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公开(公告)号：US09968693B2
公开(公告)日：2018-05-15
申请号：US15030554
申请日：2014-10-23
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services , The Research Foundation of the State University of New York
IPC分类号： C07D251/68 , A61K31/53 , A61K51/04 , A61P31/10 , C07B59/00
CPC分类号： A61K51/0461 , A61K31/53 , C07B59/002 , C07D251/68
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).
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公开(公告)号：US10383960B2
公开(公告)日：2019-08-20
申请号：US15961554
申请日：2018-04-24
申请人： The United States of America, as represented by the Secretary, Department of Health and Human Services , The Reearch Foundation of the State University of New York
IPC分类号： C07D251/68 , A61K31/53 , A61K51/04 , C07B59/00
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).
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公开(公告)号：US20180236111A1
公开(公告)日：2018-08-23
申请号：US15961554
申请日：2018-04-24
申请人： The United States of America, as represented by the Secretary, Dept. of Health and Human Services , The Research Foundation of the State University of New York
IPC分类号： A61K51/04 , C07D251/68 , C07B59/00 , A61K31/53
CPC分类号： A61K51/0461 , A61K31/53 , C07B59/002 , C07D251/68
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).
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