[EN] SUBSTITUTED TRIAZINES AS PRION PROTEIN LIGANDS AND THEIR USE TO DETECT OR REMOVE PRIONS<br/>[FR] TRIAZINES SUBSTITUES UTILISES COMME LIGANDS DES PROTEINES PRIONS, ET LEUR UTILISATION POUR LA DETECTION OU L'EXTRACTION DES PRIONS
申请人:PROMETIC BIOSCIENCES LTD
公开号:WO2006010915A1
公开(公告)日:2006-02-02
Compounds of formula (I) wherein R1 and R2 are the same or different and are each optionally substituted alkyl, optionally substitued cycloalkyl, optionally subsituted aryl or optianally substituted heteroaryl groups; R3 is hydrogen or an aryl group substituent or R3 is a solid support optionally attached via a spacer; Z represents an oxygen atom, a sulphur atom or NR4; Y represents an oxygen atom, a sulphur atom or NR5; in which R4 and R5, which may be the same or different, represent hydrogen, optionally substituted alkyl containing 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted benzyl or optionally substituted β-phenylethyl; and one of X1 and X2 represents a nitrogen atom and the other of X1 and X2 represents a nitrogen atom or CR6, in which R6 represents hydrogen or an aryl group substituent; are useful for the affinity binding of a prion protein.
式(I)中的化合物,其中R1和R2相同或不同,分别是可选择取代的烷基、可选择取代的环烷基、可选择取代的芳基或可选择取代的杂芳基;R3是氢或芳基取代基,或R3是通过空间连接的固体支持;Z代表氧原子、硫原子或NR4;Y代表氧原子、硫原子或NR5;其中R4和R5可能相同也可能不同,代表氢、含有1至6个碳原子的可选择取代的烷基、可选择取代的苯基、可选择取代的苄基或可选择取代的β-苯乙基;X1和X2中的一个代表氮原子,另一个代表氮原子或CR6,其中R6代表氢或芳基取代基;用于朊蛋白的亲和结合。