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1. 发明授权

US4433142A Process for the preparation of 7-(2-amino-2-phenylacetamido) cephem derivatives 失效
标题翻译： 7-（2-氨基-2-苯乙酰氨基）头孢烯衍生物的制备方法
公开(公告)号：US4433142A
公开(公告)日：1984-02-21
申请号：US376214
申请日：1982-05-07
申请人： Keizo Takayanagi , Yasuhide Tanaka , Tasuke Kawabata , Fujio Nakamura , Yukio Morita , Shigeto Negi , Takeo Kanai , Eiichi Morita
发明人： Keizo Takayanagi , Yasuhide Tanaka , Tasuke Kawabata , Fujio Nakamura , Yukio Morita , Shigeto Negi , Takeo Kanai , Eiichi Morita
IPC分类号： C07D501/06 , A61K31/545 , C07D501/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Improved process for the preparation of 7-(2-amino-2-phenyl-acetamido)cephem derivatives of the general formula (I): ##STR1## wherein R.sub.1 is a hydrogwn atom or hydroxyl group, n stands for 0, 1 or 2, and A denotes a nitrogen-containing heterocyclic group or a direct bond coupling directly the sulfur atom and the --(CH.sub.2).sub.n COOH group together, as well as pharmaceutically acceptable salts thereof. The process is not only simple and easy to carry out, but also provides as crystalline precipitate the intended products with a high yield. The 7-(2-amino-2-phenyl-acetamido)cephem derivatives are useful as intermediates for syntheses of antibacterial agents.
摘要翻译：用于制备通式（I）的7-（2-氨基-2-苯基 - 乙酰氨基）头孢烯衍生物的改进方法：其中R1是氢原子或羟基，n代表0,1或2 ，A表示含氮杂环基团或直接与硫原子和 - （CH 2）n COOH基团偶联的直接键，以及其药学上可接受的盐。该方法不仅简单易操作，而且可以以高产率提供目标产物的结晶沉淀。 7-（2-氨基-2-苯基 - 乙酰氨基）头孢烯衍生物可用作合成抗菌剂的中间体。

2. 发明授权

US4163864A Process for preparing 2-methyl-3-prenyl-4,5,6-trimethoxyphenol 失效
标题翻译： 2-甲基-3-异戊烯基-4,5,6-三甲氧基苯酚的制备方法
公开(公告)号：US4163864A
公开(公告)日：1979-08-07
申请号：US878470
申请日：1978-02-16
申请人： Eiichi Morita , Hirosaburo Ejiri , Keizo Takayanagi , Yukio Morita , Yasuhide Tanaka , Shizumasa Kijima , Kimio Hamamura , Isao Yamatsu
发明人： Eiichi Morita , Hirosaburo Ejiri , Keizo Takayanagi , Yukio Morita , Yasuhide Tanaka , Shizumasa Kijima , Kimio Hamamura , Isao Yamatsu
IPC分类号： A61K31/09 , A61P1/16 , A61P9/00 , A61P9/08 , A61P9/10 , B01J27/00 , C07B61/00 , C07C41/00 , C07C41/30 , C07C43/23 , C07C46/06 , C07C50/28 , C07C67/00
CPC分类号： C07C50/28 , C07C41/30 , C07C46/06
摘要： 2-METHYL-3-PRENYL-4,5,6-TRIMETHOXYPHENOL OF THE FORMULA: ##STR1## wherein R represents a group of the formula: ##STR2## WHEREIN N IS AN INTEGER OF 0 TO 9 AND A and B represent hydrogen atom or A--B may form a bond,Is prepared by reacting 6-methyl-2,3,4-trimethoxyphenol with a prenol or isoprenol substituted by the group R as defined above in the presence of a complex catalyst comprising Lewis acid and a silica-alumina compound.
摘要翻译： 2-甲基-3-丙烯基-4,5,6-三甲氧基苯酚：其中R表示下式的基团：其中N为0至9的整数，A和B表示氢原子或AB可以形成键，其是通过在包含路易斯酸和二氧化硅 - 氧化铝的复合催化剂存在下，如上定义的由如上定义的基团R取代的PRENOL或异丙苯反应6-甲基-2,3,4-三羟甲基酚制备的复合。

