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1. 发明授权

US4279904A 3-Amino-1-benzoxepine derivatives and their salts and pharmaceutical compositions thereof 失效
标题翻译： 3-氨基-1-苯并恶庚因衍生物及其盐及其药物组合物
公开(公告)号：US4279904A
公开(公告)日：1981-07-21
申请号：US173075
申请日：1980-07-28
申请人： Heinrich-Wilhelm Ohlendorf , Klaus-Ullrich Wolf , Wilhelm Kaupmann , Henning Heinemann
发明人： Heinrich-Wilhelm Ohlendorf , Klaus-Ullrich Wolf , Wilhelm Kaupmann , Henning Heinemann
IPC分类号： A61K31/335 , A61K31/35 , A61K31/55 , A61P1/00 , A61P1/14 , C07D313/08
CPC分类号： C07D313/08
摘要： Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.7 R.sub.8 ;R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.7 and R.sub.8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR.sub.9 ;R.sub.9 is hydrogen, methyl, benzyl, or phenyl;one of R.sub.3 and R.sub.4 is hydrogen and the other hydroxy, orR.sub.3 and R.sub.4 together are oxygen;R.sub.5 and R.sub.6 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.5 and R.sub.6 is trifluoromethyl or nitro and the other is hydrogen; the stereo isomers and the acid addition salts thereof. These compounds have a favorable effect upon the motility of the gastro-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of motility disorders.
摘要翻译：公开了新的3-氨基-1-苯并恶庚因衍生物及其生产方法。这些衍生物对应于式I其中：R1和R2彼此独立地是氢，C1-C5烷基，被末端苯基取代的C1-C5烷基或含有一个或两个卤素的苯基，甲基或甲氧基基团，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C 2 -C 5烷基或C 3 -C 4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 7 R 8取代的C 2 -C 5烷基; R 7和R 8彼此独立地是氢或C 1 -C 5烷基; 或R 7和R 8一起为5至7元环或所述具有异质氧，硫或氮的环，或R 1和R 2一起为5至7元环或所述具有异质的氧，硫或NR 9的环; R9是氢，甲基，苄基或苯基; R3和R4之一是氢，另一个羟基或R3和R4一起是氧; R 5和R 6彼此独立地是氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 5和R 6中的一个是三氟甲基或硝基，另一个是氢; 立体异构体及其酸加成盐。这些化合物对胃肠道的运动性具有有利的作用，因此构成用于治疗运动障碍的药物组合物和方法的活性成分。

2. 发明授权

US4320061A 2,3,4,5-Tetrahydro-1-benzoxepin-3,5-dione derivatives 失效
标题翻译： 2,3,4,5-四氢-1-苯并氧杂胨-3,5-二酮衍生物
公开(公告)号：US4320061A
公开(公告)日：1982-03-16
申请号：US243745
申请日：1981-03-16
申请人： Heinrich-Wilhelm Ohlendorf , Klaus-Ullrich Wolf , Wilhelm Kaupmann , Henning Heinemann
发明人： Heinrich-Wilhelm Ohlendorf , Klaus-Ullrich Wolf , Wilhelm Kaupmann , Henning Heinemann
IPC分类号： A61K31/335 , A61K31/37 , A61P1/00 , A61P1/14 , C07D313/08
CPC分类号： C07D313/08
摘要： Novel, 3-amino-1-benzoxepin-5(2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another are hydrogen,C.sub.1 -C.sub.3 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4 -ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 or 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR.sub.7 ;R.sub.7 is hydrogen, methyl, benzyl or phenyl;R.sub.3 and R.sub.4 are independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.3 and R.sub.4 is trifluoromethyl or nitro and the other is hydrogen;and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also described.
摘要翻译：公开了3-氨基-1-苯并氧杂-5（2H） - 酮衍生物及其生产方法。这些衍生物对应于式I：其中：R 1和R 2彼此独立地是氢，C 1 -C 3烷基，被末端苯基取代的C 1 -C 5烷基或含有一个或两个卤素的苯基，甲基或甲氧基，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C2-C5烷基，或C3-C4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 5 R 6取代的C 2 -C 5烷基; R 5和R 6彼此独立地是氢或C 1 -C 5烷基; 或R 5和R 6一起为5或7元环，或者R 5和R 6一起是具有异质氧，硫或氮的5至7元环; R 1和R 2一起为5至7元环，或者R 1和R 2一起为具有异质氧，硫或NR 7的5至7元环; R7是氢，甲基，苄基或苯基; R 3和R 4彼此独立地为氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 3和R 4中的一个是三氟甲基或硝基，另一个是氢; 及其酸加成盐。这些化合物对胃肠道痉挛的治疗具有有利的作用，因此构成了用于治疗胃肠道疾病的药物组合物和方法的活性成分。还描述了制备衍生物及其酸加成盐和中间产物用于制备的方法。

