-
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
-
公开(公告)号:US20060025452A1
公开(公告)日:2006-02-02
申请号:US11236145
申请日:2005-09-27
申请人: Craig Smith , Michel Rathbone , Margaret Petty , David Rampe
发明人: Craig Smith , Michel Rathbone , Margaret Petty , David Rampe
IPC分类号: A61K31/4439
CPC分类号: A61K31/4439 , Y10S514/903
摘要: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
-
公开(公告)号:US20090281147A1
公开(公告)日:2009-11-12
申请号:US12420390
申请日:2009-04-29
IPC分类号: A61K31/4439 , A61P25/00
CPC分类号: A61K31/4439 , Y10S514/903
摘要: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
-
公开(公告)号:US20090209595A1
公开(公告)日:2009-08-20
申请号:US12420416
申请日:2009-04-29
IPC分类号: A61K31/4439
CPC分类号: A61K31/4439 , Y10S514/903
摘要: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
-
公开(公告)号:US20050026916A1
公开(公告)日:2005-02-03
申请号:US10896166
申请日:2004-07-21
申请人: Patrick Shum , Alexandre Gross , Liang Ma , Daniel McGarry , Gregory Merriman , David Rampe , Garth Ringheim , Jeffrey Sabol , Francis Volz
发明人: Patrick Shum , Alexandre Gross , Liang Ma , Daniel McGarry , Gregory Merriman , David Rampe , Garth Ringheim , Jeffrey Sabol , Francis Volz
IPC分类号: C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/46 , C07D233/48 , C07D235/30 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/10 , A61K31/5377 , A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497
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 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
-
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:US20070129403A1
公开(公告)日:2007-06-07
申请号:US11536808
申请日:2006-09-29
申请人: Craig Smith , David Rampe , Beth Borowsky , Sathapana Kongsamut
发明人: Craig Smith , David Rampe , Beth Borowsky , Sathapana Kongsamut
IPC分类号: A61K31/4439
CPC分类号: A61K31/4439
摘要: The present invention provides methods of treating schizophrenia and/or glucoregulatory abnormalities in a patient in need thereof comprising administering to said patient a therapeutically effective amount of a compound of formula I wherein in is 0, 1 or 2; n is 0, 1 or 2; p is 0 or 1; each R is independently hydrogen, halogen, trifluoromethyl, C1-C6alkyl, C1-C6alkoxy, benzyloxy, hydroxy, nitro or amino; each R1 is independently hydrogen, C1-C6alkyl, C1-C6alkenyl, C1-C6alkanoyl, halogen, cyano, —C(O)C1-C6alkyl, —C1-C6alkyleneCN, —C1-C6alkyleneNR′R″ wherein R′ and R″ are each independently hydrogen or C1-C6alkyl, —C1-C6alkyleneOC(O)C1-C6alkyl, or —CH(OH)R4 wherein R4 is hydrogen or C1-C6alkyl; R2 is hydrogen, C1-C6alkyl optionally substituted with halogen, hydroxy or benlzyloxy, C1-C6alkenyl, C1-C6alkynyl, —CO2C1-C6alkyl, or —R5—NR′R″ wherein R5 is C1-C6alkylene, C1-C6alkenylene or C1-C6alkynylene and R′ and R″ are each independently hydrogen, C1-C6alkyl or alternatively the group —NR′R″ as a whole is 1-pyrrolidinyl; and R3 is hydrogen, nitro, amino, halogen, C1-C6alkoxy, hydroxy or C1-C6alkyl or a pharmaceutically acceptable salt thereof.
-
公开(公告)号:US07534803B2
公开(公告)日:2009-05-19
申请号:US11236145
申请日:2005-09-27
IPC分类号: A61K31/44
CPC分类号: A61K31/4439 , Y10S514/903
摘要: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
摘要翻译: 式I的N-(吡啶基)-1H-吲哚-1-胺提供钾和钠通道的阻断性质的独特组合。 这些化合物可用于治疗脱髓鞘疾病和病症如多发性硬化,脊髓损伤,创伤性脑损伤和中风。 这些化合物也可用于中风康复,膀胱刺激和功能障碍的治疗,以及治疗神经性疼痛和趋化因子诱导的疼痛。
-
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:US06967210B2
公开(公告)日:2005-11-22
申请号:US10076191
申请日:2002-02-14
IPC分类号: C07D401/12 , A61K20060101 , A61K31/4439 , A61P3/00 , A61P9/00 , A61P13/00 , A61P13/10 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61K31/44
CPC分类号: A61K31/4439 , Y10S514/903
摘要: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.
-
-
-
-
-
-
-
-
-