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1. 发明申请

US20120022069A1 ACRYLAMIDE COMPOUNDS AND THE USE THEREOF 有权
标题翻译：丙烯酰胺化合物及其用途
公开(公告)号：US20120022069A1
公开(公告)日：2012-01-26
申请号：US13260185
申请日：2010-04-02
申请人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
发明人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
IPC分类号： A61K31/445 , C07D401/12 , A61K31/4545 , C07D405/12 , A61K31/4525 , C07D409/12 , C07D265/30 , A61K31/5375 , A61P25/00 , A61P25/08 , A61P25/06 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/22 , A61P9/12 , A61P9/06 , C07D211/96
CPC分类号： C07D211/70 , C07D211/96
摘要： The invention relates to acrylamide compounds of Formula I mentioned below.The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及下述式I的丙烯酰胺化合物。本发明还涉及使用式I化合物来治疗或预防对阻塞钙通道，特别是N型钙通道有响应的病症。本发明的化合物特别适用于治疗疼痛。

2. 发明授权

US08895551B2 Acrylamide compounds and the use thereof 有权
标题翻译：丙烯酰胺化合物及其用途
公开(公告)号：US08895551B2
公开(公告)日：2014-11-25
申请号：US13260185
申请日：2010-04-02
申请人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
发明人： Hidenori Mikamiyama , Akira Matsumura , Moriyasu Masui , Kosuke Anan , Kayoko Hata
IPC分类号： A61K31/5377 , C07D265/30 , A61K31/445 , C07D211/68 , C07D401/00 , C07D405/00 , C07D211/70 , C07D211/96
CPC分类号： C07D211/70 , C07D211/96
摘要： The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及下述式I的丙烯酰胺化合物。本发明还涉及使用式I化合物来治疗或预防对阻塞钙通道，特别是N型钙通道有响应的病症。本发明的化合物特别适用于治疗疼痛。

3. 发明授权

US07935706B2 Nitrogen-containing heterocycle derivatives substituted with cyclic group 失效
标题翻译：用环状基团取代的含氮杂环衍生物
公开(公告)号：US07935706B2
公开(公告)日：2011-05-03
申请号：US12278412
申请日：2007-02-21
申请人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
发明人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
IPC分类号： A61K31/497
CPC分类号： C07D209/08 , C07D209/34 , C07D215/38 , C07D235/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D277/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , C07D513/04
摘要： It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译：发现由式（I）表示的含氮杂环衍生物特异性结合NR1 / NR2B的受体，并用作NR2B受体拮抗剂。由下式表示的化合物：其中Z为N或CR1，A1为任选取代的含氮芳族单环基团，任选取代的含氮芳族稠合环基等，A2为芳族烃环基或芳族杂环基，各自任选具有取代基，R 1，R 2，R a，R b，R c和R d各自独立地为氢，羟基等，w为2或3，t为1或2，X为 - （CR 3 R 4）m - ，-CO（CR 3 R 4）n - ， - CONR 5（CR 3 R 4）n - 等，m为1〜4的整数，n为0〜4的整数，R 3和R 4各自独立地为氢，卤素，羟基等 R5为氢或低级烷基，或其药学上可接受的盐或溶剂合物。

4. 发明申请

US20110172415A1 NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUP 审中-公开
标题翻译：用循环集团取代的含氮杂环衍生物（NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES WITH CYCLIC GROUP
公开(公告)号：US20110172415A1
公开(公告)日：2011-07-14
申请号：US13050465
申请日：2011-03-17
申请人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
发明人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
IPC分类号： C07D498/04 , C07D401/12 , C07D405/12 , C07D401/06 , C07D401/14 , C07D405/14 , C07D403/12 , C07D417/14 , C07D417/12 , C07D471/04 , C07D295/185 , C07D413/12
CPC分类号： C07D209/08 , C07D209/34 , C07D215/38 , C07D235/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D277/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , C07D513/04
摘要： It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译：发现由式（I）表示的含氮杂环衍生物特异性结合NR1 / NR2B的受体，并用作NR2B受体拮抗剂。由下式表示的化合物：其中Z为N或CR1，A1为任选取代的含氮芳族单环基团，任选取代的含氮芳族稠合环基等，A2为芳族烃环基或芳族杂环基，各自任选具有取代基，R 1，R 2，R a，R b，R c和R d各自独立地为氢，羟基等，w为2或3，t为1或2，X为 - （CR 3 R 4）m - ，-CO（CR 3 R 4）n - ， - CONR 5（CR 3 R 4）n - 等，m为1〜4的整数，n为0〜4的整数，R 3和R 4各自独立地为氢，卤素，羟基等 R5为氢或低级烷基，或其药学上可接受的盐或溶剂合物。

