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1. 发明授权

US4851420A 2,6-diamino-3-halobenzylpyridines and processes for their manufacture as well as their use in pharmaceuticals 失效
标题翻译： 2,6-二氨基-3-卤代苄基吡啶及其制备方法及其在药物中的应用
公开(公告)号：US4851420A
公开(公告)日：1989-07-25
申请号：US116807
申请日：1987-11-05
申请人： Peter Emig , Juergen Engel , Gerhard Scheffler , Carl H. Weischer , Bernd Nickel
发明人： Peter Emig , Juergen Engel , Gerhard Scheffler , Carl H. Weischer , Bernd Nickel
IPC分类号： A61K31/44 , A61K31/4418 , A61P25/04 , A61P29/00 , C07D213/73
CPC分类号： C07D213/73
摘要： 2,6-diamino-3-halobenzylpyridines of the formula I: ##STR1## wherein R.sub.1 is fluorine and R.sub.2 is hydrogen or chlorine as well as their physiologically acceptable acid addition salts, processes for their manufacture and their use in pharmaceuticals.
摘要翻译：式I的2,6-二氨基-3-卤代苄基吡啶：其中R 1是氟并且R 2是氢或氯，以及它们的生理上可接受的酸加成盐，它们的制备方法及其在药物中的用途。

2. 发明授权

US4124716A Process for the treatment of spasmodic conditions in humans 失效
标题翻译：治疗人体痉挛状况的方法
公开(公告)号：US4124716A
公开(公告)日：1978-11-07
申请号：US842092
申请日：1977-10-14
申请人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
发明人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
IPC分类号： C07D295/088 , C07D333/16 , A61K27/00 , A61K31/135 , A61K31/40 , A61K31/445
CPC分类号： C07D295/088 , C07D333/16
摘要： Process for the treatment of spasmodic conditions in humans by administering a compound of the general formula ##STR1## or a pharmacologically acceptable acid addition salt thereof to a human suffering from such conditions.
摘要翻译：通过向患有这些病症的人施用通式为“IMAGE”的化合物或其药学上可接受的酸加成盐来治疗人类痉挛状况的方法。

3. 发明授权

US4785110A Process for the production of 2-amino-3-nitro-6-(4-fluorobenzylamino)-pyridine 失效
标题翻译： 2-氨基-3-硝基-6-（4-氟苄基氨基） - 吡啶的制备方法
公开(公告)号：US4785110A
公开(公告)日：1988-11-15
申请号：US843253
申请日：1986-03-24
申请人： Winfried Orth , Jurgen Engel , Peter Emig , Gerhard Scheffler , Hans Pohle
发明人： Winfried Orth , Jurgen Engel , Peter Emig , Gerhard Scheffler , Hans Pohle
IPC分类号： C07D213/74 , C07D213/75
CPC分类号： C07D213/74 , C07D213/75 , Y02P20/582
摘要： There is described a process for the production of 2-amino-3-nitro-6-(4-fluorobenzylamino)-pyridine which consists essentially of reacting 2-amino-3-nitro-6-methoxypyridine with 4-fluorobenzylamine in water at elevated temperature; in a given case the nitro group can be subsequently reduced and a carbethoxy group introduced.
摘要翻译：描述了生产2-氨基-3-硝基-6-（4-氟苄基氨基） - 吡啶的方法，其基本上由2-氨基-3-硝基-6-甲氧基吡啶与4-氟苄胺在水中升高温度; 在给定的情况下，可以随后还原硝基并引入乙酯基。

