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    41.
    发明专利
    未知

    公开(公告)号：DK131903C

    公开(公告)日：1976-02-23

    申请号：DK349765

    申请日：1965-07-08

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K31/195 ,  C07C101/08

    Abstract: L - (-) - b - (3,4 - Dihydroxyphenyl) - a - methylalanine (" L-a -methyl-DOPA ") is made by splitting a benzyl methyl malonic monoester of the Formula II in which R is CH3 and R1 is CH3, C4H9n or benzyl and, if R1 is CH3, R may also be a benzyl or allyl radical, into its antipodes by means of an optically active base and then (A) converting the D compound of Formula II obtained into an optically inactive symmetrical di-ester by esterification with an alcohol R1OH and then converting into the inactive starting material of Formula II by hydrolysing one ester group, and (B) converting the L-compound of Formula II into the desired L-a -methyl-DOPA by (a) converting into an L-isocyanate (in which R1 is the same as R but cannot be allyl) and thence into an amino compound wherein R2 is a hydrogen atom or an acyl or carbalkoxy radical and splitting off the etherifying radicals R1, the esterifying radical R1 and any N-acyl or N-carbalkoxy group by hydrolysis or, in the case when R1 is benzyl, by hydrogenation and hydrolysis; or (b) when R is an allyl radical, hydrogenating to convert the allyl groups to n-propyl groups, converting the product by known methods, e.g. via the azide, isocyanate and carbamic ester, into an amine of the formula in which R3 is hydrogen or CH3 and splitting off the propyl groups, together with the methyl group R3 if present and any N-acyl or N-carbalkoxy group present, by the action of strong hydrohalic acids; or (c) when R is an allyl radical, converting into the amino compound and treating this by (i) reacting with a hydrohalic acid, or (ii) hydrogenating and reacting with a strong hydrohalic acid, or (iii) splitting off one allyl group together with any esterifying methyl group or N-acyl or N-carbalkoxy group by reaction with an alkali-metal alkoxide and either treating with a hydrohalic acid or hydrogenating and treating with a hydrohalic acid to remove the second allyl group. Symmetrical di-esters of the formula used for the preparation of the mono-ester starting material II are made by condensing a malonic di-ester of the formula CH2(COOR1)2 with 3,4-dihydroxybenzaldehyde or its methyl ethers and hydrogenating and C-methylating the resulting 3,4-dihydroxybenzylidene malonic acid di-ester or corresponding methylated compound. The corresponding 3,4-di-allyl or 3,4-dibenzyl ethers are obtained by allylation or benzylation of the 3,4-dihydroxy benzylmalonic di-esters and the products may, if desired, be re-esterified thus, for example, converting a di-methyl ester into a di-benzyl or di-n-butyl ester.

    42.
    发明专利
    未知

    公开(公告)号：BR6682585D0

    公开(公告)日：1973-12-27

    申请号：BR18258566

    申请日：1966-09-02

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K20060101 ,  C07G20060101 ,  C07G11/00

    Abstract: 1,154,359. Hydrogenated moenomycins. FARBWERKE HOECHST A.G. 2 Sept., 1966 [3 Sept., 1965], No. 39324/66. Heading C2A. The antibiotic activity of moenomycin complex (Specification 977,327) or its components A, B and C against gram-positive pathogenic germs is enhanced by hydrogenation. The hydrogenation is carried out with the aid of precious metal catalysts (e.g. platinum) or Raney nickel in a polar solvent such as water, glacial acetic acid, methanol or dimethyl formamide. In the case of the hydrogenated moenomycin complex, the complex may be separated into the hydrogenated single components A, B and C by the process of Specification 1,126,196. Physical data for the hydrogenated compounds are provided. Pharmaceutical compositions comprise a carrier and a hydrogenated moenomycin complex or hydrogenated component A, B or C.

