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1. 发明授权

US3786051A 1-(phenyl or pyridyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-ones 失效
标题翻译： 1-（苯基或吡啶基）-1,3-二氢-2H-哒嗪-2,4-苯并二吖庚因-2-酮
公开(公告)号：US3786051A
公开(公告)日：1974-01-15
申请号：US3786051D
申请日：1972-04-10
申请人： BOEHRINGER SOHN INGELHEIM
发明人： DANNEBERG P , MINCK K , BAUER A , WEBER K
IPC分类号： A61K20060101 , A61K31/55 , C07D20060101 , C07D213/16 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04 , C07D53/06
CPC分类号： C07D243/24
摘要： COMPOUNDS OF THE FORMULA

1-R2,2-(O=),5-R1,8-R3-1,2-DIHYDRO-3H-1,4-BENZODIAZEPINE

WHEREIN R1 IS HYDROGEN OR ALKYL OF 1 TO 4 CARBON ATOMS, R2 IS PHENYL, NITROPHENYL, TRIFLUOROMETHYL-PHENYL, A-PYRIDYL OR HALOGENOPHENYL, AND R3 IS HALOGEN, NITRO OR TRIFLUOROMETHYL; THE COMPOUNDS ARE USEFUL AS PSYCHOSEDATIVES AND ANTICONVULSIVES.

2. 发明授权

US3760074A Pharmaceutical compositions containing a 5-phenyl-7-bromo-1h-1,5-benzodiazepine-2,4-(3h,5h)-dione 失效
标题翻译：含有5-苯基-7-溴-1H-1,5-苯并二氮杂卓-2（3H，5H） - 酮的药物组合物
公开(公告)号：US3760074A
公开(公告)日：1973-09-18
申请号：US3760074D
申请日：1972-09-27
申请人： BOEHRINGER SOHN INGELHEIM
发明人： HAUPTMANN K , HAUPTMANN M , DANNESBERG P , GIESEMANN R , WEBER K , ZEILE K
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , A61K27/00
CPC分类号： C07D243/12 , A61K31/00
摘要： Psychosedative and anticonvulsive pharmaceutical compositions containing as an active ingredient a compound of the formula
WHEREIN R1 is hydrogen, methyl, ethyl, hydroxy-ethyl or (cycloalkyl of 3 to 6 carbon atoms)-methyl, and R2 is hydrogen or halogen; AND A METHOD OF TRANQUILIZING AND SUPPRESSING CONVULSIONS IN WARM-BLOODED ANIMALS THEREWITH.

D R A W I N G

3. 发明授权

US3711470A 5-phenyl-7-bromo-1h-1,5-benzodiazepine-2,4-(3h,5h)-diones 失效
标题翻译： 5-苯基-7-溴-1H-1,5-苯并二氮杂卓-2H（3H，5H） - 酮
公开(公告)号：US3711470A
公开(公告)日：1973-01-16
申请号：US3711470D
申请日：1971-02-01
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WEBER K , GIESEMANN R , HAUPTMANN K , ZEILE K , DANNEBERG P , HAUPTMANN M
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , C07D53/04
CPC分类号： C07D243/12 , A61K31/00
摘要： COMPOUNDS OF THE FORMULA

1-R1,5-(R2-PHENYL),7-BR-1H-2,3,4,5-TETRAHYDRO-1,5-BENZO

DIAZEPINE-2,4-DIONE

WHEREIN R1 IS HYDROGEN, METHYL, ETHYL, HYDROXY-ETHYL OR (CYCLOALKYL OF 3 TO 6 CARBON ATOMS)-METHYL, AND R2 IS HYDROGEN OR HALOGEN; THE COMPOUNDS ARE USEFUL AS PSYCHOSEDATIVE AND ANTICONVULSIVES.

4. 发明授权

US3711468A 3,3-dihydroxy-5-aryl-1h-1,5-benzodiazepine-2,4-(3h,5h)-diones and their anhydrous 2,3,4-trione form 失效
标题翻译： 3,3-二羟基-5-亚苄基-1H-1,5-苯并二氮杂卓-2H（3H，5H） - 和它们的2,3,4-TRIONE形式
公开(公告)号：US3711468A
公开(公告)日：1973-01-16
申请号：US3711468D
申请日：1972-01-26
申请人： BOEHRINGER SOHN INGELHEIM
发明人： BAUER A , WEBER K , DANNEBERG P , MINCK K
IPC分类号： C07D243/12 , C07D53/04
CPC分类号： C07D243/12
摘要： Compounds of the formula

WHEREIN R1, R2 and R3 have the meanings defined above; the

compounds are useful as tranquilizers and anticonvulsives,

also as intermediates for the preparation of other 1H-1,5-

benzodiazepine-2,4-(3H,5H)-diones.

