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Patent Agency Ranking
公开(公告)号：KR1020000008131A
公开(公告)日：2000-02-07
申请号：KR1019980027816
申请日：1998-07-10
Abstract: PURPOSE: L-type thionucleosides substituent manufactured by substituting no. 2' position are provided which are good for an anticancer drug or antiviral agent(anti-HBV, anti-HSV or anti-HCMV). CONSTITUTION: New thionucleosides(I) useful as an anticancer drug or antiviral agent(anti-HBV, anti-HSV or anti-HCMV) are prepared. In formula(I), R1,R2 are respectively H, halogen, azido, lower alkyl, or together methylene group; B is pyrimidine of uracil, cytosin, thymine, 5-halouracil, 5-halocytosin etc, or guanine, 6-chloropurine, hypoxanthine, 2-amino-6-cyclopropylamine, 6-methoxypurine, and 2-amino-6-methoxypurine. The acute toxicity test of thionucleosides is conducted with mice. Each compound is crushed and mixed with corn oil to afford 250 mg/kg, 1,000 mg/kg and 2,000 mg/kg. Dosage of 10 ml or 20 ml per kg is administered by using a needle for oral administration. The percentage of mortality is shown 0% to 2,000 mg/kg.
Abstract translation: 目的：将L型硫代核苷取代基取代 2'位置，对于抗癌药物或抗病毒剂（抗HBV，抗HSV或抗HCMV）是有利的。 构成：制备用作抗癌药物或抗病毒剂（抗HBV，抗HSV或抗HCMV）的新型硫代核苷（I）。 在式（I）中，R 1，R 2分别为H，卤素，叠氮基，低级烷基或亚甲基; B是尿嘧啶嘧啶，胞质蛋白，胸腺嘧啶，5-卤尿嘧啶，5-卤素等，或鸟嘌呤，6-氯嘌呤，次黄嘌呤，2-氨基-6-环丙胺，6-甲氧基嘌呤和2-氨基-6-甲氧基嘌呤。 用小鼠进行硫代核苷的急性毒性试验。 将每种化合物粉碎并与玉米油混合，得到250mg / kg，1,000mg / kg和2,000mg / kg。 通过使用口服给药来施用10ml / 20ml / kg的剂量。 死亡率百分比显示为0至2,000 mg / kg。
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公开(公告)号：WO2011074903A2
公开(公告)日：2011-06-23
申请号：PCT/KR2010/009036
申请日：2010-12-16
Applicant: 이화여자대학교 산학협력단 , 정낙신 , 이상국 , 정화진 , 이혁우
CPC classification number: C07D473/34 , A61K31/52
Abstract: 본 발명은 선택적 A 3 아데노신 수용체 효능제, 2-클로로-N 6 -(3-아이오도벤질)-4'-싸이오아데노신-5'-N-메칠유로나마이드 (thio-Cl-IB-MECA), N 6 -(3-아이오도벤질)-4'-싸이오아데노신-5'-N-메칠유로나마이드 (thio-IB-MECA), 또는 약제학적으로 허용가능한 이들의 염을 포함하는 염증성 질환, 대장암 및 전립선암 예방 또는 치료용 약제학적 조성물에 관한 것이다. 본 발명에 따른 약제학적 조성물은 종래의 A 3 아데노신 수용체 효능제에 비하여 독성이 현저히 낮아서 염증성 질환의 예방 및 치료에 유용하다. 또한 다른 A 3 아데노신 수용체 효능제에 비하여 보다 더 선택적으로 안드로젠 수용체 의존성 또는 비의존성 전립선 암 세포의 성장을 억제하므로 대장암 및 전립선암의 예방 또는 치료에 유용하다.
Abstract translation: 本发明涉及用于预防和治疗炎性疾病，结肠癌和前列腺癌的药物组合物，该组合物包括选择性A3腺苷受体激动剂，2-氯-N6-（3-碘苯甲醇）-4'-硫代腺苷-5' N-硫代-C1-MECA），N6-（3-碘苯甲醇）-4'-硫代腺苷-5'-N-甲基脲（thio-IB-MECA）或其药学上可接受的盐。 与典型的A3腺苷受体激动剂相比，本发明的药物组合物与炎性疾病的预防和治疗有关，因为其毒性显着降低。 此外，根据本发明的药物组合物可用于预防和治疗结肠癌和前列腺癌，因为与典型的A3腺苷受体相比，对雄激素受体依赖性或非依赖性前列腺癌细胞的生长具有更多的选择性抑制 激动剂。
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公开(公告)号：WO2011096642A2
公开(公告)日：2011-08-11
申请号：PCT/KR2010/009112
申请日：2010-12-20
Applicant: 이화여자대학교 산학협력단 , 정낙신 , 이상국 , 정화진 , 이혁우
IPC: A61K31/52 , A61K31/4178 , A61P29/00 , A61P19/02
CPC classification number: A61K31/52 , A61K31/7076
Abstract: 본 발명은 2-[2-클로로-6-(3-아이오도벤질)-퓨린-9-일]-테트라하이드로-싸이오펜-3,4-디올 (LJ-1888) 또는 약제학적으로 허용가능한 이것의 염을 활성 성분으로 포함하는 염증성 질환의 예방 또는 치료용 약제학적 조성물에 관한 것이다. 본 발명에 따른 약제학적 조성물은 종래의 A 3 아데노신 수용체 효능제나 길항제에 비하여 독성이 현저히 낮아서 염증성 질환의 예방 및 치료에 유용하다.
