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21. 发明授权

US3954769A Dibenzo[b,f]thiepins 失效
标题翻译： Dibenzo {8 b，f {9 thiepins
公开(公告)号：US3954769A
公开(公告)日：1976-05-04
申请号：US471100
申请日：1974-05-17
申请人： Max Gerecke , Jean-Pierre Kaplan , Emilio Kyburz
发明人： Max Gerecke , Jean-Pierre Kaplan , Emilio Kyburz
IPC分类号： C07D295/08
摘要： Compounds of the formulas ##SPC1##Wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n are as hereinafter set forth,Are described. The compounds of formulas I and Ia are prepared inter alia by reacting the corresponding dibenzo[b,f]thiepin and the corresponding piperazine compound. The end products are useful as neuroleptic agents.
摘要翻译：式WHEREIN R，R1，R2，R3，R4和n的化合物如下文所述，描述如下。式I和Ia化合物特别是通过使相应的二苯并[b，f]硫杂和相应的哌嗪化合物反应而制备。最终产品可用作神经安定药剂。

22. 发明授权

US4616010A Imidazodiazepine derivatives 失效
标题翻译：咪唑二氮衍生物
公开(公告)号：US4616010A
公开(公告)日：1986-10-07
申请号：US831206
申请日：1986-02-20
申请人： Walter Hunkeler , Emilio Kyburz
发明人： Walter Hunkeler , Emilio Kyburz
IPC分类号： A61K31/55 , A61P25/20 , C07D243/00 , C07D333/00 , C07D487/14 , C07D495/22 , C07D513/22
CPC分类号： C07D487/14
摘要： Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma., and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.
摘要翻译：作为下式的咪唑并二氮杂衍生物的化合物，其中A与由α和β表示的碳原子一起表示R1和R2之一，R2表示氢，另一个表示氢，卤素或三氟甲基，R3和R4 各自表示氢或卤素，n表示数字2或3，已经发现了以γ表示的具有（S） - 或（R，S） - 构型的化合物及其药学上可接受的酸加成盐其具有抗焦虑，抗惊厥，肌肉松弛剂和镇静催眠特性。它们可以使用合适的惰性载体制备成组合物，包括药学上可接受的组合物。

23. 发明授权

US4386028A Imidazo[1,5a][1,4]benzodiazepines 失效
标题翻译：咪唑并[1,5a] [1,4]苯并二氮杂
公开(公告)号：US4386028A
公开(公告)日：1983-05-31
申请号：US403947
申请日：1982-07-30
申请人： Walter Hunkeler , Emilio Kyburz
发明人： Walter Hunkeler , Emilio Kyburz
IPC分类号： C07D495/22 , A61K31/55 , A61K31/551 , A61P25/20 , A61P33/10 , A61P39/02 , A61P43/00 , C07D243/14 , C07D265/26 , C07D471/22 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561
CPC分类号： C07D265/26 , A61K31/55 , C07D243/14 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/906
摘要： There is provided imidazodiazepines of the formula ##STR1## wherein R.sup.1 is methyl, ethyl or isopropyl, one of R.sup.4 and R.sup.5 is hydrogen and the other is nitro or cyano, and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene and the carbon atom denoted as .gamma. has the (S)- or (R,S)-configuration, and X is an oxygen or sulphur atom,and their pharmaceutically acceptable acid addition salts. The compounds are useful in the antagonization of the central-depressant muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines. Also provided are methods for making the compounds.
摘要翻译：提供下式的咪唑并二氮杂其中R 1是甲基，乙基或异丙基，R 4和R 5之一是氢，另一个是硝基或氰基，R 2是氢，R 3是氢或低级烷基或R 2， R3一起是二亚甲基，三亚甲基或亚丙烯基，并且表示为γ的碳原子具有（S） - 或（R，S） - 构型，X是氧或硫原子，以及它们的药学上可接受的酸加成盐。该化合物可用于拮抗具有镇静作用的1,4-苯二氮卓类的中枢抑制肌肉松弛剂，共济失调，降血压和呼吸抑制剂性质。它们还可以用于抑制其他指征领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性，例如血吸虫病活性的1,4-苯并二氮杂。还提供了制备化合物的方法。

24. 发明授权

US4363762A Process for preparing imidazodiazepines 失效
标题翻译：咪唑并噻嗪的制备方法
公开(公告)号：US4363762A
公开(公告)日：1982-12-14
申请号：US322091
申请日：1981-11-16
申请人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号： A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号： C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of: ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonising the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillising activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillising participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译：其中A与表示为α和β的两个碳原子一起选自下列组成的组：虚线表示组（a）和（b）中存在的双键，，D为> C = O或> C = S，R 1选自氰基，低级烷酰基和式-COOR 4基团，R 4选自甲基，乙基，异丙基和2- 羟乙基，R 5选自氢，三氟甲基和卤素，R 6选自氢，三氟甲基，卤素和低级烷基，R 2是氢，R 3是氢或低级烷基或R 2和R 3一起是三亚甲基或亚丙烯基，并且表示为γ的碳原子具有S-或R，S-构型及其药学上可接受的盐，并且可用于拮抗中枢抑制剂，肌肉松弛剂，共济失调，降血压和呼吸具有镇静作用的1,4-苯并二氮杂的抑制剂性质。例如，可以使用它们作为解毒剂，在中毒的情况下，过量摄入具有镇定作用的1,4-苯二氮卓类药物参与，或用于缩短由该1,4-苯并二氮杂卓诱导的麻醉。它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性，例如血吸虫半衰期活性1,4-苯并二氮杂如（+） - 5-（邻 - 氯苯基））-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。还提出了产生咪唑并氮杂衍生物的方法及其中间体。

