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US4085214A Expired / Lapsed US ⏱️ 0.0 years remaining

Stable pro-drug forms of theophylline

Assignee: Interx Research Corp
•
Filing: 1976-10-18
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Granted: 1978-04-18
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Expires: 1996-10-18
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Abstract

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.

Inventors

  • 👤 Takeru Higuchi
  • 👤 Nicolae S. Bodor
  • 👤 Yu-Neng Kuo

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 08:41
CPC Classifications
C; C07; C07D; C07D473/00; C07D473/02; C07D473/04; C07D473/06; C07D473/08

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 24 words
A pro-theophylline compound of the formula: ##STR3## wherein R represents a straight or branched phenylalkenyl group having 2-8 carbon atoms in the alkenyl portion.
Claim 2
Dependent Claim 24 words
A pro-theophylline compound of the formula: ##STR3## wherein R represents a straight or branched phenylalkenyl group having 2-8 carbon atoms in the alkenyl portion.
Claim 3
Dependent Claim 6 words
The compound of claim 1: 7-(3-phenyl-propenoyl)-theophylline
Claim 4
Dependent Claim 6 words
The compound of claim 1: 7-(6-phenyl-hexen-2-oyl)-theophylline
Claim 5
Dependent Claim 6 words
The compound of claim 1: 7-(8-phenyl-octen-5-oyl)-theophylline
Claim 6
Dependent Claim 34 words
A method for inducing a non-toxic, sustained therapeuticcally effective release of theophylline in the bloodstream of a warm-blooded animal which comprises: orally administering thereto, a pharmaceutically effective amount of the compound of claim 1.
Claim 7
Dependent Claim 10 words
The method of claim 5, wherein said compound is: 7-(3-phenyl-propenoyl)-theophylline.
Claim 8
Dependent Claim 25 words
A pharmaceutical composition which comprises: (1) a pharmaceutically effective amount of the compound of claim 1 in combination with, (2) a pharmaceutically acceptable inert diluent.
Claim 9
Dependent Claim 10 words
A composition of claim 7, wherein said compound is: 7-(3-phenyl-propenoyl)-theophylline.

References Cited (Backward Citations)

US2729643A Cited
US3737433A Cited
US3737433B1 Cited
US3813394A Cited
US3935196A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-04-17 1981-10-17 1982-04-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-04-17 1985-10-17 1986-04-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-04-17 1989-10-17 1990-04-18 $7700.00 Window Closed / Lapsed

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