首页> 外国专利> SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME

SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME

机译:质子耦合的叶酸转运蛋白和叶酸受体,以及加夫他汀和/或其他叶酸代谢酶抑制剂的化合物及其使用方法

摘要

Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula II: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
机译:公开了具有通式II的稠合的环状嘧啶化合物,包括其互变异构体及其药学上可接受的盐,前药,溶剂化物和水合物:这些化合物可用于治疗癌症的方法,通过质子偶联的叶酸转运蛋白选择性靶向癌细胞,叶酸受体α和/或叶酸受体β途径,抑制癌细胞中的GARFTase和/或其他叶酸代谢酶,并选择性靶向具有自身免疫性疾病(例如类风湿性关节炎)的患者的活化巨噬细胞。

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