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1. 发明申请

WO2008108508A1 ADENOSINE DERIVATIVES, METHOD FOR THE SYNTHESIS THEREOF, AND THE PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF THE INFLAMMATORY DISEASES CONTAINING THE SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：腺苷衍生物，其合成方法和用于预防和治疗含有作为活性成分的炎症疾病的药物组合物
公开(公告)号：WO2008108508A1
公开(公告)日：2008-09-12
申请号：PCT/KR2007/001131
申请日：2007-03-07
申请人： FM THERAPEUTICS Co., Ltd. , JEONG, Lak Shin , KIM, Hea Ok , JACOBSON, Kenneth A. , CHOE, Seung Ah
发明人： JEONG, Lak Shin , KIM, Hea Ok , JACOBSON, Kenneth A. , CHOE, Seung Ah
IPC分类号： C07D473/34 , A61K31/4985
CPC分类号： C07D473/34 , C07H19/16
摘要： Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
摘要翻译：公开了腺苷衍生物，其合成方法和用于预防和治疗炎性疾病的药物组合物，其包含与活性成分相同的物质。腺苷衍生物对腺苷受体具有高结合亲和力和选择性，特别是A3腺苷受体，作为A3腺苷受体拮抗剂，具有抗炎活性。因此，腺苷衍生物可用于预防和治疗炎性疾病。

2. 发明申请

WO2011074903A3 PHARMACEUTICAL COMPOSITION CONTAINING A3 ADENOSINE RECEPTOR AGONIST 审中-公开
标题翻译：含有A3腺苷受体激动剂的药物组合物
公开(公告)号：WO2011074903A3
公开(公告)日：2011-11-10
申请号：PCT/KR2010009036
申请日：2010-12-16
申请人： UNIV EWHA IND COLLABORATION , JEONG LAK SHIN , LEE SANG KOOK , CHUNG HWA JIN , LEE HYUK WOO
发明人： JEONG LAK SHIN , LEE SANG KOOK , CHUNG HWA JIN , LEE HYUK WOO
IPC分类号： A61K31/52 , A61P29/00 , A61P35/00
CPC分类号： C07D473/34 , A61K31/52
摘要： The present invention relates to a pharmaceutical composition for prevention and treatment of inflammatory diseases, colon cancer and prostate cancer, the composition including selective A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzil)-4'-thioidenosine-5'-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzil)-4'-thioidenosine-5'-N-methyluronamide (thio-IB-MECA), or pharmaceutically acceptable salts thereof. The pharmaceutical composition according to the present invention is useful for prevention and treatment of inflammatory diseases because of the remarkably lower toxicity thereof compared with typical A3 adenosine receptor agonists. In addition, the pharmaceutical composition according to the present invention is useful for prevention and treatment of colon cancer and prostate cancer because of the more selective inhibition thereof against growth of androgen receptor-dependent or non-dependent prostate cancer cells compared with typical A3 adenosine receptor agonists.
摘要翻译：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，所述组合物包括选择性A 3腺苷受体激动剂，2-氯-N 6 - （3-碘苯偶酰）-4'-硫代鸟苷-5' （硫代-Cl-IB-MECA），N6-（3-碘苯偶酰）-4'-硫代鸟苷-5'-N-甲基糖醛酰胺（硫代-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可用于预防和治疗炎性疾病，因为其毒性显着较低。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，其更有选择地抑制雄激素受体依赖性或非依赖性前列腺癌细胞的生长激动剂。

3. 发明申请

WO2004038006A2 PURINE NUCLEOSIDES 审中-公开
标题翻译：嘌呤核苷
公开(公告)号：WO2004038006A2
公开(公告)日：2004-05-06
申请号：PCT/US0333987
申请日：2003-10-24
申请人： US GOV HEALTH & HUMAN SERV , EWHA WOMANS UNIVERSITY , JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
发明人： JEONG LAK SHIN , JACOBSON KENNETH A , MOON HYUNG RYONG , KIM HEA OK
IPC分类号： A61K31/52 , A61K31/7076 , A61P29/00 , A61P35/00 , C07D473/00 , C07D473/14 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167 , C12N
CPC分类号： C07H5/10 , C07D473/00 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167
摘要： Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; Rl is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3' are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R3 and R3' do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.
摘要翻译：公开了对A3腺苷受体具有选择性并可用于治疗癌症和炎性疾病的嘌呤核苷化合物。所述化合物由以下通式（I）表示，包括其异构体：其中X是硫或氧; R1是氢，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'是氢，羟基烷基，烷氧基羰基或烷基氨基羰基，而R3和R3'不同时具有相同的取代基; 和R4是氢或烷基。还公开了包含式（I）化合物，异构体或其药理学上可接受的盐作为活性成分的药物组合物以及用于预防或治疗各种疾病，状态或病症（包括哮喘，炎症，脑缺血，心脏疾病和癌症。

4. 发明申请

WO2011096642A3 PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING INFLAMMATORY DISEASES 审中-公开
标题翻译：用于预防和治疗炎性疾病的药物组合物
公开(公告)号：WO2011096642A3
公开(公告)日：2011-11-10
申请号：PCT/KR2010009112
申请日：2010-12-20
申请人： UNIV EWHA IND COLLABORATION , JEONG LAK SHIN , LEE SANG KOOK , CHUNG HWA JIN , LEE HYUK WOO
发明人： JEONG LAK SHIN , LEE SANG KOOK , CHUNG HWA JIN , LEE HYUK WOO
IPC分类号： A61K31/52 , A61K31/4178 , A61P19/02 , A61P29/00
CPC分类号： A61K31/52 , A61K31/7076
摘要： The present invention relates to a pharmaceutical composition for preventing and treating inflammatory diseases, containing 2-[2-chloro-6-(3-iodobenzyl)-furyn-9-yl]-tetrahydro-thiophene-3,4-diol (LJ-1888) or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition according to the present invention has a remarkably low toxicity compared with a known A3 adenosine receptor agonist or antagonist, and is thus useful for preventing and treating inflammatory diseases.
摘要翻译：本发明涉及一种含有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。与已知的A 3腺苷受体激动剂或拮抗剂相比，本发明的药物组合物具有非常低的毒性，因此可用于预防和治疗炎性疾病。

5. 发明申请

WO2004038006A3 PURINE NUCLEOSIDES 审中-公开
公开(公告)号：WO2004038006A3
公开(公告)日：2004-05-06
申请号：PCT/US2003/033987
申请日：2003-10-24
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , EWHA WOMANS UNIVERSITY , JEONG, Lak, Shin , JACOBSON, Kenneth, A. , MOON, Hyung, Ryong , KIM, Hea, Ok
发明人： JEONG, Lak, Shin , JACOBSON, Kenneth, A. , MOON, Hyung, Ryong , KIM, Hea, Ok
IPC分类号： C07H19/167
摘要： Disclosed are purine nucleoside compounds that are selective to A 3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R l is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R 2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R 3 and R 3' are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R 3 and R 3 ' do not have identical substituents simultaneously; and R 4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.

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