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公开(公告)号：US07405214B2
公开(公告)日：2008-07-29
申请号：US11095686
申请日：2005-04-01
申请人： Young Bok Lee , Chang Ho Ahn , Won Jun Choi , Lak Shin Jeong , Sang Kook Lee
发明人： Young Bok Lee , Chang Ho Ahn , Won Jun Choi , Lak Shin Jeong , Sang Kook Lee
IPC分类号： A01N43/04 , A01N43/54 , A61K31/70 , A61K31/505 , C07D239/00
CPC分类号： C07D239/47 , A61K31/513 , C07D239/54 , C07D239/553
摘要： The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.
摘要翻译： 本发明涉及由通式I和II表示的核苷衍生物，其合成方法及其药理学上可接受的盐，以及含有这些化合物的组合物。 还包括通过施用化合物治疗过度增殖性疾病的方法。
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公开(公告)号：US20120322815A1
公开(公告)日：2012-12-20
申请号：US13516634
申请日：2010-12-16
申请人： Lak Shin Jeong , Sang Kook Lee , Hwa Jin Chung , Hyuk Woo Lee
发明人： Lak Shin Jeong , Sang Kook Lee , Hwa Jin Chung , Hyuk Woo Lee
IPC分类号： A61K31/52 , C07D473/40 , A61P35/00 , A61P29/00 , A61P37/00 , A61P1/00 , A61P31/14 , A61P11/08 , A61P17/00 , A61P1/04 , A61P25/00 , C07D473/34 , A61P19/02
CPC分类号： C07D473/34 , A61K31/52
摘要： The present invention relates to a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4′-thioadenosine-5′-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4′-thioadenosine-5′-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.
摘要翻译： 本发明涉及一种预防或治疗炎性疾病，结直肠癌和前列腺癌的药物组合物，其含有A3腺苷受体激动剂，2-氯-N6-（3-碘苄基）-4'-硫代腺嘌呤-5'-N （硫代-C1-IB-MECA），N6-（3-碘苄基）-4'-硫代腺嘌呤-5'-N-甲基脲酰胺（thio-IB-MECA）或其药学上可接受的盐。 本发明的药物组合物的毒性比常规的A3腺苷激动剂毒性好，因此可用于预防或治疗炎性疾病。 此外，它比其他A3腺苷受体激动剂更有选择地抑制雄激素依赖性或独立前列腺癌细胞的生长，因此可用于预防或治疗结肠直肠癌或前列腺癌。
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3.发明申请公开(公告)号：US20100137577A1
公开(公告)日：2010-06-03
申请号：US12530086
申请日：2007-03-07
申请人： Lak Shin Jeong , Hea Ok Kim , Kenneth A. Jacobson , Seung Ah Choe
发明人： Lak Shin Jeong , Hea Ok Kim , Kenneth A. Jacobson , Seung Ah Choe
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。
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公开(公告)号：US07199127B2
公开(公告)日：2007-04-03
申请号：US10530552
申请日：2003-10-24
IPC分类号： C07D473/40 , C07D495/04 , C07D407/06 , A61K31/52 , A61P35/00
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; R1 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 alkylaminocarbonyl, 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Aβ3 +腺苷受体有选择性的嘌呤核苷化合物，可用于治疗癌症和炎性疾病。 化合物由以下通式（I）表示，包括其异构体：
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公开(公告)号：US08716304B2
公开(公告)日：2014-05-06
申请号：US13425212
申请日：2012-03-20
申请人： Lak Shin Jeong , Hyuk Woo Lee
发明人： Lak Shin Jeong , Hyuk Woo Lee
IPC分类号： A01N43/90 , A61K31/519 , C07D497/00
CPC分类号： C07D487/04
摘要： The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cyclopentenone with isopropylidene, regioselective cleavage of isopropylidene moiety, and synthesis of cyclic sulfate.
摘要翻译： 本发明涉及一种制备作为E1活化抑制剂的MLN4924的制备方法，更具体地说，涉及一种通过关键步骤进行有效立体选择性制备的方法，所述关键步骤包括环丙烯酮与异亚丙基的立体选择性还原，异丙叉部分的区域选择性裂解， 和环硫酸酯的合成。
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6.发明授权公开(公告)号：US09018371B2
公开(公告)日：2015-04-28
申请号：US12530086
申请日：2007-03-07
申请人： Lak Shin Jeong , Hea Ok Kim , Kenneth A. Jacobson , Seung Ah Choe
发明人： Lak Shin Jeong , Hea Ok Kim , Kenneth A. Jacobson , Seung Ah Choe
IPC分类号： C07H19/16 , C07H1/00 , C07D473/34
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。
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