发明名称 SMALL MOLECULE IMAGING OF FUNGI BY POSITRON EMISSION TOMOGRAPHY SCANNING
摘要 Disclosed herein are isotopically labeled calcofluor derivatives and uses of such to detect fungi, such as filamentous fungi, including Aspergillus species, such as by positron emission tomography (PET) scanning. In some examples, the disclosed compounds have a formula of;;wherein R1 is an amine, a hydroxyl group, a sulfide, a carboxylic acid, an amide, an alkyl, or aryl ; R2 is —NHC(O)—R3—L or —C(O)NH—R3—L, wherein R3 is an aryl or an aliphatic group (such as alkyl); each R4 independently may be selected from halogen, aliphatic (such as alkyl), aryl, amine, hydroxyl, haloalkyl, carboxylic acid, amide, aralkyl, cyano, ester, thiol, thioether, or alkoxy; each R5 independently may be selected from hydrogen, aralkyl, alkyl, or aryl, with any one of the aralkyl, alkyl, or aryl groups optionally being substituted with any one of the substituents provided for R4; each n independently is 1, 2, 3, 4, or 5; and L is 18F or a chelator capable of chelating a radiolabel (such as chelators for [18F]AlF, 64Cu, 68Ga), 1,4,7,10-tetraazacyclododecane-tetraacetic acid (DOTA) or 1,4,7-triazacyclononane-triacetic acid (NOTA).
申请公布号 US2016287729(A1) 申请公布日期 2016.10.06
申请号 US201415030554 申请日期 2014.10.23
申请人 THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERV ;THE RESEARCH FOUNDATION OF THE STATE UNIVERSITY OF NEW YORK 发明人 WILLIAMSON Peter R.;KIESEWETTER Dale O.;PANEPINTO John;QIU Jin
分类号 A61K51/04;C07D251/68;C07B59/00 主分类号 A61K51/04
代理机构 代理人
主权项 1. A compound according to the formula wherein R1 is an amine, a hydroxyl group, a sulfide, a carboxylic acid, an amide, an alkyl or aryl; R2 is —NHC(O)—R3—L or —C(O)NH—R3—L, wherein R3 is an aryl, aliphatic (such as alkyl), and L is 18F or a chelator capable of chelating a radiolabel (such as chelators for [18F]AlF, 64Cu, 68Ga), 1,4,7,10-tetraazacyclododecane-tetraacetic acid (DOTA) or 1,4,7-triazacyclononane-triacetic acid (NOTA).
地址 Bethesda MD US