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Summary
Novelty: The use of known and new 7-(oxoalkyl)-1,3-dialkylxanthines as immunosuppressive agents is disclosed. These agents are potentially useful to suppress host-versus-graft reaction (HVGR) and graft-versus-host reaction (GVHR) in allograft transplantation; more specifically, these agents are claimed to be useful in ameliorating GVHR in bone marrow transplantation (BMT).
Biology: The immunosuppressive activity of the xanthines was demonstrated by inhibition of the mixed lymphocyte reaction (MLR) at concentrations of 1 mM of selected agents. The clinical usefulness of the agents was assessed in a small clinical trial of thirty people receiving allograft BMT; daily doses of 1200–2000 mg po were well tolerated and were shown to ameliorate some aspects of BMT graft toxicity (e.g. fever and infection).
Chemistry: Several multistep synthetic schemes are presented for preparation of the compounds. Several compounds are specifically claimed including the known vasodilatatory agent pentoxifylline (Merck Index 7092), 1-(5-oxohexyl)-3,7-dimethylxanthine). Interestingly, the use of the known growth factor GM-CSF is specifically claimed to inhibit allograft rejection.
Structure: