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AssigneeSyntex (U.S.A.) Inc.
InventorsDavid Morgans, Jr., David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, John C. Rohloff, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.
A compound of the formula:
A process for the synthesis of (E) 6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxoisobenzofuran-5-yl)-2,4-d imethyl-4-hexenoic acid comprising the 2-alkylation of a compound of claim 7 where Z.sup.3 and Z.sup.4 are H, using methyl iodide, followed by hydrolysis of the oxazolidinone moiety using LiOH, to give a mixture of 2-(R) and 2-(S) isomers of (E) 6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxoisobenzofuran-5-yl)-2,4-d imethyl-4-hexenoic acid.
Dependencies are inferred from the claim text.