US4148879A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Inhibition of platelet aggregation with selected phosphonic and phosphinic acid esters
Assignee: Whitby Research Inc
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Filing: 1977-12-23
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Granted: 1979-04-10
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Expires: 1997-12-23
Abstract
Abstract A process for inhibiting platelet aggregation or thrombus formation by the addition of a member selected from the group consisting of a compound of the formula: ##STR1## WHEREIN X is an alkyl or alkenyl chain having 2-8 carbon atoms, one of which carbon atoms may be in the form of a carbonyl group, Y is H, alkyl, dialkylaminoethyl, aryl, aralkyl or aryl and aralkyl substituted with one or more R, and R is H, lower alkyl, lower alkoxy, halogen, CF 3 , NO 2 , OH, CN, COOR 1 , ##STR2## NHCOR 1 , NR 1 R 2 or ##STR3## where R 1 and R 2 are each selected from the group consisting of H and lower alkyl; R, R 1 and R 2 being the same or different, T is selected from the group consisting of O, NH, S and CH 2 with the proviso that only one T is O, Z is 0 or 1 and n is 0-5; and pharmaceutically acceptable salts thereof, to in vivo and in vitro platelet systems.
Inventors
- 👤 Eric L. Nelson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 15:48
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/66; A61K31/683; A61K31/685
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
171 words
A process for inhibiting platelet aggregation in in vitro platelet systems comprising the addition of an effective amount of a compound of the formula: ##STR7## wherein X is an alkyl or alkenyl chain having 2-8 carbon atoms, one of which carbon atoms may be in the form of a carbonyl group, Y is H, alkyl, dialkylaminoethyl, aryl, aralkyl or aryl and aralkyl substituted with one or more R, and R is H, lower alkyl, lower alkoxy, halogen, CF 3 , NO 2 , OH, CN, COOR 1 , ##STR8## NHCOR 1 , NR 1 R 2 or ##STR9## where R 1 and R 2 are each selected from the group consisting of H and lower alkyl; R, R 1 and R 2 being the same or different, T is selected from the group consisting of O, N, H, S and CH 2 , with the proviso that only one T is 0; Z is 0 or 1 and n is 0-5; and pharmaceutically acceptable salts thereof, to in vitro platelet systems.
Claim 2
Dependent Claim
171 words
A process for inhibiting platelet aggregation in in vitro platelet systems comprising the addition of an effective amount of a compound of the formula: ##STR7## wherein X is an alkyl or alkenyl chain having 2-8 carbon atoms, one of which carbon atoms may be in the form of a carbonyl group, Y is H, alkyl, dialkylaminoethyl, aryl, aralkyl or aryl and aralkyl substituted with one or more R, and R is H, lower alkyl, lower alkoxy, halogen, CF 3 , NO 2 , OH, CN, COOR 1 , ##STR8## NHCOR 1 , NR 1 R 2 or ##STR9## where R 1 and R 2 are each selected from the group consisting of H and lower alkyl; R, R 1 and R 2 being the same or different, T is selected from the group consisting of O, N, H, S and CH 2 , with the proviso that only one T is 0; Z is 0 or 1 and n is 0-5; and pharmaceutically acceptable salts thereof, to in vitro platelet systems.
Claim 3
Dependent Claim
24 words
The process of claim 1 wherein the amount of the compound added is from about 0.01 to 50 micrograms per ml of whole blood.
Claim 4
Dependent Claim
25 words
The process of claim 1 wherein the compound added is selected from the group consisting of p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenylpropyl] phenyl phosphonic acid and pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
172 words
A process of prophylactic treatment to prevent clot formation in humans and animals comprising the administration to a human or animal of an effective amount of a compound of the formula: ##STR10## wherein X is an alkyl or alkenyl chain having 2-8 carbon atoms, one of which carbon atoms may be in the form of a carbonyl group, Y is H, alkyl, dialkylaminoethyl, aryl, aralkyl or aryl and aralkyl substituted with one or more R, and R is H, lower alkyl, lower alkoxy, halogen, CF 3 , NO 2 , OH, CN, COOR 1 , ##STR11## NHCOR 1 , NR 1 R 2 or ##STR12## where R 1 and R 2 are each selected from the group consisting of H and lower alkyl; R, R 1 and R 2 being the same or different, T is selected from the group consisting of O, N, H, S and CH 2 with the proviso that only one T is 0; Z is 0 or 1 and n is 0-5; and pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
172 words
A process of prophylactic treatment to prevent clot formation in humans and animals comprising the administration to a human or animal of an effective amount of a compound of the formula: ##STR10## wherein X is an alkyl or alkenyl chain having 2-8 carbon atoms, one of which carbon atoms may be in the form of a carbonyl group, Y is H, alkyl, dialkylaminoethyl, aryl, aralkyl or aryl and aralkyl substituted with one or more R, and R is H, lower alkyl, lower alkoxy, halogen, CF 3 , NO 2 , OH, CN, COOR 1 , ##STR11## NHCOR 1 , NR 1 R 2 or ##STR12## where R 1 and R 2 are each selected from the group consisting of H and lower alkyl; R, R 1 and R 2 being the same or different, T is selected from the group consisting of O, N, H, S and CH 2 with the proviso that only one T is 0; Z is 0 or 1 and n is 0-5; and pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
25 words
The process of claim 4 wherein the compound added is selected from the group consisting of p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenyl-propyl] phenyl phosphonic acid and pharmaceutically acceptable salts thereof.
References Cited (Backward Citations)
US3984501A
Cited
US4016223A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-09 | 1982-10-09 | 1983-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-09 | 1986-10-09 | 1987-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-09 | 1990-10-09 | 1991-04-10 | $7700.00 | Window Closed / Lapsed |