专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2024092821-A1 优先权日:2020-03-31 标题:Synthesis of oligonucleotides and related compounds 发明人:ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA 权利人:JANSSEN BIOPHARMA INC 摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.
专利号:US-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
专利号:US-2024024489-A1 优先权日:2020-11-20 标 题:Protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof 发明人:MULARD LAURENCE; DHARA DEBASHIS; PFISTER HELENE; PAOLETTI JULIE; PHALIPON ARMELLE; GUERREIRO-INVERNO CATHERINE 权利人:PASTEUR INSTITUT 摘要:The present invention provides zwitterionic oligosaccharides, in particular fragments of the surface polysaccharides from Shigella sonnei and Shigella sonnei conjugates comprising them. The present invention also provides protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof, the disaccharide repeating unit of Shigella sonnei being: (I)
专利号:US-7816544-B2 优先权日:2004-03-23 标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A 权利人:UNIV BOSTON 摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-11447454-B2 优先权日:2015-08-07 标题:Synthesis of benzodiazepine derivatives 发明人:BOYCE MALCOLM JAMES; THOMSEN LIV; GILBERT DONALD ALAN; WOOD DAVID 权利人:TRIO MEDICINES LTD 摘要:The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I: