公开(公告)号：KR1020120053648A

公开(公告)日：2012-05-29

申请号：KR1020100114874

申请日：2010-11-18

Applicant: 한국화학연구원

Inventor： 이정옥 ,  김형래 ,  류재욱 ,  하재두 ,  조성윤 ,  정희정 ,  이종국 ,  한선영

IPC: C07D495/04 ,  A61K31/519 ,  A61P35/00

Abstract: PURPOSE: A pharmaceutical composition containing thienopyrimidine derivative is provided to prevent or treating abnormal cell growth diseases. CONSTITUTION: A thienopyrimidine derivative is denoted by chemical formula 1. A method for preparing the derivative comprises: a step of reacting a compound of chemical formula 2 with formamide to prepare a compound of chemical formula 3; a step of substituting the compound of chemical formula 3 to prepare a compound of chemical formula 4; a step of coupling the compound of chemical formula 4 with a compound of chemical formula 5 to prepare a compound of chemical formula 1a. A pharmaceutical composition for preventing or treating abnormal cell growth diseases contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract translation: 目的：提供含有噻吩并嘧啶衍生物的药物组合物，用于预防或治疗异常细胞生长疾病。 构成：噻吩并嘧啶衍生物由化学式1表示。制备衍生物的方法包括：使化学式2的化合物与甲酰胺反应以制备化学式3的化合物的步骤; 用化学式3的化合物代替化学式4的化合物的步骤; 将化学式4的化合物与化学式5的化合物偶联以制备化学式1a的化合物的步骤。 用于预防或治疗异常细胞生长疾病的药物组合物含有其衍生物或药学上可接受的盐作为活性成分。

公开(公告)号：KR1020110048337A

公开(公告)日：2011-05-11

申请号：KR1020090105097

申请日：2009-11-02

Applicant: 한국화학연구원

Inventor： 정희정 ,  이철해 ,  김재학 ,  정원장 ,  김비치 ,  박선필

IPC: C07C239/14 ,  C07C231/14 ,  A61K31/165 ,  A61P35/00

Abstract: PURPOSE: A 6-amino-N-hydroxyhexanamide compound is provided to ensure strong cell proliferation inhibitory power by inhibiting enzyme activity of histone deacetylase, thereby enabling use as anti-cancer drug or enzyme activity inhibitory agent of histone deacetylase. CONSTITUTION: A compound is selected from a 6-amido-N-hydroxyhexanamide compound represented by chemical formula 1 and pharmaceutically acceptable salts thereof. In chemical formula 1, X is a single bond or selected from the group of C1-6 alkylenyl; and R is hydroxy, C3-8 cycloalkyl, C3-8 cycloalkenyl, C1-6 alkoxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, 5-7-membered aryl, 5-7-membered heteroaryl including 1-3 hetero atoms selected from N and O, and 5-7-membered heterocycloalkyl including 1-3 hetero atoms selected from N and O.

Abstract translation: 目的：提供6-氨基-N-羟基己酰胺化合物，以通过抑制组蛋白脱乙酰酶的酶活性来确保强的细胞增殖抑制能力，从而可用作组蛋白脱乙酰酶的抗癌药物或酶活性抑制剂。 构成：化合物选自由化学式1表示的6-氨基-N-羟基己酰胺化合物及其药学上可接受的盐。 在化学式1中，X是单键或选自C 1-6亚烷基; 和R为羟基，C 3-8环烷基，C 3-8环烯基，C 1-6烷氧基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基，5-7元芳基，5-7元杂芳基，包括 1-3个选自N和O的杂原子和包含1-3个选自N和O的杂原子的5-7元杂环烷基。

公开(公告)号：KR1020100052758A

公开(公告)日：2010-05-20

申请号：KR1020080111603

申请日：2008-11-11

Applicant: 한국화학연구원

Inventor： 김광록 ,  최상운 ,  정희정 ,  안진희 ,  이철해 ,  김성수

IPC: A61K31/165 ,  A61P21/00

Abstract: PURPOSE: A composition for inducing differentiation of neural precursor cells or stem cells to neural cells is provided to usefully treat nerve injury diseases. CONSTITUTION: A composition for inducing differentiation of neural precursor cells or stem cells to neural cells contains 10-20 Um of hydroxylamide derivative of chemical formula 1 or salt thereof as an active ingredient. The hydroxyamide derivative is denoted by chemical formula 1a or 1b. The stem cells are embryonic stem cells, adult stem cells, germiparity stem cells, or embryonic tumor stem cell. The neural precursor cells or stem cells are differentiated to neural cells by culturing with the composition.

