Prodrug derivatives of carboxylic acid drugs
Patent 5073641 Issued on December 17, 1991. Estimated Expiration Date: 
December 17, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
December 17, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.InventorsApplicationNo. 188407 filed on 04/26/1988US Classes:560/56, Ortho fused rings in acid moiety548/500, Having -C(=X)-, wherein X is chalcogen, bonded directly to ring nitrogen of the five-membered hetero ring (e.g., indomethacin, etc.)549/494, Having -C(=X)-, wherein X is chalcogen, attached indirectly to the hetero ring by nonionic bonding560/39, Oxy in acid moiety560/49, Nitrogen in alcohol moiety560/105, Carboxyl, not bonded directly to a ring, in acid moiety560/153Nitrogen or halogen in acid moietyExaminersPrimary: Killos, Paul J.Attorney, Agent or FirmForeign Patent References
International ClassC07C 069/76Foreign Application Priority Data1986-08-26 DKAbstractNovel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R1 and R2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R1 and R2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution. The novel derivatives are less irritating to mucosa than the parent carboxylic acids and may provide an improved bio-availability of the drugs.Other References
Field of SearchOrtho fused rings in acid moietyOxy in acid moiety Nitrogen in alcohol moiety Carboxyl, not bonded directly to a ring, in acid moiety Nitrogen or halogen in acid moiety Having -C(=X)-, wherein X is chalcogen, bonded directly to ring nitrogen of the five-membered hetero ring (e.g., indomethacin, etc.) Having -C(=X)-, wherein X is chalcogen, attached indirectly to the hetero ring by nonionic bonding |
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