아졸로피라진유도체또는이의약제학적허용가능한염, 이들을유효성분으로포함하는 c-Met 티로신키나아제활성억제용약제학적조성물및 이상증식성질환 (hyper proliferative disorder)의예방또는치료용약제학적조성물에관한것이다. 본발명은 c-Met 티로신키나아제의활성을효율적으로억제함으로써비정상적인키나제의활성으로인한과도한세포증식및 성장과관련된다양한이상증식성질환, 예를들어암, 건선, 류마티스관절염, 당뇨병성망막증등의치료제로유용하게이용될수 있다.
Abstract translation: 本发明涉及新的三唑并吡嗪衍生物或用于预防或治疗抑制和病症增殖性病症（超增殖性病症），包括其药学上可接受的盐，的那些活性成分的c-Met的酪氨酸激酶的药物组合物的药物 ＆lt; 本发明的用于各种疾病的治疗增殖性疾病，例如癌症，牛皮癣，类风湿性关节炎，与过度的细胞增殖和生长因异常激酶活性通过有效抑制c-Met的酪氨酸激酶的活性相关的糖尿病性视网膜病 可以有用地使用。
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