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    • 6. 发明申请
    • 8-TRIAZOLYLXANTHINE DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS ADENOSINE RECEPTOR ANTAGONISTS
    • 8-三唑并噻吩衍生物,其生产方法及其用作腺苷受体拮抗剂
    • WO2012076974A1
    • 2012-06-14
    • PCT/IB2011/002987
    • 2011-12-08
    • LIFE & BRAIN GMBHMÜLLER, ChristaZIMMER, AndreasLABS, StefanieBUCHHOLZ, StephanieHINZ, Sonja
    • MÜLLER, ChristaZIMMER, AndreasLABS, StefanieBUCHHOLZ, StephanieHINZ, Sonja
    • C07D473/06C07D473/08C07D473/12A61K31/522A61P25/28
    • C07D473/08C07D473/12
    • The invention relates to derivatives of the general formulae (I) and (II) to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts or solvates or prodrugs which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as adenosine receptor antagonists, in particular for the treatment of neurodegenerative disorders, e.g. stroke, amylotrophic lateral sclerosis, dementia, Alzheimer's disease, Parkinson's disease, ischemia/reperfusion injury, inflammation, and/or neurological disorder. The blockade of adenosine receptors could also be useful for other indications regarding the metabolism, e.g. diabetic retinopathy, diabetes mellitus, hyperbaric oxygen - induced retinopathy and/or obesity. Applications could also be the treatment of allergic diseases and autoimmune diseases, including mast cell degranulation, asthma, bronchoconstriction, pulmonary fibrosis, inflammatory or obstructive airways disease and/or chronic obstructive pulmonary disease (COPD). In addition, they could be used to treat cancer. The diseases associated with adenosine receptors are also diabetes, diarrhea, inflammatory bowel disease and/or gastrointestinal tract disorders. Adenosine receptor antagonists could be effective for treating a hepatic disease or condition for reducing fat deposition in the liver or fibrosis of the liver. The use of compounds of general formulae I or II can be associated with many applications e.g., scleroderm arthritis, atherosclerosis, urticaria, myocardial infarction, myocardial reperfusion after ischemia, vasodilation, hypertension, hypersensitivity, myocardial ischemia, heart attack and/or retinopathy of prematurity.
    • 本发明涉及通式(I)和(II)的衍生物及其制备方法,含有所述化合物和/或可由其制备的生理上相容的盐或溶剂化物或前药的药物制剂以及药物 使用所述化合物,其盐或溶剂化物作为腺苷受体拮抗剂,特别是用于治疗神经变性疾病,例如 中风,肌萎缩性侧索硬化,痴呆,阿尔茨海默病,帕金森病,缺血/再灌注损伤,炎症和/或神经障碍。 腺苷受体的阻断也可用于其他有关代谢的适应症,例如, 糖尿病性视网膜病变,糖尿病,高压氧诱导的视网膜病变和/或肥胖。 应用还可以是治疗过敏性疾病和自身免疫性疾病,包括肥大细胞脱粒,哮喘,支气管收缩,肺纤维化,炎性或阻塞性气道疾病和/或慢性阻塞性肺疾病(COPD)。 此外,它们可以用于治疗癌症。 与腺苷受体相关的疾病也是糖尿病,腹泻,炎性肠病和/或胃肠道疾病。 腺苷受体拮抗剂可有效治疗肝脏疾病或病症,以减少肝脏中的脂肪沉积或肝纤维化。 使用通式I或II的化合物可与许多应用相关联,例如硬皮病关节炎,动脉粥样硬化,荨麻疹,心肌梗死,缺血后心肌再灌注,血管舒张,高血压,超敏反应,心肌缺血,心脏病发作和/或早产儿视网膜病变 。