专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:WO-2016084100-A3 优先权日:2014-11-26 标 题:Novel and efficient method for large scale synthesis of romidepsin 发明人:ALAPARTHI LAKSHMI PRASAD; VASANTHAKUMAR GANGA RAMU; CHOWDARY TALLURI BHUSHAIAH; MANTRI ANAND VIJAYKUMAR; KULKARNI GAURAV 权利人:ALAPARTHI LAKSHMI PRASAD 摘要:The present invention relates to intermediate compounds which are used as key intermediates in the synthesis of Romidepsin and process of preparation of these intermediates. The present invention also provides processes for synthesis of Romidepsin in high purity and good yields from said intermediate compounds.
专利号:US-2015344872-A1 优先权日:2014-06-02 标题 :Methods of synthesis of oligonucleotide tagged combinatorial libraries and uses thereof 发明人:HARBURY PEHR; PAIDHUNGAT MADAN; PATTEN PHILLIP; WATTS RICHARD EDWARD 权利人:DICE MOLECULES SV LLC 摘要:Provided herein are methods of synthesis of a compound which includes a functional moiety operatively linked to a tagging oligonucleotide, libraries thereof and methods of using the compound and libraries thereof to identify compounds which bind to a target.
专利号:EP-3480195-A1 优先权日:2017-11-07 标 题:Method for the synthesis of cyclic depsipeptides 权利人:BAYER ANIMAL HEALTH GMBH; THE KITASATO INST 摘要:The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, involving specific carboxylic acid group protecting tags: nTAG is preferably: nwherein m is ‰¥ 15 to ‰¤ 25, p is ‰¥ 8 to ‰¤ 18 and q is ‰¥ 15 to ‰¤ 25.
专利号:US-12122759-B2 优先权日:2017-11-07 标 题:Method for the synthesis of cyclic depsipeptides 发明人:HEIMBACH DIRK; OMURA SATOSHI; SUNAZUKA TOSHIAKI; HIROSE TOMOYASU; NOGUCHI YOSHIHIKO; Köbberling Johannes; WU ZHIJIE; FU SHUIBIAO; WU WEI; QIU JINFENG; HE LIU; WEI XUDONG 权利人:ELANCO ANIMAL HEALTH GMBH; THE KITASATO INST 摘要:The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
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