公开(公告)号：EP2880033A1

公开(公告)日：2015-06-10

申请号：EP13765756.5

申请日：2013-07-29

申请人： Purdue Pharma LP ,  Shionogi & Co., Ltd

发明人： UENO, Tatsuhiko ,  TSUNO, Naoki

IPC分类号： C07D471/08 ,  C07D498/08 ,  A61K31/498 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D401/14 ,  C07D471/08 ,  C07D498/08

摘要： The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R
1 , R
2 , Q
a , Y
1 , Z, A, B, Q
x , E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxal ine-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.

摘要翻译： 本公开涉及式（I）的环状脲或内酰胺取代的喹喔啉型哌啶化合物及其药学上可接受的衍生物：其中R1，R2，Qa，Y1，Z，A，B，Qx，E，G， M，U，W和a如本文所定义，包含有效量的环脲或内酰胺取代的喹喔啉型哌啶化合物的组合物，以及治疗或预防诸如疼痛的病症的方法，包括给予 有需要的动物有效量的循环尿素或内酰胺取代的喹喔啉哌啶化合物。

公开(公告)号：EP2324013B1

公开(公告)日：2012-09-19

申请号：EP09786064.7

申请日：2009-07-20

申请人： Purdue Pharma LP ,  Shionogi & Co., Ltd.

发明人： YAO, Jiangchao ,  WHITEHEAD, John, W., F. ,  TSUNO, Naoki ,  FUCHINO, Kouki

IPC分类号： C07D403/04 ,  A61K31/498 ,  A61P25/04

CPC分类号： C07D471/08 ,  C07D403/04 ,  C07D451/14

摘要： The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.

公开(公告)号：EP2324013A1

公开(公告)日：2011-05-25

申请号：EP09786064.7

申请日：2009-07-20

申请人： Purdue Pharma LP ,  Shionogi & Co., Ltd.

发明人： YAO, Jiangchao ,  WHITEHEAD, John, W., F. ,  TSUNO, Naoki ,  FUCHINO, Kouki

IPC分类号： C07D403/04 ,  A61K31/498 ,  A61P25/04

CPC分类号： C07D471/08 ,  C07D403/04 ,  C07D451/14

摘要： The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.

公开(公告)号：EP1988077A1

公开(公告)日：2008-11-05

申请号：EP07714666.0

申请日：2007-02-21

申请人： SHIONOGI & CO., LTD.

发明人： MASUI, Moriyasu ,  ADACHI, Makoto ,  MIKAMIYAMA, Hidenori ,  MATSUMURA, Akira ,  TSUNO, Naoki

IPC分类号： C07D209/08 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/538 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/18 ,  A61P39/00 ,  A61P43/00 ,  C07D209/34 ,  C07D263/58 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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 CR 1 , A 1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A 2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R 1 , R 2 , R a , R b , R c and R d are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is -(CR 3 R 4 )m-, -CO(CR 3 R 4 )n-, -CONR 5 (CR 3 R 4 )n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R 3 and R 4 are each independently hydrogen, halogen, hydroxy etc., and R 5 is hydrogen or lower alkyl,
or a pharmaceutically acceptable salt, or a solvate thereof.

摘要翻译： 发现式（I）所示的含氮杂环衍生物与NR1 / NR2B的受体特异性结合，用作NR2B受体拮抗剂。 由下式表示的化合物：其中Z为N或CR 1，A 1为任选取代的含氮芳香族单环基，任选取代的含氮芳香族稠合环基等，A 2为芳香族烃环 基团或芳族杂环基团，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，R 5为氢或低级烷基，或其药学上可接受的盐或溶剂合物。

公开(公告)号：EP3101018B1

公开(公告)日：2019-03-06

申请号：EP16176601.9

申请日：2008-08-29

申请人： Purdue Pharma L.P. ,  SHIONOGI & CO., LTD.

