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参考文献:Design And Synthesis Of Potent,Orally Active,Inhibitors Of Carboxypeptidase U (Tafia)
标题:Design And Synthesis Of Potent,Orally Active,Inhibitors Of Carboxypeptidase U (Tafia)
摘要:A Series Of 3-Mercapto-Propionic Acid Derivatives That Function As Reversible Inhibitors Of Carboxypeptidase U Have Been Prepared. We Present A Successful Design Strategy Using Cyclic,Low Basicity Guanidine Mimetics Resulting In Potent,Selective And Bioavailable Inhibitors Of Carboxypeptidase U (Tafla). (C) 2004 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2003.12.039

专利信息

专利号:US-9861636-B2
优先权日:2014-04-29
标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors
发明人：HE WEI
权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD
摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.