3. 发明授权

US4374846A N-Amino alkyl indole compounds compositions containing same, and a method of using same in therapy of disorders of gastrointestinal motility 失效
标题翻译：包含其的N-氨基烷基吲哚化合物组合物及其在胃肠蠕动障碍治疗中的应用方法
公开(公告)号：US4374846A
公开(公告)日：1983-02-22
申请号：US172023
申请日：1980-07-24
申请人： Henning Heinemann , Heinrich-Wilhelm Ohlendorf , Klaus-Ulrich Wolf
发明人： Henning Heinemann , Heinrich-Wilhelm Ohlendorf , Klaus-Ulrich Wolf
IPC分类号： C07D209/38 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/445 , A61K31/55 , A61P1/00 , C07D209/14 , C07D209/32 , C07D209/42 , A61K31/435 , C07D401/06
CPC分类号： C07D209/42
摘要： Novel N-amino alkyl indole compounds are disclosed. These compounds correspond to the Formula I ##STR1## In said Formula R.sub.1 indicates the hydrogen atom, an alkyl group with 1 to 4 carbon atoms, which may be substituted by a phenyl group, or the acetyl group;R.sub.2 indicates the hydroxy carbonyl group, an alkoxy carbonyl group with 1 to 4 alkyl carbon atoms, the cyano group, the amino carbonyl group, a mono-alkyl amino carbonyl group with 1 to 4 alkyl carbon atoms, or a di-alkyl amino carbonyl group with 1 to 4 alkyl carbon atoms, with the proviso that, when R.sub.2 is the hydroxy carbonyl group, then R.sub.1 is other than the hydrogen atom;A indicates an alkylene group with 2 to 5 carbon atoms;R.sub.3 and R.sub.4 are the same or different substituents and indicate the hydrogen atom, an alkyl group with 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 are an alkylene group forming, together with the nitrogen atom to which they are attached, a heterocyclic ring with 5 to 7 ring members; andR.sub.5 and R.sub.6 are the same or different substituents and indicate hydrogen and halogen atoms, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, or one of said substituents R.sub.5 and R.sub.6 being the nitro group or the trifluoro methyl group while the other one is the hydrogen atom.The acid addition salts of said compounds are also disclosed.The above mentioned novel N-amino alkyl indole compounds have a favorable effect upon the motility of the gastro-intestinal tract.The compounds are obtained, for instance, by reacting the alkali metal salts of a corresponding indole compound which is unsubstituted at its nitrogen atom, with a halogeno alkyl amine.
摘要翻译：公开了新的N-氨基烷基吲哚化合物。这些化合物对应于式I的化合物。式中R1表示氢原子，可被苯基取代的具有1至4个碳原子的烷基或乙酰基; R2表示羟基羰基，具有1-4个烷基碳原子的烷氧基羰基，氰基，氨基羰基，具有1-4个烷基碳原子的单烷基氨基羰基或二烷基氨基羰基具有1至4个烷基碳原子，条件是当R 2是羟基羰基时，则R 1不是氢原子; A表示碳原子数2〜5的亚烷基， R3和R4是相同或不同的取代基，表示氢原子，具有1至4个碳原子的烷基，或者R3和R4是与它们所连接的氮原子一起形成的亚烷基， 5至7名成员; 并且R 5和R 6是相同或不同的取代基，并且表示氢和卤素原子，具有1至3个碳原子的烷基，具有1至3个碳原子的烷氧基，或所述取代基R 5和R 6中的一个是硝基或三氟甲基，而另一个是氢原子。还公开了所述化合物的酸加成盐。上述新型N-氨基烷基吲哚化合物对胃肠道的运动具有有利的作用。化合物例如通过使在其氮原子上未取代的相应吲哚化合物的碱金属盐与卤代烷基胺反应而获得。