5. 发明申请

US20090062261A1 NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUP 失效
标题翻译：采用循环组合的含氮杂环衍生物
公开(公告)号：US20090062261A1
公开(公告)日：2009-03-05
申请号：US12278412
申请日：2007-02-21
申请人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
发明人： Moriyasu Masui , Makoto Adachi , Hidenori Mikamiyama , Akira Matsumura , Naoki Tsuno
IPC分类号： A61K31/4545 , C07D401/04 , C07D211/44 , C07D211/08 , C07D295/104 , C07D413/12 , C07D401/06 , A61K31/454 , A61K31/496 , C07D413/14 , C07D401/14 , A61K31/551 , A61K31/538 , A61K31/451 , A61K31/495
CPC分类号： C07D209/08 , C07D209/34 , C07D215/38 , C07D235/08 , C07D235/26 , C07D249/18 , C07D263/58 , C07D277/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D498/04 , C07D513/04
摘要： It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译：发现由式（I）表示的含氮杂环衍生物特异性结合NR1 / NR2B的受体，并用作NR2B受体拮抗剂。由下式表示的化合物：其中Z为N或CR1，A1为任选取代的含氮芳族单环基团，任选取代的含氮芳族稠合环基等，A2为芳族烃环基或芳族杂环基，各自任选具有取代基，R 1，R 2，R a，R b，R c和R d各自独立地为氢，羟基等，w为2或3，t为1或2，X为 - （CR 3 R 4）m - ，-CO（CR 3 R 4）n - ， - CONR 5（CR 3 R 4）n - 等，m为1〜4的整数，n为0〜4的整数，R 3和R 4各自独立地为氢，卤素，羟基等 R5为氢或低级烷基，或其药学上可接受的盐或溶剂合物。

6. 发明申请

US20130197219A1 SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG 有权
公开(公告)号：US20130197219A1
公开(公告)日：2013-08-01
申请号：US13824723
申请日：2011-09-21
申请人： Chika Takahashi , Hidenori Mikamiyama , Toshiyuki Akiyama , Kenji Tomita , Yoshiyuki Taoda , Makoto Kawai , Kosuke Anan , Masayoshi Miyagawa , Naoyuki Suzuki
发明人： Chika Takahashi , Hidenori Mikamiyama , Toshiyuki Akiyama , Kenji Tomita , Yoshiyuki Taoda , Makoto Kawai , Kosuke Anan , Masayoshi Miyagawa , Naoyuki Suzuki
IPC分类号： C07D471/04 , C07F9/6561
CPC分类号： C07D471/04 , A61K31/4738 , C07D471/14 , C07F9/6561 , C07F9/65616
摘要： The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.

7. 发明申请

US20100240703A1 OXYIMINO COMPOUNDS AND THE USE THEREOF 有权
标题翻译： OXYIMINO化合物及其用途
公开(公告)号：US20100240703A1
公开(公告)日：2010-09-23
申请号：US12602441
申请日：2008-05-30
申请人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
发明人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
IPC分类号： A61K31/445 , C07D211/96 , A61P29/00 , A61P25/00 , A61P9/06 , A61P9/12 , G01N33/53
CPC分类号： C07D211/96
摘要： The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及（式I）的氧亚氨基化合物及其药学上可接受的盐，前药和溶剂化物，其中：Y是CO或SOm; Z是氢，每个任选取代的低级烷基，低级烯基，芳基，杂环基等.R 1和R 2各自独立地为氢，各自为任选取代的低级烷基，低级烯基，环烷基，芳基，杂环基等，各X独立地为= 任选取代的低级烷基，氰基，硝基等，m为1或2，p为O，1或2，q为O或1.本发明还涉及式I的用途化合物，以治疗，预防或改善对钙通道阻断，特别是N型钙通道的阻滞作用。本发明的化合物特别适用于治疗疼痛。

