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US4017625A
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Anti-allergic N-(5-tetrazolyl)-1-oxo-1H-6-alkoxypyrimido-[1,2-a]quinoline-2-carboxamides and intermediates therefor
Assignee: Pfizer Inc
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Filing: 1976-05-24
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Granted: 1977-04-12
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Expires: 1996-05-24
Abstract
Abstract A novel series of N-(5-tetrazolyl)-1-oxo-1H-6-alkoxypyrimido[1,2-a]quinoline-2-carboxamides of the formula <IMAGE> wherein each of R1 and R2 is hydrogen, lower alkyl, lower alkoxy, fluoro or chloro; R3 is chloro, bromo or lower alkoxy; R1 and R2 when taken together are alky lenedioxy of one to two carbon atoms; intermediates therefor and the pharmaceutically-acceptable cationic salts thereof; and their use as anti-allergy agents.
Inventors
- 👤 Saul B. Kadin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 11:34
CPC Classifications
C; C07; C07D; C07D401/00; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; C07D401/14; C07D487/00; C07D487/02; C07D487/04
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
69 words
A compound of the formula ##STR11##wherein each of R 1 and R 2 is hydrogen, from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 2
Dependent Claim
69 words
A compound of the formula ##STR11##wherein each of R 1 and R 2 is hydrogen, from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 3
Dependent Claim
22 words
A compound according to claim 1 wherein each of R 1 and R 2 is hydrogen and R 3 is lower alkoxy.
Claim 4
Dependent Claim
21 words
A compound according to claim 1 wherein R 1 is hydrogen, R 2 is 8-lower alkoxy and R 3 is ethoxy.
Claim 5
Dependent Claim
22 words
A compound according to claim 1 wherein R 1 is 8-lower alkoxy, R 2 is 9-lower alkoxy, and R 3 is methoxy.
Claim 6
Dependent Claim
20 words
A compound according to claim 1 wherein R 1 is hydrogen, R 2 is fluoro and R 3 is methoxy.
Claim 7
Dependent Claim
11 words
The compound according to claim 2 wherein R 3 is methoxy.
Claim 8
Dependent Claim
11 words
The compound according to claim 2 wherein R 3 is ethoxy.
Claim 9
Dependent Claim
11 words
The compound according to claim 3 wherein R 2 is 8-methoxy.
Claim 10
Dependent Claim
16 words
The compound according to claim 4 wherein R 1 is 8-methoxy and R 2 is 9-methoxy.
Claim 11
Dependent Claim
11 words
The compound according to claim 5 wherein R 2 is 9-fluoro.
Claim 12
Independent Claim
96 words
The method of inhibiting the release of mediators of anaphylaxis in a mammalian subject which comprises administering to the subject an anaphylaxis mediator release inhibiting amount of a compound having the formula ##STR12##wherein each of R 1 and R 2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 13
Independent Claim
96 words
The method of inhibiting the release of mediators of anaphylaxis in a mammalian subject which comprises administering to the subject an anaphylaxis mediator release inhibiting amount of a compound having the formula ##STR12##wherein each of R 1 and R 2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 14
Dependent Claim
22 words
The method according to claim 11 wherein each of R 1 and R 2 is hydrogen and R 3 is lower alkoxy.
Claim 15
Dependent Claim
22 words
The method according to claim 11 and wherein R 1 is hydrogen, R 2 is 8-lower alkoxy and R 3 is ethoxy.
Claim 16
Dependent Claim
20 words
The method according to claim 11 wherein R 1 is hyrogen, R 2 is fluoro and R 3 is methoxy.
Claim 17
Dependent Claim
11 words
The method according to claim 12 wherein R 3 is methoxy.
Claim 18
Dependent Claim
11 words
The method according to claim 13 wherein R 2 is 8-methoxy.
Claim 19
Dependent Claim
11 words
The method according to claim 14 wherein R 2 is 9-fluoro.
Claim 20
Dependent Claim
82 words
A pharmaceutical composition active as an antiallergy agent comprising a pharmaceutically-acceptable carrier and a compound of the formula ##STR13##wherein each of R 1 and R 2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 21
Dependent Claim
82 words
A pharmaceutical composition active as an antiallergy agent comprising a pharmaceutically-acceptable carrier and a compound of the formula ##STR13##wherein each of R 1 and R 2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, and fluoro; R 1 and R 2 when taken together are alkylenedioxy and are selected from the group consisting of methylenedioxy and ethylenedioxy; R 3 is selected from the group consisting of chloro, bromo and lower alkoxy; and the pharmaceutically-acceptable cationic salts thereof.
Claim 22
Dependent Claim
22 words
A composition according to claim 18 wherein each of R 1 and R 2 is hydrogen and R 3 is lower alkoxy.
Claim 23
Dependent Claim
21 words
A composition according to claim 18 wherein R 1 is hydrogen, R 2 is 9-lower alkoxy and R 3 is methoxy.
Claim 24
Dependent Claim
20 words
A composition according to claim 18 wherein R 1 is hydrogen, R 2 is fluoro and R 3 is methoxy.
Claim 25
Dependent Claim
16 words
A pharmaceutical composition as claimed in claim 18 in a form suitable for administration by inhalation.
Claim 26
Dependent Claim
19 words
A pharmaceutical composition as claimed in claim 18 comprising a solution or suspension of the antiallergy agent in water.
Claim 27
Dependent Claim
19 words
A pharmaceutical composition as claimed in claim 18 comprising a suspension of the antiallergy agent in a liquefied propellant.
Claim 28
Dependent Claim
17 words
A pharmaceutical composition as claimed in claim 18 comprising the solid antiallergy agent and a solid diluent.
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) | 1980-04-11 | 1980-10-11 | 1981-04-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-04-11 | 1984-10-11 | 1985-04-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-04-11 | 1988-10-11 | 1989-04-12 | $7700.00 | Window Closed / Lapsed |