UNIVERSITY OF PITTSBURGH OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
发明人:
KLUNK, WILLIAM,MATHIS, CHESTER,WANG, YANMING
申请号：
ES10185669
公开号：
ES2536449T3
申请日:
2001.08.24
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
An amyloid binding compound of the following formula or a non-toxic water soluble salt thereof: wherein Z is S, NR , O or CR in which case the correct tautomeric form of the heterocyclic ring it be an indole in wherein R is H or a C1-C8 alkyl group: ** ** Formula Y is NR1R2, OR2 or SR2 wherein the nitrogen of Formula ** ** is not a quaternary amine each of R1 and R2 is independently selected from the group consisting of H, a C1-C8 alkyl group, (CH2) nOR (wherein n> = 1, 2, or 3), CF3, CH2-CH2X, CH2-CH2 -CH2X (wherein X> = F, Cl, Br or I), (C> = O) -R , Rph, (CH2) nRph (wherein n> = 1, 2, 3 or 4 and Rph represents an phenyl unsubstituted or substituted, wherein the substituents of Rph are selected from the group consisting of F, Cl, Br, I, a C1-C8 alkyl, (CH2) nOR (wherein n> = 1, 2, or 3 ), CF3, CH2-CH2X, O-CH2-CH2X, CH2-CH2-CH2X, O-CH2-CH2-CH2X (wherein X> = F, Cl, Br or I), CN, (C> = O) -R , N (R) 2, NO2, (C> = O) N (R ) 2, O (CO) R, oR , SR, COOR (wherein R is H or C1-C8 alkyl group), a trialkyl-tin and a chelating group (with or without a chelated metal group) of the form WL or VWL, wherein V is selected from the group consisting of -COO-, -CO-, -CH2O- - and -CH 2 NH- W is - (CH2) n where n> = 0, 1, 2, 3, 4 or 5 and L is: ** ** Formula wherein M is selected from the group consisting of Tc and re, and R is H or a C 1-C8 alkyl) each of R3-R10 are independently selected from the group consisting of H, F, Cl, Br, a C1-C8 alkyl group, (CH2) nOR (wherein n> = 1, 2, or 3), CF3, CH2 -CH2X, O-CH2-CH2X, CH2-CH2-CH2X, O-CH2-CH2-CH2X (wherein X> = F, Cl, Br or I), CN, (C> = O) -R , N (R ) 2, NO2, (C> = O) N (R) 2, O (CO) R , OR, SR , COOR, Rph, CR > = CR-Rph, CR2 > CR2-Rph = a trialkyl tin and a chelating group (with or without a chelated metal group) of the form WL or VWL, wherein V is selected from the group consisting of -COO-, -CO-, -CH2O- - and -CH 2 NH- W is - (CH2) n where n> = 0, 1, 2, 3, 4 or 5 and L is: ** ** FormulaUn compuesto fijador de amiloide de la fórmula s
