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2-Styryl-4H-pyrido(1,2-a)pyrimidin-4-ones Process for the preparation of the cephalosporanic acid derivative Iminomethylindolines N,N-disubstituted 2,1,3-benzothiadiazin-(4)-one-2,2-dioxide Production of 2,1,3-benzothiadiazin-4-one-2,2-dioxides Derivatives of 3-oxo-2,3-dihydro-1,4-benzoxazine Cephalosporin and pharmaceutical preparations containing the same Dimorpholinomethyl-(4-methyl-3-pentenyl)-cyclohexenenes Sulfosuccinate derivatives as detergent builders Conjugate addition
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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:
| 2729643 | Jan, 1956 | Stoll et al. | 260/256. |
Other Refs:
Primary Examiner:
Gallagher, R.
Assistant Examiner:
Tighe, Anne Marie T.
Attorney:
McDonnell; John J.
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