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1. 发明授权

US4402981A N.sub.1 -Acyl-N.sub.2 -phenyl-diaminopropanols and pharmaceutical compositions thereof and processes for their preparation 失效
标题翻译： N，N-酰基-N-苯基 - 二氨基丙醇及其药物组合物及其制备方法
公开(公告)号：US4402981A
公开(公告)日：1983-09-06
申请号：US243746
申请日：1981-03-16
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
IPC分类号： C07C233/35 , A61K9/28 , A61K9/48 , A61K31/16 , A61K31/165 , A61K31/245 , A61P1/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/36 , C07C233/62 , C07D213/81 , C07D213/82 , C07D303/36 , C07D307/30 , C07D307/68 , C07D317/68 , C07D319/18 , C07C103/38 , C07C103/78
CPC分类号： C07D213/81 , C07D303/36 , C07D307/68 , C07D317/68 , C07D319/18 , Y10S514/926 , Y10S514/927
摘要： N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which possess ulcer-inhibiting activities.Further disclosed are pharmaceutical compositions which are effective in the treatment and prophylaxis of ulcers and which comprise as a pharmacologically active ulcus-inhibiting ingredient N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent.Further disclosed are processes for the preparation of the N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.
摘要翻译：公开了具有溃疡抑制活性的N 1 - 酰基-N 2 - 苯基-1,3-二氨基丙-2-醇。进一步公开的是有效治疗和预防溃疡的药物组合物，其包含作为药理学活性的抑制溃疡的成分N1-酰基-N-苯基-1,3-二氨基丙-2-醇，或其药学上可接受的酸加成其盐和药学上可接受的稀释剂。进一步公开了制备N1酰基-N-苯基-1,3-二氨基丙-2-醇的方法。

2. 发明授权

US4338314A [1,2]Anellated-7-phenyl-1,4-benzodiazepine and pharmaceutical compositions thereof and use for treatment of ulcers 失效
标题翻译： [1,2] Anellated-7-苯基-1,4-苯并二氮杂及其药物组合物，用于治疗溃疡
公开(公告)号：US4338314A
公开(公告)日：1982-07-06
申请号：US67146
申请日：1979-08-16
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Insa Hell , Klaus-Ullrich Wolf
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Insa Hell , Klaus-Ullrich Wolf
IPC分类号： A61K31/55 , A61K31/5513 , A61P1/04 , A61P25/20 , C07D487/04 , C07D498/04 , C07D498/14 , C07D513/04 , C07D489/04
CPC分类号： C07D487/04 , C07D513/04 , Y10S514/925
摘要： Compounds of [1,2]anellated-7-phenyl-1,4-benzodiazepines having the formula I ##STR1## wherein X is oxygen, sulfur or NR;R is H,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl, substituted with a terminal phenyl group, which is unsubstituted or substituted by one or 2 methoxy groups, a 3,4-methylene dioxy or 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl, substituted with terminal halogen, hydroxy or methoxy or,C.sub.3 -C.sub.5 alkenylR.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are H, halogen, trifluoromethyl, nitro, alkyl, alkoxy, or alkylthio wherein alkyl is C.sub.1 -C.sub.4 alkyl or two neighboring groups represent a methylenedioxy or ethylenedioxy group and the acid addition salts thereof, ulcer treating pharmaceutical compositions containing these compounds and a method of medical treatment using same.
摘要翻译：具有式I的[1,2]蒽醌-7-苯基-1,4-苯并二氮杂的化合物，其中X是氧，硫或NR; R为H，C 1 -C 5烷基，被未取代或被1或2个甲氧基取代的末端苯基取代的C 1 -C 5烷基，3,4-亚甲基二氧基或3,4-亚乙二氧基， C5烷基，被末端卤素，羟基或甲氧基取代，或C3-C5烯基R1，R2，R3，R4和R5相同或不同，为H，卤素，三氟甲基，硝基，烷基，烷氧基或烷硫基，其中烷基是 C1-C4烷基或两个相邻基团代表亚甲二氧基或亚乙二氧基及其酸加成盐，治疗含有这些化合物的药物组合物的溃疡治疗和使用它们的药物治疗方法。