Abstract translation: 本发明涉及用于预防和治疗含有2- [2-氯-6-（3-碘苄基） - 呋喃-9-基] - 四氢 - 噻吩-3,4-二醇（LJ- 1888）或其药学上可接受的盐作为活性成分。 根据本发明的药物组合物与已知的A3腺苷受体激动剂或拮抗剂相比具有显着低的毒性，因此可用于预防和治疗炎性疾病。
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公开(公告)号：KR1020010039480A
公开(公告)日：2001-05-15
申请号：KR1019990049517
申请日：1999-11-09
CPC classification number: C12N15/70 , A61K38/164 , C07K14/005
Abstract: PURPOSE: Provided is a gene coding thermostable cytidine deaminase. And a recombinant strain, E. coli JH53 (KCTC 8971P), expressing the same is also provided. The enzyme eliminates only (+) isomer of (+)(-) isomers of glucose so that (-) isomer useful as an ingredient of medications against type B hepatitis virus can be easily separated. CONSTITUTION: A gene coding thermostable cytidine deaminase and a recombinant strain, E. coli JH53 (KCTC 8971P), expressing the enzyme are obtained by the following steps of: i) synthesizing complimentary base sequences of 5'-ACACGGATCCAATTCTAATTTTTCTGTTACATTTTTG-3' and 5'-ACACTGCAGGATTTTCCTACGTTCGGTCTTCC-3' to use them as primers in cloning cdd gene of Bacillus caldolyticus; ii) culturing Bacillus caldolyticus in Luria-broth at 65 deg.C; iii) isolating chromosome DNA by Maniatis T. method; iii) performing PCR using Tag DNA polymerase; iv) cloning foreign gene then inserting it into pDIA5304 vector to recover plasmid pCJH53; v) transforming E.coli JF611(cdd-) with the plasmid pCJH53 to obtain E.coli JH53(KCTC 8971P); vi) culturing the transformant in AB minimal medium at 37 deg.c; vii) centrifuging the cell and followed by washing with cytidine deaminase buffer solution twice and ultra-sonificating for 45 seconds twice; viii) heat-treating the supernatant at 65 deg.C for 15 minutes and performing anion exchange chromatography and Sephacryl S-2oo liquid chromatography.
Abstract translation: 目的：提供一种编码热稳定胞苷脱氨酶的基因。 并且还提供了表达其的重组菌株大肠杆菌JH53（KCTC 8971P）。 该酶仅消除葡萄糖（+）（ - ）异构体的（+）异构体，从而可以容易地分离用作抗B型肝炎病毒药物的成分的（ - ）异构体。 构成：通过以下步骤获得表达该酶的基因编码热稳定胞苷脱氨酶和重组菌株的大肠杆菌JH53（KCTC8971P）：i）合成5'-ACACGGATCCAATTCTAATTTTTCTGTTACATTTTTTG-3'和5'的互补碱基序列， -ACACTGCAGGATTTTCCTACGTTCGGTCTTCC-3'用于克隆卡氏溶血杆菌cdd基因的引物; ii）在65℃在Luria-broth中培养卡氏溶解芽孢杆菌; iii）通过Maniatis T.方法分离染色体DNA; iii）使用Tag DNA聚合酶进行PCR; iv）克隆外源基因，然后将其插入pDIA5304载体中以回收质粒pCJH53; v）用质粒pCJH53转化大肠杆菌JF611（cdd-），得到大肠杆菌JH53（KCTC 8971P）; vi）在37℃下在AB基本培养基中培养转化体; vii）离心细胞，然后用胞苷脱氨酶缓冲溶液洗涤两次，超声超声45秒两次; viii）在65℃热处理上清液15分钟，进行阴离子交换层析和Sephacryl S-2oo液相色谱。
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公开(公告)号：KR1020040036417A
公开(公告)日：2004-04-30
申请号：KR1020020065441
申请日：2002-10-25
Applicant: 정낙신
IPC: C07D473/40 , C07D473/28 , C07D473/36 , A61K31/52
Abstract: PURPOSE: Thionucleoside derivatives having anti-cancer activity and a pharmaceutical composition containing the same are provided. The compounds have selective activity to the adenosine A3 receptor, so that they can be useful for prevention and treatment of various cancers, inflammatory intestine disorders and inflammatory diseases. CONSTITUTION: Thionucleoside derivatives having anti-cancer activity represented by the formula(I) or pharmaceutically acceptable salts or isomers are provided, wherein X is sulfur or oxygen; R1 is hydrogen, C1 to C5 alkyl, benzyl, halobenzyl or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio or thio; R3 and R3' are independently C1 to C5 hydroxyalkyl, alkoxycarbonyl or C1 to C5 alkylaminocarbonyl; and R4 is hydrogen or C1 to C5 alkyl. The pharmaceutical composition having adenosine A3 receptor selective activity contains the thionucleoside derivatives of the formula(I) as an effective component and pharmaceutically acceptable carriers.
Abstract translation: 目的：提供具有抗癌活性的核苷衍生物和含有其的药物组合物。 这些化合物对腺苷A3受体具有选择性活性，因此它们可用于预防和治疗各种癌症，炎症性肠病和炎性疾病。 构成：提供具有由式（I）表示的抗癌活性的核苷衍生物或其药学上可接受的盐或异构体，其中X为硫或氧; R1是氢，C1-C5烷基，苄基，卤代苄基或苯基烷基; R2是氢，卤素，烷氧基，烯基，炔基，烷硫基或硫代; R3和R3'独立地为C1至C5羟基烷基，烷氧基羰基或C1至C5烷基氨基羰基; 并且R 4是氢或C 1至C 5烷基。 具有腺苷A3受体选择活性的药物组合物含有作为有效成分的式（I）的核苷衍生物和药学上可接受的载体。
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