Tetracyclic compounds for enhancing biosynthesis of erythropoiet

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549275, 549279, A61K 3135, A61K 31365, C07D31178

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active

059859130

ABSTRACT:
The present invention provides a compound in substantially pure form having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 may independently be hydrogen, halogen, nitro, CF.sub.3, hydroxy, C.sub.1-5 alkyl, aryl or OR.sub.9, wherein R.sub.9 is C.sub.1-5 alkyl, wherein R.sub.10 is COC.sub.1-5 alkyl; or wherein any two consecutive R groups may be members of a C.sub.5 -C.sub.6 membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R.sub.10 is present, the exocyclic-covalent bond is absent, and when R.sub.10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R.sub.10 is absent, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen and when R.sub.10 is absent, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen when either R.sub.1, R.sub.2, R.sub.3, or R.sub.4 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.

REFERENCES:
patent: 5107032 (1992-04-01), Erb et al.
Omar Farooq (1994) "Oxidation of Aromatic 1,2-Dimethanols by Activated Dimethyl Sulfoxide," Synthesis, pp. 1035-1036 (Exhibit 3).
Whitehouse M. W. and Leader J. E. (1966) "Biochemical Properties of Anti-Inflammatory Drugs-IX," Biochemical Pharmacologyvol. 16, pp. 537-551 (Exhibit 4).

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