发明名称 | Synthesis and application of novel imaging agents conjugated to DPA 713 analogs for imaging inflammation | ||
摘要 | The present invention provides analog compounds of DPA-713 which specifically bind the translocator protein (TSPO), which is upregulated in activated leukocytes, some malignant tumors and tissues involved in steroid biogenesis. These compounds are linked via a linking moiety to a variety of imaging agents, including, for example, near infra-red dyes. The compounds of the present invention are useful for both pre-clinical near-IR fluorescence imaging (NIRF) and use in optically-guided interventions including NIRF endoscopy. Methods of use in diagnosis and treatment of TSPO related disease are also provided. | ||
申请公布号 | US9498546(B2) | 申请公布日期 | 2016.11.22 |
申请号 | US201314385090 | 申请日期 | 2013.03.14 |
申请人 | THE JOHNS HOPKINS UNIVERSITY | 发明人 | Pomper Martin Gilbert;Wang Haofan;Foss Catherine Anne |
分类号 | A61B5/00;A61B8/00;A61B10/00;A61K49/00;C07D487/04;G01N33/574;G01N33/58 | 主分类号 | A61B5/00 |
代理机构 | Ward and Smith, P.A. | 代理人 | Ward and Smith, P.A. ;Childers Jeffrey W. |
主权项 | 1. A compound of formula I: wherein R1, R2, R3 and R4 independently represent hydroxyC1 to C10 alkyl, alkylamino, alkyl, alkylamino, alkenyl, alkynyl, hydroxyalkyl, alkoxy, dialkylamino thioalkyl, thioalkenyl, thioalkynyl, aryloxy, acyloxy, thioacyl, amido, and sulphonamido; wherein each of alkyl, or aryl moiety may be unsubstituted or substituted with one or more substituents selected from the group consisting of halo, hydroxy, carboxy, phosphoryl, phosphonyl, phosphono C1-C6 alkyl, carboxy C1-C6 alkyl, dicarboxy C1-C6 alkyl, dicarboxy halo C1-C6 alkyl, sulfonyl, cyano, nitro, alkoxy, alkylthio, acyl, acyloxy, thioacyl, acylthio, aryloxy, amino, alkylamino, dialkylamino, trialkylamino, arylalkylamino, guanidino, aldehydo, ureido, and aminocarbonyl, an amino acid residue, or a substituted amino acid residue; L is a linker of 1-10 carbon atoms; and I is an imaging agent covalently linked to the linker via an amide linkage. | ||
地址 | Baltimore MD US |