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1. 发明专利

IL207607A Process for producing thiophene compound and intermediate thereof 未知
公开(公告)号：IL207607A
公开(公告)日：2017-03-30
申请号：IL20760710
申请日：2010-08-12
申请人： NISSAN CHEMICAL IND LTD , KATSUAKI MIYAJI , KAZUFUMI YANAGIHARA , SHINGO UMEZAWA
发明人： KATSUAKI MIYAJI , KAZUFUMI YANAGIHARA , SHINGO UMEZAWA
摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R 1 is an aryl group or the like, R 4 is a C 1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a ³-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

2. 发明专利

IL243809A Process for the production of γ-ketosulfide compounds and γ-ketosulfide compounds obtained 未知
公开(公告)号：IL243809A
公开(公告)日：2017-03-30
申请号：IL24380916
申请日：2016-01-27
申请人： NISSAN CHEMICAL IND LTD , KATSUAKI MIYAJI , KAZUFUMI YANAGIHARA , SHINGO UMEZAWA
发明人： KATSUAKI MIYAJI , KAZUFUMI YANAGIHARA , SHINGO UMEZAWA
摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R 1 is an aryl group or the like, R 4 is a C 1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a ³-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

3. 发明授权

US08889732B2 Fused heterocyclic compounds and thrombopoietin receptor activators 有权
标题翻译：稠合杂环化合物和血小板生成素受体激活剂
公开(公告)号：US08889732B2
公开(公告)日：2014-11-18
申请号：US13503560
申请日：2010-10-22
申请人： Yukihiro Shigeta , Shingo Umezawa , Shunsuke Iwamoto , Takanori Nakamura
发明人： Yukihiro Shigeta , Shingo Umezawa , Shunsuke Iwamoto , Takanori Nakamura
IPC分类号： A61K31/38 , C07D333/32 , C07D231/18 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14 , C07D409/04 , C07D333/40
CPC分类号： C07D409/14 , C07D231/18 , C07D333/32 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/04 , C07D409/12
摘要： Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided.A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
摘要翻译：提供了可用于预防，治疗或改善血小板生成素受体活化有效的疾病的融合杂环化合物。式（I）表示的化合物（其中R 1是与饱和环等稠合的芳基A，B，L1，R2，L2，L3，Y，L4，R3和X在说明书中定义），该化合物或其溶剂化物的互变异构体，前药或药学上可接受的盐。

4. 发明授权

US08399685B2 Process for producing thiophene compound and intermediate thereof 有权
标题翻译：制备噻吩化合物及其中间体的方法
公开(公告)号：US08399685B2
公开(公告)日：2013-03-19
申请号：US12919394
申请日：2009-02-27
申请人： Kazufumi Yanagihara , Shingo Umezawa , Katsuaki Miyaji
发明人： Kazufumi Yanagihara , Shingo Umezawa , Katsuaki Miyaji
IPC分类号： C07D333/32
CPC分类号： C07D333/32 , C07C319/14 , C07C327/32 , C07C323/56
摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals.A 2-aryl acetate compound represented by the formula (1): wherein R1 is an aryl group or the like, R4 is a C1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).
摘要翻译：提供一种生产2-芳基-3-羟基-4-取代的羰基噻吩化合物或其中间体的新方法，其用作制备药物和农药的中间体。由式（1）表示的2-芳基乙酸酯化合物：其中R 1为芳基等，R 4为C 1-3烷基等，X为离去基，与硫代乙酸化合物为了形成硫代乙酰基化合物（3），硫代乙酰基化合物（3）与乙烯基酮化合物反应形成γ-酮硫醚化合物（5），其在碱性条件下环化形成二氢噻吩化合物（6），并且二氢噻吩化合物（6）通过使用氧化剂氧化，得到2-芳基-3-羟基-4-取代的羰基噻吩化合物（7）。

5. 发明申请

US20110124884A1 PROCESS FOR PRODUCING THIOPHENE COMPOUND AND INTERMEDIATE THEREOF 有权
标题翻译：生产噻吩化合物及其中间体的方法
公开(公告)号：US20110124884A1
公开(公告)日：2011-05-26
申请号：US12919394
申请日：2009-02-27
申请人： Kazufumi Yanagihara , Shingo Umezawa , Katsuaki Miyaji
发明人： Kazufumi Yanagihara , Shingo Umezawa , Katsuaki Miyaji
IPC分类号： C07D333/32 , C07C327/12
CPC分类号： C07D333/32 , C07C319/14 , C07C327/32 , C07C323/56
摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals.A 2-aryl acetate compound represented by the formula (1): wherein R1 is an aryl group or the like, R4 is a C1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).
摘要翻译：提供一种生产2-芳基-3-羟基-4-取代的羰基噻吩化合物或其中间体的新方法，其用作制备药物和农药的中间体。由式（1）表示的2-芳基乙酸酯化合物：其中R 1为芳基等，R 4为C 1-3烷基等，X为离去基，与硫代乙酸化合物为了形成硫代乙酰基化合物（3），硫代乙酰基化合物（3）与乙烯基酮化合物反应形成γ-酮硫醚化合物（5），其在碱性条件下环化形成二氢噻吩化合物（6），并且二氢噻吩化合物（6）通过使用氧化剂氧化，得到2-芳基-3-羟基-4-取代的羰基噻吩化合物（7）。

6. 发明申请

US20120209005A1 FUSED HETEROCYCLIC COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS 有权
标题翻译：融合的杂环化合物和血栓素受体激活剂
公开(公告)号：US20120209005A1
公开(公告)日：2012-08-16
申请号：US13503560
申请日：2010-10-22
申请人： Yukihiro Shigeta , Shingo Umezawa , Shunsuke Iwamoto , Takanori Nakamura
发明人： Yukihiro Shigeta , Shingo Umezawa , Shunsuke Iwamoto , Takanori Nakamura
IPC分类号： C07D409/14 , C07D333/32 , C07D401/12 , C07D409/12 , C07D231/18
CPC分类号： C07D409/14 , C07D231/18 , C07D333/32 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/04 , C07D409/12
摘要： Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided.A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
摘要翻译：提供了可用于预防，治疗或改善血小板生成素受体活化有效的疾病的融合杂环化合物。式（I）表示的化合物（其中R 1是与饱和环等稠合的芳基A，B，L1，R2，L2，L3，Y，L4，R3和X在说明书中定义），该化合物或其溶剂化物的互变异构体，前药或药学上可接受的盐。

7. 发明申请

US20130060050A1 PROCESS FOR PRODUCING THIOPHENE COMPOUND AND INTERMEDIATE THEREOF 有权
标题翻译：生产噻吩化合物及其中间体的方法
公开(公告)号：US20130060050A1
公开(公告)日：2013-03-07
申请号：US13653019
申请日：2012-10-16
申请人： Kazufumi YANAGIHARA , Shingo UMEZAWA , Katsuaki MIYAJI
发明人： Kazufumi YANAGIHARA , Shingo UMEZAWA , Katsuaki MIYAJI
IPC分类号： C07C323/56 , C07D333/32
CPC分类号： C07D333/32 , C07C319/14 , C07C327/32 , C07C323/56
摘要： Provided are γ-ketosulfide compounds represented by the formula (5): where the structural variables R1, R2, R3 and R4 are as defined herein.
摘要翻译：提供由式（5）表示的γ-酮硫醚化合物：其中结构变量R1，R2，R3和R4如本文所定义。

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