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    Triazolobenzodiazepine derivatives
    1.
    发明授权
    Triazolobenzodiazepine derivatives 失效
    三唑并苯并二氮杂衍生物

    公开(公告)号：US4427590A

    公开(公告)日：1984-01-24

    申请号：US199770

    申请日：1971-11-17

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： C07D243/26 ,  A61K31/4985 ,  A61K31/55 ,  A61P25/08 ,  A61P25/20 ,  C07D243/16 ,  C07D309/12 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D309/12

    摘要： Compounds of the class of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-lower alkanols, and their ethers and esters, 1-(fluoro-lower alkyl)-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines and the 5-oxides and pharmaceutically acceptable acid addition salts thereof have central depressant properties, in particular antiaggressive and anticonvulsant actions, and are active ingredients for pharmaceutical compositions. Specific embodients are 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-methanol and 1-(fluoromethyl)6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine.

    摘要翻译： 6-苯基-4H-3-三唑并[4,3-a] [1,4]苯并二氮杂-1-低级链烷醇类化合物及其醚和酯，1-（氟 - 低级烷基）-6- 苯并噻唑并[4,3-a] [1,4]苯并二氮杂及其5-氧化物及其药学上可接受的酸加成盐具有中枢抑制特性，特别是抗侵袭性和抗惊厥作用，并且是药物的活性成分 组合物。 具体实施方案是6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲醇和1-（氟甲基）-6-苯基-8-氯-4H- - 三唑并[4,3-a] [1,4]苯并二氮杂。

    Diazepine derivatives in the treatment of tension, agitation and epilepsy
    2.
    发明授权
    Diazepine derivatives in the treatment of tension, agitation and epilepsy 失效
    二氮衍生物治疗紧张，躁动和癫痫

    公开(公告)号：US4002764A

    公开(公告)日：1977-01-11

    申请号：US634808

    申请日：1975-11-24

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： A61K31/41

    摘要： Compounds of the class of 6-phenyl-4H-s-triazolo [4,3-a][1,4]benzodiazepine-1-carboxamides, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anti-convulsive and anti-aggressive action and potentiate the action of anaesthetics. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide, 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide, N,N-dimethyl-6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide and 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide.

    摘要翻译： 6-苯基-4H-s-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺类化合物及其药学上可接受的酸加成盐具有有价值的药理学性质并且是有活性的 治疗组合物的成分。 特别地，这些新化合物具有抗惊厥和抗侵袭作用并且增强了麻醉剂的作用。 具体实施方案是N，N-二甲基-6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂_-甲酰胺，6-苯基-8-氯-4H- 三唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺，N，N-二甲基-6-（邻氯苯基）-8-氯-4H-三唑并[4,3-a ] [1,4]苯并二氮杂-1-甲酰胺和6-（邻氯苯基）-8-氯-4H-吖唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺。

    6-Substituted-11b-phenyl-3, 11bH-oxazirino[2,3-d]-s-triazol[4,3-a][1,4]benzodiazepines
    3.
    发明授权
    6-Substituted-11b-phenyl-3, 11bH-oxazirino[2,3-d]-s-triazol[4,3-a][1,4]benzodiazepines 失效
    6-取代的-11β-苯基-3,11bH-恶唑并[8,2-d] {9-三唑{8,43-a {9 {8 1,4 {9 benzodiazepines

    公开(公告)号：US3941799A

    公开(公告)日：1976-03-02

    申请号：US360852

    申请日：1973-05-16

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： C07D487/04 ,  C07D498/14

    CPC分类号： C07D487/04 ,  Y10S514/96 ,  Y10S514/962 ,  Y10S514/966

    摘要： Compounds of the class of 6-substituted 11b-phenyl-3,11b-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4]benzodiazepines have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anticonvulsive action and inhibit somatic reflexes. Specific embodiments are 10-chloro-11b-phenyl-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4] benzodiazepine-6-methanol, 10-chloro-11b-phenyl-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4]benzodiazepine-6-carboxaldehyde-diethylacetal and 10-chloro-11b-(o-chlorophenyl)-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4]benzodiazepine-6-carboxaldehyde-diethylacetal.

    摘要翻译： 6-取代的11b-苯基-3,11b-恶唑并[2,3-d] -s-三唑并[4,3-a] [1,4]苯并二氮杂类的化合物具有有价值的药理学性质，并且是 治疗组合物。 特别地，这些新化合物具有抗惊厥作用并抑制体细胞反射。 具体实施方案是10-氯-11-11b-苯基-3,11bH-恶唑并[2,3-d] -s-三唑并[4,3-a] [1,4]苯并二氮杂-6-甲醇，10-氯-11b - 苯基-3,11bH-恶唑并[2,3-d] -s-三唑并[4,3-a] [1,4]苯并噻二唑-6-甲醛 - 二乙基缩醛和10-氯-11β-（邻氯苯基） ）-3,11bH-恶唑并[2,3-d] -s-三唑并[4,3-a] [1,4]苯并二氮杂-6-甲醛 - 二乙基缩醛。

    Triazolo benzodiazepine-1-carboxamides
    4.
    发明授权
    Triazolo benzodiazepine-1-carboxamides 失效
    三唑并苯并二氮杂-1-甲酰胺

    公开(公告)号：US3948931A

    公开(公告)日：1976-04-06

    申请号：US418137

    申请日：1973-11-21

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： A61K31/55 ,  A61P25/08 ,  A61P25/20 ,  C07D487/04

    CPC分类号： C07D487/04 ,  Y10S514/96 ,  Y10S514/966

    摘要： Compounds of the class of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamides, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anti-convulsive and anti-aggressive action and potentiate the action of anaesthetics. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide, 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide, N,N-dimethyl-6-(o-chlorophenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide and 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide.

