专利号:US-5886190-A 优先权日:1993-10-04 标 题:Rapid synthesis and use of 18F-fluoromisonidazole and analogs 发明人:WALLACE SIDNEY; YANG DAVID J; CHERIF ABDALLAH 摘要:The present invention involves a rapid synthesis of 18F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-0-acetyl-3-0-tosylpropanol, glycerol-1,3-ditosylate-2-0-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-0-diacetyl-4-0-tosylbutanol and threitol 1,4-di-tosylate-2,3-0-diacetylate, are also important aspects of the invention. A further aspect of the invention is the development of a hydrophilic PET ligand to image tumor hypoxia. Erythrotosyl analogue of 2-nitroimidazone (Ts-ETNIM) was prepared from a mixture of 2-nitromidazole, ditosylthreitol and cesium carbonate at 60 DEG C. for 1 hr. Ts-ETNIM was isolated at 70% yield. [18F]fluoroerythronitroimidazole (FETNIM) was then prepared from Ts-ETNIM and K18F/kryptofix TM . The yield for [18F]FETNIM was 26-30% (60 min, decay corrected). Results of biodistribution and PET studies indicate that [18F]FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic.
专利号:US-2007249590-A1 优先权日:2005-10-28 标 题:Substituted indolo[2,3-a]pyrrolo[3,4-c]carbazole compounds useful in treating kinase disorders 发明人:WILSON LAWRENCE J; MURRAY WILLIAM V; YANG SHYH-MING; YANG CANGMING; WANG BINGBING 权利人:WILSON LAWRENCE J; MURRAY WILLIAM V; YANG SHYH-MING; YANG CANGMING; WANG BINGBING 摘要:The present invention is directed to substituted indolo[2,3-a]pyrrolo[3,4-c]carbazole compounds of formula (I): n nand forms thereof and their synthesis and use as protein kinase inhibitors and interactions thereof.
专利号:WO-9509844-A1 优先权日:1993-10-04 标 题 :Rapid synthesis and use of 18f-fluoromisonidazole and analogs