专利号:US-9643915-B2 优先权日:2013-03-15 标题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-9708354-B2 优先权日:2013-03-15 标 题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-9428482-B2 优先权日:2011-01-27 标 题 :Process for synthesis of polyphenols 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE; SPHAERA PHARMA PTE LTD 摘要:The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
专利号:US-8981121-B2 优先权日:2010-06-25 标 题 :Process for the preparation of nitrogen substituted aminotetralins derivatives 发明人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE 权利人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE; UCB PHARMA GMBH 摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).
专利号:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
[参考文献]: P A Husain, Et Al. Hplc-Based Method For Determination Of Absolute Configuration Of Alpha-Chiral Amines. Anal Chem. 1993 May 15;65(10):1456-61. [参考文献]: Radoslaw Laufer, Et Al. Discovery Of Inhibitors Of The Mitotic Kinase Ttk Based On N-(3-(3-Sulfamoylphenyl)-1H-Indazol-5-Yl)-Acetamides And Carboxamides. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.
合成参考文献
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