公开(公告)号：KR1020030042632A

公开(公告)日：2003-06-02

申请号：KR1020010073358

申请日：2001-11-23

Applicant: 한국과학기술연구원

Inventor： 유재훈 ,  이종국 ,  권미윤 ,  신계정

IPC: C07H15/232

CPC classification number: C07H5/10 ,  C07H15/232

Abstract: PURPOSE: Provided is a heterodimer of neomycin and chloramphenicol with improved specificity to a target RNA molecule to increase the medicinal efficacy while decreasing adverse effects due to the non-specific drugs. It is effectively used as an anti-virus agent, an anti-bacteria agent, or an anti-cancer agent. CONSTITUTION: A heterodimer(formula 1) of neomycin and chloramphenicol is structured such that the heterodimer is specific-coupled to 16S rRNA, RRE RNA, or TS RNA. In the formula(1), n is an integer of 2-10 and, more particularly, 3, 6 or 9. The specific coupling of the heterodimer to the RNA is characterized by simultaneously recognizing the stem and the loop of the RNA. The specific coupling is intrinsic to the sequence of RNA.

Abstract translation: 目的：提供新霉素和氯霉素的异二聚体，对目标RNA分子具有改进的特异性，以增加药物功效，同时减少由非特异性药物引起的不良反应。 它有效地用作抗病毒剂，抗菌剂或抗癌剂。 构成：新霉素和氯霉素的异二聚体（配方1）的结构使得异二聚体与16S rRNA，RRE RNA或TS RNA特异性偶联。 在式（1）中，n是2-10的整数，更特别是3-6或9.异源二聚体与RNA的特异性偶联特征在于同时识别RNA的茎和环。 特异性偶联是RNA序列固有的。

公开(公告)号：KR100345465B1

公开(公告)日：2002-07-26

申请号：KR1020000038284

申请日：2000-07-05

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구 ,  서경재

IPC: C07D477/10

Abstract: 본 발명은 항균제로 유용한 신규의 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것으로서, 구체적으로 화학식 1로 표시되는 카바페넴 모핵의 2번 위치에 주요 관능기로서 5-(2'-이소옥사졸릴에텐닐)피롤리딘-3-티오기 또는 5-(2'-이소티아졸릴에텐닐)피롤리딘-3-티오기가 치환된 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것이며, 본 발명에 의한 1-베타메틸카바페넴 유도체는 디하이드로펩티다제-I에 대해 안정하고 그람양성균 및 그람음성균 모두에 대해 우수한 항균 활성을 보이는 유용한 항균제이다.

상기 화학식 1에서, R은 명세서에 기재된 바와 같다.

公开(公告)号：KR1020020005334A

公开(公告)日：2002-01-17

申请号：KR1020000039375

申请日：2000-07-10

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구

IPC: C07D477/10

Abstract: PURPOSE: Provided is a novel 1-β- methylcarbapenem derivative which has an antibacterial effect on both gram negative and positive bacteria and stability to dihydropeptidase-I, and is thus useful as antibacterial agent. And a pharmaceutical composition containing it and its manufacturing method are also provided. CONSTITUTION: The novel 1-β- methylcarbapenem derivative is represented by the formula(I), wherein R is described as in the description, X is ethoxycarbonyl group or hydroxymethyl group; Y is hydroxymethyl group or ethoxycarbonyl group; and Z is methyl group or carbamoylmethyl group. Its manufacturing method comprises the steps of: reacting enolphosphate with thiol derivative in the presence of base, in appropriate solvent to prepare protected carbapenem derivative; and deprotecting the protected carbapenem derivative to obtain 1-β- methylcarbapenem derivative.

Abstract translation: 目的：提供一种新型的1-β-甲基碳青霉烯衍生物，对革兰阴性和阳性细菌具有抗菌作用，对二氢肽酶-I具有稳定性，因此可用作抗菌剂。 还提供含有它的药物组合物及其制备方法。 构成：新颖的1-β-甲基碳青霉烯衍生物由式（I）表示，其中R如描述中所述，X是乙氧基羰基或羟甲基; Y是羟甲基或乙氧基羰基; Z为甲基或氨基甲酰基甲基。 其制造方法包括以下步骤：在碱的存在下，在合适的溶剂中使烯醇化磷酸酯与硫醇衍生物反应，制备保护的碳青霉烯衍生物; 并将保护的碳青霉烯衍生物脱保护得到1-β-甲基碳青霉烯衍生物。

公开(公告)号：KR100125130B1

公开(公告)日：1997-12-05

申请号：KR1019940020300

申请日：1994-08-17

Applicant: 한국과학기술연구원

Inventor： 박상우 ,  신계정 ,  김동찬

IPC: C07D413/02 ,  A01N43/26 ,  C07D263/22

CPC classification number: C07D413/04 ,  A01N43/76 ,  C07D263/42

Abstract: The oxazolinon type derivative represented by the following general formula(I) and its preparing method is disclosed with uses as herbicides wherein, R is low alkyl or halogen, low alkyl or trifluoromethyl containing phenyl, X is the same or different, halogen, carbomethoxy, nitro, or halogen, trifluoro substituted phenoxy, A is nitrogen, carbon, n is an integer of 1-3. The oxazolinon type derivative is prepared by a condensation reaction of M-amino acid of the general formula(II) and an acid chloride of the general formula(III) to produce an amino substituted M-amino acid of the general formula(IV), and then dehydration reaction after subjecting to reacting with anhydride nitric acid. The herbicide according to this invention has excellent herbicidal effectiveness in treatment of pre- or postemergency against a dicotyledonous plant.

Abstract translation: 公开了以下通式（I）表示的恶唑啉型衍生物及其制备方法，其用作除草剂，其中R为低级烷基或卤素，低级烷基或含三氟甲基的苯基，X为相同或不同的卤素，甲酯基， 硝基或卤素，三氟取代的苯氧基，A是氮，碳，n是1-3的整数。 恶唑啉型衍生物通过通式（II）的M-氨基酸与通式（III）的酰氯的缩合反应制备，得到通式（IV）的氨基取代的M-氨基酸， 然后与酸酐硝酸反应后进行脱水反应。 根据本发明的除草剂在对双子叶植物的芽前或芽后处理方面具有优异的除草效果。