3. 发明授权

US4177287A Pharmaceutical compositions of N.sub.1 -acyl-N.sub.2 -phenyldiaminopropanols and process for their preparation 失效
标题翻译： N-酰基-N-苯基二氨基丙醇的药物组合物及其制备方法
公开(公告)号：US4177287A
公开(公告)日：1979-12-04
申请号：US900973
申请日：1978-04-28
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
IPC分类号： A61K31/165 , A61K31/34 , A61K31/341 , A61P1/04 , C07D307/68
CPC分类号： C07D307/68
摘要： Pharmaceutical compositions are disclosed, which are effective in the treatment and prophylaxis of ulcers and which comprise as a pharmacologically active ulcus-inhibiting ingredient a compound selected from the group of N.sub.1 -acyl-N.sub.2 -(4-chlorophenyl)-1,3-diaminopropan-2-ols, having the formula I ##STR1## wherein R.sub.1 represents 3,4-dimethoxyphenyl, 2-fluorophenyl, 2-trifluoromethylphenyl, or furyl, and pharmaceutically acceptable acid addition salts thereof, and a pharmaceutically acceptable diluent.Further disclosed is a new process for the preparation of the compounds of formula I.
摘要翻译：公开了药物组合物，其有效治疗和预防溃疡，并且其包含选自N1-酰基-N2-（4-氯苯基）-1,3-二氨基丙胺的化合物作为药理学活性的抑制溃疡成分 -2-氧代，其具有式I的化合物，其中R 1表示3,4-二甲氧基苯基，2-氟苯基，2-三氟甲基苯基或呋喃基，及其药学上可接受的酸加成盐，和药学上可接受的稀释剂。进一步公开了制备式I化合物的新方法。

4. 发明授权

US4191770A N.sub.1 -acyl-N.sub.2 -phenyldiaminopropanols and pharmaceutical compositions thereof 失效
标题翻译： N1酰基-N-苯基二氨基丙醇及其药物组合物
公开(公告)号：US4191770A
公开(公告)日：1980-03-04
申请号：US900998
申请日：1978-04-28
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ullrich Wolf , Insa Hell , Reinhard Hempel
IPC分类号： C07C233/35 , A61K9/28 , A61K9/48 , A61K31/16 , A61K31/165 , A61K31/245 , A61P1/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/36 , C07C233/62 , C07D213/81 , C07D213/82 , C07D303/36 , C07D307/30 , C07D307/68 , C07D317/68 , C07D319/18 , C07D213/56 , A61K31/44
CPC分类号： C07D213/81 , C07D303/36 , C07D307/68 , C07D317/68 , C07D319/18 , Y10S514/926 , Y10S514/927
摘要： N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which possess ulcer-inhibiting activities.Further disclosed are pharmaceutical compositions which are effective in the treatment and prophylaxis of ulcers and which comprise as a pharmacologically active ulcus-inhibiting ingredient N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent.Further disclosed are processes for the preparation of the N.sub.1 -acyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.
摘要翻译：公开了具有溃疡抑制活性的N 1 - 酰基-N 2 - 苯基-1,3-二氨基丙-2-醇。进一步公开的是有效治疗和预防溃疡的药物组合物，其包含作为药理学活性的抑制溃疡的成分N1-酰基-N-苯基-1,3-二氨基丙-2-醇，或其药学上可接受的酸加成其盐和药学上可接受的稀释剂。进一步公开了制备N1酰基-N-苯基-1,3-二氨基丙-2-醇的方法。

