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-2024024497-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.
专利号:US-2024262834-A1 优先权日:2021-05-28 标 题:Synthesis of btk inhibitor and intermediates thereof 发明人:CHEN YONGGANG; CORRY JAMES; DESMOND RICHARD; DI MASO MICHAEL J; FORSTATER JACOB H; KUETHE JEFFREY T; KUHL NADINE; LARSON REED; LEVESQUE FRANCOIS; NARSIMHAN KARTHIK; OTTE DOUGLAS; PRIER CHRISTOPHER K; SHEVLIN MICHAEL; SIROTA ERIC; TAN LUSHI; THAISRIVONGS DAVID A; TURNBULL BEN W H; WANG ZHIXUN; XIAO KAIJIONG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient synthetic processes useful in the preparation of Compound A, a BTK inhibitor of Formula (I): or a pharmaceutically acceptable salt thereof, including the preparation of intermediates used to make Compound A or a pharmaceutically acceptable salt thereof.
专利号:US-2024199680-A1 优先权日:2021-04-02 标 题:Synthesis of fluorinated cyclic dinucleotides 发明人:AN CHIHUI; FIER PATRICK S; HIRAGA KAORI; LIU ZHIJIAN; MARSHALL NICHOLAS M; MCINTOSH JOHN; MILLER STEVEN P; MOORE JEFFREY C; MURPHY GRANT S; OBLIGACION JENNIFER V; PAN WEILAN; PENG FENG; SALEHI MARZIJARANI NASTARAN; WINSTON MATTHEW S 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated cyclic dinucleosides, such as [P(R)]-2′-deoxy-2′-fluoro-5′-O—[(R)-hydroxymercaptophosphinyl]-P-thio-β-D-arabino-adenylyl-(3′→5′)-3′-deoxy-3′-fluoroguanosine cyclic nucleotide, which is also known as (2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-7-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2, 10-bis(sulfanyl)octahydro-2H,10H, 12H-2λ 5 ,10λ 5 -5,8-methanofuro[3,2-1][1, 3,6,9,11,2,10]pentaoxadiphosphacyclotetradecine-2,10-dione. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
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