专利号:US-2016317682-A1 优先权日:2015-04-30 标题:PREPARATION OF Ag18F AND ITS USE IN THE SYNTHESIS OF PET RADIOTRACERS 发明人:SCOTT PETER J H; BROOKS ALLEN F; ICHIISHI NAOKO; SANFORD MELANIE S 权利人:UNIV MICHIGAN REGENTS; THE REGENTS OFTHE UNIV OF MICHIGAN 摘要:Copper-catalyzed radiofluorination of aryl iodides using Ag 18 F, methods of preparing Ag 18 F, and compounds obtained by copper-catalyzed radiofluorination of aryl iodides using Ag 18 F are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.
专利号:US-2012301720-A1 优先权日:2009-11-16 标题 :Metal island coatings and method for synthesis 发明人:KOBAN WIELAND; PEUKERT WOLFGANG; KLUPP TAYLOR ROBIN; DISTASO MONICA; BAO HUIXIN; VASYLYEV SERHIY 权利人:KOBAN WIELAND; PEUKERT WOLFGANG; KLUPP TAYLOR ROBIN; DISTASO MONICA; BAO HUIXIN; VASYLYEV SERHIY; BASF SE 摘要:The present invention relates to methods for synthesis of metallic island coatings with tunable island coverage and morphology on a variety of substrates. Particularly, the present invention relates to substrates coated with one or more metal islands and the use of said island-coated substrates.
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
专利号:WO-2018175954-A1 优先权日:2017-03-23 标 题 :Synthesis of imidazo[5,1-a]isoindole derivative useful as ido inhibitors 发明人:ANGELAUD REMY; BACHMANN STEPHAN; BEYELER ANDREAS; CARRERA DIANE; FISCHER ROLF; GUILLEMONT-PLASS MAUD; HOU HAIYUN; IDING HANS; KRAFT ANNE KATRIN; MANNS ANDREAS; MEIER ROLAND; NIEDERMANN KARIN; OLBRICH MARTIN; PIECHOWICZ KATARZYNA; REGE PANKAJ; REMARCHUK TRAVIS; SIROIS LAUREN; ST-JEAN FREDERIC; XU JIE 权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE; GENENTECH INC 摘要:Presently provided is a method of making a compound of the Formula (I) wherein X is halogen, which is useful for modulating the activity of indoleamine 2,3-dioxygenase (IDO) and treating diseases and conditions in which the inhibition of IDO mediated immunosuppression is beneficial.
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-9907796-B2 优先权日:2012-10-04 标题:Methods of treating tumoral diseases, or bacterial or viral infections 发明人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY 权利人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY; INHIBIKASE THERAPEUTICS INC 摘要:Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#00622 参考文献:10.1007/bf00299867 摘要:Hartley JA, Fox BW. Cross-linking between histones and DNA following treatment with a series of dimethane sulphonate esters. Cancer Chemother Pharmacol. 1986;17(1):56–62. doi: 10.1007/bf00299867.