5-芳基氨基甲酰基-2-甲基异恶唑烷-3-基-3-膦酸酯已经由N-甲基-C-二乙氧基磷酰基硝酮和N-芳基丙烯酰胺以良好收率合成。评估了本文获得的顺式和反式异恶唑烷膦酸盐对广泛的 DNA 和 RNA 病毒的活性。没有一种化合物在亚毒性浓度下具有抗病毒活性。已发现具有被卤素取代的苯基的异恶唑烷(Ar = 2-FC 6 H 4;3-Br-C 6 H 4;和 4-Br-C 6 H 4)可抑制 L1210、CEM 和 HeLa 细胞的增殖带集成电路50在 100–170 μM 范围内。
[EN] HETEROCYCLIC COMPOUNDS AND IMAGING AGENTS FOR IMAGING HUNTINGTIN PROTEIN<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET AGENTS D'IMAGERIE POUR L'IMAGERIE DE LA PROTÉINE HUNTINGTINE
申请人:CHDI FOUNDATION INC
公开号:WO2021252775A1
公开(公告)日:2021-12-16
Provided herein are certain compounds and imaging agents useful for detecting a disease or condition associated with protein aggregation, especially huntingtin protein aggregation, compositions thereof, and methods of their use.
The invention relates to novel compounds of the general formula (A-I), with Het-2 being an optionally substituted bicyclic heteroaryl of the formula (AA) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.