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method for preparing preparations with blood sugar lowering activity.formed preparations and method for the preparation of compounds with blood sugar lowering activity.
method for preparing preparations with blood sugar lowering activity.formed preparations and method for the preparation of compounds with blood sugar lowering activity.
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机译:制备具有降血糖活性的化合物的方法。形成的制剂和制备具有降血糖活性的化合物的方法。
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摘要
Novel benzenesulphonyl ureas of the formula X - CO - NR - Y - phenylene - SO2-NH-CO-NHR1 in which R is hydrogen, lower alkyl or lower phenylalkyl, R1 represents (a) C2- 8 alkyl, alkenyl or mercapto alkyl; (b) C4- 8 alkoxyalkyl, alkylmercaptoalkyl or alkysulphinylalkyl having at least 2 carbon atoms in the alkylene part of the radical; (c) phenyl-lower alkyl or phenylcyclopropyl; (d) cyclohexyl - lower alkyl, cycloheptylmethyl, cycloheptylethyl or cyclooctylmethy; (e) endoalkylene - cyclohexyl, endoalkylene-cyclohexenyl, endoalkylene - cyclohexylmethyl or endoalkylene - cyclohexenylmethyl, having 1 or 2 endoalkylene carbon atoms; (f) lower alkyl- or lower alkoxycyclohexyl; (g) C5- 8 cycloalkyl; (h) cyclohexenyl or cyclohexenylmethyl; (i) a heterocyclic ring with 4 or 5 carbon atoms and one O or S atom, optionally containing one or two ethylenic double bonds; or (k) a heterocyclic ring as in (i) linked to the nitrogen atom through a -CH2- linkage, X represents (a) thiophenyl or thiophenoxy optionally containing 1 or 2 halogen, lower alkyl, lower alkoxy, lower alkenyloxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy or aryl substituents or a -(CH2)3- or -(CH2)4-chain linked at both ends to the thiophene nucleus; (b) furyl optionally bearing halogen or methyl substituents; or (c) pyridyl optionally bearing 1 or 2 halogen or lower alkyl substituents, the radicals specified under (a), (b) and (c) being linked to the rest of the molecule directly or through a hydrocarbon chain of 1 or 2 carbon atoms, and Y is a hydrocarbon chain of 1-4 carbon atoms (the word "lower" throughout indicating a group having up to 4 carbon atoms), are made by the following processes: (a) reacting a benzenesulphonyl-isocyanate, -carbamic ester, -carbamic halide, -thiocarbamic ester or -urea, substituted by the group X.CO.NR.Y- with an amine R1NH2; (b) reacting a benzenesulphonamide, X.CO.NR.Y.-phenylene. SO2NH2, with an R1-substituted isocyanate, carbamic acid ester, thiocarbamic acid ester, carbamic halide or urea; (d) hydrolysing a correspondingly substituted benzenesulphonyl-isourea ether, -isothiourea ether or parabanic acid; (e) replacing the sulphur atom in a correspondingly substituted benzenesulphonyl-thiourea by an oxygen atom; (f) oxidizing a corresponding benzenesulphinyl or benzenesulphenyl urea; or (g) introducing the radical X-CO- by acylation into a benzenesulphonyl urea of the formula R.NH.Y.-phenylene.SO2.NH.CO.NHR1., and if desired treating the reaction products with an alkaline agent to form the salts. The preparation of 4 - (b - thiophene - 2 - carbonamido - ethyl) - benzenesulphonamide, 4-(b - 5 - chlorothiophene - 2 - carbonamidoethyl)-benzenesulphonamide, N - [4 - (b - thiophene - 2-carbonamidoethyl) - benzenesulphonyl] - N1-cyclohexyl thiourea, N - [4 - (b - thiophene - 2-carbonamidoethyl) - benzenesulphonyl] - N1-cyclohexylisourea methyl ether, 4 - (b - furoylaminoethyl) - benzenesulphonamide, 4 - (b -furyl - 2 - propionamidoethyl) - benzenesulphonamide, N - [4 - (b - furoylaminoethyl) - benzenesulphonyl] - carbamic acid methyl ester, N-[4-(b - furoylaminoethyl) - benzenesulphonyl] - urea, N - [4 - (b - furoylaminoethyl) - benzenesulphonyl]-N1 - isobutyl urea, N - [4 - (b - furoylaminoethyl) - benzenesulphonyl] - N1 - isobtuyl - isourea methyl ether and 4-(pyridine-3-carboxamidomethyl) -benzenesulphonamide, used as starting materials, is described. Pharmaceutical preparations for the treatment of diabetes comprise the above compounds of the invention in admixture or conjunction with a carrier, preferably in a form adapted to oral administration.
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