PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS
    4.
    发明申请
    PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS 有权
    作为A2B腺苷受体拮抗剂的原料的嘌呤化合物,其方法和药物应用

    公开(公告)号:US20130172249A1

    公开(公告)日:2013-07-04

    申请号:US13821481

    申请日:2011-09-09

    摘要: The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases, and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

    摘要翻译: 本公开内容涉及式(I)或式(II)的嘌呤化合物或其互变异构体,多晶型物,立体异构体,溶剂合物或其药学上可接受的盐或含有它们的药物组合物以及将由其介导的病症和疾病作为治疗方法 A2B腺苷受体拮抗剂。 本公开的化合物可用于治疗,预防或抑制可能通过腺苷A2B受体的介导而改善的疾病和病症。 这些病症包括但不限于哮喘,慢性阻塞性肺病,血管发生,肺纤维化,肺气肿,过敏性疾病,炎症,再灌注损伤,心肌缺血,动脉粥样硬化,高血压,充血性心力衰竭,视网膜病变,糖尿病,肥胖症, 包括炎症性肠病,镰状细胞病和/或自身免疫性疾病在内的炎性胃肠道疾病,以及它们在治疗哺乳动物用于各种疾病状态的用途,例如胃肠疾病,免疫学障碍,超敏反应性障碍,神经障碍和心血管疾病 细胞过度增殖和细胞凋亡等。 本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

    Substituted fused pyrimidine compounds
    5.
    发明授权
    Substituted fused pyrimidine compounds 有权
    取代的稠合嘧啶化合物

    公开(公告)号:US08859566B2

    公开(公告)日:2014-10-14

    申请号:US13256071

    申请日:2010-03-12

    摘要: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.

    摘要翻译: 本发明公开了式(I)的取代的稠合嘧啶化合物,其互变异构体,多晶型物,立体异构体,溶剂化物,药学上可接受的盐或含有它们的药物组合物以及治疗由腺苷受体(AR)活性介导的病症和疾病的方法。 本发明的化合物可用于治疗,预防或抑制可能易受腺苷受体拮抗作用改善的疾病和病症,例如哮喘,慢性阻塞性肺病,血管生成,肺纤维化,肺气肿,过敏性疾病 ,炎症,再灌注损伤,心肌缺血,动脉粥样硬化,高血压,充血性心力衰竭,视网膜病变,糖尿病,肥胖,炎性胃肠道疾病和/或自身免疫性疾病。

    Fused tricyclic compounds as adenosine receptor antagonist
    9.
    发明授权
    Fused tricyclic compounds as adenosine receptor antagonist 有权
    融合三环化合物作为腺苷受体拮抗剂

    公开(公告)号:US09006177B2

    公开(公告)日:2015-04-14

    申请号:US13825665

    申请日:2011-09-22

    摘要: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor. Such conditions include, but are not limited to, Parkinsons disease, restless leg syndrome, Alzheimers disease, neurodegenerative disorder, inflammation, wound healing, dermal fibrosis, nocturnal myoclonus, cerebral ischaemia, myocardial ischemia, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease or other disorders of basal ganglia which results in dyskinesias, post traumatic stress disorder, hepatic cirrhosis, sepsis, spinal cord injury, retinopathy, hypertension, social memory impairment, depression, neuroprotection, narcolepsy or other sleep related disorders, attention deficit hyperactivity disorder, drug addiction, post traumatic stress disorder and vascular injury and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

    摘要翻译: 本公开内容涉及式(I)的稠合三环化合物或其互变异构体,多晶型物,立体异构体,前药,溶剂合物或药学上可接受的盐或含有它们的药物组合物和将其作为A2A腺苷介导的病症和疾病的方法 受体拮抗剂。 本公开的化合物可用于治疗,预防或抑制可能通过腺苷A2A受体介导而改善的疾病和病症。 这些病症包括但不限于:帕金森病,不宁腿综合征,阿尔茨海默病,神经变性疾病,炎症,伤口愈合,真皮纤维化,夜间肌阵挛,脑缺血,心肌缺血,亨廷顿舞蹈病,多系统萎缩,皮质基底变性, 威尔逊病或基底节神经节的其他疾病,导致运动障碍,创伤后应激障碍,肝硬化,败血症,脊髓损伤,视网膜病变,高血压,社会记忆障碍,抑郁,神经保护,发作性睡眠或其他睡眠相关疾病,注意缺陷多动障碍 ,药物成瘾,创伤后应激障碍和血管损伤等。 本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。