5. 发明授权

US4271193A N1-Benzoyl-N2-phenyldiaminopropanols and pharmaceutical compositions thereof, and processes for their preparation 失效
标题翻译： N1-苯甲酰基-N-苯基二氨基丙醇及其药物组合物及其制备方法
公开(公告)号：US4271193A
公开(公告)日：1981-06-02
申请号：US51227
申请日：1979-06-22
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ulrich Wolf , Insa Hell , Reinhard Hempel
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Henning Heinemann , Klaus-Ulrich Wolf , Insa Hell , Reinhard Hempel
IPC分类号： A61K31/165 , A61K31/335 , A61K31/357 , A61P1/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/50 , C07D317/62 , C07D317/68 , C07D319/18 , A61K31/36
CPC分类号： C07D317/68 , C07D319/18
摘要： N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols are disclosed which exhibit a stabilizing effect on the gastric mucosa and enhance the stability and resistance of the gastic mucosa against harmful effects caused by, e.g., excessive alcohol consumption or drugs. The compounds are useful in the prophylaxis and treatment of gastritis.Further disclosed are pharmaceutical compositions which are effective in stabilizing the gastric mucosa and in the treatment and proplylaxis of gastritis and which comprise as a pharmacologically active ingredient N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable diluent. Further disclosed are processes for the preparation of the N.sub.1 -benzoyl-N.sub.2 -phenyl-1,3-diaminopropan-2-ols.
摘要翻译：公开了N1-苯甲酰基-N2-苯基-1,3-二氨基丙-2-醇，其对胃粘膜表现出稳定作用，并且增强了胶质粘膜对由例如过度饮酒引起的有害影响的稳定性和抗性，药物该化合物可用于预防和治疗胃炎。进一步公开的是有效稳定胃粘膜和治疗胃炎的药物组合物，其包含作为药理活性成分的N-苯甲酰基-N-苯基-1,3-二氨基丙-2-醇或药学上可接受的盐可接受的酸加成盐和药学上可接受的稀释剂。还公开了制备N1-苯甲酰基-N2-苯基-1,3-二氨基丙-2-醇的方法。

6. 发明授权

US4170649A 1,4-Benzodiazepine derivatives, pharmaceutical compositions thereof, and process for their preparation 失效
标题翻译： 1,4-苯并二氮杂衍生物，其药物组合物及其制备方法
公开(公告)号：US4170649A
公开(公告)日：1979-10-09
申请号：US996720
申请日：1978-12-05
申请人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Renke Budden , Jacqueline Bahlsen
发明人： Hans Liepmann , Rolf Hueschens , Wolfgang Milkowski , Horst Zeugner , Renke Budden , Jacqueline Bahlsen
IPC分类号： A61K31/55 , A61K31/551 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/26 , C07D243/16
CPC分类号： C07D243/16 , Y10S514/906
摘要： New 1,4-benzodiazepine derivatives are disclosed which are substituted in 2-position by cyanomethylene or carbamoylmethylene and have the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, or nitro, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents phenyl which may be substituted by halogen or CF.sub.3, and R.sub.4 represents cyano or carbamoyl. The compounds exhibit tranquilizing activities. The cyanomethylene-compounds are prepared by oxidizing corresponding cyanomethyl compounds with Cr-VI-oxide in an acidic reaction medium. The cyanomethylene-group can subsequently be hydrolyzed into the carbamoylmethylene group.
摘要翻译：公开了新的1,4-苯并二氮杂衍生物，其被氰基亚甲基或氨基甲酰基亚甲基取代在2-位，并具有下式：其中R 1表示氢，卤素或硝基，R 2表示氢或低级烷基，R 3表示可以是被卤素或CF 3取代，R 4表示氰基或氨基甲酰基。化合物显示镇静活动。通过在酸性反应介质中用Cr-VI-氧化物氧化相应的氰基甲基化合物来制备氰基亚甲基化合物。随后将氰基亚甲基基团水解成氨甲酰基亚甲基。

7. 发明授权

US4482548A Analgesic pharmaceutical compositions containing 5-phenyl-1,4-benzo diazepine compounds and a method of using same 失效
标题翻译：含有5-苯基-1,4-苯并二氮杂化合物的镇痛药物组合物及其使用方法
公开(公告)号：US4482548A
公开(公告)日：1984-11-13
申请号：US494645
申请日：1983-05-16
申请人： Dietmar Roemer , Michael Ruhland , Horst Zeugner , Wolfgang Milkowski , Hans Liepmann
发明人： Dietmar Roemer , Michael Ruhland , Horst Zeugner , Wolfgang Milkowski , Hans Liepmann
IPC分类号： C07D243/24 , A61K31/55 , A61K31/551 , A61P25/04 , C07D243/16 , C07D243/18 , A61K31/33
CPC分类号： A61K31/55
摘要： Highly effective analgesic pharmaceutical compositions and methods of using same are described. Said compositions contain, as analgesic agent, a 5-phenyl-1H-2,3-dihydro-1,4-benzodiazepine compound of the formula ##STR1## wherein R.sub.1 indicates a substituent selected from the group consisting of hydrogen and lower alkyl,R.sub.2 indicates a substituent selected from the group consisting of hydrogen, lower alkyl, and lower alkanoyl,R.sub.3 indicates a substituent selected from the group consisting of hydrogen and halogen, andR.sub.4 indicates halogen,or a physiologically compatible acid addition salt thereof.
摘要翻译：描述了高效镇痛药物组合物及其使用方法。所述组合物含有作为止痛剂的下式的5-苯基-1H-2,3-二氢-1,4-苯并二氮杂化合物，其中R 1表示选自氢和低级烷基的取代基， R2表示选自氢，低级烷基和低级烷酰基的取代基，R3表示选自氢和卤素的取代基，R4表示卤素，或其生理上相容的酸加成盐。