发明人： GOEHRING, R. Richard ,  MATSUMURA, Akira ,  SHAO, Bin ,  TAODA, Yoshiyuki ,  TSUNO, Naoki ,  WHITEHEAD, John, W., F. ,  YAO, Jiangchao ,  FUCHINO, Kouki

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D451/04 ,  C07D451/14 ,  C07D471/14 ,  A61K31/498 ,  A61K31/4985 ,  A61P25/04

公开(公告)号：EP2797912A1

公开(公告)日：2014-11-05

申请号：EP12813964.9

申请日：2012-11-30

申请人： Purdue Pharma LP ,  Shionogi & Co., Ltd.

发明人： TAFESSE, Laykea ,  TSUNO, Naoki ,  ZHOU, Xiaoming

IPC分类号： C07D401/14 ,  A61K31/498 ,  A61P25/04

CPC分类号： C07D413/14 ,  C07D401/14

摘要： The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the R
1 , R
2 , R
3 , Q, Y
1 , Z, A, B, a, and b are as defined herein, compositions comprising an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound.

公开(公告)号：EP2076506B1

公开(公告)日：2010-09-22

申请号：EP08727696.0

申请日：2008-01-15

申请人： Purdue Pharma L.P. ,  Shionogi&Co., Ltd.

发明人： BABA, Yoshiyasu ,  BROWN, Kevin C. ,  GOEHRING, R. Richard ,  TSUNO, Naoki

IPC分类号： C07D401/04 ,  C07D451/14 ,  C07D471/04 ,  C07D471/08 ,  A61K31/498 ,  A61P25/04

CPC分类号： C07D401/04 ,  C07D451/14 ,  C07D471/04 ,  C07D471/08

摘要： The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.

公开(公告)号：EP2164325A1

公开(公告)日：2010-03-24

申请号：EP08767992.4

申请日：2008-05-30

申请人： Shionogi&Co., Ltd.

发明人： TSUNO, Naoki ,  MIKAMIYAMA, Hidenori ,  MASUI, Moriyasu

IPC分类号： A01N43/40 ,  A61K31/445

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为氢，各自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= O， 任选取代的低级烷基，氰基，硝基等，m是1或2，p是0,1或2，q是0或1.本发明还涉及使用式I化合物治疗，预防或改善 对钙通道阻断有响应的病症，特别是N型钙通道。 本发明的化合物对于治疗疼痛特别有用。

公开(公告)号：EP2086958A2

公开(公告)日：2009-08-12

申请号：EP08806986.9

申请日：2008-08-29

申请人： Purdue Pharma LP ,  Shionogi Co., Ltd.

发明人： GOEHRING, Richard, R. ,  MATSUMURA, Akira ,  SHAO, Bin ,  TAODA, Yoshiyuki ,  TSUNO, Naoki ,  WHITEHEAD, John, William, Frank ,  YAO, Jiangchao

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D451/04 ,  C07D451/14 ,  C07D471/14 ,  A61K31/498 ,  A61K31/4985 ,  A61P25/04

CPC分类号： C07D451/14 ,  A61K31/498 ,  C07D401/04 ,  C07D401/14 ,  C07D451/04 ,  C07D471/08 ,  C07D471/14 ,  C07D487/04 ,  C07D498/08 ,  C07D519/00

摘要： The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds of formula (I) or formula (II), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound. Formula (I) or Formula (II).

公开(公告)号：EP2040698A2

公开(公告)日：2009-04-01

申请号：EP07810356.1

申请日：2007-07-12

申请人： SHIONOGI & CO., LTD. ,  Euro-Celtique S.A.

发明人： MATSUMURA, Akira ,  MIKAMIYAMA, Hidenori ,  TSUNO, Naoki ,  KYLE, Donald, J. ,  SHAO, Bin ,  YAO, Jiangchao

IPC分类号： A61K31/40 ,  C07D207/14

CPC分类号： C07D211/72 ,  C07D211/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

摘要： The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CR3R4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R3 and R4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is O, 1 or 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.