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Method of inhibiting aggregation using thromboxane synthetase inhibitor in combination with a cyclic AMP phosphodiesterase inhibitor

Assignee: Thomas Jefferson University
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Filing: 1984-08-10
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Granted: 1986-02-04
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Expires: 2004-08-10
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Abstract

Abstract A novel method of inhibiting blood platelet aggregation is disclosed which comprises the use of a CAMP inhibitor together with an inhibitor of thromboxane synthesis. While inhibitors of thromboxane synthesis are only weak inhibitors of platelet aggregation, the addition of only a small amount of a CAMP inhibitor has been found to result in a synergistic increase in the degree of platelet aggregation resulting from such combined additions. Marked increases over the otherwise expected culumative effects of these inhibitors have been demonstrated using combination of various thromboxane synthetase inhibitors and various CAMP inhibitors.

Inventors

  • 👤 J. Bryan Smith

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 17:04
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K31/495; A61K31/505; A61K31/519; A61K31/52

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 75 words
A method for inhibiting blood platelet aggregation comprising administering to an individual disposed toward undesirable blood platelet aggregation a combination of amounts of a thromboxane synthetase inhibitor and an inhibitor of cyclic AMP phosphodiesterase which together are effective to inhibit blood platelet aggregation in said individual, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination.
Claim 2
Independent Claim 75 words
A method for inhibiting blood platelet aggregation comprising administering to an individual disposed toward undesirable blood platelet aggregation a combination of amounts of a thromboxane synthetase inhibitor and an inhibitor of cyclic AMP phosphodiesterase which together are effective to inhibit blood platelet aggregation in said individual, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination.
Claim 3
Dependent Claim 13 words
A method according to claim 1 wherein the mode of administration is oral.
Claim 4
Dependent Claim 13 words
A method according to claim 1 wherein the mode of administration is parenteral.
Claim 5
Dependent Claim 18 words
A method for inhibiting platelet aggregation in accordance with claim 1 wherein said thromboxane synthetase inhibitor is imidazole.
Claim 6
Dependent Claim 14 words
The method of claim 1 wherein said thromboxane synthetase inhibitor is an imidazole derivative.
Claim 7
Dependent Claim 12 words
The method of claim 1 wherein said thromboxane synthetase inhibitor is pyridine.
Claim 8
Dependent Claim 14 words
The method of claim 1 wherein said thromboxane synthetase inhibitor is a pyridine derivative.
Claim 9
Dependent Claim 13 words
The method of claim 1 wherein said inhibitor cyclic AMP phosphodiesterase is quinazolinone.
Claim 10
Dependent Claim 16 words
The method of claim 1 wherein said inhibitor of cyclic AMP phosphodiesterase is a quinazolinone derivative.
Claim 11
Dependent Claim 16 words
The method of claim 1 wherein said inhibitor of cyclic AMP phosphodiesterase is a pyrimido-pyrimidine derivative.
Claim 12
Dependent Claim 14 words
The method of claim 1 wherein said inhibitor of cycli AMP phosphodiesterase is papaverine.
Claim 13
Dependent Claim 16 words
The method of claim 1 wherein said inhibitor of cyclic AMP phosphodiesterase is a methyl xanthine.
Claim 14
Dependent Claim 49 words
The method of claim 1 wherein the combined amounts of said inhibitors are administered to achieve a preselected degree of aggregation inhibition and are less than the combined amounts of said inhibitors which would be predicted as necessary to achieve said degree of inhibition based upon their individual activities.
Claim 15
Independent Claim 106 words
A method of reducing the dosage of a thromboxane synthetase inhibitor needed to achieve a desired degree of platelet aggregation inhibition in an individual, comprising the step of administering a lowered dose of said inhibitor in combination with an amount of cyclic AMP phosphodiesterase inhibitor which is effective in combination with said thromboxane synthetase inhibitor to achieve said desired degree of inhibition, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination, whereby the likelihood of causing undesirable side effects in said individual is said substantially reduced.
Claim 16
Independent Claim 106 words
A method of reducing the dosage of a thromboxane synthetase inhibitor needed to achieve a desired degree of platelet aggregation inhibition in an individual, comprising the step of administering a lowered dose of said inhibitor in combination with an amount of cyclic AMP phosphodiesterase inhibitor which is effective in combination with said thromboxane synthetase inhibitor to achieve said desired degree of inhibition, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination, whereby the likelihood of causing undesirable side effects in said individual is said substantially reduced.
Claim 17
Independent Claim 110 words
A method of reducing the dosage of a cyclic AMP phosphodiesterase inhibitor needed to achieve a desired degree of platelet aggregation inhibition in an individual, comprising the step of administering a lowered dose of said cyclic AMP phosphodiesterase inhibitor in combination with an amount of a thromboxane synthetase inhibitor which is effective in combination with said cyclic AMP phosphodiesterase inhibitor to achieve said desired degree of inhibition, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination, whereby the likelihood of causing undesirable side effects in said individual is substantially reduced.
Claim 18
Independent Claim 110 words
A method of reducing the dosage of a cyclic AMP phosphodiesterase inhibitor needed to achieve a desired degree of platelet aggregation inhibition in an individual, comprising the step of administering a lowered dose of said cyclic AMP phosphodiesterase inhibitor in combination with an amount of a thromboxane synthetase inhibitor which is effective in combination with said cyclic AMP phosphodiesterase inhibitor to achieve said desired degree of inhibition, said thromboxane synthetase inhibitor when tested alone in vitro producing a degree of blood platelet aggregation inhibition which is a minor proportion of the degree achieved by said combination, whereby the likelihood of causing undesirable side effects in said individual is substantially reduced.

References Cited (Backward Citations)

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-02-03 1989-08-05 1990-02-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-02-03 1993-08-05 1994-02-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-02-03 1997-08-05 1998-02-04 $7700.00 Window Closed / Lapsed

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