专利号:US-9993570-B2 优先权日:2014-01-05 标题:Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor 发明人:MACH ROBERT; CHU WENHUA; ZHOU DONG; MICHEL LOREN; CHEN DELPHINE 权利人:UNIV WASHINGTON 摘要:Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.
专利号:US-2016207909-A1 优先权日:2015-01-20 标 题 :Synthesis Method of Anti-Cancer Drug UK-1 and Derivatives Thereof 发明人:HUANG YUNG-TZUNG 权利人:HUANG YUNG-TZUNG 摘要:A synthesis method of anti-cancer drug UK-1 includes: mixing methyl 2-amino-3-hydroxybenzoate, aldehyde and molecular sieves to form a mixture and firstly refluxing the mixture to form a first reactant; hydrolyzing the first reactant in a basic solution to form a hydrolyzed solution and secondly refluxing the hydrolyzed solution to form a second reactant; and dehydrating the second reactant and the methyl 2-amino-3-hydroxybenzoate in an acidic solution to form a dehydrated solution and thirdly refluxing the dehydrated solution to form an anti-cancer drug UK-1 or at least one derivative thereof.
专利号:US-7541367-B2 优先权日:2005-05-31 标 题 :3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders 发明人:CHIU GEORGE; CONNOLLY PETER J; EMANUEL STUART; HUANG SHENLIN; LI SHENGJIAN; LIN RONGHUI; LU YANHUA; MIDDLETON STEVEN A 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): n nand pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of serine-threonine protein kinases and tyrosine protein kinases and interactions thereof.
专利号:CN-116606491-A 优先权日:2023-05-16 标 题 :A kind of anti-aging PE material and its synthesis process