Useful pro-drug forms of theophylline

Details Useful pro-drug forms of theophylline Useful pro-drug forms of theophylline

1974-04-22

1976-01-27

Gallagher, R.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260256, 424253, C07D47308

Patent

active

039351963

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.

REFERENCES:
patent: 2729643 (1956-01-01), Stoll et al.

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