Tetracyclic compounds for enhancing biosynthesis of erythropoietin, compositions containing same, and methods of use thereof

摘要

The present invention provides a compound in substantially pure form having the structure: wherein each of R1, R2, R3, R4, R5, R6, R7, and R8 may independently be hydrogen, halogen, nitro, CF3, hydroxy, C1-5 alkyl, aryl or OR9, wherein R9 is C1-5 alkyl, wherein R10 is COC1-5 alkyl; or wherein any two consecutive R groups may be members of a C5-C6membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R10 is present, the exocyclic-covalent bond is absent, and when R10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R10 is absent, R1, R2, R3, R4, R5, R6, R7, and R8 cannot all be hydrogen and when R10 is absent, R5, R6, R7, and R8 cannot all be hydrogen when either R1, R2, R3, or R4 is hydroxy, or R2 is carboethoxy. The present invention further provides a composition comprising the compound described above in an amount effective to modulate cellular expression of a mammalian gene encoding erythropoietin and a carrier.