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：
CA3022758
公开号：
CA3022758A1
申请日:
2017.05.17
申请国别(地区):
CA
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 R2 is 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.
