Gray, Jeffrey Lyle,Clark, Cynthia Monesa,Amarasinghe, Kande,Maier, Mathew Brian,Nichols, Ryan
申请号：
ES14166121
公开号：
ES2660571T3
申请日:
2007.06.27
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A compound to be used in the treatment of vascular leak syndromes, the compound having the formula: ** (See formula) ** in which R is a unit chosen from: i) hydrogen； ii) phenyl, 4-fluorophenyl, 2-hydroxyphenyl, 3-methylphenyl, 2-amino-4-fluorophenyl, 2- (N, N-diethylamino) phenyl, 2- cyanophenyl, 2,6-di-tert-butylphenyl and 3 -methoxyphenyl； and iii) a heteroaryl unit selected from 1,2,3,4-tetrazol-1-yl, 1,2,3,4-tetrazol-5-yl, [1,2,3] triazol-4- yl, [1,2,3] triazol-5-yl, [1,2,4] triazol-4-yl, [1,2,4] triazol-5-yl, imidazol-2-yl, imidazol-4-yl , pyrrol-2-yl, pyrrol-3-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, [ 1,2,4] oxadiazol-3-yl, [1,2,4] oxadiazol-5-yl, [1,3,4] oxadiazol-2-yl, furan-2-yl, furan-3-yl, thiophene-2-yl, thiophene-3-yl, isothiazol-3-yl, isothiazol-4-yl, isothiazol-5-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, [1 , 2,4] thiadiazol-3-yl, [1,2,4] thiadiazol-5-yl, and [1,3,4] thiadiazol-2-yl； the heteroaryl unit may be substituted with one or more units selected from methyl, ethyl, n-propyl, iso-propyl, cyclopropyl, n-butyl, sec-butyl, iso-butyl, tert-butyl, cyclopropylmethyl, methoxy, ethoxy, n-propoxy, iso-propoxy, cyclopropoxy, n-butoxy, sec-butoxy, iso-butoxy, tert-butoxy, fluoro, chloro, fluoromethyl, difluoromethyl and trifluoromethyl, Z is a substituted or unsubstituted unit of [1,3, 4] thiadiazol-2-yl having the formula: ** (See formula) ** R1 is chosen from: i) hydrogen； ii) linear, branched or cyclic unsubstituted C1-C6 alkyl, or substituted, linear, branched or cyclic C1-C6 alkyl selected from hydroxymethyl, chloromethyl, trifluoromethyl, aminomethyl, 1-chloroethyl, 2- hydroxyethyl, 1,2-difluoroethyl, 2 , 2,2-trifluoroethyl, 3-carboxypropyl and 2,3-dihydroxycyclobutyl； iii) unsubstituted C6 or C10 aryl, or substituted C6 or C10 aryl selected from 2-fluorophenyl, 3-fluorophenyl, 4- fluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2-methylphenyl5, 3-methylphenyl, 4 -methylphenyl, 2- eth
