公开(公告)号：US07326792B2

公开(公告)日：2008-02-05

申请号：US10896166

申请日：2004-07-21

申请人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

发明人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

IPC分类号： A61K31/4168 ,  A61K31/417 ,  C07D233/24 ,  C07D233/50

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D235/30 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/10

摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

摘要翻译： 本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢 - 咪唑衍生物：其中R 1，R 2，R 2 R 3，R 4，R 5，X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况 神经系统，如中风，阿尔茨海默病等

公开(公告)号：US20080227782A1

公开(公告)日：2008-09-18

申请号：US12062641

申请日：2008-04-04

申请人： Suzanne C. Aldous ,  John Ziqi Jiang ,  Jinqi Lu ,  Liang Ma ,  Lan Mu ,  Harry Randall Munson ,  Jeffrey Stephen Sabol ,  Sukanthini Thurairatnam ,  Christopher Loren Vandeusen

发明人： Suzanne C. Aldous ,  John Ziqi Jiang ,  Jinqi Lu ,  Liang Ma ,  Lan Mu ,  Harry Randall Munson ,  Jeffrey Stephen Sabol ,  Sukanthini Thurairatnam ,  Christopher Loren Vandeusen

IPC分类号： A61K31/506 ,  A61P11/00 ,  C07D239/28 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/02 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/04 ,  A61K31/505

CPC分类号： C07D239/28 ,  C07D401/04 ,  C07D403/12 ,  C07D413/04

摘要： This invention is directed to a compound of formula (I): wherein R1, R2, R3 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，R 3和L 1， / SUP>如本文所定义，包含该化合物的药物组合物和该化合物用于治疗过敏性和/或炎症性疾病，特别是诸如过敏性鼻炎，哮喘和/或慢性阻塞性肺病（COPD）的疾病的用途。

公开(公告)号：US20080132550A1

公开(公告)日：2008-06-05

申请号：US11947442

申请日：2007-11-29

申请人： Patrick SHUM ,  Alexandre GROSS ,  Liang MA ,  Daniel G. MCGARRY ,  Gregory H. MERRIMAN ,  David RAMPE ,  Garth RINGHEIM ,  Jeffrey Stephen SABOL ,  Francis A. VOLZ

发明人： Patrick SHUM ,  Alexandre GROSS ,  Liang MA ,  Daniel G. MCGARRY ,  Gregory H. MERRIMAN ,  David RAMPE ,  Garth RINGHEIM ,  Jeffrey Stephen SABOL ,  Francis A. VOLZ

IPC分类号： A61K31/4439 ,  C07D233/50 ,  A61K31/417 ,  C07D235/30 ,  A61K31/4184 ,  C07D233/42 ,  C07D401/04

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D235/30 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/10

摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

摘要翻译： 本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢 - 咪唑衍生物：其中R 1，R 2，R 2 R 3，R 4，R 5，X和Y如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况 神经系统，如中风，阿尔茨海默病等

公开(公告)号：US08202863B2

公开(公告)日：2012-06-19

申请号：US12062641

申请日：2008-04-04

申请人： Suzanne C. Aldous ,  John Ziqi Jiang ,  Jinqi Lu ,  Liang Ma ,  Lan Mu ,  Harry Randall Munson ,  Jeffrey Stephen Sabol ,  Sukanthini Thurairatnam ,  Christopher Loren Vandeusen

发明人： Suzanne C. Aldous ,  John Ziqi Jiang ,  Jinqi Lu ,  Liang Ma ,  Lan Mu ,  Harry Randall Munson ,  Jeffrey Stephen Sabol ,  Sukanthini Thurairatnam ,  Christopher Loren Vandeusen

IPC分类号： C07D239/28 ,  C07D403/12 ,  A61K31/506

CPC分类号： C07D239/28 ,  C07D401/04 ,  C07D403/12 ,  C07D413/04

摘要： This invention is directed to a compound of formula (I): wherein R1, R2, R3 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).

摘要翻译： 本发明涉及式（I）化合物：其中R1，R2，R3和L1如本文所定义，包含该化合物的药物组合物和该化合物用于治疗过敏和/或炎症性疾病，特别是疾病 如过敏性鼻炎，哮喘和/或慢性阻塞性肺疾病（COPD）。

公开(公告)号：US07741493B2

公开(公告)日：2010-06-22

申请号：US11947442

申请日：2007-11-29

申请人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

发明人： Patrick Shum ,  Alexandre Gross ,  Liang Ma ,  Daniel G. McGarry ,  Gregory H. Merriman ,  David Rampe ,  Garth Ringheim ,  Jeffrey Stephen Sabol ,  Francis A. Volz

IPC分类号： A61K31/4184 ,  C07D235/02

CPC分类号： C07D401/04 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D235/30 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/10

摘要： The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

摘要翻译： 本发明涉及式II的新一系列4,5-二苯基-2-氨基-4,5-二氢咪唑衍生物：其中R，R 1，R 2，R 3，R 4，R 5，X和Y为 本文定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是P2X7离子通道阻断剂，因此可用作药剂，特别是用于治疗和/或预防各种具有炎症成分的疾病，包括炎性肠病，类风湿性关节炎和与中枢相关的疾病状况 神经系统，如中风，阿尔茨海默病等