US4296120A
Expired / Lapsed
US
⏱️ 0.0 years remaining
(Carboxy-oxo-pyrrolidino)phenylalkenamides and esters thereof as SRS-A antagonists
Assignee: Pfizer Inc
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Filing: 1980-08-28
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Granted: 1981-10-20
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Expires: 2000-08-28
Abstract
Abstract Certain new propenamide and 2-butenamide compounds, having a (4-carboxy-2-oxo-pyrrolidino)phenyl substituent at the 3-position, and certain esters thereof, and their use for antagonizing the spasmogenic activity of slow-reacting substance of anaphylaxis (SRS-A) in a human subject. In particular, the compounds of the invention are useful for preventing and treating certain obstructive airways diseases, notably allergic bronchial asthma, allergic rhinitis and certain skin disorders, in human subjects.
Inventors
- 👤 Saul B. Kadin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:41
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/18; C07D207/22; C07D207/24; C07D207/26; C07D207/273; C07D207/277; A; A61; A61P; A61P37/00; A61P37/08; C07C; C07C205/00; C07C205/49; C07C205/56
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
92 words
An alkenamide compound of the formula ##STR25## and a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen and methyl.
Claim 2
Dependent Claim
92 words
An alkenamide compound of the formula ##STR25## and a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen and methyl.
Claim 3
Dependent Claim
11 words
A compound according to claim 1, wherein R 1 is hydrogen.
Claim 4
Dependent Claim
15 words
A compound according to claim 2, wherein R 5 and R 6 are each hydrogen.
Claim 5
Dependent Claim
12 words
A compound according to claim 3, wherein R 2 is said alkyl.
Claim 6
Dependent Claim
11 words
A compound according to claim 4, wherein said alkyl is decyl.
Claim 7
Dependent Claim
21 words
A compound according to claim 5, wherein the two substituents on the phenyl ring have a meta relationship to each other.
Claim 8
Dependent Claim
16 words
A compound according to claim 2, wherein R 5 is hydrogen and R 6 is methyl.
Claim 9
Dependent Claim
25 words
A compound according to claim 7, wherein R 2 is decyl and the substituents on the phenyl ring have a meta relationship to each other.
Claim 10
Dependent Claim
16 words
A compound according to claim 2, wherein R 5 is methyl and R 6 is hydrogen.
Claim 11
Dependent Claim
26 words
A compound according to claim 9, wherein R 2 is decyl and the two substituents on the phenyl ring have a meta relationship to each other.
Claim 12
Independent Claim
121 words
A method for antagonizing the effect of slow-reacting substance of anaphylaxis in a human subject, which comprises administering to said subject a slow-reacting substance of anaphylaxis antagonizing amount of an alkenamide compound of the formula ##STR26## or a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen and methyl.
Claim 13
Independent Claim
121 words
A method for antagonizing the effect of slow-reacting substance of anaphylaxis in a human subject, which comprises administering to said subject a slow-reacting substance of anaphylaxis antagonizing amount of an alkenamide compound of the formula ##STR26## or a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen and methyl.
Claim 14
Dependent Claim
11 words
The method according to claim 11, wherein R 1 is hydrogen.
Claim 15
Dependent Claim
15 words
The method according to claim 12, wherein R 5 and R 6 are each hydrogen.
Claim 16
Dependent Claim
12 words
The method according to claim 13, wherein R 2 is said alkyl.
Claim 17
Dependent Claim
11 words
The method according to claim 14, wherein said alkyl is decyl.
Claim 18
Dependent Claim
21 words
The method according to claim 15, wherein the two substituents on the phenyl ring have a meta relationship to each other.
Claim 19
Dependent Claim
16 words
The method according to claim 12, wherein R 5 is hydrogen and R 6 is methyl.
Claim 20
Dependent Claim
25 words
The method according to claim 17, wherein R 2 is decyl and the substituents on the phenyl ring have a meta relationship to each other.
Claim 21
Dependent Claim
16 words
The method according to claim 12, wherein R 5 is methyl and R 6 is hydrogen.
Claim 22
Dependent Claim
26 words
The method according to claim 19, wherein R 2 is decyl and the two substituents on the phenyl ring have a meta relationship to each other.
Claim 23
Dependent Claim
123 words
A pharmaceutical composition which comprises a pharmaceutically-acceptable carrier and an alkenamide compound of the formula ##STR27## or a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen an methyl; and wherein the ratio of the pharmaceutically-acceptable carrier to the alkenamide compound is in the range from 1:6 to 6:1 by weight.
Claim 24
Dependent Claim
123 words
A pharmaceutical composition which comprises a pharmaceutically-acceptable carrier and an alkenamide compound of the formula ##STR27## or a pharmaceutically-acceptable salt thereof; wherein R 1 is selected from the group consisting of hydrogen, alkyl having 1 to 4 carbons and --CH 2 --CH 2 --NR 3 R 4 , wherein R 3 and R 4 are each alkyl having 1 to 3 carbons; R 2 is selected from the group consisting of alkyl having 8 to 15 carbons and cycloalkyl having from 6 to 12 carbons; and R 5 and R 6 are selected from the group consisting of hydrogen an methyl; and wherein the ratio of the pharmaceutically-acceptable carrier to the alkenamide compound is in the range from 1:6 to 6:1 by weight.
References Cited (Backward Citations)
US3988371A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-10-19 | 1985-04-20 | 1985-10-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-10-19 | 1989-04-20 | 1989-10-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-10-19 | 1993-04-20 | 1993-10-20 | $7700.00 | Window Closed / Lapsed |