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    6-Aza-3H-1,4-benzodiazepines
    31.
    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

    Applicant: Walter von Bebenburg ,  Heribert Offermanns

    Inventor： Walter von Bebenburg ,  Heribert Offermanns

    IPC: C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/75 ,  C07D471/04

    CPC classification number: C07D213/64 ,  C07D213/57 ,  C07D213/61 ,  C07D213/73 ,  C07D213/75 ,  C07D471/04

    Abstract: 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.

    Process of making penicillamine
    36.
    发明授权
    Process of making penicillamine 失效
    制作青霉胺的过程

    公开(公告)号：US4061674A

    公开(公告)日：1977-12-06

    申请号：US657605

    申请日：1976-02-12

    Applicant: Friedrich Asinger ,  Wolf-Dieter Pfeifer ,  Heribert Offermanns ,  Paul Scherberich ,  Gerd Schreyer

    Inventor： Friedrich Asinger ,  Wolf-Dieter Pfeifer ,  Heribert Offermanns ,  Paul Scherberich ,  Gerd Schreyer

    IPC: C07D277/06 ,  C07C99/00

    CPC classification number: C07D277/06

    Abstract: Penicillamine or a homolog thereof is obtained by reacting a 2-disubstituted-5,5-alkyl-thiazolidine nitrile, alkyl having 1 to 6 carbon atoms, with a mineral acid in a two-stage proceeding wherein in the first stage relatively low temperatures and a relatively high concentration of the mineral acid are employed while in the second stage the concentration of the acid is relatively low and the temperatures are relatively high, the term "relatively" referring to the relationship of said two stages of the reaction with mineral acid.

    Abstract translation: 青霉胺或其同系物是通过2-二取代-5,5-烷基 - 噻唑烷腈，具有1至6个碳原子的烷基与无机酸反应得到的，其中在两阶段进行，其中在第一阶段相对低的温度和 使用相对高浓度的无机酸，而在第二阶段酸的浓度相对较低并且温度相对较高，术语“相对”是指反应两个阶段与无机酸的关系。

    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

    Applicant: Walter VONBebenburg ,  Heribert Offermanns

    Inventor： Walter VONBebenburg ,  Heribert Offermanns

    IPC: C07D213/57 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D471/04 ,  A61K31/44

    CPC classification number: C07D213/73 ,  C07D213/57 ,  C07D213/74 ,  C07D213/75 ,  C07D471/04

    Abstract: 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

    Applicant: Walter von Bebenburg ,  Heribert Offermanns

    Inventor： Walter von Bebenburg ,  Heribert Offermanns

    IPC: C07D471/04

    Abstract: 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.

    Abstract translation: 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

    Applicant: Walter von Bebenburg ,  Heribert Offermanns

    Inventor： Walter von Bebenburg ,  Heribert Offermanns

    IPC: A61K31/55 ,  A61P25/20 ,  A61P29/00 ,  C07D213/57 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D471/04

    CPC classification number: C07D213/73 ,  C07D213/57 ,  C07D213/74 ,  C07D213/75 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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：

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