FABBRO, Doriano,HILLMANN-WÜLLNER, Petra,STÜTZ, Anton
申请号：
SG11202004589S
公开号：
SG11202004589SA
申请日:
2018.11.22
申请国别(地区):
SG
年份:
2020
代理人:
摘要：
The present invention 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 X1X2 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, C1-C2alkoxyC1-C3alkyl, CN, or C(0)0-C1- C2alkyl； or R3 and R4 form together a bivalent residue -R5R6- selected from C1-C3alkylene optionally substituted with 1 to 4 F, -CH2-0-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 C1-C3alkylene optionally substituted with 1 to 4 F, -CH2-0-CH2- or -0- CH2CH2-0-； with the proviso that at least one of R1 and R2 is a morpholinyl of formula II； and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in a method of treating a skin disorder in a subject, wherein said skin disorder is a genodermatosis, a vascular anomaly or a skin disorder selected from scleroderma, sclerodermatous chronic graft-versus-host disease, lichen sclerosus, lichen planus, lichen ruber planus and scars.
