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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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2.发明授权Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity 失效吡咯并三唑并嘧啶衍生物，含有它们的药物组合物和治疗由腺苷A2A受体活性介导的病症和疾病的方法公开(公告)号：US07691869B2
公开(公告)日：2010-04-06
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： A61K31/505 , 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。
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公开(公告)号：US07271171B2
公开(公告)日：2007-09-18
申请号：US11169311
申请日：2005-06-27
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D457/00 , C07D491/00
CPC分类号： A61K49/0052 , A61K31/519 , A61K49/0021 , A61K51/0459 , A61K51/0491 , C07B2200/05 , C07D471/14 , C07D487/14 , G01N33/57492 , G01N2333/726 , G01N2500/00
摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.
摘要翻译： 下式的化合物：其中R，R 2，R 3和A具有说明书中给出的含义，赋予选择性A 3， 腺苷受体拮抗剂活性。 这些化合物可用于药物组合物中以治疗由过度活化的Aβ受体引起的疾病，或可用于诊断应用以确定其它化合物与A
3受体。 化合物可以被标记，例如用荧光或放射性标记，以及在体内或体外用于确定具有高浓度腺苷A 3受体的肿瘤细胞的存在的标记。 -
公开(公告)号：US07767685B2
公开(公告)日：2010-08-03
申请号：US11767575
申请日：2007-06-25
IPC分类号： C07D473/06 , A61K31/522 , C07D231/14 , A61P11/06 , A61P3/10 , A61P19/02 , A61P37/08
CPC分类号： C07D473/06 , C07D473/08
摘要： The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g., retinopathy of prematurity, macular degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack.
摘要翻译： 本发明提供了具有腺苷A2B受体拮抗剂的下式的化合物，因此可用于治疗由腺苷A2B受体活性介导的病症和疾病。 这些病症包括但不限于涉及肥大细胞脱颗粒的慢性和急性炎性疾病，例如哮喘，过敏性鼻炎和过敏性皮炎; 对胰岛素的敏感性降低，例如2型糖尿病，糖尿病前期状态和葡萄糖耐量异常; 血管发生是发病机理的关键组分的疾病，例如实体瘤和血管生成视网膜病变; 早产儿呼吸暂停; 心肌再灌注损伤; 炎症性肠病; 自身免疫性疾病，例如类风湿性关节炎，多发性硬化症和狼疮性红斑狼疮; 涉及由腺苷A2B受体介导的视网膜的微血管异常的疾病，例如早产儿视网膜病变，黄斑变性和糖尿病性视网膜病变; 心脏病，包括高血压，动脉硬化和心脏病发作的增生。
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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。
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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：US07335655B2
公开(公告)日：2008-02-26
申请号：US11359661
申请日：2006-02-22
IPC分类号： C07D473/06 , C07D473/08 , A61K31/522 , A61P11/06 , A61P19/02
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , Y10S436/804
摘要： The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.
摘要翻译： 本发明一般涉及式（I）的化合物：其中X是含有一至四个选自氮，氧或硫的杂原子的五元或六元杂芳环，条件是至少一个杂原子是氮; 和G 1和G 2独立地是CH或N.本发明还涉及化合物，其药物制剂及其在药物中作为有效的或 选择性Aβ2A腺苷受体拮抗剂及其用于治疗哮喘，自身免疫性疾病和视网膜血管疾病的用途。
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公开(公告)号：US07470698B2
公开(公告)日：2008-12-30
申请号：US11774784
申请日：2007-07-09
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： A61K49/0052 , A61K31/519 , A61K49/0021 , A61K51/0459 , A61K51/0491 , C07B2200/05 , C07D471/14 , C07D487/14 , G01N33/57492 , G01N2333/726 , G01N2500/00
摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.
摘要翻译： 下式的化合物：其中R，R2，R3和A具有说明书中给出的含义，具有选择性的A3腺苷受体拮抗剂活性。 这些化合物可用于药物组合物中以治疗由A3受体的过度活化引起的疾病，或可用于诊断应用以确定其它化合物与A3受体的相对结合。 化合物可以用例如荧光或放射性标记物标记，以及在体内或体外用于测定具有高浓度腺苷A3受体的肿瘤细胞的存在的标记物。
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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：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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