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    2-benzoyl -3-amino-pyridines
    1.
    发明授权
    2-benzoyl -3-amino-pyridines 失效
    2-苯甲酰基-3-氨基吡啶

    公开(公告)号：US3875176A

    公开(公告)日：1975-04-01

    申请号：US34736173

    申请日：1973-04-03

    Applicant: DEGUSSA

    Inventor： VON BEBENBURG WALTER ,  OFFERMANNS HERIBERT

    IPC: C07D213/50 ,  C07D213/30 ,  C07D213/38 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D31/42

    CPC classification number: C07D213/64 ,  C07D213/57 ,  C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75

    Abstract: WHERE R1 is halogen, R2 and R3 are hydrogen, halogen, trifluoromethyl, hydroxy, cyano, lower alkyl or lower alkoxy, R4 is hydrogen or lower alkyl, and R5 is hydrogen, lower alkyl, benzoyl, substituted benzoyl, lower carbalkoxy or
    There are prepared compounds of the formula
    WHERE A is oxygen, sulfur, imino or lower alkylimino and R6 is lower alkyl, lower alkyl having 1 to 3 halogen atoms, lower alkenyl, hydroxymethyl, carboxymethyl, carb-lower alkoxy methyl, amino lower alkyl or alkylaminoalkyl having 2 to 13 carbon atoms or where any hydroxy or primary or secondary amino group is substituted by an alkanoyl group of 2 to 8 carbon atoms, carbalkoxy having 1 to 6 carbon atoms, carbophenoxy or carbobenzyloxy or a pharmacologically acceptable salt thereof. The compounds are useful in emotional disturbances, tension, anxiety, increased irritability.

    Abstract translation: 制备下式的化合物，其中R1是卤素，R2和R3是氢，卤素，三氟甲基，羟基，氰基，低级烷基或低级烷氧基，R4是氢或低级烷基，R5是氢，低级烷基，苯甲酰基，取代的 苯甲酰基，低级烷氧基或其中A是氧，硫，亚氨基或低级烷基亚氨基，R6是低级烷基，具有1至3个卤素原子的低级烷基，低级烯基，羟甲基，羧甲基，低级烷氧基甲基，氨基低级烷基或烷基氨基烷基， 2至13个碳原子或任何羟基或伯或仲氨基被2至8个碳原子的烷酰基取代，碳原子数1〜6的碳烷氧基，碳苯氧基或苄氧羰基或其药理学上可接受的盐。 这些化合物可用于情绪障碍，紧张，焦虑，烦躁不安。

    6-aza-3h-1,4-benzodiazepines
    2.
    发明授权
    6-aza-3h-1,4-benzodiazepines 失效
    6-AZA-3H-1,4-BENZODIAZEPINES

    公开(公告)号：US3900466A

    公开(公告)日：1975-08-19

    申请号：US46808874

    申请日：1974-05-08

    Applicant: DEGUSSA

    Inventor： VON BEBENBURG WALTER ,  OFFERMANNS HERIBERT

    IPC: C07D213/75 ,  C07D471/04 ,  C07D57/04

    CPC classification number: C07D213/75 ,  C07D471/04

    Abstract: There are prepared compounds of the formula:

    WHEREIN: N IS AN INTEGER FROM 1 TO 4; R1 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 R1 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(R1) A is the cyano group; B is oxygen, sulfur, an imino group or an alkylimino group having 1 to 6 carbon atoms; R2 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(CH2)n-C( A)-R1; No is nitrogen or an NO group; and R3 and R4 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, antipsychotic and antiphlogistic activity.

    New 6-aza-1,4 -benzodiazepine
    3.
    发明授权
    New 6-aza-1,4 -benzodiazepine 失效
    新的6-氮杂-1,4-苯并二氮杂

    公开(公告)号：US3920633A

    公开(公告)日：1975-11-18

    申请号：US46313074

    申请日：1974-04-22

    Applicant: DEGUSSA

    Inventor： VONBEBENBURG WALTER ,  OFFERMANNS HERIBERT

    IPC: A61K31/55 ,  A61P25/20 ,  A61P29/00 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: WHERE: R1 is a halogen; R2 and R3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, alkyl of 1 to 6 carbon atoms or alkoxy of 1 to 6 carbon atoms; R4 is hydrogen, hydroxy, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, carbamoyloxy (H2NCO-O-) or carbamoxyloxy substituted with (1) an alkyl group of 1 to 6 carbon atoms, (2) alkenyl of 2 to 6 carbon atoms, or (3) cycloalkyl of 3 to 6 carbon atoms; Z is nitrogen or the group *NO; R5 is carbamoyl, thiocarbamoyl or carbamoyl or thiocarbamoyl substituted with (1) alkyl of 1 to 6 carbon atoms, (2) alkenyl of 2 to 6 carbon atoms, or (3) cycloalkyl of 3 to 6 carbon atoms; and A is oxygen, sulfur or N-R where R is hydrogen or alkyl of 1 to 6 carbon atoms and the group -C( A)-CHR4 can also be in the tautomeric form -(C(AR4)-CH- and pharmaceutically acceptable salts thereof. The compounds have psychosedative, anxiolytic and antiphlogistic activity.