Abstract translation: 目的：提供用于诱导神经前体细胞或干细胞向神经细胞分化的组合物，以有效治疗神经损伤疾病。 构成：用于诱导神经前体细胞或干细胞分化为神经细胞的组合物含有10-20Um的化学式1的羟基酰胺衍生物或其盐作为活性成分。 羟基酰胺衍生物由化学式1a或1b表示。 干细胞是胚胎干细胞，成体干细胞，胚胎干细胞或胚胎肿瘤干细胞。 通过用组合物培养将神经前体细胞或干细胞分化成神经细胞。

公开(公告)号：KR1020090118601A

公开(公告)日：2009-11-18

申请号：KR1020080044485

申请日：2008-05-14

Applicant: 한국화학연구원

Inventor： 고종성 ,  류재욱 ,  이정옥 ,  이종국 ,  정희정 ,  조성윤 ,  하재두 ,  한선영

IPC: C07D413/04 ,  C07D413/02 ,  A61P35/00

CPC classification number: C07D413/14

Abstract: PURPOSE: A pharmaceutical composition containing pyridine derivative which is substituted with a novel benzoxazole is provided to ensure high effect to protein kinase in treating cell proliferation disorder. CONSTITUTION: A pyridine derivative which is substituted with a benzoxazole is denoted by the chemical formula 1. A method for preparing the derivative or its pharmaceutically acceptable salt comprises: a step of reacting a compound of the chemical formula 2 with a compound of the chemical formula 3 under the presence of metal; and a step of performing deprotection of a compound of the chemical formula 4.

Abstract translation: 目的：提供一种含有新的苯并恶唑代替的吡啶衍生物的药物组合物，以确保蛋白激酶在治疗细胞增殖紊乱中的高效应。 构成：用苯并恶唑取代的吡啶衍生物由化学式1表示。制备衍生物或其药学上可接受的盐的方法包括：使化学式2化合物与化学式 3在金属的存在下; 以及对化学式4的化合物进行脱保护的工序。

公开(公告)号：KR1020060020081A

公开(公告)日：2006-03-06

申请号：KR1020040068821

申请日：2004-08-31

Applicant: 한국화학연구원

Inventor： 김봉진 ,  김재학 ,  김광호 ,  정희정 ,  이철해 ,  공재양 ,  조희영 ,  최영로 ,  김창섭

IPC: C07D477/20

CPC classification number: C07D477/20

Abstract: 본 발명은 하기 화학식 1의 2-아릴메틸아제티딘 카바페넴 유도체 및 그의 제조 방법에 관한 것으로, 본 발명의 2-아릴메틸아제티딘 카바페넴 유도체는 그람 양성균 및 그람 음성균에 대하여 광범위하게 항균활성을 나타내며, 메티실린 내성균주(MRSA) 및 퀴놀론 내성균주(QRSA)에 대한 항균효과가 매우 우수하여, 광범위 항생제 및 난치성 내성균 감염에 대한 항생제로서 유용하다.
화학식 1

상기 식에서,
R
1 은 수소, 또는 페닐기의 특정 위치에 치환된 1개 이상의 C
1 -C
3 알킬기, C
1 -C
3 알킬옥시기, 하이드록시기, 아민기, 알킬아민기, 알킬싸이올기, 트라이플루오로메틸기 또는 할로겐 원자이고,
R
2 는 수소 또는 C
1 -C
3 알킬기이고,
M은 수소 또는 약리학적으로 허용가능한 염을 형성하는 짝이온이다.

Abstract translation: 本发明涉及2-芳基甲基 - 氮杂环丁烷盖青霉烯衍生物，并且涉及制造方法，2-芳基甲基氮杂环丁烷盖青霉烯式（I）的本发明的衍生物的方法代表对革兰氏阳性和革兰氏阴性细菌具有广泛的抗菌活性的 上的耐甲氧西林状态（MRSA）和耐喹诺酮状态抗菌效果（QRSA）是优秀的，它是作为抗生素的广谱抗生素和难熔性的感染是有用的。

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

Inventor： 김봉진 ,  이철해 ,  정원장 ,  정희정 ,  김재학 ,  편도규

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。

公开(公告)号：KR100385364B1

公开(公告)日：2003-05-27

申请号：KR1020020052421

申请日：2002-09-02

Applicant: 동화약품주식회사 ,  한국화학연구원

Inventor： 이철해 ,  김봉진 ,  정원장 ,  김재학 ,  정희정 ,  김은정 ,  송신섭 ,  정용호 ,  곽현정 ,  이진수 ,  편도규

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。

公开(公告)号：KR100286381B1

公开(公告)日：2001-04-16

申请号：KR1019980011976

申请日：1998-04-04

Applicant: 한국화학연구원 ,  동화약품주식회사

Inventor： 이철해 ,  이진수 ,  정용호 ,  정희정 ,  김재학 ,  김용주 ,  이홍우 ,  허재두

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.

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

Inventor： 김완주 ,  김경수 ,  정희정 ,  황태섭 ,  이미정 ,  안구현 ,  김홍기

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.

公开(公告)号：KR102128018B1

公开(公告)日：2020-06-30

申请号：KR1020180051686

申请日：2018-05-04

Applicant: 한국화학연구원

Inventor： 김필호 ,  조성윤 ,  하재두 ,  김형래 ,  황종연 ,  윤창수 ,  정희정 ,  박지훈 ,  이정옥 ,  이창훈 ,  안선주

IPC: C07D487/04 ,  A61K31/519 ,  A23L33/10