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:WO-2009152051-A1 优先权日:2008-06-12 标题:Synthesis of a macrocyclic hcv protease inhibitor 发明人:WANG PENG 权利人:PHENOMIX CORP; WANG PENG 摘要:The present invention provides a method of synthesis of a macrocyclic compound known as a potent inhibitor of a protease produced by the hepatitis C virus (HCV). Inhibition of the viral protease blocks assembly of mature viral particles in an infected mammalian host. The method of synthesis involves a ring-closing metathesis step using a ruthenium catalyst. Hydrogenation and boronate deprotection provide the HCV protease-inhibitory product.
专利号:US-2010087658-A1 优先权日:1996-08-06 标 题 :Methods and intermediates for synthesis of selective dpp-iv inhibitors 发明人:CAMPBELL DAVID ALAN; LEITAO EMILIA P T; WU ZHEN-PING; WANG PENG 权利人:PHENOMIX CORP 摘要:Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-9862745-B2 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds 发明人:AMMOSCATO VINCE; BISHOP JOHN E; CHIU FANG-TING; GEISER ACHIM; GOMEZ JEAN-MARC; HETT ROBERT; KOELLNER CHRISTOPH; KULKARNI VITHALANAND R; LO YOUNG; MUNK STEPHEN; PICKERSGILL I FRASER 权利人:MILLENNIUM PHARM INC; MILLENNIUM PHARM INC 摘要:The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
专利号:US-2012289733-A1 优先权日:2011-05-11 标 题 :Novel borate derivatives and their applications 发明人:HEISE GLENN L; MYSLINSKA MALGORZATA 权利人:HEISE GLENN L; MYSLINSKA MALGORZATA; ANDERSON DEV CO 摘要:Borates, compositions comprising chiral (cyclic and acyclic) and achiral (cyclic and acyclic) borates; chiral (cyclic and acyclic) and achiral (cyclic and acyclic) biborates; and methods for their synthesis. Additionally, a significantly improved synthetic protocol for the synthesis of wide range of boronates starting from borates or biborates and Grignard or organolithium reagents that can be used for kilo lab and commercial scale production.
1: Duporté G, Flaud PM, Geneste E, Augagneur S, Pangui E, Lamkaddam H, Gratien A, Doussin JF, Budzinski H, Villenave E, Perraudin E. Experimental Study of the Formation of Organosulfates from α-Pinene Oxidation. Part I: Product Identification, Formation Mechanisms and Effect of Relative Humidity. J Phys Chem A. 2016 Oct 13;120(40):7909-7923. Epub 2016 Sep 29. doi: 10.1016/j.foodchem.2016.06.098. Epub 2016 Jun 29. doi: 10.1016/j.chembiol.2014.06.009. Epub 2014 Jul 31. 4: Frasinyuk MS, Kwiatkowski S, Wagner JM, Evans TJ, Reed RW, Korotkov KV, Watt DS. Pentapeptide boronic acid inhibitors of Mycobacterium tuberculosis MycP1 protease. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3546-8. doi: 10.1016/j.bmcl.2014.05.056. Epub 2014 May 27. 5: Schobesberger S, Junninen H, Bianchi F, Lönn G, Ehn M, Lehtipalo K, Dommen J, Ehrhart S, Ortega IK, Franchin A, Nieminen T, Riccobono F, Hutterli M, Duplissy J, Almeida J, Amorim A, Breitenlechner M, Downard AJ, Dunne EM, Flagan RC, Kajos M, Keskinen H, Kirkby J, Kupc A, Kürten A, Kurtén T, Laaksonen A, Mathot S, Onnela A, Praplan AP, Rondo L, Santos FD, Schallhart S, Schnitzhofer R, Sipilä M, Tomé A, Tsagkogeorgas G, Vehkamäki H, Wimmer D, Baltensperger U, Carslaw KS, Curtius J, Hansel A, Petäjä T, Kulmala M, Donahue NM, Worsnop DR. Molecular understanding of atmospheric particle formation from sulfuric acid and large oxidized organic molecules. Proc Natl Acad Sci U S A. 2013 Oct 22;110(43):17223-8. doi: 10.1073/pnas.1306973110. Epub 2013 Oct 7.