Pyridobenzodiazepinones, pharmaceutical compositions and method of use
thereof
    6.
    发明授权
    Pyridobenzodiazepinones, pharmaceutical compositions and method of use thereof 失效
    吡啶并二氮杂酮,药物组合物及其使用方法

    公开(公告)号:US4424222A

    公开(公告)日:1984-01-03

    申请号:US462183

    申请日:1983-01-31

    摘要: New pyridobenzodiazepinones of the formula ##STR1## are described wherein X represents oxygen, --NH-- or --NCH.sub.3 -- and R represents 1-methyl-4-piperidinyl or 4-methyl-1-piperazinyl group optionally substituted by a methyl group, or a 3.alpha.- or 3.beta.-tropanyl group, and the nontoxic pharmaceutically acceptable acid addition salts thereof. The specification also describes processes for preparing these compounds, pharmaceutical compositions containing these compounds and new intermediate products used in preparing them. The compounds of formula I have antiulcerative effects and an inhibitory effect on gastric acid secretion, without the side effects such as dryness of the mouth and mydriasis which occur with other substances having an anticholinergic activity.

    摘要翻译: 描述了式(I)的新的吡啶并苯并二氮杂酮,其中X表示氧,-NH-或-NCH 3 - ,R代表1-甲基-4-哌啶基或4-甲基-1-哌嗪基,任选被甲基取代 ,或3α-或3β-丙酰基,以及其无毒的药学上可接受的酸加成盐。 本说明书还描述了制备这些化合物的方法,含有这些化合物的药物组合物和用于制备它们的新的中间产物。 式I化合物具有抗溃疡作用和对胃酸分泌的抑制作用,而没有与具有抗胆碱能活性的其它物质发生的口腔干燥和散瞳等副作用。

    2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and
salts thereof
    7.
    发明授权
    2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and salts thereof 失效
    2,5-二氢-1,2-噻嗪(5,6-b)吲哚-3-甲酰胺-1,1-二氧化物及其盐

    公开(公告)号:US4137313A

    公开(公告)日:1979-01-30

    申请号:US872889

    申请日:1978-01-27

    摘要: Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.

    摘要翻译: 式中的化合物,其中R1是氢,甲基或乙基; R2是甲基或乙基; Y是氢,氟,氯,溴,甲氧基,甲基,乙基或三氟甲基; 并且Ar是可以具有一个或两个连接到其上的甲基或乙基取代基的2-噻唑基; 5,6-二氢-4H-环戊基噻唑-2-基; 4,5,6,7-四氢-2-苯并噻唑基; 2-苯并噻唑基 可具有与其连接的甲基取代基的3-异噻唑基; 可以具有连接到其上的甲基或羟基取代基的2-吡啶基; 3-吡啶基; 4-吡啶基; 4-嘧啶基; 吡嗪基 2-苯并咪唑基; 可具有与其连接的甲基取代基的2-恶唑基; 2-苯并恶唑基; 或可具有与其连接的氟,氯,溴,甲基,乙基,三氟甲基或甲氧基取代基的苯基; 和与无机或有机碱形成的无毒的,药学上可接受的盐。 化合物及其盐可用作消炎剂和血小板聚集抑制剂。

    (4-Biphenylyl)-butenols
    8.
    发明授权
    (4-Biphenylyl)-butenols 失效
    (4-联苯基) - 丁烯醇

    公开(公告)号:US3969418A

    公开(公告)日:1976-07-13

    申请号:US485574

    申请日:1974-07-03

    IPC分类号: C07C31/34 C07C31/14

    摘要: Compounds of the formula ##SPC1##Wherein A is ##EQU1## or WHERE Z is hydrogen or methyl, andR.sub.1 is halogen or, when A is ##EQU2## also hydrogen, THE COMPOUNDS ARE USEFUL AS ANTIPHLOGISTICS.

    摘要翻译: 式WHEREIN A的化合物是Z CH 3 | | C = CH-CH 2 - 或-C = CH-或者其中Z是氢或甲基,并且R 1是卤素,或者当A是Z | -C = CH-CH 2 - ,也是氢,化合物作为抗肿瘤药物有用。