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

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。

6. 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。

7. 发明授权

US5723454A Method for obtaining estrogens from pregnant mare urine by solid phase extraction on a semi-polar adsorber resin 失效
标题翻译：通过在半极性吸附树脂上固相萃取从怀孕母乳中获得雌激素的方法
公开(公告)号：US5723454A
公开(公告)日：1998-03-03
申请号：US753508
申请日：1996-11-26
申请人： Ivan Ban , Henning Heinemann , Gerhard Mechtold , Heinz-Helmer Rasche
发明人： Ivan Ban , Henning Heinemann , Gerhard Mechtold , Heinz-Helmer Rasche
IPC分类号： C07J20060101 , C07J1/00 , A61K31/56
CPC分类号： C07J1/0051
摘要： A method for obtaining an extract containing the natural mixture of conjugated estrogens from mare urine by solid-phase extraction of the mixture of conjugated estrogens from the urine of pregnant mares on non-ionic semi-polar polymeric adsorber resins.
摘要翻译：一种通过在非离子半极性聚合物吸附树脂上从怀孕母马的尿液中固相萃取共轭雌激素混合物来获得含有母马共轭雌激素的天然混合物的提取物的方法。

8. 发明授权

US4442102A 1,5-Diphenylpyrazolin-3-one compounds, process and intermediates for preparation thereof and pharmaceutical compositions containing same 失效
标题翻译： 1,5-二苯基吡唑啉-3-酮化合物，其制备方法和中间体以及含有它们的药物组合物
公开(公告)号：US4442102A
公开(公告)日：1984-04-10
申请号：US409631
申请日：1982-08-19
申请人： Henning Heinemann , Daniel Jasserand , Wolfgang Milkowski , Dimitri Yavordios , Horst Zeugner
发明人： Henning Heinemann , Daniel Jasserand , Wolfgang Milkowski , Dimitri Yavordios , Horst Zeugner
IPC分类号： A61K31/415 , A61K31/495 , A61P37/08 , C07D231/22 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D498/04 , C07D403/06 , C07D231/08
CPC分类号： C07D401/12 , C07D231/22 , C07D405/04 , C07D405/12 , C07D409/12
摘要： New 1,5-diphenylpyrazolin-3-one compounds and a method of preparing them are described. The compounds have the general formula I ##STR1## where R.sub.1 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or lower alkanoyloxy radical, R.sub.2 is a hydrogen or halogen atom, or a lower alkyl, or lower alkoxy radical, or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or lower alkanoyloxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy radical, or R.sub.3 and R.sub.4 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical, Z is an alkylene radical with 2 to 6 carbon atoms and R.sub.5 is an optionally substituted pyridyl radical, a thienyl radical or an optionally substituted phenyl radical. The compounds have pharmacological properties, for example antiallergic properties.
摘要翻译：描述了新的1,5-二苯基吡唑啉-3-酮化合物及其制备方法。该化合物具有通式I，其中R 1是氢或卤素原子，或低级烷基，低级烷氧基，羟基，三氟甲基或低级烷酰氧基，R2是氢或卤素原子，或低级烷基，或或低级烷氧基，或R 1和R 2与相邻的碳原子键合，并且一起表示亚甲二氧基或亚乙二氧基，R 3是氢或卤原子，或低级烷基，低级烷氧基，羟基，三氟甲基或低级烷酰氧基，R 4是氢或卤素原子，或低级烷基，低级烷氧基，或者R 3和R 4与相邻的碳原子键合，并且一起表示亚甲二氧基或亚乙二氧基，Z是具有2-6个碳原子的亚烷基，R 5是任意取代的吡啶基，噻吩基或任选取代的苯基。这些化合物具有药理学性质，例如抗过敏性质。

