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公开(公告)号：US4083948A
公开(公告)日：1978-04-11
申请号：US784101
申请日：1977-04-04
CPC分类号： C07K16/44 , C07D243/24 , G01N33/60 , Y10S436/804 , Y10S436/815 , Y10S436/823
摘要： An improved radioimmunoassay for benzodiazepines such as diazepam, chlordiazepoxide, oxazepam, demoxepam and metabolites thereof is disclosed. Such immunoassay employs novel .sup.125 I-labelled 4'-hydroxy derivatives of these compounds as tracer.
摘要翻译： 公开了用于苯二氮卓类的改进的放射免疫测定法，例如地西泮，氯氮卓，奥沙西泮，地塞米松及其代谢物。 这种免疫测定采用这些化合物的新型125I标记的4'-羟基衍生物作为示踪剂。
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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：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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公开(公告)号：US3989681A
公开(公告)日：1976-11-02
申请号：US419582
申请日：1973-11-28
申请人： Rodney Ian Fryer , Armin Walser
发明人： Rodney Ian Fryer , Armin Walser
IPC分类号： C07D243/26 , C07C107/04
CPC分类号： Y10S514/906
摘要： Novel 1,4-benzodiazepin-2-ones of the formula ##SPC1##WhereinR.sub.1 is selected from the group consisting of hydrogen, lower alkyl, cycloalkyl-lower alkyl, hydroxylower alkyl, lower alkoxy-lower alkyl and di-lower alkylamino-lower alkyl;R.sub.2 signifies hydrogen or lower alkyl; R.sub.3 signifies hydrogen or halogen; R.sub.4 signifies lower alkylAnd the pharmaceutically acceptable acid addition salts thereof, are disclosed together with processes for preparing these compounds and novel intermediates used in these processes. These 7-azoxy substituted-1,4-benzodiazepin-2-ones are useful as muscle relaxant, anti-convulsant and sedative agents.
摘要翻译： 新颖的1,4-苯并二氮杂-2-酮，式WHEREIN R1选自氢，低级烷基，环烷基 - 低级烷基，羟基低级烷基，低级烷氧基 - 低级烷基和二 - 低级烷基氨基 - 低级烷基; R2表示氢或低级烷基; R3表示氢或卤素; R4表示低级烷基和其药学上可接受的酸的添加剂，与制备这些化合物和在这些方法中使用的新型中间体的方法无关。 这些7-氧杂取代的1,4-苯并二氮杂-2-酮可用作肌肉松弛剂，抗惊厥剂和镇静剂。
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公开(公告)号：US3965151A
公开(公告)日：1976-06-22
申请号：US557438
申请日：1975-03-11
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。
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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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