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公开(公告)号：KR100299045B1
公开(公告)日：2001-09-22
申请号：KR1019990001313
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D211/64
Abstract: 종래의세로토닌수용체영상용화합물의단점을극복하면서 5-HT에대한친화성을높게유지할수 있고방사화학적으로가장최적의물리적조건(제조용이성, 반감기, 방사능세기, 구매용이성)을가지는, 아릴피페라진유도체와 NS리간드의결합에의한티올형화합물을제공하여이에테크네슘을표지할수 있도록한다.
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公开(公告)号：KR100285271B1
公开(公告)日：2001-05-02
申请号：KR1019980056952
申请日：1998-12-21
Applicant: 주식회사대성미생물연구소 , 한국과학기술연구원
IPC: C12N15/63
Abstract: 본 발명은 파이타제 (phytase)를 고발현하는 재조합 플라스미드 pJPK 및 이에 의해 형질전환된 바실러스 서브틸리스 (
Bacillus subtilis ) pJPK에 관한 것으로서, 더욱 상세하게는 동물의 소화생리에 적합하며 사료제조시 효소의 잔존활성이 뛰어난 바실러스 아밀로리퀴페이션스 (
Bacillus amyloliquefaciens ) DS-11이 생산하는 파이타제를 바실러스 서브틸리스에서 고발현하기 위한 재조합 플라스미드 및 이에 의해 형질전환된 바실러스 서브틸리스 pJPK, 그리고 이를 이용한 파이타제의 고효율 제조방법에 관한 것이다.-
公开(公告)号：KR1020000051075A
公开(公告)日：2000-08-16
申请号：KR1019990001313
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D211/64
Abstract: PURPOSE: Arylpiperazine derivatives attached with an N2S2 ligand useful as an imaging compound for serotonin receptors and preparing process thereof are provided which have the advantage of labelling a technetium being free from amide hydrolysis and having high affinity with 5-HT1A. CONSTITUTION: A process for preparing tetrabenazine derivatives represented by the formula (1) comprises the steps of synthesizing arylpiperazine derivatives, synthesizing an N2S2 ligand and attaching the N2S2 ligand to the arylpiperazine derivatives. In formula, X denotes methoxy, trifluoromethyl, or chloro; Y denotes carbon or nitrogen; Z denotes carbon or nitrogen. The compound has the advantage of labeling a technetium having the radiochemically optimum physical conditions(manufacturing easiness, half-life period, radioactive strength and purchase easiness).
Abstract translation: 目的：提供用作用作血清素受体成像化合物的N2S2配体附着的芳基哌嗪衍生物及其制备方法，其具有标记锝不含酰胺水解并且与5-HT1A具有高亲和力的优点。 构成：由式（1）表示的制备丁苯那嗪衍生物的方法包括合成芳基哌嗪衍生物，合成N 2 S 2配体并将N 2 S 2配体连接到芳基哌嗪衍生物的步骤。 在式中，X表示甲氧基，三氟甲基或氯; Y表示碳或氮; Z表示碳或氮。 该化合物具有标记具有放射化学最佳物理条件（制造容易度，半衰期，放射性强度和购买容易度）的锝的优点。
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公开(公告)号：KR1020000041160A
公开(公告)日：2000-07-15
申请号：KR1019980056952
申请日：1998-12-21
Applicant: 주식회사대성미생물연구소 , 한국과학기술연구원
IPC: C12N15/63
Abstract: PURPOSE: Phytase expression vector, pJPK has strong BJ27 promoter. Bacillus subtilis pJPK (KCTC 0526BP) transformed with pJPK expresses phytase highly, secrets expressed protein and is nontoxic to animal because of lacking endotoxin such as lipopolysaccharides. CONSTITUTION: Bacillus expression vector pJH27, having strong promoter BJ27, is ligated with 2.2 kb phytase gene originated from Bacillus amyloliquefaciens DS-11. The 2.2kb DNA includes SD sequence of phytase gene complementary to Bacillus subtilis 16S rRNA sequence (UCCUCC) for the overexpression of phytase. Resulting recombinant plasmid, pJPK, is introduced into E. coli JM83. Purified pJPK is transformed into Bacillus subtilis DB104 by protoplast transformation. Modified LB medium is consisted of 1% of potassium phosphate, 0.045% of magnesium sulfate, 4% of glucose, 1% of tryptone, 0.5% of yeast extract, 0.5% of NaCl and trace elements. 500-1000 unit of phytase is added to 1kg of animal feed. Animal experiment with porcine reveals that phytase produced from bacillus effectively degrades phytic acid in the animal feed.
