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    51.
    发明专利
    未知

    公开(公告)号：BR7107378D0

    公开(公告)日：1973-08-16

    申请号：BR737871

    申请日：1971-11-05

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C12N9/88

    53.
    发明专利
    未知

    公开(公告)号：BR6348375D0

    公开(公告)日：1973-08-14

    申请号：BR14837563

    申请日：1963-04-10

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C07C69/732

    Abstract: The invention comprises compounds of the general formula (wherein AC represents a formyl, acetyl or propionyl group) and physiologically tolerable acid addition salts thereof, their preparation by acylating one of the four stereoisomers of 4, 4-diphenyl-6-dimethylaminoheptanol-(3) with a reactive derivative of mandelic acid, the free hydroxy group of which is converted into a formyloxy, acetyloxy or propionyloxy group either before or after the acylation, optionally followed by acid addition salt formation, and pharmaceutical preparations containing them. The compounds of the invention have a beneficial action on the heart and the blood circulation and some of them possess analgesic properties. They may be administered parenterally or orally in the form of pharmaceutical preparations (e.g. tablets or dragees) containing them in admixture or conjunction with a carrier.

    54.
    发明专利
    未知

    公开(公告)号：BR6465307D0

    公开(公告)日：1973-08-02

    申请号：BR16530764

    申请日：1964-12-14

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K31/64 ,  C07C311/54

    Abstract: The invention comprises sulphonyl ureas of the formula and their physiologically tolerable salts, wherein R1 is a C1- 8 alkyl, C5- 8 cycloalkyl or ((C5- 8 cycloalkyl)-alkyl group having 1-3 carbon atoms in the alkyl portion, X is a hydrocarbon group of 1 or 2 carbon atoms, e.g. methylene, ethylene, ethenylene or ethylidene and R2 is (a) a C2- 8 alkyl group, (b) a phenyl-C1- 3 alkyl or cyclohexyl-C1- 3 alkyl group, (c) an endoalkylenecyclohexyl, -cyclohexenyl, -cyclohexylmethyl or -cyclohexenylmethyl group containing 1 or 2 endoalkylene carbon atoms, (d) a C1- 4-alkylcyclohexyl group, or (e) a C5- 8 cycloalkyl group. The compounds are prepared by (a) reaction of an R1OOC.X- substituted benzenesulphonamide (suitably in the form of a salt) with an isocyanate R2CNO or a corresponding carbamic acid ester or halide, thiocarbamic ester, urea or N2-substituted urea, (b) reaction of an amine R2NH2 or a salt thereof with a benzenesulphonyl urea isocyanate, R1OOC.X.C6H4.SO2-NCO or a corresponding carbamic ester or halide, thiocarbamic ester, urea or N2-substituted urea, (c) reaction of a benzenesulphonyl chloride R1OOC.X.C6H4.SO2Cl with an R2 substituted urea, isourea ether, isothiourea ether or parabanic and hydrolysis of a benzenesulphonyl isourea ether, isothiourea ether or parabanic acid obtained in this way or by another method, (d) exchange of the sulphur atom in a corresponding benzenesulphonylthiourea for an oxygen atom by oxidation or reaction with a heavy metal salt, and (e) oxidation of a corresponding benzenesulphenyl or benzenesulphinyl urea. If desired, carboxylic acids HOOC.X.C6H4.SO2.NH.CO.NHR2 formed by the above reactions or in another way may be esterified to introduce the group R1. Alternatively a compound wherein X is -CH = CH- may be hydrogenated to form a product wherein X is -CH2-CH2-. 4 - Sulphamoyl - phenylacetic acid is made by chlorosulphonating phenylacetic acid and reacting the resulting acid chloride with ammonia. N - (4 - Carbo - n - butoxy - methyl - benzenesulphonyl)-urea is made by the action of potassium cyanate on the corresponding benzenesulphonamide. 4 - b - Carbethoxyvinyl - benzenesulphonamide is made by esterifying the free acid. N - 4 - Carbethoxymethyl - benzenesulphonyl - N1-cyclohexyl-urea is made by the action of chloroformic methyl ester on the corresponding sulphonamide. 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 suitable for oral administration such as tablets.

    56.
    发明专利
    未知

    公开(公告)号：BR6352525D0

    公开(公告)日：1973-07-17

    申请号：BR15252563

    申请日：1963-09-04

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C07C311/54 ,  C07C311/59

    Abstract: Novel sulphonyl ureas of the formula and physiologically tolerable salts thereof, wherein R and R1 are each hydrogen or halogen or a C1- 6 alkyl or alkoxy group or, when R1 is hydrogen, R may also be azido, trifluoromethyl, or C1- 7 acyl group, and R2 is a C2- 4 alkyl group, are made by reacting an R,R1-substituted benzenesulphonyl isocyanate or a compound which reacts as an isocyanate such as the corresponding benzenesulphonyl carbamic ester, carbamic halide or thiocarbamic ester or the reaction product of a benzenesulphonyl isocyanate and an acid amide, e.g. caprolactam or butyrolactam, or a weakly basic amine, e.g. carbazole, with an R2-substituted cyclohexylamine or its acyl derivative, or conversely, reacting an R2-substituted cyclohexyl isocyanate, or a compound which behaves as a cyclohexyl isocyanate such as the carbamic ester or halide, with the corresponding benzenesulphonamide. Alternatively, a benzenesulphonyl urea, benzenesulphonyl-N1-acyl-urea or bis-benzenesulphonyl urea is reacted with a cyclohexylamine, or a cyclohexyl urea, N1-acyl-cyclohexyl urea, N1,N1-diphenyl cyclohexyl urea or N,N1-bis-cyclohexyl urea is reacted with a benzenesulphonamide. Further processes include reacting a cyclohexyl isourea ether, isothiourea ether or guanidine or the tertiary amine salt of a cyclohexyl-substituted parabanic acid with the appropriate benzenesulphonyl halide and converting the resulting benzeneslphonyl isourea ether, isothiourea ether, guanidine or parabanic acid to the desired benzenesulphonyl urea. 4-Isopropyl-cyclohexyl urea is made by reacting 4 - isopropylcyclohexylamine hydrochloride with potassium cyanate. 4-Isopropyl-cyclohexyl isocyanate is made by the action of phosgene on cyclohexylamine hydrochloride. Pharmaceutical preparations for oral treatment of diabetes mellitus comprise the above compounds of the invention in admixture or conjunction with a carrier suitably in the form of tablets.

    57.
    发明专利
    未知

    公开(公告)号：BR6353832D0

    公开(公告)日：1973-07-12

    申请号：BR15383263

    申请日：1963-10-18

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    59.
    发明专利
    未知

    公开(公告)号：BR6245528D0

    公开(公告)日：1973-05-10

    申请号：BR14552862

    申请日：1962-12-18

    Applicant: HOECHST AG

    Inventor： HOECHST AG

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