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1.发明授权Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs 失效2-芳烷氧基腺嘌呤，2-烷氧基腺苷及其类似物的合成公开(公告)号：US07342003B2
公开(公告)日：2008-03-11
申请号：US11155212
申请日：2005-06-16
申请人： Allan R. Moorman , Michael Scannell , Thiagarajan Balasubramanian , Russell Outcalt , Edward Leung
发明人： Allan R. Moorman , Michael Scannell , Thiagarajan Balasubramanian , Russell Outcalt , Edward Leung
IPC分类号： C07H19/167 , A61K31/70
CPC分类号： C07H19/16 , C07H19/167 , Y02P20/55
摘要： Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
摘要翻译： 提供了合成芳烷氧基腺苷或烷氧基腺苷的方法。 该方法包括用保护基保护羟基糖基团以产生被保护的卤代腺苷。 保护的卤代腺苷被烷氧基化，被保护的卤代腺苷的羟基糖基脱保护，得到芳烷氧基腺苷或烷氧基腺苷。
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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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![CRYSTAL FORMS OF 2-[2-(4-CHLOROPHENYL)ETHOXY]ADENOSINE](/abs-image/US/2010/12/23/US20100324279A1/abs.jpg.150x150.jpg)
公开(公告)号：US20100324279A1
公开(公告)日：2010-12-23
申请号：US12742768
申请日：2008-12-18
IPC分类号： C07H19/167
CPC分类号： C07H19/00 , C07H19/167
摘要： The present invention provides novel crystal forms of 2-[2-(4-chlorophenyl)ethoxy]adenosine of the formula processes for the production of such crystal forms, and methods for the manufacture of pharmaceutical compositions for the treatment of diseases or conditions modulated by the adenosine A2 receptors, in particular the A2A receptor, in a mammal in need thereof, by employing such crystal forms. The crystal forms of the present invention are especially useful in the preparation of topical compositions for accelerating wound healing, e.g., for the treatment of diabetic foot ulcers.
摘要翻译： 本发明提供了具有下列通式的2- [2-（4-氯苯基）乙氧基]腺苷的新型结晶形式：制备这种结晶形式的方法，以及制备用于治疗疾病或病症调节的疾病或病症的药物组合物的方法 腺苷A2受体，特别是A2A受体，在需要的哺乳动物中，通过使用这种晶体形式。 本发明的晶体形式特别可用于制备用于加速伤口愈合的局部组合物，例如用于治疗糖尿病足溃疡。
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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：US20130136693A1
公开(公告)日：2013-05-30
申请号：US13546595
申请日：2012-07-11
IPC分类号： C07H19/167 , A61K49/00 , A61K31/7076
CPC分类号： C07H19/167 , A61K31/7076 , A61K49/00
摘要： The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
摘要翻译： 本发明提供2-环己基亚甲基亚肼基腺苷的新型结晶多晶型物，也称为二十二碳烯酮，其制备方法，以及通过使用这种晶型制备药物组合物的方法，特别是用于将二十二碳烯酮用于 受试者，需要其作为产生冠状动脉血管扩张的药理学应激剂。
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公开(公告)号：US20110044904A1
公开(公告)日：2011-02-24
申请号：US12918213
申请日：2009-02-27
IPC分类号： A61K49/00 , C07H19/167 , A61K31/7076 , A61P27/02 , A61P9/10
CPC分类号： C07H19/167 , A61K31/7076 , A61K49/00
摘要： The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
摘要翻译： 本发明提供2-环己基亚甲基亚肼基腺苷的新型结晶多晶型物，也称为二十二碳烯酮，其制备方法，以及通过使用这种晶型制备药物组合物的方法，特别是用于将二十二碳烯酮用于 受试者，需要其作为产生冠状动脉血管扩张的药理学应激剂。
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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：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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