公开(公告)号：US20080125438A1

公开(公告)日：2008-05-29

申请号：US11938465

申请日：2007-11-12

申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

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。

公开(公告)号：US07101905B2

公开(公告)日：2006-09-05

申请号：US10112613

申请日：2002-03-29

申请人： Allan R. Moorman ,  Romeo Romagnoli ,  Pier Giovanni Baraldi

发明人： Allan R. Moorman ,  Romeo Romagnoli ,  Pier Giovanni Baraldi

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.

公开(公告)号：US20100324279A1

公开(公告)日：2010-12-23

申请号：US12742768

申请日：2008-12-18

申请人： Patricia M.J. Andres ,  Ron C. Kelly ,  Allan R. Moorman ,  Matthew Strange

发明人： Patricia M.J. Andres ,  Ron C. Kelly ,  Allan R. Moorman ,  Matthew Strange

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。

公开(公告)号：US20130136693A1

公开(公告)日：2013-05-30

申请号：US13546595

申请日：2012-07-11

申请人： Allan R. Moorman ,  Michael H. O'Neal

发明人： Allan R. Moorman ,  Michael H. O'Neal

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。

公开(公告)号：US20110044904A1

公开(公告)日：2011-02-24

申请号：US12918213

申请日：2009-02-27

申请人： Allan R. Moorman ,  Michael H. O'Neill

发明人： Allan R. Moorman ,  Michael H. O'Neill

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。

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。

公开(公告)号：US07723343B2

公开(公告)日：2010-05-25

申请号：US12056423

申请日：2008-03-27

申请人： Allan R. Moorman

发明人： Allan R. Moorman

IPC分类号： A61K31/505 ,  C07D491/00

CPC分类号： C07D487/14

摘要： The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g., dystonia, akathisia, pseudoparkinsonism and tardive dyskinesia, and disorders of abnormal movement such as restless leg syndrome (RLS) and periodic limb movement in sleep (PLMS); cirrhosis, and fibrosis and fatty liver; dermal fibrosis in diseases such as scleroderma; and the mitigation of addictive behavior. In particular, the compounds of the present invention may be employed to improve motor-impairment due to neurodegenerative diseases such as Parkinson's disease.

摘要翻译： 本发明提供下式的化合物，其中R 1和R 2具有本说明书中定义的含义。 式（I）化合物是腺苷A 2A受体拮抗剂，因此可用于治疗由腺苷A 2A受体活性介导的病症和疾病。 这些病症包括但不限于中枢神经系统疾病如抑郁症，认知功能疾病和神经变性疾病如帕金森氏病，老年痴呆症如阿尔茨海默病或精神病和中风。 本发明的化合物还可用于治疗注意力相关疾病如注意力缺陷障碍（ADD）和注意缺陷多动障碍（ADHD），额外的锥体综合征，例如肌张力障碍，厌食症，假性帕金森综合征和迟发性运动障碍，以及 异常运动障碍，如不宁腿综合征（RLS）和睡眠周期性肢体运动（PLMS）; 肝硬化，纤维化和脂肪肝; 皮肤纤维化等疾病如硬皮病; 并减轻上瘾行为。 特别地，本发明的化合物可用于改善由于神经变性疾病如帕金森病引起的运动障碍。

公开(公告)号：US20080242673A1

公开(公告)日：2008-10-02

申请号：US12056423

申请日：2008-03-27

申请人： Allan R. Moorman

发明人： Allan R. Moorman

IPC分类号： A61K31/519 ,  C07D487/14 ,  A61P25/00

CPC分类号： C07D487/14

摘要： The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g., dystonia, akathisia, pseudoparkinsonism and tardive dyskinesia, and disorders of abnormal movement such as restless leg syndrome (RLS) and periodic limb movement in sleep (PLMS); cirrhosis, and fibrosis and fatty liver; dermal fibrosis in diseases such as scleroderma; and the mitigation of addictive behavior. In particular, the compounds of the present invention may be employed to improve motor-impairment due to neurodegenerative diseases such as Parkinson's disease.

公开(公告)号：US20080242672A1

公开(公告)日：2008-10-02

申请号：US12056403

申请日：2008-03-27

申请人： Allan R. Moorman

发明人： Allan R. Moorman

IPC分类号： A61K31/496 ,  C07D487/14 ,  A61P25/24 ,  A61P25/16 ,  A61P25/28 ,  A61K31/519

CPC分类号： C07D487/14

摘要： The present invention provides compounds of the formula wherein R1 and R2 have meaning as defined herein in the specification. The compounds of formula (I) are adenosine A2A receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2A receptor activity. Such conditions include, but are not limited to, diseases of the central nervous system such as depression, cognitive function diseases and neurodegenerative diseases such as Parkinson's disease, senile dementia as in Alzheimer's disease or psychoses and stroke. The compounds of the present invention may also be employed for the treatment of attention related disorders such as attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD), extra pyramidal syndrome, e.g., dystonia, akathisia, pseudoparkinsonism and tardive dyskinesia, and disorders of abnormal movement such as restless leg syndrome (RLS) and periodic limb movement in sleep (PLMS); cirrhosis, and fibrosis and fatty liver; dermal fibrosis in diseases such as scleroderma; and the mitigation of addictive behavior. In particular, the compounds of the present invention may be employed to improve motor-impairment due to neurodegenerative diseases such as Parkinson's disease.

摘要翻译： 本发明提供下式的化合物，其中R 1和R 2 2具有如本说明书中定义的含义。 式（I）化合物是腺苷A 2A 2受体拮抗剂，因此可用于治疗由腺苷A 2A受体活性介导的病症和疾病。 这些病症包括但不限于中枢神经系统疾病如抑郁症，认知功能疾病和神经变性疾病如帕金森氏病，老年痴呆症如阿尔茨海默病或精神病和中风。 本发明的化合物还可用于治疗注意力相关疾病如注意力缺陷障碍（ADD）和注意缺陷多动障碍（ADHD），额外的锥体综合征，例如肌张力障碍，厌食症，假性帕金森综合征和迟发性运动障碍，以及 异常运动障碍，如不宁腿综合征（RLS）和睡眠周期性肢体运动（PLMS）; 肝硬化，纤维化和脂肪肝; 皮肤纤维化等疾病如硬皮病; 并减轻上瘾行为。 特别地，本发明的化合物可用于改善由于神经变性疾病如帕金森病引起的运动障碍。

公开(公告)号：US06951932B2

公开(公告)日：2005-10-04

申请号：US10281291

申请日：2002-10-24

申请人： Allan R. Moorman

发明人： Allan R. Moorman

IPC分类号： C07H19/167 ,  C07H19/16 ,  C07H19/173

CPC分类号： C07H19/167 ,  C07H19/16 ,  C07H19/173

摘要： The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.

摘要翻译： 本发明提供了合成2-芳烷氧基腺嘌呤和2-烷氧基腺苷的新方法。 本发明特别可用于2- [2-（4-氯苯基）乙氧基]腺苷的合成。 本发明的优选方法包括活化鸟苷化合物，然后水解; 将水解的化合物进行烷基化，随后进行动画以提供2-芳烷氧基腺苷或2-烷氧基腺苷化合物。