发明名称 Benzimidazole derivs
摘要 - A = an opt. subst. aromatic or heteroaromatic residue with less than 3 condensed rings, such as R6 or R6CO, where R6 = aryl, aralkyl, heteroaryl, or heteroaralkyl - R' = -CH2-, -CH2CH2-, or -CH(Me)- - R2 = H, halogen, or an organic substit., e.g. OH, (1-6 C) alkyl,(1-6 C) Alkyl, nitroamino, NH alkyl, N(alkyl)2, NH(alkanoyl), alkanoyl, N(hydroxyalkyl)2, - SO2N(alkyl)2, SCH2Ph, aminoalkyl, CF3S, PhCH2O, (2-6 C) alkenyl, (2-6 C) alkenyl O-, , , cyclopropylalkoxy, or cyclobutylalkoxy - R3 = H, halogen, CF3, (1-6 C) alkyl or (1-6 C) Alkyl - M = OZ where Z = a cation, OY, where Y = acyl, the residues - or the groups R4 or R5 where - R4 = NH2, NHMe, NHEt, NHPr, NHBu, NMe2, NEt2, MEET, NMeBu, NBu2, glycosamino, glycosylamino, NHalkyl, phenylethylamino, N-ethyl phenylethyl-beta-hydroxy-ethylamino, 1-ethyl-2-aminomethylpiperidino, tetrahydrofurfurylamino, 1,25,6-tetrahydropyridino, sodium beta-sulphoethylamino, N,N-dimethyl-carboxamido-methylamino, Et2NCH2CH2NH- , or a 1-methyl-2-amino-methylpyrrolidine residue, amd R6 = a substd. hydroxy, hydrocarbonoxy, or polyhydroxy residue, or a cyclic alkylaminoalkyl) residue derived from N-(beta-hydroxyethyl) piperidine, pyrrolidine, N-methylpiperazine, or morpholine, 4-dimethylamonocyclohexyl, N methyl-2-hydroxymethyl-piperidine or pyrrolidine, N-ethyl-3-hydroxymethylpiperidine, or 3-hydroxyquinuclidine. - (III) X = halogen, CF3, Alkyl, alkyl, NO2, or N(alkyl)2. - (IV);(I), (II) and (III), where the posts. alpha- to the CO gp. (i.e. in R') are substd. by opt. subst. alkyl, aryl, or aralkyl. - (III) Intermediates for (I) and (II). - (I) and (III) Anti-inflammatories, antipyretics, and analgesics. - Dose 10-2,000 mg./d.
申请公布号 CH509321(A) 申请公布日期 1971.06.30
申请号 CH19700005050 申请日期 1967.11.29
申请人 MERCK & CO., INC. 发明人 SHEN,TSUNG-YING;RICHARD MATZUK,ALEXANDER;SCHWAM,HARVEY
分类号 C07D235/06;C07D235/08;C07D235/10;C07D235/12;C07D235/14;C07D235/16;C07D235/18;(IPC1-7):C07D49/38 主分类号 C07D235/06
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