3. 发明授权

US4721788A 4-cyanopiperidine derivatives 失效
标题翻译： 4-氰基哌啶衍生物
公开(公告)号：US4721788A
公开(公告)日：1988-01-26
申请号：US883697
申请日：1986-07-08
申请人： Hiroshi Yamauchi , Seiichiro Nomoto , Isao Sugiyama , Yuuki Komatu , Takeo Kanai , Keizo Takayanagi , Yasuhide Tanaka , Atsushi Koiwa , Shinichi Endoh
发明人： Hiroshi Yamauchi , Seiichiro Nomoto , Isao Sugiyama , Yuuki Komatu , Takeo Kanai , Keizo Takayanagi , Yasuhide Tanaka , Atsushi Koiwa , Shinichi Endoh
IPC分类号： C07D211/62 , C07D453/02 , C07D211/26
CPC分类号： C07D453/02 , C07D211/62
摘要： A novel 4-cyanopiperidine derivative, which is represented by the following general formula (I): ##STR1## wherein X means a halogen atom, or an acid addition salt thereof, is prepared by reacting N-(2-hydroxyethyl)-4-carbamoylpiperidine or an acid addition salt thereof with a dehydrating and halogenating agent; or by reacting 4-cyanopiperidine or a salt thereof with a compound represented by the following general formula (IV):X--CH.sub.2 CH.sub.2 --Y (IV)wherein X has the same meaning as defined above and Y denotes the same halogen atom as X or another halogen atom. The derivative is useful as intermediate for synthesis of quinuclidine derivative which is in turn useful as intermediate for the production of medicines, chemicals, etc.
摘要翻译：由下列通式（I）表示的新颖的4-氰基哌啶衍生物：其中X表示卤素原子或其酸加成盐的方法是通过使N-（2-羟基乙基） -4-氨基甲酰基哌啶或其酸加成盐与脱水和卤化剂反应; 或通过使4-氰基哌啶或其盐与下述通式（IV）表示的化合物反应：X-CH 2 CH 2 -Y（IV）其中X具有与上述相同的含义，Y表示与X相同的卤素原子或另一个卤素原子。该衍生物可用作合成奎宁环衍生物的中间体，其可用作药物，化学品等的生产中间体。

4. 发明授权

US06545024B1 Sulfoxide compounds and acetone complexes, and a process for producing the same 有权
标题翻译：亚砜化合物和丙酮络合物及其制备方法
公开(公告)号：US06545024B1
公开(公告)日：2003-04-08
申请号：US09688810
申请日：2000-10-17
申请人： Masahiko Tsujii , Nobuo Niikawa , Keizo Takayanagi , Shigeharu Nochi
发明人： Masahiko Tsujii , Nobuo Niikawa , Keizo Takayanagi , Shigeharu Nochi
IPC分类号： A61K3144
CPC分类号： C07D401/12
摘要： The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same. Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula: (wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.
摘要翻译：本发明提供了可用作胃酸分泌抑制剂和抗溃疡剂等药物的亚砜化合物的丙酮配合物，或作为制造药物的中间体的方法及其使用方法。名义上，它是由下式表示的亚砜化合物或其药学上可接受的盐的丙酮络合物：其中R1表示氢原子，甲氧基或二氟甲氧基，R2表示甲基或甲氧基，R3表示3 甲氧基丙氧基，甲氧基或2,2,2-三氟乙氧基，R 4表示氢原子或甲基，n和m分别表示1〜4的整数，B表示氢原子，碱金属原子或1/2碱土金属原子），其通过用丙酮处理亚砜化合物或其药学上可接受的盐而获得。

5. 发明授权

US06180652B2 Sulfoxide compounds and acetone complexes, and a process for producing the same 有权
标题翻译：亚砜化合物和丙酮络合物及其制备方法
公开(公告)号：US06180652B2
公开(公告)日：2001-01-30
申请号：US09433786
申请日：1999-11-03
申请人： Masahiko Tsujii , Nobuo Niikawa , Keizo Takayanagi , Shigeharu Nochi
发明人： Masahiko Tsujii , Nobuo Niikawa , Keizo Takayanagi , Shigeharu Nochi
IPC分类号： A61K3144
CPC分类号： C07D401/12
摘要： The present invention provides acetone complexes of sulfoxide compounds, useful as medicines such as inhibitors of gastric acid secretion and anti-ulcer agents or as intermediates for production of medicines, a process for producing the same and a purification method of using the same. Namely, it is the acetone complexes of sulfoxide compounds or of pharmaceutically acceptable salts thereof represented by the following formula: (wherein R1 represents a hydrogen atom, a methoxy group or a difluoromethoxy group, R2 represents a methyl group or a methoxy group, R3 represents a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group, R4 represents a hydrogen atom or a methyl group, n and m independently represent an integer of 1 to 4, and B represents a hydrogen atom, an alkali metal atom or ½ alkaline earth metal atom), which are obtained by treating the sulfoxide compounds or pharmaceutically acceptable salts thereof with acetone.
摘要翻译：本发明提供了可用作胃酸分泌抑制剂和抗溃疡剂等药物的亚砜化合物的丙酮配合物，或作为制造药物的中间体的方法及其使用方法。名义上，它是由下式表示的亚砜化合物或其药学上可接受的盐的丙酮络合物：其中R1表示氢原子，甲氧基或二氟甲氧基，R2表示甲基或甲氧基，R3表示3 - 甲氧基丙氧基，甲氧基或2,2,2-三氟乙氧基，R4表示氢原子或甲基，n和m独立地表示1〜4的整数，B表示氢原子，碱金属原子或½碱土金属原子），其通过用丙酮处理亚砜化合物或其药学上可接受的盐而获得。

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