US4006237A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Tetrahydrocarbostyril derivatives for the prophylaxis of asthma, hayfever and rhinitis
Assignee: Beecham Group PLC
•
Filing: 1975-05-21
•
Granted: 1977-02-01
•
Expires: 1995-05-21
Abstract
Abstract Pharmaceutical compositions having anti-allergy activity in which the active anti-allergy agents are certain 3-nitro-α-pyridones and their pharmaceutically acceptable salts formulated in one or more pharmaceutically acceptable carriers.
Inventors
- 👤 Derek Richard Buckle
- 👤 Barrie Christian Charles Cantello
- 👤 Harry Smith
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 00:42
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/20; C07D215/22; C07D221/00; C07D221/02; C07D221/04
Claims Analysis
Total Claims: 50
Claim 1
Independent Claim
66 words
A pharmaceutical composition in a form suitable for administration to humans which comprises a compound of the formula ##STR25## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl, and Z is a cyclohexyl ring fused to the pyridone ring in an amount sufficient to be effective for the prophylaxis of of asthma, hayfever or rhinitis in combination with a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim
66 words
A pharmaceutical composition in a form suitable for administration to humans which comprises a compound of the formula ##STR25## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl, and Z is a cyclohexyl ring fused to the pyridone ring in an amount sufficient to be effective for the prophylaxis of of asthma, hayfever or rhinitis in combination with a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim
11 words
A pharmaceutical composition according to claim 1, wherein R is hydrogen.
Claim 4
Dependent Claim
31 words
A pharmaceutical composition according to claim 1 whrein R is hydrogen or lower alkyl and the cyclohexyl ring Z is unsubstituted or substituted by alkyl of 1 to 4 carbon atoms.
Claim 5
Dependent Claim
72 words
A pharmaceutical composition according to claim 1 wherein the compound is of the formula (V): ##STR26## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl and R 1 , r 2 , r 3 and R 4 are each selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy sec-butoxy, tert-butoxy, phenoxy, benzyloxy, benzyl, fluoro, chloro, bromo and iodo.
Claim 6
Dependent Claim
44 words
A composition according to claim 1 wherein R, and R 4 are hydrogen and one or two of R 1 , R 2 and R 3 are hydrogen or alkyl, and the remaining R 1 , R 2 and R 3 groups are hydrogen.
Claim 7
Dependent Claim
11 words
A composition according to claim 5 wherein R 2 is hydrogen.
Claim 8
Dependent Claim
17 words
A pharmaceutical composition according to claim 1 wherein the compound is in the form of a salt.
Claim 9
Dependent Claim
14 words
A pharmaceutical composition according to claim 7 wherein the salt is the sodium salt.
Claim 10
Dependent Claim
16 words
A pharmaceutical composition according to claim 1 in the form of a microfine powder for insufflation.
Claim 11
Dependent Claim
16 words
A pharmaceutical composition according to claim 9 which additionally contains a small amount of a bronchodilator.
Claim 12
Dependent Claim
12 words
A pharmaceutical composition according to claim 10 wherein the bronchodilator is isoprenaline.
Claim 13
Dependent Claim
18 words
A pharmaceutical composition according to claim 1 in which the carrier is a sterile liquid suitable for injection.
Claim 14
Dependent Claim
15 words
A pharmaceutical composition according to claim 1 in which the carrier is a solid carrier.
Claim 15
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 16
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 4-hydroxy-7-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 17
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 5,7-dimethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 18
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 4-hydroxy-6-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 19
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 1-ethyl-4-hydroxy-3-nitro-5,6,7,8tetrahydrocarbostyril.
Claim 20
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 4-hydroxy-3-nitro-1-n-propyl-5,6,7,8-tetrahydrocarbostyril.