WHEREIN R1 is hydrogen, straight or branched alkyl of one to four carbon atoms, omega -hydroxy-(alkyl of one to four carbon atoms) or allyl, R2 is phenyl, halo-phenyl, hydroxy-phenyl, trifluoromethylphenyl, nitro-phenyl or pyridyl, and R3 is fluorine, chlorine, bromine, trifluoromethyl or nitro, AND THEIR ANHYDROUS 2,3,4-TRIONE ANALOGS OF THE FORMULA

WHEREIN R1, R2 and R3 have the meanings defined above; the compounds are useful as tranquilizers and anticonvulsives, and also as intermediates for the preparation of other 1H-1,5benzodiazepine-2,4-(3H,5H)-diones.
摘要翻译：式WHEREIN R1的化合物是氢，一至四个碳原子的直链或支链烷基，ω-羟基 - （一至四个碳原子的烷基）或烯丙基，R 2是苯基，卤素 - 苯基，羟基 - 苯基，三氟甲基 - 苯基，硝基 - 苯基或吡啶基，R 3是氟，氯，溴，三氟甲基或硝基，以及它们的化合物，其中R1，R2和R3具有上述定义的无机2,3,4-三烯类似物; 该化合物可用作镇定剂和抗惊厥药，也可用作制备其它1H-1,5-苯并二氮杂-2,4- [3H，5H] - 二酮的中间体。

5. 发明授权

US3836652A Pharmaceutical compositions containing a 5-phenyl-7-trifluoromethyl-1h-1,5-benzodiazepine-2,4-dione 失效
标题翻译：含有5-苯基-7-三氟甲基-1H-1,5-苯并二氮杂卓-2,4-二酮的药物组合物
公开(公告)号：US3836652A
公开(公告)日：1974-09-17
申请号：US29274972
申请日：1972-09-27
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WEBER K , ZEILE K , HAUPTMANN K , HAUPTMANN M , DANNEBERG P , GIESEMANN R
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , A61K27/00
CPC分类号： C07D243/12 , A61K31/00
摘要： PHYSCHOSEDATIVE AND ANTICONVULSIVE PHARMACEUTICAL COMPOSITIONS CONTAINING AS AN ACTIVE INGREDIENT A COMPOUND OF THE FORMULA

1-R1,5-(R2-PHENYL),7-(F3C-)-2,3,4,5-TETRAHYDRO-1,5-BENZODI

AZEPINE-2,4-DIONE

WHEREIN R1 IS HYDROGEN. ALKYL OR 1 TO 3 CARBON ATOMS, HYDROXYALKYL OF 2 TO 3 CARBON ATOMS, ALLYL OR (CYCLOALKYL OF 3 TO 6 CARBON ATOMS)-METHYL, AND R2 IS HYDROGEN, HALOGEN, TRIFLUOROMETHYL OR METHOXY; AND A METHOD OF INDUCING PSYCHOSEDATION AND SUPPRESSING CONVULSIONS IN A WARM-BLOODED ANIMAL THEREWITH.

6. 发明授权

US3711509A 5-phenyl-1h-1,5-benzodiazepine-2,4-(3h,5h)-diones 失效
标题翻译： 5-苯基-1H-1,5-苯并噻吩-2,4-（3H，5H） - 酮
公开(公告)号：US3711509A
公开(公告)日：1973-01-16
申请号：US3711509D
申请日：1971-02-01
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WEBER K , ZEILE K , HAUPTMANN K , HAUPTMANN M , DANNEBERG P , GIESEMANN R
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , C07D53/04
CPC分类号： C07D243/12 , A61K31/00
摘要： COMPOUNDS OF THE FORMULA

1-R1,5-(R2,R3-PHENYL),7-R4-1H-1,5-BENZODIAZEPINE-2,4-(3H,

5H)-DIONE

WHEREIN R1 IS HYDROGEN, STRAIGHT OR BRANCHED ALKYL OF 1 TO 5 CARBON ATOMS, HYDROXY-ALKYL OF 2 TO 4 CARBON ATOMS OR CARBON ATOMS, R2 IS HALOGEN, TRIFLUOROMETHYL OR METHOXY, R3 IS HYDROGEN, HALOGEN, METHYL OR ETHYL, AND R4 IS HYDROGEN, FLUORINE OR CHLORINE; THE COMPOUNDS ARE USEFUL ASPSYCHOSEDATIVES AND ANTICONVULSIVES.

