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

Inventor： 정낙신 ,  케네스에이제이콥슨 ,  문형룡 ,  김혜옥

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。

公开(公告)号：KR1020000008131A

公开(公告)日：2000-02-07

申请号：KR1019980027816

申请日：1998-07-10

Applicant: 정낙신 ,  문형룡

Inventor： 정낙신 ,  문형룡

IPC: C07H19/24 ,  A61K31/70

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。