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    • 6. 发明申请
    • SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS
    • 取代的氟化吡啶化合物
    • WO2010103547A2
    • 2010-09-16
    • PCT/IN2010/000145
    • 2010-03-12
    • ADVINUS THERAPEUTICS PRIVATE LIMITEDPALLE, VenkataRAMDAS, VidyaBARAWKAR, DineshBASU, SujayKOUL, SummonWAMAN, YogeshPATEL, MeenaPANMAND, Anil
    • PALLE, VenkataRAMDAS, VidyaBARAWKAR, DineshBASU, SujayKOUL, SummonWAMAN, YogeshPATEL, MeenaPANMAND, Anil
    • C07D473/30
    • C07D473/40A61K31/522A61K31/5377C07D473/06C07D473/18C07D473/30
    • The present invention discloses substituted fused pyrimidine compounds of formula I, their tautomers, polymorphs, stereoisomers, prodrugs, 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 present invention also provides provide the use of compounds of formula (II), or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, for the treatment of a pathological disease susceptible to improvement by antagonism of adenosine receptors. 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.
    • 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,前药,溶剂合物,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。 本发明还提供式(II)化合物或其互变异构体,多晶型物,立体异构体,前药,溶剂化物或其药学上可接受的盐在治疗易受腺苷受体拮抗作用改善的病理疾病中的用途。 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。
    • 7. 发明申请
    • PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS
    • 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
    • WO2012035548A1
    • 2012-03-22
    • PCT/IN2011/000620
    • 2011-09-09
    • ADVINUS THERAPEUTICS PRIVATE LIMITEDBARAWKAR, DineshBASU, SujayRAMDAS, VidyaPALLE, Venkata PoornapragnacharyuluWAMAN, YogeshPATEL, MeenaPANMAND, Anil
    • BARAWKAR, DineshBASU, SujayRAMDAS, VidyaPALLE, Venkata PoornapragnacharyuluWAMAN, YogeshPATEL, MeenaPANMAND, Anil
    • C07D473/30C07F9/02C07F9/06A61K31/522A61P11/06
    • A61K31/522A61K31/675A61K45/06C07D473/30C07F9/65616
    • 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. {Formulas should be inserted here} 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.
    • 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。 {这里应插入配方}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, 包括炎性肠病,镰状细胞病和/或自身免疫性疾病的炎症性胃肠道疾病。 以及它们用于治疗各种疾病状态的哺乳动物,例如胃肠道疾病,免疫学障碍,超敏反应性障碍,神经障碍以及由于细胞过度增殖和凋亡引起的心血管疾病等。 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。