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61. 发明专利

SE339221B 未知
公开(公告)号：SE339221B
公开(公告)日：1971-10-04
申请号：SE1635867
申请日：1967-11-29
申请人： HOECHST AG
发明人： WEYER R , MUTH K , WEBER H , AUMUELLER W , SCHMIDT F
IPC分类号： A61K31/64 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/59 , C07C143/833

62. 发明专利

DK121115B 未知
公开(公告)号：DK121115B
公开(公告)日：1971-09-13
申请号：DK343866
申请日：1966-07-01
申请人： HOECHST AG
发明人： SCHMIDT F
IPC分类号： A61K31/64 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/58 , C07D335/02 , C07C143/78
摘要： 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.

63. 发明专利

DK119456B 未知
公开(公告)号：DK119456B
公开(公告)日：1971-01-11
申请号：DK337466
申请日：1966-06-29
申请人： HOECHST AG
发明人： SCHMIDT F
IPC分类号： A61K31/17 , A61K31/64 , A61P3/08 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/58 , C07D335/02 , C07C127/22 , C07C143/78 , C07D27/50

64. 发明专利

NO119679B 未知
公开(公告)号：NO119679B
公开(公告)日：1970-06-22
申请号：NO15768365
申请日：1965-04-13
申请人： HOECHST AG
发明人： WEBER H , AUMUELLER W , WEYER R , MUTH K , SCHMIDT F
IPC分类号： A61K31/64 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/58 , C07D335/02
摘要： 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.

65. 发明专利

NO118555B 未知
公开(公告)号：NO118555B
公开(公告)日：1970-01-12
申请号：NO16030665
申请日：1965-11-02
申请人： HOECHST AG
发明人： SCHMIDT F , MUTH K , WEYER R , AUMUELLER W , WEBER H

66. 发明专利

NO118553B 未知
公开(公告)号：NO118553B
公开(公告)日：1970-01-12
申请号：NO16030465
申请日：1965-11-02
申请人： HOECHST AG
发明人： MUTH K , WEYER R , WEBER H , SCHMIDT F , AUMUELLER W

67. 发明专利

NO118548B 未知
公开(公告)号：NO118548B
公开(公告)日：1970-01-12
申请号：NO15518864
申请日：1964-10-17
申请人： HOECHST AG
发明人： MUTH K , SCHMIDT F , WEBER H , AUMUELLER W , WEYER R
IPC分类号： A61K31/64 , C07C311/59 , C07D307/22 , C07D307/52 , C07D309/04 , C07D317/68 , C07D333/20 , F16D65/095
摘要： Cpds. (I) where Z = C4-5 alkyl, cycloalkyl, alkoxy or cycloalkoxy; lower alkylmercapto, alkylsulphinyl or alkylsulphonyl; Ph, PhCH2, PhCH2O, lower alkanoyl, aroyl, CF3, OH, acyloxy, COOH or CN; or carbamyl optionally subst. by lower alkyl groups; Z' = H or (when Z = OH or COOH) also halogen, lower alkyl or lower alkoxy; Y = C1-3 straight or branched hydrocarbon residue; R1 = saturated or unsaturated C2-8 alkyl; C4-8 alkyl interrupted by O or S; PhCH2, phenyl-ethyl, cyclohexylmethyl or cyclohexylethyl; cyclohexyl subst. by Me, Et, Pr, i-Pr, MeO, EtO, PrO or i-PrO; C5-8 cycloalkyl; or saturated or unsaturated cycloalkyl or cycloalkylmethyl with 4-5 ring C atoms and contng. an O or S atom in the ring; and their salts. Strong and long-acting hypoglycaemics. N-(4-(2-(4-BuO-benzamido) ethyl)-benzenesulphonyl)-N'-cyclohexylurea, m.p. 197-9 deg. (from MeOH/dioxan.).