Abstract translation: 目的：植酸酶表达载体pJPK具有较强的BJ27启动子。 用pJPK转化的枯草芽孢杆菌pJPK（KCTC 0526BP）高度表达植酸酶，秘密表达蛋白质，由于缺乏内毒素，如脂多糖，对动物无毒。 构成：具有强启动子BJ27的芽孢杆菌表达载体pJH27与源自解淀粉芽孢杆菌DS-11的2.2kb植酸酶基因连接。 2.2kb DNA包括与枯草芽孢杆菌16S rRNA序列（UCCUCC）互补的植酸酶基因的SD序列，用于过表达植酸酶。 将得到的重组质粒pJPK导入大肠杆菌JM83中。 纯化的pJPK通过原生质体转化转化到枯草芽孢杆菌DB104中。 改性LB培养基由1％磷酸钾，0.045％硫酸镁，4％葡萄糖，1％胰蛋白胨，0.5％酵母提取物，0.5％NaCl和微量元素组成。 将500-1000单位的植酸酶加入1kg动物饲料中。 猪的动物实验显示，由芽孢杆菌产生的植酸酶有效降解动物饲料中的植酸。
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公开(公告)号：KR1020000020033A
公开(公告)日：2000-04-15
申请号：KR1019980038443
申请日：1998-09-17
Applicant: 한국과학기술연구원
Abstract: PURPOSE: A preparation method of methylene diphosphonic acid by using diidomethane having a higher boiling point than reaction temperature is provided which produces the title compound in high yield, improves high productivity and is very economic by reusing trialkylphosphate as a starting material. CONSTITUTION: A process is disclosed for preparing methylene diphosphonic acid(1) which comprises: (a)preparing tetralkylmethylenediphosphonic acid ester(4) by reacting trialkyl phosphate(2) with diiodomethane(3); (b)separating the compound(4) from the reactant by removing alkyl iodine; (c)recovering excess trialkylphosphate by distillation at 180°C and recycling to the process(a); (d)removing alkyl groups by thermal-cracking the ester at 200-210°C and recrystallizing. In formula, R is allyl, isopropyl, t-butyl, isobutyl. The compound is useful as raw material of radioactive pharmaceuticals for diagnosis.
Abstract translation: 目的：提供通过使用沸点比反应温度高的二甲基亚甲基二膦酸的制备方法，其以高产率产生标题化合物，提高高生产率，并且通过重复使用三烷基磷酸酯作为起始原料是非常经济的。 公开：制备亚甲基二膦酸（1）的方法，其包括：（a）通过使三烷基磷酸酯（2）与二碘甲烷（3）反应制备四烷基亚甲基二膦酸酯（4）; （b）通过除去烷基碘将化合物（4）与反应物分离; （c）通过在180℃下蒸馏回收过量的三烷基磷酸酯并再循环至方法（a）; （d）通过在200-210℃下热裂解酯并重结晶来除去烷基。 在式中，R是烯丙基，异丙基，叔丁基，异丁基。 该化合物可用作放射性药物的诊断原料。
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Patent Agency Ranking
公开(公告)号：KR100134565B1
公开(公告)日：1998-04-20
申请号：KR1019930023229
申请日：1993-11-03
Applicant: 한국과학기술연구원
IPC: C07C251/32 , C07C249/08
Abstract: 본 발명은 1단계 또는 2단계 반응에 의한 의학 진단용 시약인 (RR/SS)-4, 8-디아자-3, 6, 6, 9-테트라 메틸 운데칸-3, 8-디엔-2, 10-디온 비스 옥심의 제조방법에 관한 것이다. 본 발명에 의해 d, l-HM-PAO가 효과적으로 얻어질 수 있다.
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公开(公告)号：KR100275792B1
公开(公告)日：2000-12-15
申请号：KR1019980038442
申请日：1998-09-17
Applicant: 한국과학기술연구원
IPC: C07C321/04
Abstract: 본발명은 신규의 지방산 유도체, 즉 15-메르캅토-3-메틸-펜타데칸산 및 그의 제조방법에 관한 것으로서, 15-메르캅토-3-메틸-펜타데칸산의 테크네슘(Technetium)화합물은 의학 진단용 영상화제로 유용하다.
