| 摘要 |
This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by the following formula:wherein: R4 is -NR1R2 or oxo; R5 is -CN, or -CSNR1R2, or -CONR1R2; R6 is -H, or halo, or -NR1R2; wherein R1 and R2 are independently -H or an aliphatic group; and R7 is of the formula R3-Ar, wherein R3 is an aliphatic group and Ar is an unsubstituted aryl or an aryl independently substituted with halo, nitro, amino, or aliphatic groups; provided that when R5 is a -CN or -CSNH2, and R6 is a -H or -NH2, and Ar is a -C6H5 or a phenyl substituted with only one aliphatic group, R3 is an aliphatic group other than methyl such that -R3- is not a -CH2-; and pharmaceutically acceptable salts, prodrugs and derivatives thereof. |