    44.
    发明专利
    未知

    公开(公告)号：BR6679522D0

    公开(公告)日：1973-12-26

    申请号：BR17952266

    申请日：1966-05-17

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A23B4/10 ,  A23B7/153 ,  A23B7/16 ,  A23C19/10 ,  A23L3/3508 ,  B65D81/28

    Abstract: 1,142,171. Preserving cheese &c. FARBWERKE HOECHST A.G. 16 May, 1966 [17 May, 1965], No. 21565/66. Addition to 1,061,014. Heading A2D. Food, especially hard cheese, is preserved against mould growth by dipping into an aqueous suspension of calcium sorbate which is obtained by reacting an aqueous solution of a sorbic acid salt with an aqueous solution of a calcium salt and which contains 4 to 15% by weight of calcium sorbate. The preferred salts are sodium sorbate and calcium chloride, but potassium sorbate and calcium acetate are also specified.

    45.
    发明专利
    未知

    公开(公告)号：BR6685060D0

    公开(公告)日：1973-10-25

    申请号：BR18506066

    申请日：1966-12-02

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C07D307/52

    48.
    发明专利
    未知

    公开(公告)号：BR6676790D0

    公开(公告)日：1973-09-11

    申请号：BR17679066

    申请日：1966-01-28

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: C09B44/18

    49.
    发明专利
    未知

    公开(公告)号：BR6574471D0

    公开(公告)日：1973-09-06

    申请号：BR17447165

    申请日：1965-10-29

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K31/64 ,  C07C311/54 ,  C07D209/48 ,  C07D333/34

    Abstract: Novel compounds of the formula X-Y-phenylene-SO2-NH-CO-NHR and their salts, wherein X is a phthalimide group which may be wholly or partly hydrogenated and/or may be mono- or di-substituted by one or two halogen, lower alkyl or lower alkoxy substituents, or is a tetrahydro- or hexahydro - endomethylene - or endoethylene - phthalimide group or a napthalimide, napththalene - 1, 2 - dicarbonimide or naphthalene - 2, 3 - dicarbonimide group; Y is a branched or unbranched C1- 4 hydrocarbon group; the "phenylene" group is an unsubstituted or halogen, C1- 4 alkyl or C1- 4 alkoxy substituted phenylene radical and R is a C2- 8 alkyl, alkenyl or mercapto alkyl group, a C4- 8 alkoxyalkyl or alkylmercaptoalkyl group (having at least two carbon atom in the alkylene portion), a phenyl lower alkyl or phenylcyclopropyl group, a cyclohexyl-lower alkyl, cycloheptylmethyl, cycloheptylethyl or cyclo-octylmethyl group, an endoalkylene - cyclohexyl, - cyclohexenyl, -cyclohexylmethyl or cyclohexenylmethyl group, a lower alkyl or lower alkoxycyclohexyl group, a C5- 8 cycloalkyl group, a cyclohexenyl or cyclohexenylmethyl group or a heterocyclic group having 4 or 5 carbon atoms and an oxygen or sulphur atom which may have one or two ethylenic double bonds and is attached to the N-atom directly or through a methylene group, are made by the usual sulphonyl urea syntheses, i.e. reaction of the appropriate benzenesulphonyl urea with an isocyanate RNCO or an equivalent carbamic ester or halide, thiocarbamic ester or urea derivative, or conversely reacting an amine R-NH2 or its salt with an X-Y-substituted benzenesulphonyl isocyanate or its equivalent; reacting a sulphonyl chloride of the formula X-Y-phenylene -SO2Cl with an R-substituted urea, isourea ether, isothiourea ether or parabanic acid and, if required, hydrolysing the product; replacing sulphur by oxygen in the corresponding benzenesulphonyl thiourea, or oxidizing a corresponding benzenesulphenyl or benzenesulphonyl urea; and also by converting a corresponding benzenesulphonyl urea of the formula Z-Y-phenylene-SO2-NH-CO-NHR, in which Z is a phthalic acid mono-amide group which may be partially hydrogenated and/or substituted into the corresponding phthalimide compound by cyclization. Pharmaceutical preparations having hypoglaycaemic comprise the above compounds of the invention in admixture or conjunction with a carrier, preferably in a form adapted to oral administration.

    50.
    发明专利
    未知

    公开(公告)号：BR6574379D0

    公开(公告)日：1973-09-06

    申请号：BR17437965

    申请日：1965-10-27

    Applicant: HOECHST AG

    Inventor： HOECHST AG

    IPC: A61K31/64 ,  C07C67/00 ,  C07C301/00 ,  C07C303/36 ,  C07C303/40 ,  C07C311/54 ,  C07C311/58 ,  C07D335/02

    Abstract: 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.

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