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    • 8. 发明公开
    • 7-AMINO-2-ALKYLTHIOPTERIDIN-4-YL-AMINES FOR THE TREATMENT OF CHEMOKINE-RELATED DISEASES
    • 用于治疗与趋化因子有关的疾病的7-氨基-2-烷基哌啶-4-基 - 胺
    • EP1328319A1
    • 2003-07-23
    • EP01977001.5
    • 2001-10-16
    • AstraZeneca AB
    • BONNERT, RogerWALTERS, Iain
    • A61P17/06A61P29/00
    • C07D475/06
    • Pteridine compounds of formula (I) in which R?1, R2, R3 and R4¿ are as specified in the claims, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in the treatment of inflammatory diseases such as psoriasis, rheumatoid arthritis, diseases in which angiogenesis is assocated with raised CXCR2 chemokine levels (diabetic retinopathy) and COPD. The compounds are ligands for chemokine receptors and medical indications mentioned in the description include: diseases of the respiratory tract (COPDD, asthma, bronchitis, rhinitis, fibroid lung, pneumonia, etc.), diseases of the bones and joints (arthritis, etc.), skin-diseases (psoriasis, etc), diseases of the gastrointestinal tract, diseases in other tissues and systemic disease (multipe sclerosis, atherosclerosis, AIDS, type 1 diabetes, leprosy, sepsis, etc.), allograft rejection, cancers, cystic fibrosis, stroke, burn wounds, skin ulcers, reproductive disease and more.
    • 其中R 1,R 2,R 3和R 4如权利要求中所述的式(I)的蝶啶化合物,其制备中使用的方法和中间体,含有它们的药物组合物以及它们在治疗炎性疾病例如牛皮癣 ,类风湿性关节炎,其中血管发生与升高的CXCR2趋化因子水平(糖尿病视网膜病变)和COPD相关的疾病。 该化合物是趋化因子受体的配体,说明书中提及的医学适应症包括:呼吸道疾病(COPDD,哮喘,支气管炎,鼻炎,纤维性肺,肺炎等),骨骼和关节疾病(关节炎等) ),皮肤疾病(牛皮癣等),胃肠道疾病,其他组织中的疾病和全身性疾病(多发性硬化,动脉粥样硬化,艾滋病,1型糖尿病,麻风病,败血症等),同种异体移植排斥,癌症, 纤维化,中风,烧伤,皮肤溃疡,生殖系统疾病等等。