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11. 发明授权

US4510141A Tricyclic polyazaheterocycles for treating depression or anxiety 失效
标题翻译：用于治疗抑郁或焦虑的三环多环杂环
公开(公告)号：US4510141A
公开(公告)日：1985-04-09
申请号：US417788
申请日：1982-09-13
申请人： Roland Heckendorn
发明人： Roland Heckendorn
IPC分类号： C07D249/10 , C07D471/14 , C07D487/04 , A61K31/50 , A61K31/535
CPC分类号： C07D471/14 , C07D249/10 , C07D487/04
摘要： The invention relates to novel polycyclic polyazaheterocycles having psychopharmacological properties, especially antidepressive and anxiolytic activity, corresponding to the formula I ##STR1## in which R.sub.1 and R.sub.2 each represents, independently of the other, hydrogen, lower alkyl or hydroxy-lower alkyl, or together represent lower alkylene or ethyleneoxyethylene, ethyleneazaethylene or N-lower alkyl- or N-(2-hydroxy-lower alkyl)-ethyleneazaethylene, R.sub.3 represents hydrogen or a lower aliphatic hydrocarbon radical or a saturated lower cycloaliphatic hydrocarbon radical or unsubstituted or substituted phenyl, R.sub.4 and R.sub.5 represent hydrogen or lower alkyl, and Ar represents an unsubstituted or substituted benzo or pyrido radical, and to acid addition salts of compounds of the general formula I, especially the pharmaceutically acceptable acid addition salts of compounds of the general formula I, to pharmaceutical preparations containing these novel substances and to a method of treating conditions of depression or anxiety by administering them.
摘要翻译：本发明涉及对应于式I（I）的精神药理学特性，特别是抗抑郁和抗焦虑活性的新型多环多环杂环，其中R 1和R 2各自独立地代表氢，低级烷基或羟基 - 低级烷基，或一起表示低级亚烷基或亚乙氧基亚乙基，亚乙基亚乙烯基或N-低级烷基 - 或N-（2-羟基 - 低级烷基）亚甲基亚乙基亚甲基，R3表示氢或低级脂族烃基或饱和的低级脂环族烃基或未取代或取代的苯基，R 4和R 5表示氢或低级烷基，Ar表示未取代或取代的苯并或吡啶基，以及通式I化合物的酸加成盐，特别是通式I化合物的药学上可接受的酸加成盐，含有这些新物质的药物制剂和治疗con的方法抑郁症或焦虑症的治疗方式。

12. 发明授权

US4209515A Triazole derivatives 失效
标题翻译：三唑衍生物
公开(公告)号：US4209515A
公开(公告)日：1980-06-24
申请号：US942081
申请日：1978-09-13
申请人： Roland Heckendorn , Rene Meier
发明人： Roland Heckendorn , Rene Meier
IPC分类号： C07D249/08 , A61K31/41 , A61K31/535 , C07D413/06
CPC分类号： C07D249/08
摘要： The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl, R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anticonvulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation. Specific embodiments are the 1-[2-(o-chlorobenzoyl)-4-chlorophenyl]-5-(morpholinomethyl)-1H-1,2,4-triazole-3-carboxamide and the N,N-dimethyl-1-[2-(o-fluorobenzoyl)-4-chlorophenyl]-5-[(dimethylamino)-methyl]-1H-1,2,4-triazole-3-carboxamide.
摘要翻译：本发明涉及式（I）的新的三唑衍生物，其中R 1表示氢，低级烷基，任选酯化或醚化的羟甲基，甲酰基，任选的官能改性的羧基或任选的单或二取代的氨基甲基，R 2表示低级烷基并且R 3表示氢或低级烷基，其中作为低级烷基的R 2和R 3可以直接键合，也可以通过氧，硫或亚氨基或低级亚烷基亚氨基自由键合在β-或γ-位。和B彼此独立地可以是未取代的或取代的，以及它们与无机和有机酸的加成盐，特别是药学上可接受的酸加成盐。这些新化合物具有宝贵的药理学特性。特别是它们具有抗惊厥活性，并且可用于治疗癫痫以及张力和搅动条件。具体实施方案是1- [2-（邻氯苯甲酰基）-4-氯苯基] -5-（吗啉代甲基）-1H-1,2,4-噻唑-3-甲酰胺和N，N-二甲基-1- [2-（邻氟苯甲酰基）-4-氯苯基] -5 - [（二甲基氨基） - 甲基] -1H-1,2,4-三唑-3-甲酰胺。

13. 发明授权

US4111950A Triazolyl benzophenones 失效
标题翻译：三唑基二苯甲酮
公开(公告)号：US4111950A
公开(公告)日：1978-09-05
申请号：US765573
申请日：1977-02-04
申请人： Andre Gagneux , Roland Heckendorn , Rene Meier
发明人： Andre Gagneux , Roland Heckendorn , Rene Meier
IPC分类号： A61K31/55 , C07D249/08 , C07D249/10 , C09B29/32 , C07D401/06 , C07D403/06 , C07D413/06 , C07D487/04
CPC分类号： A61K31/55 , C07D249/10 , C09B29/32
摘要： Compounds of the class of 6-phenyl-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-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 inhibit somatic reflexes. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide, 6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide, N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide and N,N-dimethyl-6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carboxamide.
摘要翻译： 6-苯基-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂-2-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抑制体细胞反射。具体实施方案是N，N-二甲基-6-苯基-8-氯-4H-s-三唑并[1,5-a] [1,4]苯并二氮杂-2-甲酰胺，6-（邻氟苯基）-8- 5-氯-4H-三唑并[1,5-a] [1,4]苯并二氮杂-2-甲酰胺，N，N-二甲基-6-（邻氟苯基）-8-氯-4H-三唑并[1 ，5-a] [1,4]苯并二氮杂-2-甲酰胺和N，N-二甲基-6-（邻氯苯基）-8-氯-4H-三唑并[1,5-a] 4]苯并二氮杂-2-甲酰胺。

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