4. 发明授权

US4643995A Analgesic pyridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring 失效
标题翻译：具有含氮脂环族的止痛性吡啶-2-醚或吡啶-2-硫醚
公开(公告)号：US4643995A
公开(公告)日：1987-02-17
申请号：US682773
申请日：1984-12-17
申请人： Jurgen Engel , Vladimir Jakovlev , Bernd Nickel , Klaus Thiemer , Gerhard Scheffler
发明人： Jurgen Engel , Vladimir Jakovlev , Bernd Nickel , Klaus Thiemer , Gerhard Scheffler
IPC分类号： C07D401/12 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/46 , A61K31/55 , A61P25/04 , A61P29/00 , C07D211/54 , C07D213/643 , C07D213/70 , C07D213/71 , C07D213/89 , C07D243/00 , C07D317/00 , C07D405/12 , C07D405/14 , C07D451/02 , C07D451/06 , C07D453/02
CPC分类号： C07D213/70 , C07D211/54 , C07D213/89 , C07D401/12 , C07D405/14 , C07D451/06 , C07D453/02
摘要： There are disclosed pyridine-2-ethers and pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring corresponding to the formula ##STR1## the pyridine-N-oxides and/or amine oxides thereof and the pharmaceutically acceptable salts thereof. The compounds show analgesic activity.
摘要翻译：公开了具有对应于式I的吡啶-N-氧化物和/或氧化胺及其药学上可接受的盐的含氮脂环族的吡啶-2-醚和吡啶-2-硫醚。化合物显示止痛活性。

5. 发明授权

US4065501A Basic enol ether and acid addition salts thereof 失效
标题翻译：碱性烯醇醚及其酸加成盐
公开(公告)号：US4065501A
公开(公告)日：1977-12-27
申请号：US557535
申请日：1975-03-12
申请人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
发明人： Peter Emig , Hans Pohle , Gerhard Scheffler , Norbert Brock , Hans-Dieter Lenke , Jorg Pohl
IPC分类号： A61K31/135 , A61K31/075 , A61K31/13 , A61P9/08 , C07C67/00 , C07C213/00 , C07C217/08 , C07C217/10 , C07C217/12 , C07D213/30 , C07D295/088 , C07D295/092 , C07D333/16 , C07C91/16
CPC分类号： C07D295/088 , C07D333/16
摘要： The present invention is related to new basic enol ethers having the general formula ##STR1## and to the pharmacologically acceptable acid addition salts thereof. The invention is further related to process for the treatment of spasmodic conditions in humans by administering a compound of the above general formula or a pharmacologically acceptable acid addition salt thereof to a human suffering from such conditions.
摘要翻译：本发明涉及具有通式“IMAGE”的新的碱性烯醇醚及其药学上可接受的酸加成盐。本发明还涉及通过向患有这些病症的人施用上述通式的化合物或其药理学上可接受的酸加成盐来治疗人的痉挛状况的方法。

