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公开(公告)号：US20090233878A1
公开(公告)日：2009-09-17
申请号：US12201157
申请日：2008-08-29
CPC分类号： A61K31/7076 , C07H19/16
摘要： The present invention provides compounds of the formula wherein Ar, R and R1 have a meaning as defined herein in the specification. Compounds of formula (I) are agonists of the A3 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A3 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of behavioral depression, cerebral ischemia, hypotension, chemically induced seizures, inflammatory diseases, asthma, and cancer diseases expressing the adenosine A3 receptor.
摘要翻译： 本发明提供下式的化合物其中Ar，R和R 1具有本说明书中定义的含义。 式（I）的化合物是A3腺苷受体的激动剂，因此可用于治疗由A3腺苷受体介导的病症。 因此，式（I）化合物可用于治疗行为抑制，脑缺血，低血压，化学诱导的癫痫发作，炎性疾病，哮喘和表达腺苷A3受体的癌症疾病。
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公开(公告)号：US07691825B2
公开(公告)日：2010-04-06
申请号：US11757559
申请日：2007-06-04
IPC分类号： A61K31/70 , C07H19/167
CPC分类号： C07H19/19
摘要： The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.
摘要翻译： 本发明提供下式的化合物，其中R1，R2，R3和n具有说明书中所述的含义，其制备方法和含有它们的药物组合物。 式（I）化合物是腺苷A2B受体激动剂，因此可用于治疗由A2B受体介导的哺乳动物疾病，包括但不限于脓毒性休克，囊性纤维化，阳ence，腹泻， 和心脏病。 心脏疾病包括高血压，动脉硬化和心脏病发作的增生。 本发明还提供了通过使用式（I）化合物诱导药理学应力以促进局部缺血区域的冠状动脉成像的方法。 式（I）化合物可以用例如放射性同位素标记，因此可用于动力学结合实验。
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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：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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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：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：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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