Substituted dibenzodiazepinones
    42.
    发明授权
    Substituted dibenzodiazepinones 失效
    取代的二苯并二氮杂酮

    公开(公告)号:US4447434A

    公开(公告)日:1984-05-08

    申请号:US462149

    申请日:1983-01-31

    摘要: The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3,2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds.The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.

    摘要翻译: 该说明书描述了式(Ⅰ)的新的取代二苯并二氮杂酮,其中R 1是氢或氯原子,R是(1-甲基-4-哌啶基)甲基,(1-甲基-1,2,5,6-四氢 - 4-吡啶基)甲基,1-甲基-1,2,5,6-四氢-4-吡啶基,(1-甲基-4-亚哌啶基)甲基,(2,3-脱氢-8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基) - 甲基,(8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基) - 甲基或内 - 或外 - - (8-甲基-8-氮杂双环[3,2,1]辛-3-基)甲基,其各自任选被杂环上的一个或两个甲基取代,及其无毒的药学上可接受的酸加成盐,用于 制备它们和含有这些化合物的药物组合物。 式I化合物具有抗溃疡作用和对具有抗胆碱能活性的胃物质分泌的抑制作用,例如口干和散瞳。

    2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and
salts thereof
    47.
    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
    48.
    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。