본 발명의 15-메르캅토-3-메틸-펜타데칸산는 테크네슘과의 표지효율이 우수하고, 테크네슘-화합물은 심장의 β-산화 대사를 조영하는 방사성 의약품으로서 β-메틸기를 가지고 있어 심장에서의 보유기간이 길어 SPECT 등에 유효하다는 장점을 가지고 있다.-
公开(公告)号：KR1020000059736A
公开(公告)日：2000-10-05
申请号：KR1019990007559
申请日：1999-03-08
Applicant: 한국과학기술연구원
CPC classification number: C12N9/0004 , C12N15/81 , C12R1/685
Abstract: PURPOSE: Provided is a method for mass producing glucose oxidase, from Aspergillus niger by that glucose oxidase is accumulated in high concentration, thereby, purification process is simplified and a production yield is promoted. CONSTITUTION: The mass production method of glucoseoxidase comprises following steps of: preparing an expression plasmid having galactosedehydroginase (GAL10) promoter and galactodehydroginase (GAL7) terminator from yeast, signal sequence and structural gene of Aspergillus niger ATCC-9029; obtaining transformed yeast pJKGo(designation No. KCTC-0581 BP) by introduction of the expression plasmid into Saccharomyces cerevisiae (ATCC-2805); preparing glucose oxidase by the transformed yeast; and then secreting glucose oxidase to outside of cell membrane.
Abstract translation: 目的：提供从葡萄糖氧化酶以高浓度积累葡萄糖氧化酶的方法，通过葡萄糖氧化酶积累葡萄糖氧化酶，从而简化了纯化过程，提高了产率。 构成：糖酵解酶的大量生产方法包括以下步骤：制备具有半乳糖脱氢酶（GAL10）启动子和来自酵母的半乳糖脱氢酶（GAL7）终止子的表达质粒，黑曲霉ATCC-9029的信号序列和结构基因; 通过将表达质粒引入酿酒酵母（ATCC-2805）中获得转化酵母pJKGo（命名号KCTC-0581BP）; 由转化酵母制备葡萄糖氧化酶; 然后将葡萄糖氧化酶分泌到细胞膜外。
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公开(公告)号：KR1020000051077A
公开(公告)日：2000-08-16
申请号：KR1019990001315
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D221/06
Abstract: PURPOSE: Tetrabenazine derivatives attached with an N2S2 ligand useful as an imaging compound for endoplasmic reticulum transporter or reuptake site and preparing process thereof are provided which label a technetium having the radiochemically optimum physical conditions. CONSTITUTION: A tetrabenazine derivatives represented by the formula (1) have the advantage of labelling a technetium having the optimum physical conditions such as manufacturing easiness, half-life period, radioactive strength and purchase easiness. Also the compound can image an endoplasmic reticulum transporter as a marker of Parkinson's disease by attaching an N2S2 ligand to tetrabenazine to introduce technetium into tetrabenazine and providing an imaging compound of the transporter as a radioligand.
Abstract translation: 目的：提供与用作内质网转运体或再摄取位点的成像化合物的N2S2配体连接的丁苯那嗪衍生物及其制备方法，其标记具有放射化学最佳物理条件的锝。 构成：由式（1）表示的丁苯那嗪衍生物具有标记具有制造容易性，半衰期，放射性强度和购买容易性等最佳物理条件的锝的优点。 此外，化合物可以通过将N2S2配体连接到丁苯那嗪来将内质网转运蛋白图像化为帕金森病的标记物，以将锝引入到丁苯那嗪中，并将转运体的成像化合物作为放射性配体提供。
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公开(公告)号：KR1020000051076A
公开(公告)日：2000-08-16
申请号：KR1019990001314
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D207/00
Abstract: PURPOSE: Rachlopride derivative attached with an N2S2 ligand useful as imaging compound for a dopamin D2 acceptor and preparing process thereof are provided which label a technetium having the radiochemically optimum physical conditions. CONSTITUTION: A rachlopride derivative represented by the formula (1) is that an N2S2 ligand is introduced into rachlopride to introduce the technetium to the raclopride for the attachment of technetium. The compound has the advantage of labeling a technetium having the optimum physical conditions such as manufacturing easiness, half-life period, radioactive strength and purchase easiness. Also described is a process for preparing the rachlopride.
Abstract translation: 目的：提供与用作多巴胺D2受体的成像化合物的N2S2配体连接的Rachlopride衍生物及其制备方法，其标记具有放射化学最佳物理条件的锝。 构成：由式（1）表示的rachlopride衍生物是将N 2 S 2配体引入rachlopride以将锝引入到raclopride中以连接锝。 该化合物具有标记具有制造容易性，半衰期，放射性强度和购买容易性等最佳物理条件的锝的优点。 还描述了制备rachlopride的方法。
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