Patent US4751224A successfully refreshed from Google Patents.
US4751224A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Treatment of metastasis
Assignee: Brown University Research Foundation Inc
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Filing: 1986-01-21
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Granted: 1988-06-14
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Expires: 2006-01-21
Abstract
Abstract A method for reducing the incidence of metastasis in tumor victims without treating the primary tumor per se resides in the administration of forskolin or its analogs which are potent inhibitors of platelet aggregation. Forskolin compounds are generally defined as labdane diterpenoids having the general formula: ##STR1## These compounds may be administered alone or in combination with other inhibitors of platelet aggregation.
Inventors
- 👤 Kailash C. Agarwal
- 👤 Robert E. Parks, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 13:10
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/35
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
131 words
A method for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor, the method comprising: administering a forskolin compound to said human or animal in amount effective to inhibit metastatic tumor cell-platelet interactions, the compound having the formula: ##STR4## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen.
Claim 2
Independent Claim
131 words
A method for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor, the method comprising: administering a forskolin compound to said human or animal in amount effective to inhibit metastatic tumor cell-platelet interactions, the compound having the formula: ##STR4## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen.
Claim 3
Dependent Claim
13 words
The method of claim 1 wherein the forskolin compound has the formula: ##STR5##
Claim 4
Dependent Claim
54 words
The method of claim 1 wherein the method further includes administering to said human or animal suffering from a tumor in conjunction with said forskolin compound a nucleoside transport inhibitor selected from the group consisting of p-nitrobenzylthionosine, dilazep, dipyridamole, oxagrelate and papaverine in an amount effective to retard adenosine uptake by red blood cells.
Claim 5
Dependent Claim
56 words
The method of claim 1 wherein the method further includes administering to said human or animal suffering from a tumor in conjunction with said forskolin compound a cAMP-blocking agent selected from the group consisting of theophylline, dipyridamole, oxagrelate and papaverine in an amount effective to block the action of cAMP phosphodiesterase in converting cAMP to AMP.
Claim 6
Dependent Claim
53 words
The method of claim 1 wherein the method further includes administering to said human or animal suffering from a tumor in conjunction with said forskolin compound as adenylate cyclase stimulating agent selected from the group consisting of prostaglandin E, N 6 -phenyladenosine and 2-fluoroadenosine in an amount effective to stimulate membrane adenylate cyclase.
Claim 7
Dependent Claim
147 words
A pharmaceutical composition for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor, the composition comprising an effective amount of forskolin compound having the formula ##STR6## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, carbonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen, and a nucleoside transport inhibitor selected from the group consisting of p-nitrobenzylthionosine, dilazep, dipyridamole, oxagrelate and papervine in an amount effective to retard adenosine uptake by red blood cells.
Claim 8
Dependent Claim
147 words
A pharmaceutical composition for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor, the composition comprising an effective amount of forskolin compound having the formula ##STR6## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, carbonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen, and a nucleoside transport inhibitor selected from the group consisting of p-nitrobenzylthionosine, dilazep, dipyridamole, oxagrelate and papervine in an amount effective to retard adenosine uptake by red blood cells.
Claim 9
Dependent Claim
14 words
The composition of claim 6 wherein the forskolin compound has the following formula: ##STR7##
Claim 10
Dependent Claim
150 words
A pharmaceutical composition for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor the composition comprising an effective amount of a forskolin compound having the formula: ##STR8## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen, and a cAMP-blocking agent selected from the group consisting of theophylline, dipyridamole, oxagrelate and papaverine in an amount effective to block the action of cAMP phosphodiesterase in converting cAMP to AMP.
Claim 11
Dependent Claim
150 words
A pharmaceutical composition for preventing metastatic disease in a human or animal suffering from a tumor without treating the primary tumor the composition comprising an effective amount of a forskolin compound having the formula: ##STR8## where R 1 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 2 is a hydroxy, carbonate, acetyl, or acetoxy or lower alkanoyl group; where R 3 is a hydroxy, carbonate, acetyl or acetoxy or lower alkanoyl or tosyl group; where R 4 is hydrogen or a hydroxy or lower alkoxy, sulfonate or carbonate group; where R 5 is either double-bonded oxygen or separately bound hydrogen and hydroxy groups; and where R 6 is a lower alkene or oxygen, and a cAMP-blocking agent selected from the group consisting of theophylline, dipyridamole, oxagrelate and papaverine in an amount effective to block the action of cAMP phosphodiesterase in converting cAMP to AMP.
Claim 12
Dependent Claim
11 words
The composition of claim 8 wherein the cAMP-blocking agent is oxagrelate.
Claim 13
Dependent Claim
14 words
The composition of claim 8 wherein the forskolin compound has the following formula: ##STR9##
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-06-14 | 1991-12-14 | 1992-06-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-06-14 | 1995-12-14 | 1996-06-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-06-14 | 1999-12-14 | 2000-06-14 | $7700.00 | Window Closed / Lapsed |