9. 发明授权

US4594436A Isomeric 2-chloromethyl-1,4-benzodiazepine or 3-chloro-1,5-benzodiazocine compound 失效
标题翻译：异构的2-氯甲基-1,4-苯并二氮杂或3-氯-1,5-苯并二氮辛啶化合物
公开(公告)号：US4594436A
公开(公告)日：1986-06-10
申请号：US707037
申请日：1985-03-01
申请人： Hans Liepmann , Michael Ruhland , Herbert Muesch , Werner Benson , Henning Heinemann , Horst Zeugner
发明人： Hans Liepmann , Michael Ruhland , Herbert Muesch , Werner Benson , Henning Heinemann , Horst Zeugner
IPC分类号： A61K31/55 , A61K31/5513 , A61P25/00 , C07D307/54 , C07D333/38 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D487/04 , C07D491/04 , C07D491/056 , C07D491/14 , C07D491/147 , C07D498/04 , C07D498/14 , C07D513/04 , C07D319/08 , A61K31/495
CPC分类号： C07D405/04 , C07D307/54 , C07D333/38 , C07D407/04 , C07D409/04 , C07D487/04 , C07D491/04 , C07D491/14 , C07D513/04
摘要： [1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R.sub.1 is a hydrogen or halogen atom, lower alkyl radical, a lower alkoxy radical or a nitro group and R.sub.2 is a hydrogen or halogen atom, a lower alkyl radical, a lower alkoxy radical or a nitro group, or if R.sub.1 is a hydrogen atom, R.sub.2 may also be a lower alkylthio radical, or, if R.sub.1 is a hydrogen atom and X is a sulfur atom or an imino group, R.sub.2 may be a trifluoromethyl radical; or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical; R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl or pyridyl radical and n is zero or, if R.sub.3 is furyl or thienyl, n may be 0 or 1. The compounds may be in the form of their optical isomers or acid addition salts. The compounds exhibit neuroleptic properties. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.
摘要翻译： [1,2] - 稠合的1,4-苯并二氮杂化合物对应于通式I的化合物，其中X是氧或硫原子或任选取代的亚氨基，R 1是氢或卤原子，低级烷基基团，低级烷氧基或硝基，R 2是氢或卤素原子，低级烷基，低级烷氧基或硝基，或者如果R 1是氢原子，则R 2也可以是低级烷硫基，或者，如果R1是氢原子，X是硫原子或亚氨基，则R2可以是三氟甲基; 或R 1和R 2与相邻的碳原子键合并且一起表示亚甲二氧基或亚乙二氧基; R3是任选取代的呋喃基，噻吩基，吡咯基或吡啶基，n是0，或者如果R3是呋喃基或噻吩基，则n可以是0或1.这些化合物可以是其旋光异构体或酸加成盐的形式。该化合物表现出精神安定药物的特性。还公开了制备含有它们的化合物和药物组合物的方法。

10. 发明授权

US4537975A 1-Phenylindazol-3-one compounds 失效
标题翻译： 1-苯基吲哚-3-酮化合物
公开(公告)号：US4537975A
公开(公告)日：1985-08-27
申请号：US564398
申请日：1983-12-22
申请人： Henning Heinemann , Daniel Jasserand , Wolfgang Milkowski , Dimitri Yavordios , Horst Zeugner
发明人： Henning Heinemann , Daniel Jasserand , Wolfgang Milkowski , Dimitri Yavordios , Horst Zeugner
IPC分类号： A61K31/415 , A61K31/495 , A61P37/08 , C07D231/56 , C07D401/12 , C07D405/12 , C07D409/12 , C07D403/06
CPC分类号： C07D231/56 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds corresponding to the formula: ##STR1## wherein R.sub.1 and R.sub.3 each represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sub.2 and R.sub.4 each represent hydrogen, halogen, lower alkyl or lower alkoxy; Z represents an alkylene radical with 2 to 6 carbon atoms and Y" is halogen, hydroxyl, lower alkanesulphonyl, benzenesulphonyl, or lower alkyl or halogen substituted benzenesulphonyl, and acid addition salts thereof, with the proviso the Y" is other than chlorine if R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each are hydrogen and Z is ethylene or propylene. The claimed compounds are useful intermediates in the synthesis of 1-phenyl-2-[(4-substituted piperazinyl) alkyl]-1,2-dihydro-3H-indazol-3-ones which exhibit antiallergic activity.
摘要翻译：对应于下式的化合物：其中R 1和R 3各自代表氢，卤素，低级烷基，低级烷氧基或三氟甲基; R2和R4各自表示氢，卤素，低级烷基或低级烷氧基; Z代表具有2至6个碳原子的亚烷基，Y“是卤素，羟基，低级链烷磺酰基，苯磺酰基或低级烷基或卤素取代的苯磺酰基，及其酸加成盐，条件是Y”不是氯如果R1，R2，R3和R4各自为氢，Z为乙烯或丙烯。要求保护的化合物是合成具有抗过敏活性的1-苯基-2 - [（4-取代哌嗪基）烷基] -1,2-二氢-3H-吲唑-3-酮的有用中间体。

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