6-Aza-3H-1,4-benzodiazepines
    32.
    再颁专利
    6-Aza-3H-1,4-benzodiazepines 失效
    6-氮杂-3H-1,4-苯并二氮杂

    公开(公告)号:USRE31071E

    公开(公告)日:1982-11-02

    申请号:US298513

    申请日:1981-09-01

    摘要: There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula ##STR1## where R.sub.1 is a halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy, R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic aid of 2 to 6 carbon atoms, lower alkoxy, lower alkyl, benzyl, lower aliphatic acyl, carboxy or carb-lower alkoxy, Z is nitrogen or NO, R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms, lower hydroxyalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, lower alkyl substituted with 5 to 7 membered N-heterocyclic ring, containing 0 to 1 additional nitrogen or oxygen atoms, and A is oxygen, sulfur, .dbd.NR.sub.5, .dbd.NOR.sub.5, .dbd.NH--NHR.sub.5 or two hydrogen atoms and the --N(R.sub.5)--C--(.dbd.A)-- can also be in the tautomeric form --N.dbd.C(AR.sub.5) 13 and pharmacologically acceptable salts thereof. The compounds have spasmolytic, antiphlogistic and tranquilizer activity.

    6-Aza-3H-1,4-benzodiazepines
    37.
    发明授权
    6-Aza-3H-1,4-benzodiazepines 失效
    6-AZA-3H-1,4-BENZODIAZEPINES

    公开(公告)号:US4009271A

    公开(公告)日:1977-02-22

    申请号:US590285

    申请日:1975-06-25

    摘要: There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula: ##STR1## wherein R.sub.1 is the group --NR.sub.a R.sub.b or --NR.sub.a R.sub.b R.sub.c halide and R.sub.a and R.sub.b are the same or different and are hydrogen, alkyl groups of 1 to 6 carbon atoms, or alkyl groups of 1 to 6 carbon atoms substituted by hydroxy, phenyl or a carboxy group, and R.sub.c can be as defined for R.sub.a and R.sub.b except it cannot be hydrogen and wherein the group --NR.sub.a R.sub.b also can be a saturated closed 5, 6 or 7 membered ring which in a given case has a further oxygen atom or nitrogen atom or contains a nitrogen atom substituted with an alkyl group having 1 to 4 carbon atoms;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl or lower alkoxy;R.sub.4 is hydrogen;Z is a nitrogen atom or the NO group;R.sub.5 is hydrogen, lower alkyl, lower alkenyl, aminoalkyl of 2 to 4 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 4 carbon atoms; andA is oxygen, and the --N(R.sub.5)--C--(=A)--can also be in the tautomeric form --N=C(AR.sub.5)--, pharmacologically acceptable salts and quaternary ammonium and alkyl ammonium compounds thereof. The compounds have pharmacodynamic properties including psychosedative and anxiolytic properties as well as antiphlogistic properties.

    Certain pyrido[3,2-e]1,4-diazepinones and derivatives
    39.
    发明授权
    Certain pyrido[3,2-e]1,4-diazepinones and derivatives 失效
    某些吡啶并[8 3,2-e {9,4-二氮杂酮及其衍生物

    公开(公告)号:US3972873A

    公开(公告)日:1976-08-03

    申请号:US576112

    申请日:1975-05-09

    IPC分类号: C07D471/04

    摘要: There are prepared compounds of the formula: ##SPC1##Wherein:n is an integer from 1 to 4;R.sub.1 is alkyl of 1 to 6 carbon atoms, a hydroxy group, an amino group, an alkoxy group having 1 to 6 carbon atoms, a phenyl group or a phenyl group substituted with alkyl of 1 to 6 carbon atoms, an alkoxy group of 1 to 6 carbon atoms, trifluoromethyl, fluorine or chlorine;A is oxygen, sulfur, the imino group, or an alkylimino group having 1 to 6 carbon atoms, or when R.sub.1 is phenyl or substituted phenyl A also is two alkoxy groups having 1 to 6 carbon atoms or alkylenedioxy with 2 to 4 carbon atoms or --C(R.sub.1)=A is the cyano group;B is oxygen, sulfur, an imino group or an alkylimino group having 1 to 6 carbon atoms;R.sub.2 is hydrogen, a hydroxy group, an alkyl group with 1 to 6 carbon atoms, an alkoxy group with 1 to 6 carbon atoms, or the group --O(CH.sub.2).sub.n -- C(=A)--R.sub.1 ;N.sub.o is nitrogen or an N-oxide group; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, chlorine, fluorine, the trifluoromethyl group, alkyl groups of 1 to 6 carbon atoms or alkoxy groups with 1 to 6 carbon atoms, the tautomeric forms thereof and pharmaceutically acceptable salts thereof. The compounds have psychosedative, anxiolytic, spasmolytic and antipsychotic activity.

    摘要翻译: 制备下式的化合物:

    6-Aza-3H-1,4-benzodiazepines
    40.
    发明授权
    6-Aza-3H-1,4-benzodiazepines 失效
    6-氮杂-3H-1,4-苯并二氮杂

    公开(公告)号:US3941775A

    公开(公告)日:1976-03-02

    申请号:US460525

    申请日:1974-04-12

    摘要: There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula: ##SPC1##Wherein R.sub.1 is the group --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or --NR.sub.a acyl and R.sub.a, R.sub.b and R.sub.c are the same or different and are hydrogen, alkyl groups of 1 to 6 carbon atoms, or alkyl groups of 1 to 6 carbon atoms substituted by hydroxy, an alkoxy group of 1 to 6 carbon atoms, a carboxy group, a nitrile group, a carbamide group, a carbalkoxy group with 1 to 6 carbon atoms in the alkoxy, a phenyl group or a halogen and acyl is an aliphatic acyl group with 2 to 6 carbon atoms and wherein the group --NR.sub.a R.sub.b also can be a saturated closed 5, 6 or 7 membered ring which in a given case has a further oxygen atom or nitrogen atom or contains a nitrogen atom substituted with an alkyl group having 1 to 4 carbon atoms;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy and R.sub.2 also can be --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or the group --NR.sub.a acyl with the proviso that if R.sub.2 is --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or --NR.sub.a acyl then R.sub.1 can be halogen;R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic acid of 2 to 6 carbon atoms, a lower alkoxy group, a lower alkyl group, a benzyl group, lower aliphatic acyl, a carboxy group or a lower carbalkoxy group;Z is a nitrogen atom or the NO group;R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms, lower hydryxoalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms, aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, aminoalkyl of 2 to 7 carbon atoms substituted with a 5 to 7 membered heterocyclic ring including the amino nitrogen containing 0 to 1 additional nitrogen or oxygen atom; andA is oxygen, sulfur, =NR.sub.5, =NOR.sub.5, =NH--NHR.sub.5 or two hydrogen atoms, and the --N(R.sub.5)--C--(=A)-- can also be in the tautomeric form --N=C(AR.sub.5)--, pharmacologically acceptable salts and quaternary compounds thereof. The compounds have pharmacodynamic properties including psychosedative and anxiolytic properties as well as antiphlogistic properties.

    摘要翻译: 产生下式的6-氮杂-3H-1,4-苯并二氮杂和6-氮杂-1,2-二氢-3H-1,4-苯并二氮杂: