公开(公告)号：BR6465221D0

公开(公告)日：1973-09-11

申请号：BR16522164

申请日：1964-12-11

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07D235/06 ,  C07D235/08 ,  C07D235/18

Abstract: The invention comprises compounds of formula wherein R is halogen, alkyl or alkoxy, R1 is alkyl, R2 is H, alkyl, aralkyl or aryl, R3 is alkyl or aralkyl and X is an anion, and their double salts with ZnCl2. These compounds are prepared by quaternization of the corresponding benzimidazoles with R3X, optionally followed by double salt formation with ZnCl2.

公开(公告)号：BR6571713D0

公开(公告)日：1973-08-14

申请号：BR17171365

申请日：1965-07-30

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: A61K31/64 ,  C07D209/46 ,  C07D335/02

Abstract: 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.

公开(公告)号：BR6569651D0

公开(公告)日：1973-08-14

申请号：BR16965165

申请日：1965-05-14

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07F7/22

公开(公告)号：BR6462883D0

公开(公告)日：1973-08-07

申请号：BR16288364

申请日：1964-09-24

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07D295/18

Abstract: 1,054,758. Sulphonyl ureas. FARBWERKE HOECHST A.G. March 31, 1964 [Sept. 25, 1963], No. 13165/64. Heading C2C. Novel benzenesulphonyl ureas of the formula and their physiologically tolerable salts, wherein R 1 is a C 1-4 alkyl radical, a cycloalkyl radical of up to 8 carbon atoms, an alkyl substituted cycloalkyl radical or a cyclohexylmethyl or cyclohexylethyl radical, R 2 is hydrogen or a C 1-4 alkyl radical or R 1 and R 2 together with the nitrogen atom form a heterocyclic nucleus of 4-6 carbon atoms, X is -CH 2 -,-CH 2 CH 2 -, -CH = CH- or -CH(CH 3 )- and R 3 is a C 5-8 cycloalkyl, C 5-8 cycloalkenyl, lower alkyl substituted cyclohexyl, cyclohexylmethy), cyclohexylethyl or a benzyl or phenethyl radical are made by known methods for the manufacture of sulphonylureas as follows: (a) an R 1 R 2 N.CO.X-substituted benzenesulphonyl isocyanate or a compound which reacts as an isocyanate e.g. corresponding benzenesulphonyl carbamic or thiocarbamic esters or halides or benzenesulphonyl ureas and their N 1 -acyl derivatives is reacted with an amine R 3 NH 2 ; (b) an isocyanate R 3 NCO or a corresponding compound which reacts as an isocyanate e.g. a corresponding carbamic or thiocarbamic ester or halide or a urea or urea derivative R 3 NH. CO.NH 2 , R 3 NH.CO.NH Acyl or R 3 NH.CO.N (C 6 H 5 ) 2 is reacted with an R 1 R 2 N.CO.X- substituted benzenesulphonamide; or (c) a corresponding R 1 R 2 N.CO.X-substituted benzenesulphonyl isourea or isothiourea ether, parabanic acid or thiourea is oxidized or hydrolysed to the desired sulphonyl urea. Pharmaceutical preparations for the treatment of diabetes, preferably by oral administration comprise the above compounds in admixture or conjunction with a carrier, preferably in the form of tablets.

公开(公告)号：BR7108598D0

公开(公告)日：1973-07-03

申请号：BR859871

申请日：1971-12-27

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07D205/08 ,  C07D501/10 ,  C07F9/54 ,  C07F9/568

公开(公告)号：BR6347876D0

公开(公告)日：1973-06-14

申请号：BR14787663

申请日：1963-03-22

Applicant: HOECHST AG

Inventor： HOECHST AG

公开(公告)号：BR6347198D0

公开(公告)日：1973-06-12

申请号：BR14719863

申请日：1963-02-22

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07C311/54 ,  C07C311/56 ,  C07C311/58 ,  C07C311/59

Abstract: The invention comprises 1 - chloro - N-sulphonyl-formamidines of the formula wherein R is an aliphatic or cycloaliphatic hydrocarbon radical or an aromatic hydrocarbon radical, optionally bearing 1 or 2 substituents selected from halogen atoms, alkyl, alkoxy or acyl groups or groups convertible into amino by reduction or hydrolysis, a phenoxyphenyl or a phenylalkyl radical and R1 represents a saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon radical, which may be interrupted by oxygen, or a phenylalkyl radical; and the process for their preparation by reacting a sulphonyl thiourea of the formula R.SO2.NH.CS.NH.R1 with phosgene or a compound that splits off phosgene, e.g. chloroformic acid trichloromethyl ester. The compounds of the invention may be reacted with sodium hydroxide, methanol, ammonia or sodium acetate to give the corresponding sulphonyl urea, sulphonyl-isourea methyl ether, sulphonyl-guanidine or O-acetyl-sulphonyl-isourea, respectively. Pharmaceutical preparations having hypoglycermic activity, for oral treatment of diabetes comprise the above compounds of the invention in admixture or conjunction with a carrier, suitably in the form of tablets. Specification 885,468 is referred to.

公开(公告)号：BR6134027D0

公开(公告)日：1973-05-31

申请号：BR13402761

申请日：1961-11-09

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C07C29/147 ,  C07C33/24

公开(公告)号：BR6132519D0

公开(公告)日：1973-05-31

申请号：BR13251961

申请日：1961-09-13

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: A61K31/26 ,  C07C331/30

公开(公告)号：BR7108596D0

公开(公告)日：1973-05-17

申请号：BR859671

申请日：1971-12-27

Applicant: HOECHST AG

Inventor： HOECHST AG

IPC: C09B62/515