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    • 26. 发明专利
    • SE345661B
    • 1972-06-05
    • SE483865
    • 1965-04-13
    • HOECHST AG
    • WEBER HAUMUELLER WSCHMIDT FWEYER RMUTH K
    • A61K31/64C07C67/00C07C301/00C07C303/36C07C303/40C07C311/54C07C311/58C07D335/02C07C143/82
    • The invention comprises compounds of formula wherein R is H or (optionally Ph substituted) C1- 4 alkyl; R1 is (a) C2- 8 alkyl, alkenyl or mercaptoalkyl, (b) C4- 8 alkoxyalkyl*, alkylmercaptoalkyl* or alkylsulphonylalkyl* (alkyl* at least C2), (c) phenyl-C1- 4 alkyl or -cyclopropyl, (d) cyclohexyl-C1- 4 alkyl, cycloheptyl-methyl or -ethyl, or cyclooctylmethyl, (e) C1- 2 endoalkylene-cyclohexyl, -cyclohexenyl, -cyclohexylmethyl or -cyclohexenylmethyl, (f) C1- 4-alkyl- or -alkoxy-cyclohexyl, (g) C5- 8 cycloalkyl, (h) cyclohexenyl or cyclohexenylmethyl, (i) a C4- 5+O or S heterocyclic nucleus which may be bound to the adjacent N by a methylene group; X is (i) C4- 11 alkyl, alkenyl, alkoxyalkyl, alkylmercaptoalkyl, cycloalkoxyalkyl, cycloalkylmercaptoalkyl, cycloalkylalkoxyalkyl or cycloalkylalkylmercaptoalkyl, (ii) (C4- 8 ring) cycloalkyl, cycloalkenyl, cycloalkyl-C1- 4 alkyl, cycloalkenyl-C1- 4 alkyl, C1- 4 alkyl-cycloalkyl or C1- 4 alkyl-cycloalkenyl, (iii) C1- 2 endoalkylene-cyclohexyl or -cyclohexenyl, (iv) alkyl, cycloalkyl or cycloalkylalkyl mono- or disubstituted by Cl, Br or CN; Y is a C1- 4 hydrocarbon radical. A large number of such compounds (with m.p.s.) are listed in the Specification. The compounds are prepared by (a) synthesizing the sulphonylurea group from compounds or oxidizing corresponding sulphonylthioureas sulphinylureas or sulphonylureas, (b) acylating corresponding aminoalkylphenylenesulphonylureas or (c) hydrogenating the corresponding compounds in which X is unsaturated. The above compounds are stated to possess blood sugar lowering properties and may be applied, as such or as salts, in the form of tablets containing the usual adjuncts such as talc, starch, lactose, tragacanth and Mg stearate.
    • 30. 发明专利
    • DK121116B
    • 1971-09-13
    • DK343966
    • 1966-07-01
    • HOECHST AG
    • SCHMIDT F
    • A61K31/64C07C67/00C07C301/00C07C303/36C07C303/40C07C311/54C07C311/58C07D335/02C07C143/78
    • The invention comprises compounds of formula wherein R is H or (optionally Ph substituted) C1- 4 alkyl; R1 is (a) C2- 8 alkyl, alkenyl or mercaptoalkyl, (b) C4- 8 alkoxyalkyl*, alkylmercaptoalkyl* or alkylsulphonylalkyl* (alkyl* at least C2), (c) phenyl-C1- 4 alkyl or -cyclopropyl, (d) cyclohexyl-C1- 4 alkyl, cycloheptyl-methyl or -ethyl, or cyclooctylmethyl, (e) C1- 2 endoalkylene-cyclohexyl, -cyclohexenyl, -cyclohexylmethyl or -cyclohexenylmethyl, (f) C1- 4-alkyl- or -alkoxy-cyclohexyl, (g) C5- 8 cycloalkyl, (h) cyclohexenyl or cyclohexenylmethyl, (i) a C4- 5+O or S heterocyclic nucleus which may be bound to the adjacent N by a methylene group; X is (i) C4- 11 alkyl, alkenyl, alkoxyalkyl, alkylmercaptoalkyl, cycloalkoxyalkyl, cycloalkylmercaptoalkyl, cycloalkylalkoxyalkyl or cycloalkylalkylmercaptoalkyl, (ii) (C4- 8 ring) cycloalkyl, cycloalkenyl, cycloalkyl-C1- 4 alkyl, cycloalkenyl-C1- 4 alkyl, C1- 4 alkyl-cycloalkyl or C1- 4 alkyl-cycloalkenyl, (iii) C1- 2 endoalkylene-cyclohexyl or -cyclohexenyl, (iv) alkyl, cycloalkyl or cycloalkylalkyl mono- or disubstituted by Cl, Br or CN; Y is a C1- 4 hydrocarbon radical. A large number of such compounds (with m.p.s.) are listed in the Specification. The compounds are prepared by (a) synthesizing the sulphonylurea group from compounds or oxidizing corresponding sulphonylthioureas sulphinylureas or sulphonylureas, (b) acylating corresponding aminoalkylphenylenesulphonylureas or (c) hydrogenating the corresponding compounds in which X is unsaturated. The above compounds are stated to possess blood sugar lowering properties and may be applied, as such or as salts, in the form of tablets containing the usual adjuncts such as talc, starch, lactose, tragacanth and Mg stearate.