Acetamide compounds
    41.
    发明公开
    Acetamide compounds 失效
    乙酰胺,Verbindungen。

    公开(公告)号:EP0356176A1

    公开(公告)日:1990-02-28

    申请号:EP89308426.9

    申请日:1989-08-18

    CPC分类号: C07D213/74

    摘要: Novel acetamide compounds of the formula,
    [wherein R₁ and R₂, each independently represents a hydrogen atom, a C₁ to C₆ straight- or branched-­chain alkyl or alkenyl group, C₃ to C₆ cycloalkyl or cycloalkenyl group or an C₆ to C₁₀ aromatic group or R₁ and R₂ join with each other in combination with the adjacent N and carbon atoms or further with at least one of nitrogen, oxygen and sulfur atoms to represent a 5- or 6-membered heterocyclic ring group: R₃ represents a C₁-C₆ straight- or branched-chain alkyl or alkenyl group, C₃ to C₆ cycloalkyl or cycloalkenyl group, a halogen atom, a C₁-C₆ straight or branched-chain alkoxyl group, or a C₃-C₆ cyclo­alkoxy or cycloalkenoxy group and n is 0 to 4] and their pharmaceutically acceptable salts are useful in the treatment of ulcers in mammals.

    摘要翻译: 下式的新型乙酰胺化合物 [其中R1和R2各自独立地表示氢原子,C1-C6直链或支链烷基或烯基,C3至C6环烷基或环烯基或C6至C10 芳族基团或R 1和R 2彼此结合,与相邻的N和碳原子结合,或者与氮原子,氧原子和硫原子中的至少一个结合,代表5-或6-元杂环基团:R3代表C1- C6直链或支链烷基或烯基,C3至C6环烷基或环烯基,卤素原子,C1-C6直链或支链烷氧基或C3-C6环烷氧基或环烯氧基,n为0至 4]及其药学上可接受的盐可用于治疗哺乳动物的溃疡。

    Quaternary ammonium salts
    42.
    发明公开
    Quaternary ammonium salts 失效
    QuaternäreAmmoniumsalze。

    公开(公告)号:EP0356152A1

    公开(公告)日:1990-02-28

    申请号:EP89308369.1

    申请日:1989-08-17

    摘要: Novel quaternary ammonium compounds of the formula,
    [wherein R₁ and R₂, each independently represents a hydrogen atom, a C₁ to C₈ alkyl or alkenyl group, C₃ to C₈ cycloalkyl or cycloalkenyl, aralkyl or aryl group; or R₁ and R₂ join with each other in combination with the adjacent N and carbon atoms or further with at least one of nitrogen, oxygen and sulfur atoms to represent a 3- to 8-membered heterocyclic ring group: R₃, R₄ and R₅, each independently represents a C₁ to C₈ alkyl or alkenyl group, C₃ to C₈ cycloalkyl or cycloalkenyl, aralkyl or aryl group; or either two of R₃, R₄ and R₅ combine with each other in combination with the adjacent N and carbon atoms or further with at least one of nitrogen, oxygen and sulfur atoms to represent a 3- or 8-membered heterocyclic ring group, with the remaining being the same as defined above; or R₃, R₄ and R₅ combine with one another in combination with the adjacent N to represent a nitrogen-containing bicyclo ring or nitrogen-containing aromatic ring group: n is an integer of 1 to 8; and X⁻ represents an anion] and their pharmaceutically acceptable salts are useful in the treatment of ulcers in mammals.

    摘要翻译: 下式的新型季铵化合物 [其中R 1和R 2各自独立地表示氢原子,C 1至C 8烷基或烯基,C 3至C 8环烷基或环烯基,芳烷基或芳基; 或R 1和R 2彼此结合,与相邻的N和碳原子结合,或者与氮,氧和硫原子中的至少一个相互结合,以表示3-8元杂环基团:R 3,R 4和R 5,每个 独立地表示C1至C8烷基或烯基,C3至C8环烷基或环烯基,芳烷基或芳基; 或者R 3,R 4和R 5中的任一个与相邻的N和碳原子相结合或者与氮,氧和硫原子中的至少一个相结合,以代表3-或8-元杂环基,其中 与上述相同; 或R 3,R 4和R 5相互结合,与相邻的N相结合,代表含氮双环或含氮芳族环基团:n为1至8的整数; 和X'代表阴离子]及其药学上可接受的盐可用于治疗哺乳动物的溃疡。

    DRUG FOR PROPHYLAXIS AND TREATMENT OF HEPATOPATHY
    43.
    发明公开
    DRUG FOR PROPHYLAXIS AND TREATMENT OF HEPATOPATHY 失效
    ARZNEIMITTELFÜRDIE PROPHYLAXE UND DIE BEHANDLUNG VON LEBERKRANKHEITEN。

    公开(公告)号:EP0313654A1

    公开(公告)日:1989-05-03

    申请号:EP87904314.9

    申请日:1987-07-02

    IPC分类号: A61K31/415 C07D233/64

    CPC分类号: A61K38/04

    摘要: Anovel drug for prophylaxis and treatment of alcoholic hepatopathy, viral hepatitis, or other hepatopathies caused by drugs, poisons, radiation, etc., which contains carnosine as effective ingredient and which is administered orally to exhibit significant effects.

