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44 条记录 (耗时 0.047 秒)

    Unsaturated amino acids
    15.
    发明授权
    Unsaturated amino acids 失效
    不饱和氨基酸

    公开(公告)号：US5175344A

    公开(公告)日：1992-12-29

    申请号：US731580

    申请日：1991-07-17

    申请人： Christof Angst ,  Derek E. Brundish ,  John G. Dingwall ,  Graham E. Fagg ,  Hans Allgeier ,  Guido Bold ,  Rudolf Duthaler ,  Roland Heckendorn ,  Antonio Togni

    发明人： Christof Angst ,  Derek E. Brundish ,  John G. Dingwall ,  Graham E. Fagg ,  Hans Allgeier ,  Guido Bold ,  Rudolf Duthaler ,  Roland Heckendorn ,  Antonio Togni

    IPC分类号： C07F9/30 ,  C07F9/32 ,  C07F9/38 ,  C07F9/40 ,  C07F9/48

    CPC分类号： C07F9/4825 ,  C07F9/302 ,  C07F9/3217 ,  C07F9/3826 ,  C07F9/4015

    摘要： The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.

    摘要翻译： 本发明涉及式I（I）的不饱和氨基酸，其中R 1表示羟基或醚化羟基，R 2表示氢，烷基，羟基或醚化羟基，R 3表示氢，烷基，卤代烷基，羟基烷基，低级烷氧基烷基， 芳基烷基，低级烯基，卤素或芳基，R 4表示氢，烷基或芳基，R 5表示氢或烷基，R 6表示羧基或酯化或酰胺化羧基，R 7表示氨基或被烷基或酰基取代的氨基，A表示未取代或烷基取代 具有1至3个碳原子的α，ω-亚烷基或表示键，并且B表示亚甲基或键，条件是当B表示键时A不是键，以及其盐。 它们可以例如根据Michaelis-Arbuzov反应制造，并且可以用作药理活性物质。

    6-Substituted-11b-phenyl-3, 11bH-oxazirino[2,3-d]-s-triazol[4,3-a][1,4]benzodiazepines
    16.
    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。

    4-substituted 2-aminoalk-3-enoic acids
    18.
    发明授权
    4-substituted 2-aminoalk-3-enoic acids 失效
    4-取代的2-氨基-3-烯酸

    公开(公告)号：US5294734A

    公开(公告)日：1994-03-15

    申请号：US851437

    申请日：1992-03-16

    申请人： Christof Angst ,  Hans Allgeier ,  Roland Heckendorn ,  Daniel Wallach

    发明人： Christof Angst ,  Hans Allgeier ,  Roland Heckendorn ,  Daniel Wallach

    IPC分类号： C07F9/38 ,  C07F9/59 ,  A61K31/66

    CPC分类号： C07F9/592 ,  C07F9/3826

    摘要： Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by optionally acylated or aliphatically or araliphatically etherified hydroxy, by halogen, by optionally acylated and/or aliphatically substituted amino or by an aza-, diaza-, azoxa- or oxa-cycloaliphatic radical, or is an oxacycloaliphatic hydrocarbon radical bonded via a carbon atom, or is an optionally aliphatically N-substituted or N-acylated azacycloaliphatic hydrocarbon radical, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.

    摘要翻译： 取代的式I的2-氨基-3-烯酸衍生物其中R 1是被任选被酰化或脂族或芳烷基醚化的羟基，被卤素任选被酰化和/或脂族取代的脂族烃基 氨基或氮杂 - ，二氮杂 - 氮杂 - 或氧杂 - 脂环族基团，或是通过碳原子键合的氧杂环脂族烃基，或任选地是脂族N-取代或N-酰化氮杂环脂族烃基，R2是游离的 或酯化的羧基，它们的盐表现出NMDA-拮抗性质，可用作抗惊厥药物的活性成分。

    Triazolobenzodiazepine derivatives
    19.
    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
    20.
    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。