Dl-精氨酸 反应生成 雷帕霉素 参考文献:Drug Delivery Medical Device 标题:Drug Delivery Medical Device 摘要:公开了一种释放药物剂量到目标部位的医疗设备.该医疗设备包括一个气球,以及气球至少一部分的涂层.药物剂量的每个颗粒都至少部分地被聚合物层包裹.该方法包括以下步骤:提供一个包括气球和气球至少一部分的涂层的设备,涂层包括药物剂量的颗粒,每个药物剂量的颗粒都至少部分地被聚合物层包裹;将该设备定位到允许气球到达目标部位;以及充气该设备的气球.
专利信息
专利号:US-7202256-B2 优先权日:2004-04-14 标题:Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 发明人:GU JIANXIN; RUPPEN MARK E; RAVEENDRANATH PANOLIL; CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
专利号:US-7268144-B2 优先权日:2004-04-14 标 题 :Regiospecific synthesis of rapamycin 42-ester derivatives 发明人:GU JIANXIN; CAI PING; RUPPEN MARK E 权利人:WYETH CORP 摘要:A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.
专利号:US-9938297-B2 优先权日:2014-08-04 标 题:Process for the synthesis of everolimus and intermediates thereof 发明人:RAO DHARMARAJ RAMACHANDRA; MALHOTRA GEENA; PULLELA VENKATA SRINIVAS; ACHARYA VINOD PARAMESHWARAN 权利人:CIPLA LTD; CIPIA LTD 摘要:The present invention relates to a novel process for the synthesis of everolimus of formula (I): n nand intermediates thereof.
专利号:US-8258299-B2 优先权日:2009-03-27 标题:Process for preparation of temsirolimus 发明人:LEE KWANG-CHUNG; LEE TING-HUEI; TUNG YEN-SHIH; KAO CHIA-CHEN; LEE TZU-AI 权利人:LEE KWANG-CHUNG; LEE TING-HUEI; TUNG YEN-SHIH; KAO CHIA-CHEN; LEE TZU-AI; CHUNGWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779. n Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.
专利号:US-7153957-B2 优先权日:2003-08-07 标 题:Regioselective synthesis of CCI-779 发明人:CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:A method for regioselective synthesis of CCl-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method.
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
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合成参考文献
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