8. 发明授权

US08563732B2 Oxyimino compounds and the use thereof 有权
标题翻译：氧亚氨基化合物及其用途
公开(公告)号：US08563732B2
公开(公告)日：2013-10-22
申请号：US12602441
申请日：2008-05-30
申请人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
发明人： Moriyasu Masui , Hidenori Mikamiyama , Naoki Tsuno
IPC分类号： A61K31/44 , C07D211/00
CPC分类号： C07D211/96
摘要： The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及（式I）的氧亚氨基化合物及其药学上可接受的盐，前药和溶剂化物，其中：Y是CO或SOm; Z是氢，每个任选取代的低级烷基，低级烯基，芳基，杂环基等.R 1和R 2各自独立地为氢，各自为任意取代的低级烷基，低级烯基，环烷基，芳基，杂环基等，各X独立地为= 任选取代的低级烷基，氰基，硝基等，m为1或2，p为O，1或2，q为O或1.本发明还涉及式I的用途化合物，以治疗，预防或改善对钙通道阻断，特别是N型钙通道的阻滞作用。本发明的化合物特别适用于治疗疼痛。

9. 发明授权

US08987441B2 Substituted polycyclic carbamoyl pyridone derivative prodrug 有权
标题翻译：取代多环氨甲酰吡啶酮衍生物前药
公开(公告)号：US08987441B2
公开(公告)日：2015-03-24
申请号：US13824723
申请日：2011-09-21
申请人： Chika Takahashi , Hidenori Mikamiyama , Toshiyuki Akiyama , Kenji Tomita , Yoshiyuki Taoda , Makoto Kawai , Kosuke Anan , Masayoshi Miyagawa , Naoyuki Suzuki
发明人： Chika Takahashi , Hidenori Mikamiyama , Toshiyuki Akiyama , Kenji Tomita , Yoshiyuki Taoda , Makoto Kawai , Kosuke Anan , Masayoshi Miyagawa , Naoyuki Suzuki
IPC分类号： C07D413/00 , C07D253/08 , C07D471/00 , C07D241/04 , C07D471/04 , C07F9/6561 , C07D471/14
CPC分类号： C07D471/04 , A61K31/4738 , C07D471/14 , C07F9/6561 , C07F9/65616
摘要： The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
摘要翻译：本发明提供具有抗病毒作用的化合物，特别是具有对流感病毒的生长抑制活性的化合物，该化合物的优选实例是具有cap依赖性内切核酸酶抑制活性的取代的3-羟基-4-吡啶酮衍生物前药。

10. 发明申请

US20110190300A1 AMIDE COMPOUNDS AND THE USE THEREOF 审中-公开
标题翻译： AMIDE化合物及其用途
公开(公告)号：US20110190300A1
公开(公告)日：2011-08-04
申请号：US12602392
申请日：2008-05-30
申请人： Akira Matsumura , Hidenori Mikamiyama , Jiangchao Yao
发明人： Akira Matsumura , Hidenori Mikamiyama , Jiangchao Yao
IPC分类号： A61K31/5377 , C07D211/96 , C07D417/12 , C07D401/12 , C07D413/12 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , G01N33/53 , A61P9/00 , A61P25/00 , A61P25/08 , A61P29/00 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/22 , A61P9/12 , A61P9/06
CPC分类号： C07D211/96 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is ═O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0-2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及式I的酰胺化合物：（I）及其药学上可接受的盐，前药和溶剂合物，其中：Y是CO或SOm; Z各自为任选取代的低级烷基，低级烯基，环烷基，芳基，杂环基等; R 1和R 2各自独立地为氢，卤素，氰基，任选取代的低级烷基，任选取代的环烷基，任选取代的芳基或任选取代的杂环基等。R 3和R 4是氢，各自任选取代的低级烷基，环烷基，芳基或杂环基等; X是= 0，任意取代的低级烷基，卤素，氰基，硝基等，n为0-5，m为1或2，p为0-2。本发明还涉及使用式I的化合物来治疗，预防或改善对阻断钙通道，特别是N型钙通道有响应的病症。本发明的化合物特别适用于治疗疼痛。

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