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TRAITEMENT DE LÉSIONS CUTANÉES
专利权人:
PIQUR THERAPEUTICS AG;THE TRUSTEES OF THE UNIVERSITY OF PENNESYLVANIA
发明人:
FABBRO, Doriano,HEBEISEN, Paul,HILLMANN-WUELLNER, Petra,STUETZ, Anton,SEYKORA, John, T.,BEAUFILS, Florent
申请号:
EPEP2017/025137
公开号:
WO2017/198347A1
申请日:
2017.05.17
申请国别(地区):
EP
年份:
2017
代理人:
摘要:
The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1 X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1alkoxyC1-C3alkyl, CN, or C(O)O-C1-C2alkyl; or R3 and R4 form together a bivalent residue -R5R6- selected from C1-C3alkylene optionally substituted with 1 to 4 F, -CH2-O-CH2-, -CH2-NH-CH2-, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue-R8R9- selected from Ci-C3alkylene optionally substituted with 1 to 4 F, -CH2-O-CH2- or -O-CH2CH2-O-; with the proviso that at least one of R1 and R2is a morpholinyl of formula II; and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a skin lesion in a subject.La présente invention concerne un composé de formule (I), où X1, X2 et X3 sont, indépendamment les uns des autres, N ou CH; sous réserve qu'au moins deux éléments parmi X1, X2 et X3 soient N; Y est N ou CH; W est H ou F; sous réserve que, lorsque W est F, X1, X2 et X3 soient N; R1 et R2 sont, indépendamment l'un de l'autre, (i) un morpholinyl de la formule (II) où la flèche représente la liaison dans la formule (I); et où R3 et R4 sont, indépendamment l'un de l'autre, H, un alkyle en C1-C3
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