    摘要翻译： 6-苯基-4H-s-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺类化合物及其药学上可接受的酸加成盐具有有价值的药理学性质并且是有活性的 治疗组合物的成分。 特别地，这些新化合物具有抗惊厥和抗侵袭作用并且增强了麻醉剂的作用。 具体实施方案是N，N-二甲基-6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂_-甲酰胺，6-苯基-8-氯-4H- 三唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺，N，N-二甲基-6-（邻氯苯基-8-氯-4H-吖唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺和6-（邻氯苯基）-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲酰胺。

    Acetal derivatives of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde
    5.
    发明授权
    Acetal derivatives of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde 失效
    6-苯基-4H-s-三唑并[8,3,3-a {9 {8 1,4 {9苯并二氮杂-1-甲醛

    公开(公告)号：US3946032A

    公开(公告)日：1976-03-23

    申请号：US406060

    申请日：1973-10-12

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： Compounds of the class of acetals of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde and the 5-oxides and pharmaceutically acceptable acid addition salts thereof have valuable pharmacological properties, in particular anticonvulsant effectiveness. Further, they show central depressant and muscle-relaxing activity and are active ingredients for therapeutic preparations. Specific embodiments are 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal, 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal and 6-(o-fluorophenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde-diethylacetal.

    摘要翻译： 6-苯基-4H-3-三唑并[4,3-a] [1,4]苯并二氮杂-1-甲醛的缩醛类化合物及其5-氧化物和药学上可接受的酸加成盐具有有价值的药理学性质， 特别是抗惊厥效果。 此外，它们显示中枢抑制剂和肌肉松弛活性，并且是治疗制剂的活性成分。 具体实施方案是6-苯基-8-氯-4H-三唑并[4,3-a] [1,4]苯并二氮杂1-甲醛二乙基缩醛，6-（邻氯苯基）-8-氯-4H - 三唑并[4,3-a] [1,4]苯并二氮杂-1-甲醛 - 二乙基缩醛和6-（邻 - 氟苯基-8-氯-4H-三唑并[4,3-a] 4]苯并二氮杂-1-c芳樟醛 - 二乙基缩醛。

    Etherified triazolobenzodiazepine derivatives
    6.
    发明授权
    Etherified triazolobenzodiazepine derivatives 失效
    醚化三唑并苯并二氮杂衍生物

    公开(公告)号：US4178378A

    公开(公告)日：1979-12-11

    申请号：US833421

    申请日：1977-09-15

    申请人： Hans Allgeier ,  Andre Gagneux

    发明人： Hans Allgeier ,  Andre Gagneux

    IPC分类号： A61K31/53 ,  A61K31/55 ,  A61P25/08 ,  A61P25/20 ,  C07D317/22 ,  C07D487/04 ,  A61K31/62

    CPC分类号： C07D487/04 ,  C07C243/00 ,  C07D317/22

    摘要： Etherified diazepine derivatives of the formula ##STR1## in which R.sub.1 represents hydrogen or alkyl having up to 3 carbon atoms, R.sub.2 and R.sub.3 independently of one another each represent hydrogen or alkyl having up to 7 carbon atoms, or represent the partial formula R.sub.4 --(OCH.sub.2 --CH.sub.2).sub.m, in which R.sub.4 represents hydrogen or alkyl having up to 7 carbon atoms and m represents the number 1 to 3, A.sub.1 represents alkylidene or alkylene having up to 3 carbon atoms, A.sub.2, depending on the meaning of n, represents alkylene or alkanetriyl having up to 5 carbon atoms, no carbon atom in the radical A.sub.2 being bonded to more than one oxygen atom, n represents the number 0 or 1, Ph represents substituted or unsubstituted 1,2-phenylene and Ar represents an aromatic radical, and their addition salts are manufactured according to methods known per se. They are useful in the treatment of states of epilepsy, stress and agitation.

    摘要翻译： 其中R 1表示氢或具有至多3个碳原子的烷基的式（I）的醚化二氮杂衍生物，R 2和R 3彼此独立地表示氢或具有至多7个碳原子的烷基，或表示部分式 R 4 - （OCH 2 -CH 2）m，其中R 4表示氢或具有至多7个碳原子的烷基，m表示数1至3，A 1表示亚烷基或具有至多3个碳原子的亚烷基，取决于 n表示具有至多5个碳原子的亚烷基或烷三三基，基团A2中的碳原子不连接至多于一个氧原子，n表示数字0或1，Ph表示取代或未取代的1,2-亚苯基，Ar表示 芳族基团，并且它们的加成盐按照本身已知的方法制备。 它们可用于治疗癫痫，压力和激动的状态。