Publication number: 20170119702
Abstract: A compound of formula I: wherein X is O, S, SO or SO2; R1 is halogen, trihalomethyl, —OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, —CH2—OH, —CH2—CH2—OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3 H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or C1-4alkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a) wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula II wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alko
Type:
Application
Filed:
October 19, 2016
Publication date:
May 4, 2017
Applicant:
Novartis AG
Inventors:
Peter Gergely, Erik Wallstroem, Eric Legangneux
Publication number: 20170119750
Abstract: Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
Type:
Application
Filed:
November 15, 2016
Publication date:
May 4, 2017
Inventors:
Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Robert John Sheppard, Ann Louise Walker, Christopher Wellaway, David Matthew Wilson