专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
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.
专利号:US-2025026766-A1 优先权日:2022-01-12 标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors 发明人:LI JING; XU WENQING; WANG ZHIWEI 权利人:BEIGENE LTD 摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.
专利号:US-11286268-B1 优先权日:2019-07-02 标题:EIF4E-inhibiting compounds and methods 发明人:SPERRY SAMUEL; XIANG ALAN X; ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; SHAGHAFI MIKE; MICHELS THEO; NILEWSKI CHRISTIAN; TRAN CHINH VIET; PACKARD Garrick Kenneth; GRUBBS ALAN; URKALAN KAVERI; MUKAIYAMA TAKASUKE 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n n n n n n n n n n For Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , Q, L 1 , L 2 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:CN-116655637-A 优先权日:2023-04-13 标 题 :A kind of PI3Kδ inhibitor and its synthesis method and application
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合成参考文献
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