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TREATMENT OF AUTOIMMUNE DISEASES
专利权人:
NOVARTIS AG
发明人:
ERIK WALLSTROEM,PETER GERGELY
申请号:
BR112012028190
公开号:
BR112012028190A2
申请日:
2011.05.05
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
treatment of autoimmune diseases. The present invention relates to the use of a compound of formula I: wherein x is o, s, so or so2; R1 is halide, trialomethyl, -oh, C1-7 alkyl, C1-4 alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, -ch2-oh, -ch2-ch2-oh, C1-alkylthio -4-alkylsulfinyl, C 1-4 alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylac 1-4 alkyl or phenyl-C 1-4 alkoxy, each phenyl group thereof being optionally substituted by halide, C 3-3, C 1-4 alkyl or C 1-4 alkoxy; R 2 is h, halide, rialomethyl, C 1-4 alkoxy, C 1-7 alkyl, phenethyl or benzyloxy; R 3 is halide, C 1-3, oh, C 1-7 alkyl, C 1-4 alkoxy, benzyloxy, phenyl or C 1-4 alkoxymethyl; 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 halide; and right an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula ii wherein R 1a is halide, trialomethyl, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, aralkyl, optionally substituted phenoxy or aralkyloxy; R 2a is h, halide, trialomethyl, C 1-4 alkyl, C 1-4 alkoxy, aralkyl or aralkyloxy; R 3a is h, halide, C 1-3, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio or benzyloxy; R 4a is h, C 1-4 alkyl, phenyl, optionally substituted by benzyl or benzoyl, or C 1-5 lower aliphatic acyl; R 5a is h, monohalomethyl, C 1-4 alkyl, C 1-4 alkoxy methyl, C 1-4 alkylthiomethyl, hydroxyethyl, hydroxypropyl, phenyl, aralkyl, C 2-4 alkenyl or alkynyl; R 6a is h or C 1-4 alkyl; R7a is C1-4alkyl or a residue of formula (a) as defined above, xa is o, s, so or so2; and na is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isometer or prodrug thereof; in the manufacture of a medicament for the treatment or prophylaxis of subacute cutaneous lupus erythematosus (scl
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