8. 发明授权

US4649137A 2-acylaminomethyl-1,4-benzodiazepine compounds, the preparation thereof, and pharmaceutical compositions containing them 失效
标题翻译： 2-酰氨基甲基-1,4-苯并二氮杂化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4649137A
公开(公告)日：1987-03-10
申请号：US847112
申请日：1986-04-03
申请人： Horst Zeugner , Dietmar Romer , Hans Liepmann , Wolfgang Milkowski
发明人： Horst Zeugner , Dietmar Romer , Hans Liepmann , Wolfgang Milkowski
IPC分类号： C07D243/14 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , C07D213/50 , C07D243/26 , C07D245/06 , C07D267/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D401/04 , C07D213/50 , C07D267/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , Y10S514/821 , Y10S514/825 , Y10S514/869
摘要： New 2-acylaminomethyl-1H-2,3-dihydro-1,4-benzodiazepine compounds are described having the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl or alkenyl radical or the cyclopropylmethyl radical, R.sub.2 is a hydrogen atom, n is 0, 1 or 2, R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl, pyridyl or phenyl radical, R.sub.4 is an optionally substituted furyl, thienyl or, pyrrolyl radical, R.sub.5 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxyl, lower alkylthio, nitro, trifuloromethyl, cyano, amino, lower mono- or dialkylamino, lower monoalkanoylamino, lower N-alkyl-N-alkanoylamino or lower alkanoyloxy radical, and R.sub.6 is a hydrogen atom, or a lower alkyl or lower alkoxy radical or R.sub.5 and R.sub.6 together denote a methylenedioxy or ethylenedioxy radical. The compounds have pharmacological, for example, analgesic, properties.
摘要翻译：描述了新的2-酰基氨基甲基-1H-2,3-二氢-1,4-苯并二氮杂化合物，其具有通式I其中R 1是氢原子或低级烷基或烯基或环丙基甲基，R 2是氢原子，n为0,1或2，R3为任选取代的呋喃基，噻吩基，吡咯基，吡啶基或苯基，R4为任选取代的呋喃基，噻吩基或吡咯基，R5为氢或卤素原子，或低级烷基，低级烷氧基，羟基，低级烷硫基，硝基，三氟甲基，氰基，氨基，低级单烷基氨基或二烷基氨基，低级单烷酰氨基，低级N-烷基-N-烷酰基氨基或低级烷酰氧基，R6为氢原子，低级烷基或低级烷氧基或R5和R6一起表示亚甲二氧基或亚乙二氧基。这些化合物具有药理学，例如止痛剂，特性。