25. 发明授权

US4346036A Process for preparing imidazodiazepine derivatives 失效
标题翻译：制备咪唑并氮杂衍生物的方法
公开(公告)号：US4346036A
公开(公告)日：1982-08-24
申请号：US322113
申请日：1981-11-16
申请人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号： A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号： C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration,and pharmaceutically acceptable salts thereof are presented and have utility for antagonising the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译：其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式（a）和（b）中存在的双键： D是> C = O或> C = S，R 1选自氰基，低级烷酰基和式-COOR 4基团，R 4选自甲基，乙基，异丙基和2-羟基乙基 R5选自氢，三氟甲基和卤素，R6选自氢，三氟甲基，卤素和低级烷基，R2是氢，R3是氢或低级烷基或R2和R3一起是三亚甲基或丙烯并且表示为γ的碳原子具有S-或R，S-构型及其药学上可接受的盐，并且具有拮抗中枢抑制剂，肌肉松弛剂，共济失调，降血压和呼吸的效用具有镇静作用的1,4-苯并二氮杂类的抑制剂性质。例如，可以使用它们作为解毒剂，在中毒的情况下，过量摄入具有镇静作用的1,4-苯二氮卓类药物参与，或用于缩短由1,4-苯并二氮杂卓诱导的麻醉。它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性，例如血吸虫半衰期活性1,4-苯并二氮杂如（+） - 5-（邻 - 氯苯基））-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。还提出了产生咪唑并氮杂衍生物的方法及其中间体。

26. 发明授权

US4346034A Process for preparing imidazodiazepines 失效
标题翻译：咪唑并噻嗪的制备方法
公开(公告)号：US4346034A
公开(公告)日：1982-08-24
申请号：US321941
申请日：1981-11-16
申请人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号： A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号： C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is
摘要翻译：其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式（a）和（b）中存在的双键： D是

27. 发明授权

US4346033A Thienodiazepinone and benzodiazepinone intermediates 失效
标题翻译：噻吩并二氮酮和苯并二氮杂酮中间体
公开(公告)号：US4346033A
公开(公告)日：1982-08-24
申请号：US321821
申请日：1981-11-16
申请人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人： Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号： A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号： C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonizing the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译：其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式（a）和（b）中存在的双键： D是> C = O或> C = S，R 1选自氰基，低级烷酰基和式-COOR 4基团，R 4选自甲基，乙基，异丙基和2-羟基乙基 R5选自氢，三氟甲基和卤素，R6选自氢，三氟甲基，卤素和低级烷基，R2是氢，R3是氢或低级烷基或R2和R3一起是三亚甲基或丙烯并且表示为γ的碳原子具有S-或R，S-构型及其药学上可接受的盐，并且具有拮抗中枢抑制剂，肌肉松弛剂，共济失调，降血压和呼吸的效用具有镇静作用的1,4-苯并二氮杂类的抑制剂性质。例如，可以使用它们作为解毒剂，在中毒的情况下，过量摄入具有镇静作用的1,4-苯二氮卓类药物参与，或用于缩短由1,4-苯并二氮杂卓诱导的麻醉。它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性，例如血吸虫半衰期活性1,4-苯并二氮杂如（+） - 5-（邻 - 氯苯基））-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。还提出了产生咪唑并氮杂衍生物的方法及其中间体。

28. 发明授权

US4329467A Phenyl-quinolizidines 失效
标题翻译：苯基喹喔啉
公开(公告)号：US4329467A
公开(公告)日：1982-05-11
申请号：US217887
申请日：1980-12-18
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： A61K20060101 , A61K31/435 , C07D20060101 , C07D211/76 , C07D221/00 , C07D235/00 , C07D455/02 , C07D471/04
CPC分类号： C07D211/76 , C07D455/02 , Y10S514/872
摘要： Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
摘要翻译：描述了其中X，Y，R 1和R 2如下文所述的式“IMAGE”I的苯基 - 喹嗪子。式I化合物可用作抗精神病药，止吐药和镇痛药。

29. 发明授权

US4272627A Phenyl-quinolizinones 失效
标题翻译：苯基喹诺酮类
公开(公告)号：US4272627A
公开(公告)日：1981-06-09
申请号：US148646
申请日：1980-05-12
申请人： Rene Imhof , Emilio Kyburz
发明人： Rene Imhof , Emilio Kyburz
IPC分类号： A61K20060101 , A61K31/435 , C07D20060101 , C07D211/76 , C07D221/00 , C07D235/00 , C07D455/02 , C07D471/04
CPC分类号： C07D211/76 , C07D455/02 , Y10S514/872
摘要： Phenyl-quinolizidines of the formula ##STR1## wherein X,Y,R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.
摘要翻译：描述了其中X，Y，R 1和R 2如下文所述的式“IMAGE”I的苯基 - 喹嗪子。式I化合物可用作抗精神病药，止吐药和镇痛药。

30. 发明授权

US4105664A Dibenz[b,f]oxepin derivatives 失效
标题翻译： DIBENZ（B，F）OXEPIN衍生物
公开(公告)号：US4105664A
公开(公告)日：1978-08-08
申请号：US779196
申请日：1977-03-18
申请人： Max Gerecke , Emilio Kyburz , Jean-Pierre Kaplan
发明人： Max Gerecke , Emilio Kyburz , Jean-Pierre Kaplan
IPC分类号： C07D313/14 , C07D405/04 , C07D405/14 , C07D413/14
CPC分类号： C07D405/04 , C07D313/14 , C07D405/14 , C07D413/14
摘要： Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.

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