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公开(公告)号：US4017532A
公开(公告)日：1977-04-12
申请号：US676092
申请日：1976-04-12
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。
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公开(公告)号：US4014883A
公开(公告)日：1977-03-29
申请号：US596684
申请日：1975-07-16
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。
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公开(公告)号：US4111934A
公开(公告)日：1978-09-05
申请号：US861084
申请日：1977-12-15
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.
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公开(公告)号：US4080323A
公开(公告)日：1978-03-21
申请号：US775347
申请日：1977-03-07
申请人： Armin Walser , Rodney Ian Fryer
发明人： Armin Walser , Rodney Ian Fryer
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , C07D243/12 , C07D487/04
CPC分类号： C07D487/04 , C07D243/12 , Y10S514/906
摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be differentAnd the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
摘要翻译： 本发明涉及下式的化合物，其中X是氢或卤素; R1是氢，卤素或三氟甲基; R2是氢或低级烷基; 并且R 3是氢，-COO低级烷基或CON（R 4）2，其中R 4是低级烷基或氢，并且可以是不同的，并且其药学上可接受的盐。
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公开(公告)号：US4014916A
公开(公告)日：1977-03-29
申请号：US676091
申请日：1976-04-12
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。
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6.发明授权
公开(公告)号：US3979410A
公开(公告)日：1976-09-07
申请号：US615436
申请日：1975-09-22
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07C205/45
摘要： o-nitrobenzylketones are prepared by reacting a trans-.beta.-substituted amino-2-nitrostyrene with a lower alkanoyl halide, halo-lower alkanoyl halide, phthalimido-lower alkanoyl halide, benzoyl halide or substituted benzoyl halide, and subsequently hydrolyzing the resulting product to yield the desired o-nitrobenzylketone.
摘要翻译： 邻硝基苄基酮通过反式-β-取代的氨基-2-硝基苯乙烯与低级烷酰卤，卤代低级烷酰卤，苯二甲酰亚氨基 - 低级烷酰卤，苯甲酰卤或取代的苯甲酰卤反应制备，随后将所得产物水解成 得到所需的邻硝基苄基酮。
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公开(公告)号：US4111931A
公开(公告)日：1978-09-05
申请号：US874074
申请日：1978-02-01
申请人： Armin Walser , Rodney Ian Fryer
发明人： Armin Walser , Rodney Ian Fryer
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , C07D243/12 , C07D487/04
CPC分类号： C07D487/04 , C07D243/12 , Y10S514/906
摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.2 is lower alkyl or hydrogen and may be differentand the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
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公开(公告)号：US4017531A
公开(公告)日：1977-04-12
申请号：US676077
申请日：1976-04-12
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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公开(公告)号：US3931225A
公开(公告)日：1976-01-06
申请号：US435050
申请日：1974-01-21
IPC分类号： C07C49/76 , C07D209/08 , C07D209/10 , C07D209/48
CPC分类号： C07D209/48 , C07C201/12 , C07D209/08 , C07D209/10
摘要： o-nitrobenzylketones are prepared by reacting a trans-.beta.-substituted amino-2-nitrostyrene with a lower alkanoyl halide, halo-lower alkanoyl halide, phthalimido-lower alkanoyl halide, benzoyl halide or substituted benzoyl halide, and subsequently hydrolyzing the resulting product to yield the desired o-nitrobenzylketone.
摘要翻译： 邻硝基苄基酮通过反式-β-取代的氨基-2-硝基苯乙烯与低级烷酰卤，卤代低级烷酰卤，苯二甲酰亚氨基 - 低级烷酰卤，苯甲酰卤或取代的苯甲酰卤反应制备，随后将所得产物水解成 得到所需的邻硝基苄基酮。
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10.发明授权Preparation of 7-substituted-1-(2-diethylaminoethyl)-5-(2-halophenyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-ones 失效7-取代的1-（2-二乙基氨基乙基）-5-（2-咔唑基）-1,3-二氢-2H-哒嗪-2,3-苯并二吖庚因-2-酮的制备
公开(公告)号：US3691157A
公开(公告)日：1972-09-12
申请号：US3691157D
申请日：1970-08-12
IPC分类号： C07D209/48 , C07D53/06
CPC分类号： C07D209/48
摘要： 7-Substituted-1-(2-diethylaminoethyl)-5-(2-halophenyl)-1,3dihydro-2H-1,4 -benzodiazepin-2-ones are prepared starting with a 4-substituted-2-(2-halobenzoyl)aniline by a multi-step procedure. The product compounds produced by the process of the present invention are useful as tranquillizers, muscle relaxants, anticonvulsants and hypnotics.
摘要翻译： 7-取代的1-（2-二乙基氨基乙基）-5-（2-卤代苯基）-1,3-二氢-2H-1,4-苯并二氮杂-酮由4-取代-2-（2 - 苯甲酰基）苯胺。 通过本发明方法生产的产品化合物可用作镇静剂，肌肉松弛剂，抗惊厥药和催眠药。
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