Title: Useful pro-drug forms of theophylline

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Claims: What we claim is:

1. A pro-drug of theophylline having the formula ##SPC7##

wherein R represents a member selected from the group consisting of straight or branched C.sub.4 -C.sub.20 alkyl, straight or branched C.sub.4 -C.sub.20 alkenyl, substituted phenyl or substituted or unsubstituted naphthyl whose substituents are selected from the group consisting of hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acyloxy derived from an alkanoic acid of up to 4 carbon atoms chlorine, bromine, and iodine, and 2-,3-,4-pyridyl or quinoline and wherein A represents a member selected from the group consisting of --CO--, --CO--(CH.sub.2).sub.n --CO-- wherein n represents an integer of from 1 to 16, --CO--CH=CH-- CO-(cis or trans), ##SPC8##

and ##SPC9##

2. The compound of claim 1 wherein R represents an odd numbered alkyl of from C-7 to C-20.

3. The compound of claim 1 wherein R represents oleyl.

4. The compound of claim 1 wherein R represents phenyl substituted in the 4-position with hydroxy or C.sub.1 -C.sub.4 alkoxy, 2-hydroxyphenyl, or 2-acyloxyphenyl wherein the acyloxy is derived from an alkanoic acid of up to 4 carbon atoms.

5. The compound of claim 1 wherein A represents --CO--(CH.sub.2).sub.n --CO-- in which n is an integer of from 1-4.

6. The compound of claim 1 wherein A represents trans --CO--CH=CH--CO--.

7. The compound of claim 1: 7-hexanoyltheophylline.

8. The compound of claim 1: 7-octanoyltheophylline.

9. The compound of claim 1: 7-decanoyltheophylline.

10. The compound of claim 1: 7-dodecanoyltheophylline.

11. The compound of claim 1: 7-myristyltheophylline.

12. The compound of claim 1: 7-palmityltheophylline.

13. The compound of claim 1: 7-stearyltheophylline.

14. The compound of claim 1: 7-[2-hydroxy]-benzoyltheophylline.

15. The compound of claim 1: 7-[2-acetyloxy]-benzoyltheophylline.

16. The compound of claim 1: 7,7'-carbonylditheophylline.

17. The compound of claim 1: 7,7'-succinylditheophylline.

18. . The compound of claim 1: 7,7'-terephthaloylditheophylline.

19. The compound of claim 1: 7,7'-fumaroylditheophylline.

20. The compound of claim 1: 7,7'-glutarylditheophylline.

21. The compound of claim 1: 7,7'-adipyldilheophylline.

Other info:

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:

2729643

Jan, 1956

Stoll et al.

260/256.

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