9. 发明授权

US4505908A 7-Bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepine pharmaceuticals 失效
标题翻译： 7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂药物
公开(公告)号：US4505908A
公开(公告)日：1985-03-19
申请号：US422297
申请日：1982-09-23
申请人： Horst Zeugner , Michael Ruhland , Hans Liepmann , Wolfgang Milkowski , Herbert Muesch
发明人： Horst Zeugner , Michael Ruhland , Hans Liepmann , Wolfgang Milkowski , Herbert Muesch
IPC分类号： A61K31/55 , A61K31/551 , A61P21/02 , A61P25/00 , A61P25/20 , C07D243/16 , C07D245/06 , C07D487/04
CPC分类号： C07D487/04 , C07D243/16 , C07D245/06
摘要： Disclosed are 7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines of the formula I ##STR1## in which R.sub.1 is a hydrogen atom or a lower alkoxy or alkanoyloxy radical and R.sub.2 is a halogen atom. The compounds possess psychopharmacological, and especially anti-aggressive properties. To manufacture compounds of formula I, corresponding 2-halomethyl-7-bromo-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines are cyclized to corresponding 7-bromo-1,2-methylene-5-(2-halophenyl)-1H-2,3-dihydro-1,4-benzodiazepines and in these the aziridine ring is opened through treatment with a lower alcohol or a lower carboxylic acid in the presence of a Lewis acid.
摘要翻译：公开了式I的7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂其中R 1是氢原子或低级烷氧基或烷酰氧基， R2是卤素原子。这些化合物具有精神药理学，特别是抗侵袭性。为了制备式I化合物，将相应的2-卤代甲基-7-溴-5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂环化为相应的7-溴-1,2-亚甲基 -5-（2-卤代苯基）-1H-2,3-二氢-1,4-苯并二氮杂并且在路易斯酸存在下，通过用低级醇或低级羧酸处理来打开氮丙啶环。

10. 发明授权

US4533662A 2-Acylaminomethyl-1,4-benzodiazepine compounds and analgesic use 失效
标题翻译： 2-酰氨基甲基-1,4-苯并二氮杂化合物和止痛用途
公开(公告)号：US4533662A
公开(公告)日：1985-08-06
申请号：US330324
申请日：1981-12-14
申请人： Horst Zeugner , Dietmar Roemer , Hans Liepmann , Wolfgang Milkowski
发明人： Horst Zeugner , Dietmar Roemer , Hans Liepmann , Wolfgang Milkowski
IPC分类号： A61K31/55 , A61K31/551 , A61P25/04 , C07D243/16 , C07D405/12 , C07D491/04 , C07D491/056 , C07D405/10
CPC分类号： C07D491/04 , C07D243/16
摘要： Novel 2-acyl amino methyl-5-phenyl-1H-2,3-dihydro-1,4-benzo diazepine compounds of the following Formula I ##STR1## which have valuable pharmacological properties are provided. In said Formula I the acyl group --CO--R.sub.3 represents a benzoyl group or a phenyl alkanoyl group which may be unsubstituted or mono- or di-substituted in the phenyl ring. The substituent R.sub.1 in said compounds indicates lower alkyl, lower alkenyl, or cyclopropyl methyl, and the substituent R.sub.2 indicates hydrogen, lower alkyl, or lower alkenyl, while the substituent R.sub.6 indicates hydrogen, halogen, lower alkyl, lower alkoxy, hydroxyl, lower alkylthio, nitro, trifluoro methyl, cyano, amino, mono- or di-lower alkyl amino, lower mono-alkanoyl amino, lower N-alkyl-N-alkanoyl amino, or lower alkanoyloxy, and the substituent R.sub.7 indicates hydrogen, halogen, lower alkyl, lower alkoxy, hydroxyl, or lower alkanoyloxy, whereby R.sub.6 and R.sub.7, when attached to adjacent carbon atoms, may form together the methylene dioxy or the ethylene dioxy group. The substituents R.sub.8 and R.sub.9 designate the same substituents as indicated for the substituents R.sub.6 and R.sub.7.The compounds of Formula I have a surprising analgesic activity.
摘要翻译：提供了具有有价值的药理学性质的下列通式I的2-酰基氨基甲基-5-苯基-1H-2,3-二氢-1,4-苯并二氮杂化合物。在所述式I中，酰基-CO-R 3表示苯基或苯基烷酰基，其可在苯环中未被取代或单取代或二取代。所述化合物中的取代基R 1表示低级烷基，低级烯基或环丙基甲基，取代基R 2表示氢，低级烷基或低级烯基，而取代基R 6表示氢，卤素，低级烷基，低级烷氧基，羟基，低级烷硫基硝基，三氟甲基，氰基，氨基，一或二低级烷基氨基，低级单烷酰基氨基，低级N-烷基-N-烷酰基氨基或低级烷酰氧基，取代基R7表示氢，卤素，低级烷基，低级烷氧基，羟基或低级烷酰氧基，其中当连接到相邻碳原子上时，R 6和R 7可以一起形成亚甲基二氧基或亚乙基二氧基。取代基R8和R9表示与取代基R6和R7相同的取代基。式I的化合物具有惊人的止痛活性。

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