US3960847A
Expired / Lapsed
US
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9-Substituted-4-oxopyrido(1,2-α)pyrimidine-3-carboxylic acids and derivatives thereof
Assignee: ER Squibb and Sons LLC
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Filing: 1974-05-28
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Granted: 1976-06-01
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Expires: 1994-05-28
Abstract
Abstract 9-Substituted-4-oxopyrido[1,2-α]pyrimidine-3-carboxylic acids and related compounds are disclosed. In addition, their methods of preparation and use as central nervous system depressants and hypotensive agents are taught.
Inventors
- 👤 Harry Louis Yale
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 21:24
CPC Classifications
A; A23; A23K; A23K20/00; A23K20/10; A23K20/116; A23K20/137
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
121 words
A compound of the formula: ##SPC10## wherein R 1 is selected from the group consisting of hydrogen and straight or branched chain alkyl of from 1 to 4 carbon atoms; and R 4 is selected from the group consisting of benzyl, phenethyl, substituted benzyl or phenethyl, and ##EQU3## wherein n is zero or one, -------- represents a triple bond .tbd. when n is zero and a double bond = when n is one, A is hydrogen, phenyl, or substituted phenyl, and said phenyl, benzyl and phenethyl substituent is selected from the group consisting of mono (halogen), di(halogen), mono(carboethoxy), mono(trifluoromethyl), mono(alkyl) of 1 to 4 carbon atoms, mono(alkoxy) of 1 to 4 carbon atoms, and mono(NC); and a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
121 words
A compound of the formula: ##SPC10## wherein R 1 is selected from the group consisting of hydrogen and straight or branched chain alkyl of from 1 to 4 carbon atoms; and R 4 is selected from the group consisting of benzyl, phenethyl, substituted benzyl or phenethyl, and ##EQU3## wherein n is zero or one, -------- represents a triple bond .tbd. when n is zero and a double bond = when n is one, A is hydrogen, phenyl, or substituted phenyl, and said phenyl, benzyl and phenethyl substituent is selected from the group consisting of mono (halogen), di(halogen), mono(carboethoxy), mono(trifluoromethyl), mono(alkyl) of 1 to 4 carbon atoms, mono(alkoxy) of 1 to 4 carbon atoms, and mono(NC); and a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
42 words
The compound of claim 1 wherein R 4 is benzyl or substituted benzyl wherein said substituent is selected from the group consisting of mono(halogen), di(halogen), mono-(carboethoxy), mono(trifluoromethyl), mono(alkyl) of 1 to 4 carbon atoms, mono(alkoxy) of 1to 4 carbon atoms, and mono(NC).
Claim 4
Dependent Claim
12 words
The compound of claim 2 having the name 9-[(2-bromo-4-chlorobenzyl)oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 5
Dependent Claim
12 words
The compound of claim 2 having the name 9-[(o-bromobenzyl)oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 6
Dependent Claim
12 words
The compound of claim 2 having the name 9-[(o-chlorobenzyl)oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 7
Dependent Claim
12 words
The compound of claim 2 having the name 4-oxo-9-[[(p-trifluoromethyl)benzyl]oxy]-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 8
Dependent Claim
13 words
The compound of claim 2 having the name 9-[[(o-carboethoxy)benzyl]oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester, hydrobromide.
Claim 9
Dependent Claim
12 words
The compound of claim 2 having the name 9-[(o-methylbenzyl)oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 10
Dependent Claim
12 words
The compund of claim 2 having the name 9-[[(o-isocyanido)benzyl]oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 11
Dependent Claim
12 words
The compound of claim 2 having the name 9-[(2-bromo-4-chlorobenzyl)oxy]-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, potassium salt.
Claim 12
Dependent Claim
14 words
The compound of claim 1 having the name 4-oxo-9-(phenethyloxy)-4H-pyrido[1,2-α]pyrimidine 3-carboxylic acid, ethyl ester, maleate.
Claim 13
Dependent Claim
10 words
The compound of claim 1 wherein R 4 is ##EQU4##
Claim 14
Dependent Claim
11 words
The compound of claim 12 having the 4-oxo-9-(2-propynyloxy)-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 15
Dependent Claim
12 words
The compound of claim 12 having the name 9-(allyloxy)-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
Claim 16
Dependent Claim
12 words
The compound of claim 12 having the name 9-(allyloxy)-4-oxo-4H-pyrido[1,2-α]pyrimidine-3-carboxylic acid, ethyl ester.
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) | 1979-06-01 | 1979-12-01 | 1980-06-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-06-01 | 1983-12-01 | 1984-06-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-06-01 | 1987-12-01 | 1988-06-01 | $7700.00 | Window Closed / Lapsed |