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Title: Useful pro-drug forms of theophylline

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.sub.4 -C.sub.20 alkyl group, a straight or branched C.sub.4 -C.sub.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.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.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.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.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.sub.2).sub.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.


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Inventors: Higuchi, Takeru (Lawrence, KS, US)
Bodor, Nicolae S. (Lawrence, KS, US)
Kuo, Yu-Neng (Lawrence, KS, US)

Application Number: 463092
Filing Date: 1974-04-22
Publication_date: 1976-01-27
Assignee: Interx Research Corporation (Lawrence, KS)
Primary Class(es): 544/271 514/826, 544/268, 544/269
Other Classes:
US Patent Ref:
2729643Jan, 1956Stoll et al.260/256.

Other Refs:
Primary Examiner: Gallagher, R.
Assistant Examiner: Tighe, Anne Marie T.
Attorney: McDonnell; John J.