BENZENSULFONYL-UREAS AND THEIR PREPARATION

    公开(公告)号:KR790000180B1

    公开(公告)日:1979-03-26

    申请号:KR730001284

    申请日:1973-08-07

    Applicant: HOECHST AG

    Abstract: Benzenesulfonylureas (I; X = 2-quinolyl, 4-methyl-2-quinoyl, 2-pyridyl, R = Me, Et, Pr, R1 = alkyl, cycloalkyl, cycloalkylmethyl, Benzyl) were prepd. by heating 5.6g 4-(β-N'- 2-quinolyl-N'-methylureidoethyl)-benzenesulfonylmethylcarbamate and a mixt. of 1.lg cyclopentylamine and 75ml dioxane. When I was administered orally to rabbits at 10mg/kg, the blood sugar level was decreased by 4.3% after one hr, 49% after 24hr, and 18% after 47hr.

    PROCESS FOR PREPARATION OF BENZENE-SULFONYL UREA

    公开(公告)号:KR790000046B1

    公开(公告)日:1979-02-28

    申请号:KR730001943

    申请日:1973-11-21

    Applicant: HOECHST AG

    Abstract: Title compds. [I; R = lower alkyl, lower alkoxy, halogen, - NH2, trifluoromethyl, acetyl or acylaminoalkyl (acyl = aliphatic, cycloaliphatic aromatic, heterocyclic carboxyl or carbaminic aicd, alkyl = having 1-4 carbon atoms) R1 = lower alkyl, cycloalkyl, cycloalkenyl, R2 = hydrogen or 5-7 atomic ring with R1 and neighboring nitrogen atom, R3 = alkyl having 1-3 carbon atoms , useful as hypoglycemic agent, were prepd. by reacting benzenesulfonyl-isourea ether with organic base.

    Benzenesulfonyl-ureas and process for their preparation
    4.
    发明授权
    Benzenesulfonyl-ureas and process for their preparation 失效
    苯并呋喃及其制备方法

    公开(公告)号:US3835188A

    公开(公告)日:1974-09-10

    申请号:US37166373

    申请日:1973-06-20

    Applicant: HOECHST AG

    CPC classification number: Y10S514/866

    Abstract: R1 represents hydrogen, lower molecular alkyl, acyl, phenyl, R2 is hydrogen, lower molecular alkyl, R3 is alkyl having 3 to 6 carbon atoms, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl having each 5 to 9 carbon atoms, cyclohexenylmethyl, chlorocyclohexyl, bicycloheptenylmethyl, bicycloheptylmethyl, bicycloheptenyl, bicycloheptyl, nortricyclyl, adamantyl, benzyl, phenylethyl, which as substance or in the form of their salts have pypoglycemic properties and which are distinguished by a strong and continuous lowering of the blood sugar level; processes for preparing them as well as pharmaceutical preparations containing the sulfonyl-ureas as an active substance.

    IN WHICH X represents hydrogen, chlorine, bromine, methoxy or methyl, Y represents -CH(CH3)-CH2-, -CH2-CH(CH3)-or preferably -CH2-CH2-, Z represents hydrogen or together with Y and the phenylene radical the radical

    Sulfonyl-ureas of the formula

    Abstract translation: 磺酰脲,其中X表示氢,氯,溴,甲氧基或甲基,Y表示-CH(CH 3)-CH 2 - , - CH 2 -CH(CH 3) - 优选-CH 2 -CH 2 - ,Z表示氢 或与Y和亚苯基一起,基团R1代表氢,低级分子烷基,酰基,苯基,R2是氢,低级分子烷基,R3是具有3至6个碳原子的烷基,环烷基,烷基环烷基,环烷基,环烯基,烷基环烯基, 每个5至9个碳原子,环己烯基甲基,氯代环己基,双环庚烯基甲基,双环庚基甲基,双环庚烯基,双环庚基,二环己基,金刚烷基,苄基,苯乙基,其物质或其盐形式具有降血糖性质,并且通过强烈和连续降低 的血糖水平; 制备它们的方法以及含有磺酰脲类作为活性物质的药物制剂。