7. 发明授权

US3836653A Pharmaceutical compositions containing a 5-phenyl-7-bromo-1h-1,5-benzodiazepine-2,4-(3h,5h)-dione 失效
标题翻译：含有5-苯基-7-溴-1H-1,5-苯并二氮杂卓-2（3H，5H） - 酮的药物组合物
公开(公告)号：US3836653A
公开(公告)日：1974-09-17
申请号：US30189672
申请日：1972-10-30
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WEBER K , ZEILE K , DANNEBERG P , HAUPTMANN M , GIESEMANN R , HAUPTMANN K
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , A61K27/00
CPC分类号： C07D243/12 , A61K31/00
摘要： PSYCHOSEDATIVE AND ANTICONVULSIVE PHARMACEUTICAL CONTAINING AS AN ACTIVE INGREDIENT A COMPOUND OF THE FORMULA

1-R1,5-(R2,R3-PHENYL),7-R4-2,3,4,5-TETRAHYDRO-1,5-BENZODI

AZEPINE-2,4-DIONE

WHEREIN R1 IS HYDROGEN, STRAIGHT OR BRANCHED ALKYL OF 1 TO 5 CARBON ATOMS, HYDROXY-ALKYL OF 2 TO 4 CARBON ATOMS OR DI(ALKYL OF 1 TO 4 CARBON ATOMS) AMINO-ALKYL OF 2 TO 4 CARBON ATOMS, R2 IS HALOGEN, TRIFLUOROMETHYL OR METHOXY, R3 IS HYDROGEN, HALOGEN, METHYL OR ETHYL, AND R4 IS HYDROGEN, FLUORINE OR CHLORINE; AND A METHOD OF INDUCING PSYCHOSEDATION AND SUPPRESSING CONVULSIONS IN A WARM-BLOODED ANIMAL THEREWITH.

8. 发明授权

US3766169A Process for the preparation of 3-aminomethylidene - 1,5 - benzodiazepine-2,4-(3h,5h)-diones 失效
标题翻译：制备3-氨基甲酰基-1,5-苯并噻吩-2,4-（3H，5H） - 酮的方法
公开(公告)号：US3766169A
公开(公告)日：1973-10-16
申请号：US3766169D
申请日：1971-10-27
申请人： BOEHRINGER SOHN INGELHEIM
发明人： BAUER A , WEBER K , POOK K
IPC分类号： C07D243/12 , C07D53/04
CPC分类号： C07D243/12
摘要： A PROCESS FOR THE PREPARATION OF A 3-AMINOMETHYLIDENE5-PHENYL-1,5-BENZODIAZEPINE-2,4-(3H,5H)-DIONE BY REACTING A 5-PHENYL - 1,5 - BENZODIAZEPINE-2,4-(3H,5H)-DIONE WITH A PHOSPHORUS PENTAHALIDE AND A DIALKYLFORMAMIDE, OPTIONALLY ADDING AMMONIA OR A PRIMARY OR SECONDARY AMINE TO THE REACTION MIXTURE, AND RECOVERING THE REACTION PRODUCT. THE 3-AMINOMETHYLIDENE-5-PHENYL-1,5BENZODIAZEPINE-2,4-(3H,5H)-DIONES OBTAINED THEREBY ARE USEFUL AS INTERMEDIATES FOR THE PREPARATION OF OTHER 3SUBSTITUTED 1,5-BENZODIAZEPINE-2,4-(3H,5H)-DIONES HAVING TRANQUILIZING AND ANTICONVULSIVE PROPERTIES.

9. 发明授权

US3711467A 2-(alkoxy or alkylmercapto)-5-phenyl-4h-3,5-dihydro-1,5-benzodiazepin-4-ones 失效
标题翻译： 2-（烷氧基或烷基）-5-苯基-4H-3,5-二氢-1,5-苯并二恶英-4-酮
公开(公告)号：US3711467A
公开(公告)日：1973-01-16
申请号：US3711467D
申请日：1971-10-19
申请人： BOEHRINGER SOHN INGELHEIM
发明人： DANNEBERG P , MINCK K , WEBER K , BAUER A
IPC分类号： C07D243/12 , C07D53/04
CPC分类号： C07D243/12
摘要： Compounds of the formula

WHEREIN R1 is straight or branched alkyl of one to four carbon atoms, R2 is phenyl, o-halo-phenyl, o-nitro-phenyl or otrifluoromethyl-phenyl, R3 is halogen, nitro or trifluromethyl, and X is oxygen or sulfur; THE COMPOUNDS ARE USEFUL AS PSYCHOSEDATIVES AND AS INTERMEDIATES FOR THE PREPARATION OF TRANQUILLIZERS.
摘要翻译：式WHERE R1的化合物是1-4个碳原子的直链或支链烷基，R2是苯基，邻 - 苯基 - 邻 - 硝基 - 苯基或邻 - 三氟甲基 - 苯基，R3是卤素，硝基或三氟甲基，X是是氧或硫; 化合物作为精神药物有用，也是制备转铁蛋白的中间体。

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