6. 发明授权

US4738983A Ethylenediamine and guanidine-derivatives 失效
标题翻译：乙二胺和胍衍生物
公开(公告)号：US4738983A
公开(公告)日：1988-04-19
申请号：US558984
申请日：1983-12-07
申请人： Peter Emig , Gerhard Scheffler , Klaus Thiemer , Carl-Heinrich Weischer
发明人： Peter Emig , Gerhard Scheffler , Klaus Thiemer , Carl-Heinrich Weischer
IPC分类号： A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P1/04 , C07D307/52 , C07D333/20 , C07D307/02
CPC分类号： C07D307/52 , C07D333/20
摘要： This invention relates to new compounds corresponding to the general formula: ##STR1## R.sub.1 represents a C.sub.3 -C.sub.10 cycloalkyl group substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.3 -C.sub.19 -cycloalkyl-C.sub.1 -C.sub.4 alkyl group which may be substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.6 -C.sub.8 bicycloalkyl group, a C.sub.6 -C.sub.8 bicycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.10 tricycloalkyl group, a C.sub.6 -C.sub.10 tricycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.9 tetracycloalkyl group or a C.sub.6 -C.sub.9 -tetracycloalkyl-C.sub.1 -C.sub.4 alkyl group,R.sub.2 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group, a phenyl-C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.6 alkyl group which is substituted by halogen atoms, nitro groups, hydroxy groups, C.sub.2 -C.sub.6 alkanoyloxy groups, C.sub.1 -C.sub.4 alkoxy groups, C.sub.1 -C.sub.4 alkoxy carbonyl groups or carboxy groups,R.sub.3 represented hydrogen, the 2-[5-(dimethylaminomethyl)-2-furyl-methylthio]-ethyl group, a C.sub.1 -C.sub.18 -alkyl group, a C.sub.3 -C.sub.6 -cycloalkyl group, a C.sub.3 -C.sub.6 -alkenyl group, a C.sub.3 -C.sub.6 -alkinyl group, an amino-C.sub.1 -C.sub.4 -alkyl group, a C.sub.2 -C.sub.6 -alkanoylamino-C.sub.1 -C.sub.4 -alkyl group, a mono-C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl group, a di-C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl group or a C.sub.1 -C.sub.18 -alkyl group, which is substituted by halogen atoms, nitro groups, hydroxy groups, C.sub.2 -C.sub.6 alkanoyloxy groups, C.sub.1 -C.sub.4 alkoxy groups, C.sub.1 -C.sub.4 alkoxycarbonyl groups or carboxy groups,A represents a nitrogen atom or a methine group,B represents a cyano radical or a nitro group, andX represents an oxygen atom or a sulphur atom, and salts thereof.The compounds inhibit the secretion of gastric juice. Moreover, they have an ulcer-inhibiting and stomach-spasmolytic effect.
摘要翻译：本发明涉及对应于通式的新化合物：其中R1表示被C1-C6烷基取代的C3-C10环烷基，可被C1取代的C3-C19-环烷基-C1-C4烷基 -C 6烷基，C 6 -C 8双环烷基，C 6 -C 8双环烷基-C 1 -C 4烷基，C 6 -C 10三环烷基，C 6 -C 10三环烷基-C 1 -C 4烷基，C 6 -C 9四环烷基或 C 6 -C 9 - 四环烷基-C 1 -C 4烷基，R 2表示氢，C 1 -C 6烷基，苯基-C 1 -C 4烷基或被卤素原子取代的C 1 -C 6烷基，硝基，羟基基团，C 2 -C 6烷酰氧基，C 1 -C 4烷氧基，C 1 -C 4烷氧基羰基或羧基，R 3表示氢，2- [5-（二甲基氨基甲基）-2-呋喃基 - 甲硫基] - 乙基， -C 18 - 烷基，C 3 -C 6 - 环烷基，C 3 -C 6 - 烯基，C 3 -C 6 - 炔基，氨基-C 1 -C 4 - 烷基，C 2 -C 6 - 烷酰基氨基-C 1 -C 4 - 烷基，单-C 1 -C 6烷基烯基-C 1 -C 4 - 烷基，被卤素原子取代的二-C 1 -C 6烷基氨基-C 1 -C 4 - 烷基或C 1 -C 18烷基，硝基，羟基，C 2 -C 6烷酰氧基基团，C 1 -C 4烷氧基，C 1 -C 4烷氧基羰基或羧基，A表示氮原子或次甲基，B表示氰基或硝基，X表示氧原子或硫原子，其中。这些化合物抑制胃液的分泌。此外，它们具有溃疡抑制和胃解痉作用。

7. 发明授权

US5859003A Salts of azelastine having improved solubility 失效
标题翻译：具有改善溶解性的氮卓斯汀盐
公开(公告)号：US5859003A
公开(公告)日：1999-01-12
申请号：US691415
申请日：1996-08-02
申请人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
发明人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
IPC分类号： A61K31/50 , A61K31/55 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D403/04
CPC分类号： C07D403/04 , A61K31/55 , Y10S514/863 , Y10S514/886 , Y10S514/887
摘要： The present invention relates to salts of azelastine having improved solubility in water. The salts of the present invention are prepared by reacting azelastine with acetic acid, gluconic acid, lactic acid or malic acid. A pharmaceutical composition may be prepared containing an azelastine salt and a pharmaceutically-acceptable carrier or diluent therefor. The pharmaceutical composition is useful in the treatment of allergies, asthma, inflammatory and psoriasis disorders and provides a cytoprotective effect.
摘要翻译：本发明涉及在水中具有改善的溶解性的氮卓斯汀盐。本发明的盐通过将萘曲斯汀与乙酸，葡萄糖酸，乳酸或苹果酸反应来制备。可以制备药物组合物，其含有氮卓斯坦盐及其药学上可接受的载体或稀释剂。药物组合物可用于治疗过敏，哮喘，炎性和银屑病，并提供细胞保护作用。

