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    • 51. 发明专利
    • Benzenesulphonyl-ureas and process for preparing them
    • CY451A
    • 1968-08-23
    • CY45168
    • 1968-08-23
    • HOECHST AG
    • A61K31/64C07D209/46C07D335/02C07D27/50
    • Novel benzenesulphonyl ureas of the Formula I and their physiologically tolerable salts wherein R is H or CH3, Z and Z1 are H or halogen atoms or C1- 4 alkyl or alkoxy groups, Y is a straight or branched chain hydrocarbon group of 1-4 carbon atoms and R1 is (a) a 3 or 4 carbon atom alkyl group; (b) a cyclohexylmethyl group; (c) a C1- 3-alkyl-cyclohexyl or C1- 3 alkoxy-cyclohexyl group; (d) a C5- 8 cycloalkyl group; (e) a cyclohexenyl or cyclohexenylmethyl group; or (f) an endoalkylenecyclohexyl, - cyclohexenyl, - cyclohexylmethyl or -cyclohexenylmethyl group each containing 1 or 2 endoalkylene carbon atoms, are made by (a) reacting an appropriately substituted benzenesulphonyl isocyanate, carbamic ester, thiocarbamic ester, carbamic halide or urea with an amine R1NH2; (b) reacting an R1 substituted isocyanate, carbamic or thiocarbamic ester, carbamic halide or urea with the appropriately substituted benzenesulphonamide; (c) hydrolysing the corresponding isourea or isothiourea ether or parabanic acid compound; (d) replacing the sulphur atom in a corresponding benzenesulphonylthiourea by oxygen by known methods; (e) oxidizing a benzenesulphuryl or benzenesulphenyl urea; or (f) subjecting a compound of the Formula III or IV to ring closure Phthalimidinoalkyl - benzenesulphonamides 4-(b - Phthalimidinoethyl) - benzenesulphonamide is made by reacting phthalide with 4-(b -aminoethyl) - benzenesulphonamide and subjecting the resulting 4-(b -o-hydroxymethyl-benzamidoethyl) - benzenesulphonamide to ring closure. 4 - (b - Phthalimidino - a - methylethyl)- benzenesulphonamide is made by reacting 4-a -methyl - b - aminoethyl) benzenesulphonamide with phthalic anhydride and reducing the resulting 4 - (b - phthalimido - a - methylethyl)-benzenesulphonamide with tin and HCl. 4-(b - 5 - Chlorophthalimidoethyl) - benzenesulphonamide is made by reducing the corresponding phthalimide derivative. 4 - Phthalimidinomethyl - benzenesulphonamide and 4 - (b - 3 ethyl - phthalimidinoethyl)-benzenesulphonamide are made by chlorosulphonating the corresponding phthalimidinoalkyl benzenes and treating the resulting sulphonyl chlorides with ammonia. 4 - (b - o - Hydroxymethylbenzamidoethyl)-benzenesulphonamide is prepared by reaction of 4 - (b - aminoethyl) - benzenesulphonamide with phthalide. N - [4 - (b - Phthalimidino - ethyl) - benzenesulphonyl] - N1 - cyclohexyl - isourea methyl ether is formed by treating the corresponding thiourea compound with mercury oxide in methanol. N - [4 - (b - Phthalimidinoethyl) - benzenesulphonyl]-carbamic acid methyl ester is obtained by the action of methyl chloroformate on the corresponding sulphonamide. Pharmaceutical preparations having hypoglycaemic activity comprise the above novel compounds in admixture or conjunction with a carrier preferably in a form adapted to oral administration such as tablets.
    • 56. 发明专利
    • HU166919B
    • 1975-06-28
    • HURO000767
    • 1974-02-06
    • C07D209/48C07D209/44C07D401/04C07D27/50
    • Procedure for preparing new isoindoline derivatives, of general formula: ** formula ** in which Ar represents a phenyl radical or a pyridyl radical, optionally substituted by 1 or 2 atoms or radicals, identical or different, chosen from among the atoms of halogen and alkyl radicals containing 1 to 4 carbon atoms, alkyloxy, the alkyl part of which contains 1 to 4 carbon atoms, cyano and trifluoromethyl, T represents a straight or branched alkylene radical containing 2 to 6 atoms of carbon, and R1 and R2 identical or different, represent a hydrogen atom or a straight or branched alkyl radical containing from 1 to 4 carbon atoms, as well as their addition salts with acids, characterized in that an amine is reacted, of general formula ** formula ** in which R1 and R2 are defined as above, on an isoindoline derivative, of general formula ** formula ** in which Ar and T are defined as above and Z represents a residue of this reagent and then the product obtained is eventually transformed into an addition salt with an acid. (Machine-translation by Google Translate, not legally binding)