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31. 发明授权

US4138572A Malonanilic derivatives 失效
标题翻译：丙二醇衍生物
公开(公告)号：US4138572A
公开(公告)日：1979-02-06
申请号：US731988
申请日：1976-10-13
申请人： Silvano Rossi
发明人： Silvano Rossi
IPC分类号： C07D243/12 , C07C103/147
CPC分类号： C07D243/12
摘要： This invention relates to substituted 1,5-benzediazepines having the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or substituentsR.sub.3 is hydrogen or substituentsR.sub.4 is methyl or aryl group as well as the process of producing the same.The compounds of the invention are tranquillizing analgesic, antipyretic and anti-inflammatory agents.
摘要翻译：本发明涉及具有式“IMAGE”的取代的1,5-苯并二氮杂，其中R 1和R 2为氢或取代基R 3为氢或取代基R 4为甲基或芳基，以及其制备方法。

32. 发明授权

US4111931A 1,2,3,5-Tetrahydro-4H-1,5-benzodiazepine-4-ones 失效
标题翻译： 1,2,3,5-四氢-4H- 1,5-BENZODIAZEPINE-4-ONES
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.

33. 再颁专利

USRE28972E 5-Aryl-1H-1,5-benzodiazepine-2,4-diones 失效
标题翻译： 5-芳基-1H-1,5-苯并二氮杂卓-2,4-二酮
公开(公告)号：USRE28972E
公开(公告)日：1976-09-21
申请号：US637585
申请日：1975-12-04
申请人： Karl-Heinz Weber , Herbert Merz , Karl Zeile , Rolf Giesemann , Peter Danneberg
发明人： Karl-Heinz Weber , Herbert Merz , Karl Zeile , Rolf Giesemann , Peter Danneberg
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： 5-Aryl-1H-1,5-benzodiazepine-2,4-diones of a formula selected from the group consisting of ##SPC1##Wherein ##SPC2##-- A -- Xwherein R.sub.1 is allyl, methylallyl, dimethylallyl, chloroallyl, cyclohexyl, cycloalkylmethyl, cycloalkenylmethyl of 4 to 7 carbon atoms, phenyl, tolyl, xylyl, methoxyphenyl, dimethoxyphenyl, halophenyl, phenylalkyl of 7 to 8 carbon atoms, pyridyl or--A --Xwhere A is straight or branched alkylene of 1 to 4 carbon atoms, andX is hydroxyl, alkoxy, acyloxy, dialkylamino of 2 to 4 carbon atoms, or a 5- to 6-membered nitrogen-containing heterocyclic ring linked to A through a ring nitrogen atom,R.sub.2 is hydrogen or methyl,R.sub.3 is naphthyl, pyrimidyl, thienyl, pyridyl, methylpyridyl or halopyridyl,R.sub.4 is hydrogen, methyl, methoxy, trifluoromethyl, cyano, halogen, lower alkanoyl or (lower alkoxy of 1 to 2 carbon atoms)-carbonyl, R.sub.5 is hydrogen, methyl, ethyl, methoxy, trifluoromethyl, cyano, nitro, halogen, lower alkanoyl or lower alkoxy-carbonyl,R.sub.6 is hydrogen, methyl, ethyl, methoxy or halogen,R.sub.7 is cyano.[.,.]. .Iadd.or .Iaddend.lower alkanoyl .[.or lower alkoxycarbonyl.].,R.sub.8 is cyano, nitro, lower alkanoyl or lower alkoxycarbonyl,R.sub.9 is hydrogen, methyl, ethyl, methoxy or halogen, andR.sub.10 is hydrogen, methyl, methoxy, trifluoromethyl or halogen,Useful as psychosedatives and anticonvulsives in warm-blooded animals.

34. 发明授权

US3944579A 2-Amino-5-phenyl-4H-3,5-dihydro-1,5-benzodiazepin-4-ones and salts thereof 失效
标题翻译： 2-氨基-5-苯基-4H-3,5-二氢-1,5-苯并二氮杂-4-酮及其盐
公开(公告)号：US3944579A
公开(公告)日：1976-03-16
申请号：US487221
申请日：1974-07-10
申请人： Adolf Bauer , Karl Heinz Weber , Klaus Minck , Peter Danneberg
发明人： Adolf Bauer , Karl Heinz Weber , Klaus Minck , Peter Danneberg
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 and R.sub.2 are each hydrogen or methyl, andR.sub.3 is chlorine, bromine or nitro, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as tranquilizers.
摘要翻译：式WHEREIN R1和R2各自为氢或甲基，R3为氯，溴或硝基的化合物及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作镇定剂。

35. 发明授权

US3911126A Compositions comprising thiocarbamic acid derivatives and method of using same 失效
标题翻译：包含硫代氨基甲酸衍生物的组合物及其使用方法
公开(公告)号：US3911126A
公开(公告)日：1975-10-07
申请号：US46671974
申请日：1974-05-03
申请人： BAYER AG
发明人： BOSHAGEN HORST , PLEMPEL MANFRED
IPC分类号： C07D241/42 , C07D243/12 , A61K31/54
CPC分类号： C07D241/42 , C07D243/12
摘要： Pharmaceutical compositions which have utility as antimycotics in the treatment of fungal infections which are pathogenic to humans and animals wherein the active ingredient is an N(aryloxy-thiocarbonyl)-benzothiazine and method of using same.
摘要翻译：在治疗对人和动物致病的真菌感染中具有抗真菌作用的药物组合物，其中活性成分是N- [芳氧基 - 硫代羰基] - 苯并噻嗪及其使用方法。

36. 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.

