Useful pro-drug forms of theophylline

Abstract

Abstract There is provided novel and useful pro-drug forms of theophylline having the formula: ##SPC1## Wherein R represents a member selected from the group consisting of a straight or branched C 4 -C 20 alkyl group, a straight or branched C 4 -C 20 alkenyl group, a substituted phenyl group of a substituted or unsubstituted naphthyl group whose substituents are selected from the group consisting of a hydroxy group, a C 1 -C 4 alkyl group, a C 1 -C 4 alkoxy group, a C 1 -C 4 acyloxy group, and a halogen atom (Cl, Br, I), and a substituted or unsubstituted heteroaromatic group whose substituents are selected from the group consisting of a hydroxy group, a C 1 -C 4 alkyl group, a C 1 -C 4 alkoxy group, a C 1 -C 4 acyloxy group, and a halogen atom (Cl, Br, I), and wherein A represents a member selected from the group consisting of a --CO-- group, a --CO--(CH 2 ) n --CO-- group, wherein n represents an integer of from 1 to 16, a --CO--CH=CH--CO-- group (cis or trans), a ##SPC2## Group, and a ##SPC3## Group. The compounds of this invention are useful in the treatment of asthma in warm-blooded animals. Upon administration, the compounds of this invention slowly go into solution and subsequently cleave prior to and/or during the absorption process, releasing theophylline in a sustained manner at a non-toxic, therapeutic level; that is, without the large blood level variations normally observed when theophylline per se is administered.

Inventors

• 👤 Takeru Higuchi
• 👤 Nicolae S. Bodor
• 👤 Yu-Neng Kuo

Bibliographic Details