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1. 发明授权

US3954753A 2-Aroyl-3-amino pyrazines and the 3(-2haloacetamide derivatives thereof 失效
标题翻译： 2-芳酰基-3-氨基吡嗪及其3（ - 2-卤代乙酰胺衍生物）
公开(公告)号：US3954753A
公开(公告)日：1976-05-04
申请号：US549566
申请日：1975-02-13
申请人： George Francis Field , Leo Henryk Sternbach , Armin Walser
发明人： George Francis Field , Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D241/20 , C07D401/06 , C07D403/06 , C07D487/04 , C07D241/14
CPC分类号： C07D401/06 , C07D241/20 , C07D403/06 , C07D487/04
摘要： Novel pyrazino-1,4-diazepines are disclosed together with processes for their preparation and novel intermediates used in these processes. These novel diazepines are useful as sedatives, muscle-relaxants and anti-convulsants.
摘要翻译：公开了新的吡嗪-1,4-二氮杂及其制备方法和用于这些方法的新型中间体。这些新的二氮杂类药物可用作镇静剂，肌肉松弛剂和抗惊厥药。

2. 发明授权

US4014883A Indoloquinolines, intermediates and processes 失效
标题翻译：吲哚喹啉，中间体和工艺
公开(公告)号：US4014883A
公开(公告)日：1977-03-29
申请号：US596684
申请日：1975-07-16
申请人： Rodney Ian Fryer , Robert Ye-Fong Ning , Leo Henryk Sternbach , Armin Walser
发明人： Rodney Ian Fryer , Robert Ye-Fong Ning , Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D209/42 , C07D215/38 , C07D471/04
CPC分类号： C07D215/38 , C07C251/72 , C07D209/42 , C07D471/04
摘要： Derivatives of 7H-indolo[2,3-c]quinolin-6(5H)-one and 7H-indolo[2,3-c]quinoline, prepared, inter alia, from the corresponding 3-azido-4-phenylcarbostyrils or corresponding N-(lower alkylamino)-3-(2-fluorophenyl)-indole-2-carboxamides, are described. The end products of the invention are useful as anti-tumor agents, i.e., they inhibit the growth of transplantable tumors.
摘要翻译： 7H-吲哚并[2,3-c]喹啉-6（5H） - 酮和7H-吲哚并[2,3-c]喹啉的衍生物，特别是由相应的3-叠氮基-4-苯基苯甲腈或相应的描述了N-（低级烷基氨基）-3-（2-氟苯基） - 吲哚-2-甲酰胺。本发明的最终产物可用作抗肿瘤剂，即它们抑制可移植肿瘤的生长。

3. 发明授权

US3970664A Preparation of triazolo benzodiazepines 失效
标题翻译：三唑并苯并二氮杂的制备
公开(公告)号：US3970664A
公开(公告)日：1976-07-20
申请号：US540626
申请日：1975-01-13
申请人： Leo Henryk Sternbach , Armin Walser
发明人： Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D243/20 , C07D401/04 , C07D487/04
CPC分类号： C07D243/20 , C07D401/04 , C07D487/04
摘要： Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anticonvulsants, muscle relaxants and sedative agents.
摘要翻译：公开了三唑并苯并二氮杂类的新型制剂。还公开了新颖的6-吡啶基-4H-三唑并[4,3-a] -1,4-苯并二氮杂和新的中间体，其可用作抗惊厥药，肌肉松弛剂和镇静剂。

4. 发明授权

US4111934A 1,5-Benzodiazepin-4-ones 失效
标题翻译： 1,5-BENZODIAZEPIN-4-ONES
公开(公告)号：US4111934A
公开(公告)日：1978-09-05
申请号：US861084
申请日：1977-12-15
申请人： Rodney Ian Fryer , Leo Henryk Sternbach , Armin Walser
发明人： Rodney Ian Fryer , Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D243/12 , C07D487/04
CPC分类号： C07D487/04 , C07D243/12 , Y10S514/906
摘要： Novel 1,5-benzodiazepin-4-one derivatives, bearing between the 1,2-positions a triazolo ring, as disclosed. These 1,2-triazolo-1,5-benzodiazepin-4-ones are useful as muscle-relaxant, anti-convulsant and sedative agents.

5. 发明授权

US4044016A Preparation of triazolo benzodiazepines and novel compounds 失效
标题翻译：三唑并苯并二氮杂类和新化合物的制备
公开(公告)号：US4044016A
公开(公告)日：1977-08-23
申请号：US684435
申请日：1976-05-07
申请人： Leo Henryk Sternbach , Armin Walser
发明人： Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D401/04 , C07D487/04 , C07D213/24 , A61K31/44
CPC分类号： C07D401/04 , C07D487/04 , Y10S514/906
摘要： Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anticonvulsants, muscle relaxants and sedative agents.
摘要翻译：公开了三唑并苯并二氮杂类的新型制剂。还公开了新颖的6-吡啶基-4H-三唑并[4,3-a] -1,4-苯并二氮杂和新的中间体，其可用作抗惊厥药，肌肉松弛剂和镇静剂。

6. 发明授权

US3954728A Preparation of triazolo benzodiazepines and novel compounds 失效
标题翻译：三唑并苯并二氮杂类和新化合物的制备
公开(公告)号：US3954728A
公开(公告)日：1976-05-04
申请号：US540756
申请日：1975-01-13
申请人： Leo Henryk Sternbach , Armin Walser
发明人： Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D243/20 , C07D401/04 , C07D213/00
CPC分类号： C07D243/20 , C07D401/04
摘要： Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anti-convulsants, muscle relaxants and sedative agents.
摘要翻译：公开了三唑并苯并二氮杂类的新型制剂。还公开了新颖的6-吡啶基-4H-三唑并[4,3-a] -1,4-苯并二氮杂并且可用作抗惊厥药，肌肉松弛剂和镇静剂的新型中间体。