    There are prepared compounds of the formula:

    Abstract translation: 制备下式的化合物：

    Process of making penicillamine
    4.
    发明授权
    Process of making penicillamine 失效
    制备苯胺胺的方法

    公开(公告)号：US3888923A

    公开(公告)日：1975-06-10

    申请号：US28323372

    申请日：1972-08-23

    Applicant: DEGUSSA

    Inventor： ASINGER FRIEDRICH ,  GLUZEK KARL-HEINZ ,  OFFERMANNS HERIBERT

    IPC: C07C319/02 ,  C07C67/00 ,  C07C227/16 ,  C07C241/00 ,  C07C313/00 ,  C07C323/58 ,  C07C101/20 ,  C07C99/00

    CPC classification number: C07C227/16

    Abstract: Penicillamine or a derivative thereof is made by starting from 2-isopropyl-5,5-dimethylthiazolidine of the formula

    WHEREIN A is an ester group having one to five carbon atoms in the alcohol moiety, a carboxylic amide or thiocarboxylic amide group or one of the latter two groups which is mono- or disubstituted by alkyl of one to six carbon atoms or phenyl or wherein A is a carboxyl group. The starting compound is reacted with a carbonyl reagent in the presence of water and of a water immiscible inert organic solvent and the two phases formed in the reaction are then separated and the penicillamine or its derivative is isolated from the aqueous phase.

    Certain 2-oxy-5-phenyl-6-aza-7-chloro-1,2-dihydro-3H-1,4-benzodiazepines
    5.
    发明授权
    Certain 2-oxy-5-phenyl-6-aza-7-chloro-1,2-dihydro-3H-1,4-benzodiazepines 失效
    某些2-氧基-5-苯基-6-氮杂-7-氯-1,2-二氢-3H-1,4-苯并二氮杂

    公开(公告)号：US3917629A

    公开(公告)日：1975-11-04

    申请号：US46312974

    申请日：1974-04-22

    Applicant: DEGUSSA

    Inventor： VON BEBENBURG WALTER ,  OFFERMANNS HERIBERT

    IPC: A61K31/55 ,  A61P25/20 ,  A61P29/00 ,  C07D471/04 ,  C07D243/06

    CPC classification number: C07D471/04 ,  Y10S514/916

    Abstract: There are produced 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula:

    wherein: R1 is hydrogen, a lower alkyl group, a lower alkenyl group, a cycloalkyl group, a hydroxy lower alkyl group a lower alkoxy lower alkyl group, an amino-alkyl group, mono or dialkyl aminoalkyl or a 5 to 7 membered heterocyclic ring having 1 to 2 nitrogen atoms or 1 nitrogen atom and 1 oxygen atom in the ring attached to alkyl; R2 is hydrogen, lower alkyl or lower alkoxy lower alkyl; R3 is hydrogen, lower alkyl or lower alkoxy; and R4 is hydrogen or halogen and pharmaceutically acceptable salts thereof. The compounds have pharmacodynamic properties including psychosedative and especially anxiolytic properties as well as spasmolytic and antiphlogistic action.

    Abstract translation: 产生下式的6-氮杂-1,2-二氢-3H-1,4-苯并二氮杂：R1OR2 || N-CH角度CH-R3 I Cl | C = N | | R4其中：

    Process of making thiazolines-3
    6.
    发明授权
    Process of making thiazolines-3 失效
    制备噻唑啉-3的方法

    公开(公告)号：US3700683A

    公开(公告)日：1972-10-24

    申请号：US3700683D

    申请日：1969-09-04

    Applicant: DEGUSSA

    Inventor： ASINGER FRIEDRICH ,  OFFERMANNS HERIBERT ,  GHYCZY MIKOLS

    IPC: C07D277/10 ,  C07D91/24

    CPC classification number: C07D277/10

    Abstract: 2,5,5-substituted thiazolines- Delta 3 of the formula IN WHICH R1 and R2 are alkyl and may be the same or different, alkyl having one to four carbon atoms are made by reacting an aldehyde of the formula WHEREIN R has the same meaning as above, with sulfur and ammonia or an ammonium or sulfur compound in the presence of a secondary or tertiary amine while azeotropically removing the reaction water. The process results in very high yields.

    Abstract translation: 具有1-4个碳原子的烷基，其中R 1和R 2为烷基并且可以相同或不同的具有1-4个碳原子的烷基的2,5,5-取代噻唑啉-D-3TA是通过使式WHEREIN R的醛与 如上所述，在仲胺或叔胺的存在下用硫和氨或铵或硫化合物，同时共沸除去反应水。

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