    Benzenesulfonyl ureas having hypoglycemic activity
    8.
    发明授权
    Benzenesulfonyl ureas having hypoglycemic activity 失效
    具有高血压活性的苯二甲酸尿素

    公开(公告)号:US3709908A

    公开(公告)日:1973-01-09

    申请号:US3709908D

    申请日:1970-10-07

    Applicant: HOECHST AG

    CPC classification number: C07D317/66 C07D209/08 C07D215/08

    Abstract: BENZENESULFONYL UREA COMPOUNDS THAT ARE EFFECTIVE AS ORAL ANTIDIABETIC AGENTS ARE DISCLOSED TO HAVE THE FORMULA

    (4-(X-N(-X1)-CO-NH-Y-)PHENYL)-SO2-NH-CO-NH-R

    WHEREIN R IS (A) ALKYL OR ALKENYL OF 3-6 CARBON ATOMS, (B) ENDOALKYLENE-CYCLOHEXYL, ENDOALKYLENE-CYCLOHEXENYL, ENDOALKYLENE-CYCLOHEXYLMETHYL OR ENDOALKYLENE-CYCLOHEXENYLMETHYL OF 1-2 ENDOALKYLENE CARBON ATOMS, (C) BENZYL, PHENYLETHYL, (D) CYCLOHEXYL METHYL, (E) LOWER ALKYL CYCLOHEXYL OR DIALKYL CYCLOHEXYL, METHYL CYCLOPENTYL, (F) CYCLOALKYL OF 5-8 CARBON ATOMS IN THE RING (G) CYCLOHEXENYL, CYCLOHEXENYL-METHYL, METHYLCYCLOHEXENYL, OR (H) NORTRICYCLYL,

    X-N(-X1)-

    IS INDOLINO OR TETRAHYDROQUINOLINO, AND Y IS ALKYLENE OF 1 TO 3 CARBON ATOMS.

    Benzenesulfonyl-semicarbazides and process for their manufacture
    9.
    发明授权
    Benzenesulfonyl-semicarbazides and process for their manufacture 失效
    苯并呋喃半胱氨酸及其制备方法

    公开(公告)号:US3813398A

    公开(公告)日:1974-05-28

    申请号:US14974671

    申请日:1971-06-03

    Applicant: HOECHST AG

    CPC classification number: A61K31/47 C07D215/48

    Abstract: HYPOGLYCEMICALLY ACTIIVE BENZENESULFONYL - SEMICARBAZIDES OF THE FORMULA

    1-((X-QUINOL-8-YL)-CO-NH-Y-),4-(R-NH-CO-NH-SO2-),Z-

    BENZENE

    WHEREIN X IS HYDROGEN, CHLORINE, BROMINE, METYL OR METHOXY, Y IS -CH(CH3)-CH3-, PREFERABLY

    -CH2-CH2-,

    Z IS HYDROGEN OR A HYDROCARBON RADICAL OF 1 OR 2 CARBON ATOMS, WHICH FORMS TOGETHER WITH A 5- OR 6-MEMBERED RING, R IS ALKYLENE-IMINO OF 3 TO 7 CARBON ATOMS IN THE RING WHICH MAY BE UNSATURATED OR SUBSTITUTED BY 1 OR 2 METHYL OR LOWER ALKYL OR METHOXY, PENTAMETHYLENIMINO SUBSTITUTED BY ENDOALKYLENE OF 1 TO 3 CARBON ATOMS, HEXAMETHYLENE-IMINO SUBSTITUTED BY ENDOETHYLENE IN B-EPOSITIONS, TETRAHYDRO-ISO-INDOLINE, 4,7 - ENDOALKYLENE-HEXAHYDRO- OR -TETRAHYDRO-ISO-INDOLINE, THE ENDOALKYLENE CONTAINING 1 OR 2 CARBON ATOMS AND THE DOUBLE BOND OF THE TETRAHYDRO COMPOUND BEING IN 5,6 POSITION, AND THE SALTS THEREOF.

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