US4051236A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Inhibition of blood platelet aggregation
Assignee: ER Squibb and Sons LLC
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Filing: 1976-05-20
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Granted: 1977-09-27
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Expires: 1996-05-20
Abstract
Abstract The activity of PGE 1 in inhibiting aggregation of blood platelets is enhanced by employing PGE 1 in combination with certain inhibitors of cyclic 3',5'-adenosine monophosphate phosphodiesterase (PDE).
Inventors
- 👤 Don Navarro Harris
- 👤 Marie B. Phillips
- 👤 Harold Jacob Goldenberg
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 18:32
CPC Classifications
A; A61; A61K; A61K35/00; A61K35/12; A61K35/14; A61K35/16; A61K31/00; A61K31/185; A61K31/19; A61K31/205; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/47; A61K31/55; A61K35/19
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
96 words
A method of inhibiting aggregation of human blood platelets which comprises contacting the platelets with PGE 1 and a compound which potentiates the effectiveness of PGE 1 , which compound is a member selected from the group consisting of 4-(Butylamino)-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester 4-Chloro-1-ethyl-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-acetonitrile 1-Ethyl-4-(isopropylidenehydrazino)-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester, or its hydrochloride, hemihydrate 3-Ethyl-7,12-dimethylpyrazolo[4',3':5,6]pyrido[4,3-b]-[1,5]benzodiazepin-6-(3H)-one 3-Ethyl-7,12-dihydro-9-methoxy-7,12-dimethylpyrazolo[3',4':2,3]pyrido[4,5-b][1,5]benzodiazepin-6(3H)-one 4-(Butylamino)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid, ethyl ester 4-(Butylamino)-1-ethyl-1,7-dihydro-7-hydroxy-5H-furo-[3,4-e]pyrazolo[3,4-b]pyridin-5-one 10-Chloro-3-ethyl-7,12-dimethyl-7,12-dihydropyrazolo-[4',3':5,6]pyrido[4,3-b][1,5]benzodiazepin-6(3H)-one, said PGE 1 being present in a concentration of from about 10 -6 molar to about 10 -9 molar, and said compound being present in a concentration of from about 0.1 mM to about 4 mM.
Claim 2
Independent Claim
96 words
A method of inhibiting aggregation of human blood platelets which comprises contacting the platelets with PGE 1 and a compound which potentiates the effectiveness of PGE 1 , which compound is a member selected from the group consisting of 4-(Butylamino)-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester 4-Chloro-1-ethyl-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-acetonitrile 1-Ethyl-4-(isopropylidenehydrazino)-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester, or its hydrochloride, hemihydrate 3-Ethyl-7,12-dimethylpyrazolo[4',3':5,6]pyrido[4,3-b]-[1,5]benzodiazepin-6-(3H)-one 3-Ethyl-7,12-dihydro-9-methoxy-7,12-dimethylpyrazolo[3',4':2,3]pyrido[4,5-b][1,5]benzodiazepin-6(3H)-one 4-(Butylamino)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid, ethyl ester 4-(Butylamino)-1-ethyl-1,7-dihydro-7-hydroxy-5H-furo-[3,4-e]pyrazolo[3,4-b]pyridin-5-one 10-Chloro-3-ethyl-7,12-dimethyl-7,12-dihydropyrazolo-[4',3':5,6]pyrido[4,3-b][1,5]benzodiazepin-6(3H)-one, said PGE 1 being present in a concentration of from about 10 -6 molar to about 10 -9 molar, and said compound being present in a concentration of from about 0.1 mM to about 4 mM.
Claim 3
Dependent Claim
16 words
A method according to claim 1 wherein the human blood platelets are in whole human blood.
Claim 4
Dependent Claim
16 words
A method according to claim 1 wherein the human blood platelets are in platelet rich plasma.
Claim 5
Dependent Claim
15 words
A method according to claim 1 wherein the human blood platelets are in platelet concentrate.
Claim 6
Dependent Claim
90 words
A composition for inhibiting aggregation of human blood platelets which comprises PGE 1 and a member which potentiates the effectiveness of PGE 1 , which member is selected from the group consisting of 4-(Butylamino)-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester 4-Chloro-1-ethyl-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-acetonitrile 1-Ethyl-4-(isopropylidenehydrazino)-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ester, or its hydrochloride, hemihydrate 3-Ethyl-7,12-dimethylpyrazolo[4',3':5,6]pyrido[4,3-b]-[1,5]benzodiazepin-6-(3H)-one 3-Ethyl-7,12-dihydro-9-methoxy-7,12-dimethyl-pyrazolo[3',4':2,3]pyrido [4,5-b][1,5]benzodiazepin-6(3H)-one 4-(Butylamino)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid, ethyl ester 4-(Butylamino)-1-ethyl-1,7-dihydro-7-hydroxy-5H-furo[3,4-e]pyrazolo[3,4-b]pyridin-5-one 10-Chloro-3-ethyl-7,12-dimethyl-7,12-dihydropyrazolo-[4',3':5,6]pyrido[4,3-b][1,5]benzodiazepin-6(3H)-one, said PGE 1 being present in a concentration of from about 10 -6 molar to about 10 -9 molar, and said member being present in a concentration of from about 0.1 mM to about 4 mM
Claim 7
Dependent Claim
90 words
A composition for inhibiting aggregation of human blood platelets which comprises PGE 1 and a member which potentiates the effectiveness of PGE 1 , which member is selected from the group consisting of 4-(Butylamino)-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ethyl ester 4-Chloro-1-ethyl-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-acetonitrile 1-Ethyl-4-(isopropylidenehydrazino)-3-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid, ester, or its hydrochloride, hemihydrate 3-Ethyl-7,12-dimethylpyrazolo[4',3':5,6]pyrido[4,3-b]-[1,5]benzodiazepin-6-(3H)-one 3-Ethyl-7,12-dihydro-9-methoxy-7,12-dimethyl-pyrazolo[3',4':2,3]pyrido [4,5-b][1,5]benzodiazepin-6(3H)-one 4-(Butylamino)-1H-pyrazolo[3,4-b]pyridine-6-carboxylic acid, ethyl ester 4-(Butylamino)-1-ethyl-1,7-dihydro-7-hydroxy-5H-furo[3,4-e]pyrazolo[3,4-b]pyridin-5-one 10-Chloro-3-ethyl-7,12-dimethyl-7,12-dihydropyrazolo-[4',3':5,6]pyrido[4,3-b][1,5]benzodiazepin-6(3H)-one, said PGE 1 being present in a concentration of from about 10 -6 molar to about 10 -9 molar, and said member being present in a concentration of from about 0.1 mM to about 4 mM
Claim 8
Dependent Claim
12 words
The method as defined in claim 1 wherein said compound is 3-ethyl-7,12-dihydro-9-methoxy-7,12-dimethylpyrazolo-[3',4':2,3]pyrido[4,5-b][1,5]benzodiazepin-6(3H)-one.
Claim 9
Dependent Claim
12 words
The composition as defined in claim 6 wherein said member is 3-ethyl-7,12-dihydro-9-methoxy-7,12-dimethyl-pyrazolo-[3',4':2,3]pyrido[4,5-b][1,5]benzodiazepin-6-(3H)-one.
References Cited (Backward Citations)
US3755565A
Cited
US3974195A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-09-26 | 1981-03-28 | 1981-09-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-09-26 | 1985-03-28 | 1985-09-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-09-26 | 1989-03-28 | 1989-09-27 | $7700.00 | Window Closed / Lapsed |