US4239778A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Azaprostanoic acid analogs and their use as inhibitors of platelet aggregation
Assignee: University of Illinois Foundation
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Filing: 1978-09-12
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Granted: 1980-12-16
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Expires: 1998-09-12
Abstract
Abstract Novel azaprostanoic acid analogs of the formula <IMAGE> (I) wherein: R is C1 to C8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, and their pharmaceutically acceptable salts and esters. Preferred 13-aza and 15-aza compounds are active in the inhibition of arachidonic acid-induced platelet aggregation and, more specifically, are direct and specific antagonists of the activity of prostaglandin H2 and thromboxane A2.
Inventors
- 👤 Duane L. Venton
- 👤 Guy C. Le Breton
- 👤 Steven E. Enke
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 13:08
CPC Classifications
C; C07; C07C; C07C405/00; C07C405/0008; C07C405/0041; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/40; C07F9/4003; C07F9/4006
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
37 words
Azaprostanoic acids of the formula ##STR15## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, and their pharmaceutically acceptable salts and lower alkyl esters.
Claim 2
Dependent Claim
37 words
Azaprostanoic acids of the formula ##STR15## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, and their pharmaceutically acceptable salts and lower alkyl esters.
Claim 3
Dependent Claim
26 words
Compounds according to claim 1 wherein the sum of the numerical value of a and the number of carbon atoms in the R group totals 7.
Claim 4
Dependent Claim
13 words
Azaprostanoic acids according to claim 1 wherein a has a value of 0.
Claim 5
Dependent Claim
13 words
Azaprostanoic acids according to claim 1 wherein a has a value of 2.
Claim 6
Dependent Claim
18 words
A compound according to claim 1 which is named, 13-azaprostanoic acid, and its pharmaceutically acceptable salts and esters.
Claim 7
Dependent Claim
18 words
A compound according to claim 1 which is named, 15-azaprostanoic acid, and its pharmaceutically acceptable salts and esters.
Claim 8
Independent Claim
74 words
The method of antagonizing the activity of prostaglandin H 2 and thromboxane A 2 in the circulatory system of an animal, said method comprising administering to the circulatory system of the animal an effective amount of an azaprostanoic acid of the formula, ##STR16## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, or its pharmaceutically acceptable salts and lower alkyl esters.
Claim 9
Independent Claim
74 words
The method of antagonizing the activity of prostaglandin H 2 and thromboxane A 2 in the circulatory system of an animal, said method comprising administering to the circulatory system of the animal an effective amount of an azaprostanoic acid of the formula, ##STR16## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, or its pharmaceutically acceptable salts and lower alkyl esters.
Claim 10
Dependent Claim
20 words
The method of claim 7 wherein the amount of azaprostanoic acid administered comprises from about 1 to about 100 mg/kg.
Claim 11
Dependent Claim
66 words
A pharmaceutical composition suitable for use in antiplatelet therapy, said composition comprising, as an active ingredient, an azaprostanoic acid compound of the formula ##STR17## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, or its pharmaceutically acceptable salts and lower alkyl esters, in combination with a pharmaceutically acceptable carrier for said active ingredient.
Claim 12
Dependent Claim
66 words
A pharmaceutical composition suitable for use in antiplatelet therapy, said composition comprising, as an active ingredient, an azaprostanoic acid compound of the formula ##STR17## wherein: R is C 1 to C 8 alkyl or benzyl; and a has a value of from 0 to 6 inclusive, or its pharmaceutically acceptable salts and lower alkyl esters, in combination with a pharmaceutically acceptable carrier for said active ingredient.
References Cited (Backward Citations)
DE2535343A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-12-16 | 1984-06-16 | 1984-12-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-12-16 | 1988-06-16 | 1988-12-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-12-16 | 1992-06-16 | 1992-12-16 | $7700.00 | Window Closed / Lapsed |