    摘要翻译: 用于预防和治疗肝脏疾病(口服给药)的药物含有肌肽锌盐作为活性成分。 县。 制作 包括肌肽与氯化锌的反应。 在一个实例中,将L-肌肽(147g)溶于水(441ml)中并用溶胶处理。 的氯化锌(88.6g)在水中的溶液177ml)。 mixt。 搅拌,4N水溶液。 在30分钟内滴加NaOH(325ml)。 mixt。 过滤,残余物用水洗涤直至洗涤液为中性。 然后将其干燥(在40℃下2天),得到无色粉末的L-肌肽锌盐(175g),m.pt。 高于300度 C; 干燥失重(60℃/ 3小时)7.63%。

    Crystalline L-carnosine zinc complex and production thereof
    45.
    发明公开
    Crystalline L-carnosine zinc complex and production thereof 失效
    Kristalliner L-Carnosin-Zink-Komplex und dessen Herstellung。

    公开(公告)号:EP0303380A2

    公开(公告)日:1989-02-15

    申请号:EP88307090.6

    申请日:1988-08-01

    IPC分类号: C07K5/06 C07K1/02 A61K37/02

    CPC分类号: C07D233/64 C07F3/003

    摘要: A novel crystalline L-carnosine zinc complex is produced by reacting L-carnosine, a zinc salt and an alkali metal compound in an anhydrous or hydrous polar organic sol­vent.
    The crystalline L-carnosine zinc complex substantially corresponds to the formula C₉H₁₂N₄O₃Zn and has physi­cal properties clearly different from the known amorphous L-carnosine zinc complex.
    As compared with the amorphous complex, the crystal­line complex is very low in impurity, stable to heat and moisture, and easy to filtrate, and has higher anti­ulcer activity.

    摘要翻译: 通过在无水或含水极性有机溶剂中使L-肌肽,锌盐和碱金属化合物反应,生成新的结晶L-肌肽锌络合物。 结晶L-肌肽锌络合物基本上对应于式C9H12N4O3Zn,并且具有与已知的无定形L-肌肽锌复合物明显不同的物理性质。 与无定形复合物相比,结晶复合物杂质非常低,对热和水分稳定,易于滤液,抗溃疡活性更高。

    1,5-Benzothiazepine derivatives and production thereof
    47.
    发明公开
    1,5-Benzothiazepine derivatives and production thereof 失效
    1,5-Benzothiazepin-Derivate und Verfahren zu ihrer Herstellung。

    公开(公告)号:EP0137083A1

    公开(公告)日:1985-04-17

    申请号:EP83306147.6

    申请日:1983-10-11

    IPC分类号: C07D281/10 A61K31/55

    摘要: Novel 1,5-benzothiazepine derivatives having the formula:
    wherein R,, R 2 and R 3 each denotes hydrogen, a halogen, a lower alkyl group, a lower alkoxy group or a hydroxy group; R 4 denotes a lower alkyl group, an allyl group, a lower alkoxyalkyl group, a lower alkyl group substituted with a hydroxy group or a halogen, a lower alkylaminoalkyl group or a morpholino lower alkyl group; X denotes a halogen or hydrogen, are produced from corresponding 1,4-benzothiazine by a ring expansion reaction with trimethylhalosilane, hydrogen peroxide and water. The derivatives have analgesic, antipyretic and antiarrhythmic activities.

    摘要翻译: 具有下式的新的1,5-苯并硫氮杂衍生物:其中R 1,R 2和R 3各自表示氢,卤素,低级烷基,低级烷氧基或羟基; R4表示低级烷基,烯丙基,低级烷氧基烷基,被羟基或卤素取代的低级烷基,低级烷基氨基烷基或吗啉代低级烷基。 X表示卤素或氢,通过与三甲基卤硅烷,过氧化氢和水的环膨胀反应由相应的1,4-苯并噻嗪制备。 衍生物具有镇痛,解热和抗心律失常作用。