8. 发明授权

US5086050A Method of treating inflammatory disorders and psoriasis with salts of azelastine 失效
标题翻译：用AZELASTINE治疗炎症性疾病和PSORIASIS的方法
公开(公告)号：US5086050A
公开(公告)日：1992-02-04
申请号：US652986
申请日：1991-02-08
申请人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
发明人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
IPC分类号： A61K31/50 , A61K31/55 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D403/04
CPC分类号： C07D403/04 , A61K31/55 , Y10S514/863 , Y10S514/886 , Y10S514/887
摘要： Salts of azelastine with acetic acid, gluconic acid, lactic acid or malic acid.
摘要翻译：萘曲宁与醋酸，葡萄糖酸，乳酸或苹果酸的盐。

9. 发明授权

US4239761A Basically substituted ureas and processes for the treatment of virus diseases 失效
标题翻译：用于治疗病毒性疾病的基本取代的脲和方法
公开(公告)号：US4239761A
公开(公告)日：1980-12-16
申请号：US69335
申请日：1979-08-23
申请人： Rolf Rebling , Gerhard Scheffler , Klaus Pressler , Klaus D. Schenk
发明人： Rolf Rebling , Gerhard Scheffler , Klaus Pressler , Klaus D. Schenk
IPC分类号： C07D295/12 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P1/00 , A61P11/00 , A61P25/00 , A61P31/12 , C07D295/13 , C07D295/20 , C07D295/215 , C07D295/22 , C07D295/26 , C07D295/10 , C07D295/16
CPC分类号： C07D295/215 , C07D295/13 , C07D295/26 , Y10S514/849 , Y10S514/888 , Y10S514/894 , Y10S514/915 , Y10S514/934
摘要： The present invention is related to new basically substituted ureas having the general Formula I ##STR1## and the pharmaceutically acceptable acid addition salts thereof which produce an improved antiviral activity against DNS- and RNS-viruses. The invention is further related to the treatment of humans or animals suffering from diseases caused by viruses by administering compositions containing such ureas or salts thereof as active agent.
摘要翻译：本发明涉及具有通用式I的新基本取代的脲和其药学上可接受的酸加成盐，其产生针对DNS-和RNS-病毒的改进的抗病毒活性。本发明还涉及通过施用含有这种脲或其盐作为活性剂的组合物治疗患有由病毒引起的疾病的人或动物。

10. 发明授权

US6017909A Salts of azelastine having improved solubility effective at treating psoriasis and providing a cytoprotective effect 有权
标题翻译：具有改善溶解性的阿伐斯他汀盐治疗银屑病并提供细胞保护作用
公开(公告)号：US6017909A
公开(公告)日：2000-01-25
申请号：US136971
申请日：1998-08-20
申请人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
发明人： Helmut Hettche , Reinhard Muckenschnabel , Gerhard Scheffler , Ilona Fleischhauer , Wolfgang Morick
IPC分类号： A61K31/50 , A61K31/55 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D403/04
CPC分类号： C07D403/04 , A61K31/55 , Y10S514/863 , Y10S514/886 , Y10S514/887
摘要： Salts of azelastine with acetic acid, gluconic acid, lactic acid or malic acid.
摘要翻译：萘曲宁与醋酸，葡萄糖酸，乳酸或苹果酸的盐。

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