Useful pro-drug forms of theophylline

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

1975-09-26

1977-01-11

Schenkman, Leonard

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

A61K 3152

Patent

active

040027562

ABSTRACT:
There is provided novel and useful pro-drug forms of theophylline having the formula: ##STR1## 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.14 -C.sub.20 alkenyl group, a substituted phenyl group or 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.14 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 presents a member selected from the group consistng of a --CO-- group, a --CO--(CH.sub.2).sub.n --C-- group, wherein n represents an integer of from 1 to 16, a --CO--CH=CH--CO-- group (cis or trans), ##STR2## AND A ##STR3## 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.
patent: 3935196 (1976-01-01), Higuchi et al.

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