7. 发明授权

US4017532A Intermediates for the production of tricyclic benzodiazepines 失效
标题翻译：用于生产三环苯并二氮杂类的中间体
公开(公告)号：US4017532A
公开(公告)日：1977-04-12
申请号：US676092
申请日：1976-04-12
申请人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
发明人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
IPC分类号： C07D213/24 , C07D243/16 , C07C69/96
CPC分类号： C07D243/16 , C07D213/24
摘要： Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. "A" bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. "A" bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. "A" are useful as sedative, muscle relaxant and anti-convulsant agents.
摘要翻译：描述了在1-位上带有羟基低级烷基取代基的三环苯并二氮杂衍生物（“A”）和苯并二氮杂部分位置4和5之间连接的杂环。杂环将含有出现在苯并二氮杂环的第4位的氮原子以及与苯并二氮杂环的5-位的碳原子连接的可以是氧或氮的杂原子。在新的杂环中带有氧原子的“A”可以通过在酸催化剂的存在下用环氧化合物处理由相应的4,5-不饱和的苯并二氮杂卟啉形成。在新杂环中带有氮原子或氧原子的“A”可以通过相应的开放化合物的环化来制备。 “A”可用作镇静剂，肌肉松弛剂和抗惊厥剂。

8. 发明授权

US3965151A Intermediates for tricyclic benzodiazepines 失效
标题翻译：三环苯并二氮杂类中间体
公开(公告)号：US3965151A
公开(公告)日：1976-06-22
申请号：US557438
申请日：1975-03-11
申请人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
发明人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
IPC分类号： C07D213/24 , C07D243/16 , C07C97/10 , C07C103/42
CPC分类号： C07D243/16 , C07D213/24
摘要： Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. "A" bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. "A" bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. "A" are useful as sedative, muscle relaxant and anti-convulsant agents.
摘要翻译：描述了在1-位上带有羟基低级烷基取代基的三环苯并二氮杂衍生物（“A”）和苯并二氮杂部分位置4和5之间连接的杂环。杂环将含有出现在苯并二氮杂环的第4位的氮原子以及与苯并二氮杂环的5-位的碳原子连接的可以是氧或氮的杂原子。在新的杂环中带有氧原子的“A”可以通过在酸催化剂的存在下用环氧化合物处理由相应的4,5-不饱和的苯并二氮杂卟啉形成。在新杂环中带有氮原子或氧原子的“A”可以通过相应的开放化合物的环化来制备。 “A”可用作镇静剂，肌肉松弛剂和抗惊厥剂。

9. 发明授权

US3931217A 2,3-Dihydro-5-alkoxy-5-phenyl-5H-imidazo[2,1-a]isoindoles 失效
标题翻译： 2,3-二氢-5-烷氧基-5-苯基-5H-咪唑并[8,2,1-a {9异吲哚
公开(公告)号：US3931217A
公开(公告)日：1976-01-06
申请号：US467428
申请日：1974-05-06
申请人： Werner Metlesics , Leo Henryk Sternbach
发明人： Werner Metlesics , Leo Henryk Sternbach
IPC分类号： A61K31/00 , C07C45/41 , C07C49/86 , C07C51/363 , C07D209/44 , C07D233/22 , C07D487/04 , C07D235/02
CPC分类号： C07D487/04 , A61K31/00 , C07C45/29 , C07C45/41 , C07C51/363 , C07D209/44 , C07D233/22 , Y10S514/916
摘要： Novel 2[2-(1,3-diazacycloalk-2-enyl)]benzophenone compounds and novel 1,3-diazacycloalkenyl[2,1-a]isoindole compounds having useful analgesic and psychostimulant properties are prepared inter alia by condensation of o-benzoylbenzaldehydes with aliphatic diamines.
摘要翻译：新颖的2- [2-（1,3-二氮杂环烯-2-烯基）]二苯甲酮化合物和具有有用的止痛和精神兴奋剂性质的新的1,3-二氮杂环烯基[2,1-a]异吲哚化合物特别是通过o- 苯甲酰基苯甲醛与脂族二胺。

10. 发明授权

US4017531A Intermediates for the production of tricyclic benzodiazepines 失效
标题翻译：用于生产三环苯并二氮杂类的中间体
公开(公告)号：US4017531A
公开(公告)日：1977-04-12
申请号：US676077
申请日：1976-04-12
申请人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
发明人： Michael Edward Derieg , James Valentine Earley , Rodney Ian Fryer , Leo Henryk Sternbach
IPC分类号： C07D213/24 , C07D243/16 , C07C69/96
CPC分类号： C07D243/16 , C07D213/24
摘要： Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. A bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. A bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. A are useful as sedative, muscle relaxant and anti-convulsant agents.
摘要翻译：描述了在1-位上带有羟基低级烷基取代基的三环苯并二氮杂衍生物（“A”）和苯并二氮杂部分位置4和5之间连接的杂环。杂环将含有出现在苯并二氮杂环的第4位的氮原子以及与苯并二氮杂环的5-位的碳原子连接的可以是氧或氮的杂原子。在新杂环中带有氧原子的A可以通过在酸催化剂存在下用环氧化合物处理由相应的4,5-不饱和苯并二氮杂卟啉形成。在新杂环中带有氮原子或氧原子的化合物可以通过相应的开放化合物的环化来制备。 A可用作镇静剂，肌肉松弛剂和抗惊厥剂。

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