Claim 21
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 4-hydroxy-1-isopropyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 22
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 1-ethyl-4-hydroxy-7-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 23
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 7-ethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 24
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 6,7-diethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 25
Dependent Claim
12 words
A pharmaceutical composition according to claim 1 wherein the compound is 6,7-dimethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 26
Independent Claim
109 words
A method for the prophylaxis of asthma, hayfever and rhinitis in humans which comprises administering to a human in need thereof a compound of the formula (II): ##STR27## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl, and Z is a cyclohexyl ring fused to the pyridone ring unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, phenoxy, benzyloxy, phenyl, benzyl, hydroxy, nitro, and halogen, in an amount sufficient to be effective for the prophylaxis of asthma, hayfever or rhinitis in combination with a pharmaceutical carrier.
Claim 27
Independent Claim
109 words
A method for the prophylaxis of asthma, hayfever and rhinitis in humans which comprises administering to a human in need thereof a compound of the formula (II): ##STR27## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl, and Z is a cyclohexyl ring fused to the pyridone ring unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, phenoxy, benzyloxy, phenyl, benzyl, hydroxy, nitro, and halogen, in an amount sufficient to be effective for the prophylaxis of asthma, hayfever or rhinitis in combination with a pharmaceutical carrier.
Claim 28
Dependent Claim
10 words
A method according to claim 25, wherein R is hydrogen.
Claim 29
Dependent Claim
30 words
A method according to claim 25 wherein R is hydrogen or lower alkyl and the cyclohexyl ring Z is unsubstituted or substituted by alkyl of 1 to 4 carbon atoms.
Claim 30
Dependent Claim
71 words
A method according to claim 25 wherein the compound is of the formula (V): ##STR28## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or lower alkyl and R 1 , r 2 , r 3 and R 4 are each selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, sec-butoxy, tert-butoxy, phenoxy, benzyloxy, benzyl, fluoro, chloro, bromo and iodo.
Claim 31
Dependent Claim
44 words
A method according to claim 25 wherein R, and R 4 are hydrogen and one or two of R 1 , R 2 and R 3 are hydrogen or alkyl, and the remaining R 1 , R 2 and R 3 groups are hydrogen.
Claim 32
Dependent Claim
11 words
A method according to claim 29 wherein R 2 is hydrogen.
Claim 33
Dependent Claim
16 words
A method according to claim 25 wherein the compound is in the form of a salt.
Claim 34
Dependent Claim
13 words
A method according to claim 31 wherein the salt is the sodium salt.
Claim 35
Dependent Claim
22 words
A method according to claim 25 wherein the compound and the carrier are in the form of a microfine powder for insufflation.
Claim 36
Dependent Claim
18 words
A method according to claim 33 wherein the compound is combined with a small amount of a bronchodilator.
Claim 37
Dependent Claim
11 words
A method according to claim 34 wherein the bronchodilator is isoprenaline.
Claim 38
Dependent Claim
18 words
A method according to claim 25 in which the carrier is a sterile liquid carrier suitable for injection.
Claim 39
Dependent Claim
13 words
A method according to claim 25 wherein the carrier is a solid carrier.
Claim 40
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarabostyril.
Claim 41
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 4-hydroxy-7-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 42
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 5,7-dimethyl-4-hydroxy-3-nitro-5,6,7,8-tatrahydrocarbostyril.
Claim 43
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 4-hydroxy-6-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 44
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 1-ethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 45
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 4-hydroxy-3-nitro-1-n-propyl-5,6,7,8-tetrahydrocarbostyril.
Claim 46
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 4-hydroxy-1-isopropyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 47
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 1-ethyl-4-hydroxy-7-methyl-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 48
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 7-ethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 49
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 6,7-diethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
Claim 50
Dependent Claim
11 words
A method according to claim 25 wherein the compound is 6,7-dimethyl-4-hydroxy-3-nitro-5,6,7,8-tetrahydrocarbostyril.
References Cited (Backward Citations)
FR1369634A
Cited
US3864493A
Cited
FR2009119A1
Cited
US3885038A
Cited
US3883653A
Cited
US3879544A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-02-01 | 1980-08-02 | 1981-02-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-02-01 | 1984-08-02 | 1985-02-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-02-01 | 1988-08-02 | 1989-02-01 | $7700.00 | Window Closed / Lapsed |