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公开(公告)号：US20120108636A1
公开(公告)日：2012-05-03
申请号：US13347999
申请日：2012-01-11
IPC分类号： A61K31/4436 , C07D409/04 , A61K31/381 , A61P29/00 , A61P9/10 , A61P25/08 , A61P25/24 , A61P9/00 , A61P9/06 , C07D333/36 , A61P25/00
CPC分类号： C07D333/36 , C07D409/04
摘要： The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
摘要翻译： 本发明提供式（I）化合物，其中W，R 1，R 5和R 6具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构增强子，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛，炎症性疼痛，心脏病或病症如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死 和中风，神经系统疾病或损伤，睡眠障碍，癫痫和抑郁症。
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公开(公告)号：US20090281145A1
公开(公告)日：2009-11-12
申请号：US12437344
申请日：2009-05-07
IPC分类号： A61K31/4436 , C07D333/36 , A61K31/381 , C07D409/04 , A61P25/00
CPC分类号： C07D333/36 , C07D409/04
摘要： The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.
摘要翻译： 本发明提供式（I）化合物，其中W，R 1，R 5和R 6具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构增强子，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛，炎症性疼痛，心脏病或病症如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死 和中风，神经系统疾病或损伤，睡眠障碍，癫痫和抑郁症。
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公开(公告)号：US07855209B2
公开(公告)日：2010-12-21
申请号：US11938465
申请日：2007-11-12
IPC分类号： A61K31/497 , C07D403/06
CPC分类号： C07D333/36 , C07D409/04 , C07D409/06 , C07D409/12 , C07D487/08 , C07D487/10 , C07D491/10
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和Q具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构调节剂，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。
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公开(公告)号：US20080125438A1
公开(公告)日：2008-05-29
申请号：US11938465
申请日：2007-11-12
IPC分类号： A61K31/497 , C07D333/36 , A61P9/00 , A61K31/38 , C07D405/02
CPC分类号： C07D333/36 , C07D409/04 , C07D409/06 , C07D409/12 , C07D487/08 , C07D487/10 , C07D491/10
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4， 和Q具有本说明书中定义的含义。 式（I）化合物是A 1 N 2腺苷受体的变构调节剂，因此可用于治疗由Aβ1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。
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公开(公告)号：US07101905B2
公开(公告)日：2006-09-05
申请号：US10112613
申请日：2002-03-29
IPC分类号： A61K31/381 , C07D333/50
CPC分类号： A61K31/4365 , A61K31/381 , A61K31/4743
摘要： New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.
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公开(公告)号：US20110053917A1
公开(公告)日：2011-03-03
申请号：US12939601
申请日：2010-11-04
IPC分类号： A61K31/551 , A61K31/496 , A61K31/4535 , A61K31/4995 , A61K31/407 , A61K31/438 , A61P25/00 , A61P29/00 , A61P9/00
CPC分类号： C07D333/36 , C07D409/04 , C07D409/06 , C07D409/12 , C07D487/08 , C07D487/10 , C07D491/10
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the Al adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和Q具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构调节剂，因此可用于治疗由腺嘌呤受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。
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公开(公告)号：US07897596B2
公开(公告)日：2011-03-01
申请号：US11938514
申请日：2007-11-12
IPC分类号： A61K31/55 , A61K31/497 , A61K31/44 , A61K31/38 , C07D243/08 , C07D403/06 , C07D491/10 , C07D333/20
CPC分类号： C07D491/113 , C07D333/36 , C07D409/06 , C07D409/12 , C07D487/10
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和Q具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构调节剂，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗塞和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。
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公开(公告)号：US07449490B2
公开(公告)日：2008-11-11
申请号：US11402240
申请日：2006-04-11
IPC分类号： A61K31/381
CPC分类号： A61K31/4365 , A61K31/381 , A61K31/4743
摘要： New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.
摘要翻译： 提供新的稠合噻吩化合物和使用这些化合物用于各种治疗适应症的方法。 本发明的化合物特别可用于治疗神经性疼痛。
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公开(公告)号：US20080119460A1
公开(公告)日：2008-05-22
申请号：US11938514
申请日：2007-11-12
IPC分类号： A61K31/551 , C07D333/20 , A61K31/381 , C07D403/06 , A61P25/02 , A61P9/00 , A61P25/00 , A61K31/496 , C07D491/113 , A61K31/438
CPC分类号： C07D491/113 , C07D333/36 , C07D409/06 , C07D409/12 , C07D487/10
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
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公开(公告)号：US07511133B2
公开(公告)日：2009-03-31
申请号：US10944245
申请日：2004-09-17
IPC分类号： C07H19/00 , C07H19/16 , C07H19/22 , C07H19/167 , C07H19/173
CPC分类号： C07H19/16 , A61K31/7076 , C07H1/00 , G01N33/74 , G01N2333/726
摘要： The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5′ position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido derivatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
摘要翻译： 下式的化合物：其中Ar，R和R 1具有说明书中给出的含义。 该系列具有5'位保守脲酰胺基团的亚磺酰氨基衍生物提供了优异的A3受体亲和力以及选择性。 这些新的腺苷激动剂是用脂肪族（环状或直链）或芳族基团N-取代的亚磺酰氨基衍生物。
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