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Title: Stable pro-drug forms of theophylline

Abstract: There is provided exceptionally stable and useful pro-drug forms of theophylline having the formula: ##STR1## wherein R represents a straight or branched phenylalkenyl group having 2-8 carbon atoms in the alkenyl portion. 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: 732979
Filing Date: 1976-10-18
Publication_date: 1978-04-18
Assignee: INTERx Research Corporation (Lawrence, KS)
Primary Class(es): 514/263.36 544/267
Other Classes:
US Patent Ref:
2729643Jan, 1956Stoll et al.260/256.
3737433Jun, 1973Mohler et al.260/256.
3813394May, 1974Tensho et al.260/252.
3935196Jan, 1976Higuchi et al.260/240.

Other Refs:
Primary Examiner: Schenkman, Leonard
Assistant Examiner:
Attorney: Bacon & Thomas