发明名称 AMINO ALCOHOL DERIVATIVES FOR THE TREATMENT OF DEMYELINATING PERIPHERAL NEUROPATHIES.
摘要 A compound of formula V or formula Vl for use in the treatment of a demyelinating peripheral neuropathy: 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 is H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or CMalkoxymethyl; 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; and the N-oxide derivatives thereof or prodrugs thereof, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4alkylsulifinyl, C1-4alkyl-sulfonyl, aralkyl, optionally substituted phenoxy or aralkyloxy; R2a is H, halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, aralkyl or aralkyloxy; R3a is H, halogen, CF3, C1-4alkyl, C1-4alkoxy, C1-4alkylthio or benzyloxy; R4a is H, C1-4alkyl, phenyl, optionally substituted benzyl or benzoyl, or lower aliphatic C1-5acyl; R5a is H, monohalomethyl, C1-4alkyl, C1-4alkoxy-methyl, C1-4alkyl-thiomethyl, hydroxyethyl, hydroxypropyl, phenyl, araikyl, C2-4alkenyl or -alkynyl; R6a is H or C1-4alkyl; R7a is H, C1-4alkyl or a residue of formula (a) as defined above, X3 is O, S, SO or SO2; na is an integer of 1 to 4; and designates a chiral centre of (R) or (S) configuration and the formula includes racemic and other mixtures of (R) and (S) configuration molecules; and the N-oxide derivatives thereof or prodrugs thereof, or a pharmaceutically acceptable salt, solvate or hydrate thereof.
申请公布号 MX2011001881(A) 申请公布日期 2011.05.30
申请号 MX20110001881 申请日期 2009.08.17
申请人 NOVARTIS AG. 发明人 BARBARA NUESSLEIN-HILDESHEIM;DAVID LEPPERT;ERIK WALLSTROEM
分类号 A61K31/137;A61K31/16;A61K31/34;A61K31/417;A61K31/42;A61K31/436;A61K31/52;A61K31/56;A61K31/675;A61K38/13;A61K38/21;A61K39/395;A61K45/06;A61P25/00 主分类号 A61K31/137
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