68. 发明专利

NO117479B 未知
公开(公告)号：NO117479B
公开(公告)日：1969-08-18
申请号：NO15999865
申请日：1965-10-08
申请人： HOECHST AG
发明人： AUMUELLER W , WEYER R , SCHMIDT F , WEBER H , MUTH K
IPC分类号： A61K31/64 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/58 , C07D335/02
摘要： Novel sulphonyl ureas of the formula wherein R is hydrogen or a lower alkyl or a phenyl lower alkyl group; R1 is (a) an alkyl, alkenyl or mercaptoalkyl group of 2-8 carbon, atoms, (b) an alkoxyalkyl, alkylmercaptoalkyl or alkylsulphinylalkyl group of 4-8 carbon atoms at least two of which form the alkylene portion of the group, (c) a phenyl lower alkyl or phenylcyclopropyl group, (d) a cyclohexyl lower alkyl, cycloheptylmethyl, cycloheptylethyl or cyclooctylmethyl group, (e) an endoalkylene-cyclohexyl, endoalkylene-cyclohexenyl, endoalkylene-cyclohexylmethyl or endoalkylene-cyclohexenylmethyl group each containing 1 or 2 endoalkylene carbon atoms, (f) a lower alkyl-cyclohexyl or a lower alkoxycyclohexyl group, (g) a cycloalkyl group containing 5-8 carbon atoms, (h) a cyclohexenyl or cyclohexenylmethyl group, (i) a heterocyclic ring containing 4 or 5 carbon atoms and one oxygen or sulphur atom optionally containing 1 or 2 ethylenic double bonds or (k) a heterocyclic ring as defined under (i) linked to the nitrogen atom by a methylene group; X is a C1- 6 hydrocarbon group optionally bearing halogen, hydroxy, oxo, lower acyloxy or lower alkoxy substituents; Y is a C1- 4 hydrocarbo group; Z is hydrogen or a halogen or a lower alkyl, lower alkoxy, C5- 6 cycloalkoxy, cyclohexyl, lower alkylmercapto, lower alkylsulphinyl, lower alkylsulphonyl, phenylsulphonyl, phenyl, phenyl lower alkyl, lower acyl, benzoyl, trifluoromethyl, hydroxyl, lower acyloxy, benzyloxy, carboxyl, carbalkoxy, nitrile, carbamoyl, lower alkylcarbamoyl, di-lower alkyl-carbamoyl or nitro group; Z1 and Z2 (if Z is hydrogen or halogen or an hydroxyl, carboxyl, alkyl or alkoxy group) may each be hydrogen, halogen, lower alkyl or lower alkoxy or (if Z is a hydrogen atom) may together form a methylenedioxy group or (if Z has any other meaning) are each a hydrogen atom, and the "phenylene" radical optionally bears halogen, alkyl or alkoxy substituents (the term "lower" being used to denote a group of up to 4 carbon atoms) are made by the following methods (a) reaction between an amine R1NH2 and the appropriate benzenesulphonyl isocyanate or a compound which reacts like an isocyanate such as a carbamic ester, carbamic halide, thiocarbamic ester or urea, or conversely, by reaction of an R1 substituted isocyanate or its equivalent with an appropriately substituted benzenesulphonamide; (b) reaction of a benzenesulphonyl chloride bearing the appropriate phenylalkanoylaminoalkyl substituent with an R1 substituted urea, iso-urea ether, isothiourea ether or parabanic acid and, if required, hydrolysing the product obtained; (c) replacement of the sulphur atom in a corresponding benzenesulphonyl thiourea by oxygen; (d) oxidation of the corresponding benzenesulphenyl or benzenesulphinyl ureas; (e) acylation of a benzenesulphonyl urea of the formula R2N.Y.phenylene.SO2.NH.CO.NHR1 to introduce the appropriate phenyl-X-CO-radical; (f) treatment of a benzenesulphonyl urea of the formula given which contains etherified hydroxy or esterified carboxylic groups to liberate the free hydroxy or carboxylic group; (g) hydrogenation of a compound of the above general formula in which X contains an ethylenic double bond to give the corresponding saturated compound. Pharmaceutical preparations having hypoglycaemic activity comprise the above compounds of the invention in admixture or conjunction with a carrier, preferably in a form adapted to oral administration.

69. 发明专利

NO117177B 未知
公开(公告)号：NO117177B
公开(公告)日：1969-07-14
申请号：NO15975465
申请日：1965-09-18
申请人： HOECHST AG
发明人： WEBER H , AUMUELLER W , SCHMIDT F , WEYER R , MUTH K
IPC分类号： A61K31/64 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/54 , C07C311/58 , C07D327/06 , C07D335/02

70. 发明专利

SE311151B 未知
公开(公告)号：SE311151B
公开(公告)日：1969-06-02
申请号：SE1245964
申请日：1964-10-16
申请人： HOECHST AG
发明人： WEBER H , AUMUELLER W , WEYER R , MUTH K , SCHMIDT F
IPC分类号： A61K31/64 , C07C311/59 , C07D307/22 , C07D307/52 , C07D309/04 , C07D317/68 , C07D333/20 , F16D65/095 , C07C143/833
摘要： Cpds. (I) where Z = C4-5 alkyl, cycloalkyl, alkoxy or cycloalkoxy; lower alkylmercapto, alkylsulphinyl or alkylsulphonyl; Ph, PhCH2, PhCH2O, lower alkanoyl, aroyl, CF3, OH, acyloxy, COOH or CN; or carbamyl optionally subst. by lower alkyl groups; Z' = H or (when Z = OH or COOH) also halogen, lower alkyl or lower alkoxy; Y = C1-3 straight or branched hydrocarbon residue; R1 = saturated or unsaturated C2-8 alkyl; C4-8 alkyl interrupted by O or S; PhCH2, phenyl-ethyl, cyclohexylmethyl or cyclohexylethyl; cyclohexyl subst. by Me, Et, Pr, i-Pr, MeO, EtO, PrO or i-PrO; C5-8 cycloalkyl; or saturated or unsaturated cycloalkyl or cycloalkylmethyl with 4-5 ring C atoms and contng. an O or S atom in the ring; and their salts. Strong and long-acting hypoglycaemics. N-(4-(2-(4-BuO-benzamido) ethyl)-benzenesulphonyl)-N'-cyclohexylurea, m.p. 197-9 deg. (from MeOH/dioxan.).

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