37. 发明授权

US3821385A Thiocarbamic acid derivatives for treating mycotic infections 失效
标题翻译：用于治疗MYCOTIC感染的甲硫氨酸衍生物
公开(公告)号：US3821385A
公开(公告)日：1974-06-28
申请号：US27900072
申请日：1972-08-09
申请人： BAYER AG
发明人： BOSHAGEN H , PLEMPEL M
IPC分类号： C07D209/08 , C07D215/06 , C07D215/08 , C07D215/22 , C07D215/233 , C07D241/42 , C07D243/12 , A61K27/00
CPC分类号： C07D215/233 , C07D209/08 , C07D215/06 , C07D215/08 , C07D241/42 , C07D243/12
摘要： WHEREIN X, Y, R and n are as above defined with a thiocarbonic acid ester halide of the formula:

WHEREIN X is sulphur, oxygen, NR1, CO, CHR1 or CR1 wherein R1 is hydrogen or straight or branched chain lower alkyl, Y is a straight or branched chain aliphatic moiety of 1 to 3 carbon atoms, or said aliphatic moiety linked to X by a double bond, R is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylmercapto or trifluoromethyl, N IS 1, 2 OR 3, AND Ar is an unsubstituted or substitued aromatic moiety, ARE PRODUCED BY REACTING A COMPOUND OF THE FORMULA:

Compounds of the formula:

38. 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.

39. 发明授权

US3684798A 5-phenyl-7-chloro-1h-1,5-benzodiazepin e-2,4-(3h,5h)-diones 失效
标题翻译： 5-苯基-7-氯代-1H-1,5-苯并二氮杂E-2,4-（3H，5H） - 酮
公开(公告)号：US3684798A
公开(公告)日：1972-08-15
申请号：US11171671
申请日：1971-02-01
申请人： HAUPTMANN MARIA , BOEHRINGER SOHN INGELHEIM
发明人： WEBER KARL-HEINZ , ZEILE KARL , DANNEBERG PETER , GIESEMANN ROLF , HAUPTMANN KARL HEINZ
IPC分类号： A61K31/00 , C07D20060101 , C07D243/12 , C07D53/04
CPC分类号： C07D243/12 , A61K31/00
摘要： WHEREIN R1 is hydroxy-alkyl of two to four carbon atoms; haloalkyl of two to four carbon atoms; di(alkyl of two to four carbon atoms)amino-alkyl of two to four carbon atoms; gamma piperidino-propyl; alkoxy of one to two carbon atoms - alkyl of one to four carbon atoms; (alkoxy of one to two carbon atoms)carbonyl-alkyl of one to four carbon atoms; (alkyl of one to two carbon atoms) mercapto-alkyl of one to four carbon atoms; straight or branched alkenyl of three to five carbon atoms; (alkoxy of one to two carbon atoms)carbonyl-alkenyl of two to four carbon atoms; or halo-alkenyl of two to four carbon atoms; THE COMPOUNDS ARE USEFUL AS PSYCHOSEDATIVES AND ANTICONVULSIVES.

Compounds of the formula
摘要翻译：式WHERE R1的化合物是2至4个碳原子的羟基 - 烷基; 2至4个碳原子的卤代烷基; 二（二至四个碳原子的烷基）二至四个碳原子的氨基 - 烷基; γ-哌啶子基 - 丙基; 一至二个碳原子的烷氧基 - 一至四个碳原子的烷基; （一至二个碳原子的烷氧基）羰基 - 一至四个碳原子的烷基; （一至二个碳原子的烷基）1-4个碳原子的巯基 - 烷基; 三至五个碳原子的直链或支链烯基; （一至二个碳原子的烷氧基）二至四个碳原子的羰基 - 烯基; 或二至四个碳原子的卤代烯基; 该化合物作为精神药物和抗生素有用。

40. 发明授权

US3678033A 7-nitro-1h-1, 5-benzodiazepine-2,4-(3h,5h)-diones 失效
标题翻译： 7-硝基-1H-（1H-，5-BENZODIAZEPINE-2,4-（3H，5H） - 酮
公开(公告)号：US3678033A
公开(公告)日：1972-07-18
申请号：US3678033D
申请日：1971-02-02
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WEBER KARL-HEINZ , BAUER ADOLF , MERZ HERBERT , MINCK KLAUS
IPC分类号： C07D243/12 , C07D53/04
CPC分类号： C07D243/12
摘要： Compounds of the formula

WHEREIN R1 is hydrogen, straight or branched alkyl of one to four carbon atoms, hydroxy-(alkyl of one to four carbon atoms), methoxy(alkyl of one to four carbon atoms), acetoxy-(alkyl of one to four carbon atoms), cyclopropyl-methyl, cyclohexyl or allyl, and R2 is hydrogen, phenyl, o-halo-phenyl, o-trifluoromethyl-phenyl, o-nitro-phenyl, o-cyano-phenyl or pyridyl, PROVIDED, HOWEVER, THAT R1 and R2 are other than both hydrogen at the same time; the compounds are useful as psychosedatives and anticonvulsives.
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，羟基 - （一至四个碳原子的烷基），甲氧基 - （一至四个碳原子的烷基），乙酰氧基 - （一个环丙基 - 甲基，环己基或烯丙基，R 2为氢，苯基，邻 - 卤代 - 苯基，邻三氟甲基 - 苯基，邻硝基 - 苯基，邻 - 氰基 - 苯基或吡啶基，，R1和R2同时为氢; 该化合物可用作精神病药和抗惊厥药。

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