US4083953A
Expired / Lapsed
US
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Pharmaceutical composition containing 5:6-benzo-alpha-pyrone derivatives and method of use thereof
Assignee: Pfizer Italia SRL
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Filing: 1976-10-27
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Granted: 1978-04-11
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Expires: 1996-10-27
Abstract
Abstract A pharmaceutical composition, and method of treating allergic conditions therewith, is disclosed, wherein said composition contains a 5:6-benzo-γ-pyrone derivative, such as, for instance, 6-carboxy-2'-isopropoxy-flavone. The composition may be used to treat various allergic conditions, including bronchial asthma, allergic rhinitis, hay fever, urticaria and dermatosis.
Inventors
- 👤 Gianfederico Doria
- 👤 Pier Nicola Giraldi
- 👤 Francesco Lauria
- 👤 Maria Luisa Corno
- 👤 Piero Sberze
- 👤 Marcello Tibolla
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 17:13
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
132 words
A pharmaceutical composition suitable for the treatment of allergies, said composition in the form of a tablet, pill, capsule, cream or paste which comprises a suitable carrier for oral or topical administration and a pharmaceutically effective amount of compound having the formula: ##STR44## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
132 words
A pharmaceutical composition suitable for the treatment of allergies, said composition in the form of a tablet, pill, capsule, cream or paste which comprises a suitable carrier for oral or topical administration and a pharmaceutically effective amount of compound having the formula: ##STR44## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
40 words
A composition of claim 1 wherein said compound is selected from the group consisting of: 6-carboxy-flavone, 6-carboxy-2'-isopropoxy-flavone, 6-carboxy-2'-methoxy-flavone, 6-carboxy-2'-ethoxy-flavone, 6-carboxy-2'-propoxy-flavone, 6-carboxy-2'-butoxy-flavone, 6-carboxy-2'-(2-methyl-propoxy)-flavone, 6-carboxy-2'-(1-methyl-propoxy)-flavone, 6-carboxy-2'-(2-ethoxy-ethoxy)-flavone, 6-carboxy-4'-(2-ethoxy-ethoxy)-flavone, 6-carboxy-2'-(2-hydroxy-ethoxy)-flavone, 6-carboxy-2'-(2-hydroxy-propoxy)-flavone, 6-carboxy-2'-(3-hydroxy-propoxy)-flavone, 6-carboxy-2'-(2,3-dihydroxy-propoxy)-flavone, 6-carboxy-2'-(2-hydroxy-butoxy)-flavone, 6-carboxy-2'-(2-hydroxy-2-methyl-propoxy)-flavone, 6-carboxy-2'-(2-hydroxy-2-methyl-butoxy)-flavone, 6-carboxy-2'-(2-hydroxy-3-methyl-butoxy)-flavone, 6-carboxy-4'-(2-hydroxy-propoxy)-flavone, and a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
101 words
A pharmaceutical composition suitable for the treatment of allergies, said composition comprising a suitable carrier and a pharmaceutically effective amount of a compound having the formula: ##STR45## wherein R is carboxy or --COOR 1 3, wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; R 8 is a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is C 1 -C 6 alkyl which may be unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and R 7 is hydrogen; and a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
101 words
A pharmaceutical composition suitable for the treatment of allergies, said composition comprising a suitable carrier and a pharmaceutically effective amount of a compound having the formula: ##STR45## wherein R is carboxy or --COOR 1 3, wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; R 8 is a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is C 1 -C 6 alkyl which may be unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and R 7 is hydrogen; and a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
14 words
A pharmaceutical composition according to claim 3 in a form suitable for oral administration.
Claim 7
Dependent Claim
14 words
A pharmaceutical composition according to claim 3 in a form suitable for parenteral administration.
Claim 8
Dependent Claim
14 words
A pharmaceutical composition according to claim 3 in a form suitable for topical administration.
Claim 9
Dependent Claim
13 words
A pharmaceutical composition according to claim 3 in a form suitable for inhalation.
Claim 10
Dependent Claim
152 words
A pharmaceutical composition suitable for the treatment of allergies, said composition in the form of a tablet, pill, capsule, cream, paste, aerosol formulation which is a suspension or solution in a liquified propellant, or powder for insufflation admixed with a diluent powder which comprises a suitable carrier for oral or topical administration and a pharmaceutically effective amount of compound having the formula: ##STR46## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
152 words
A pharmaceutical composition suitable for the treatment of allergies, said composition in the form of a tablet, pill, capsule, cream, paste, aerosol formulation which is a suspension or solution in a liquified propellant, or powder for insufflation admixed with a diluent powder which comprises a suitable carrier for oral or topical administration and a pharmaceutically effective amount of compound having the formula: ##STR46## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 12
Independent Claim
122 words
A method for the prevention and treatment of allergic conditions, said method comprising the administration to a host in need thereof of a therapeutically effective amount of a compound of the formula: ##STR47## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 13
Independent Claim
122 words
A method for the prevention and treatment of allergic conditions, said method comprising the administration to a host in need thereof of a therapeutically effective amount of a compound of the formula: ##STR47## wherein R is a carboxy group or a group --COOR 13 , wherein R 13 is C 1 -C 12 alkyl; R 5 is hydrogen, allyl or propyl; each of R 7 and R 8 , which may be the same or different, is hydrogen or a radical --(O) m --R 14 , wherein m is zero or 1 and R 14 is a C 1 -C 6 alkyl group, which is unsubstituted or substituted with hydroxy or C 1 -C 6 alkoxy; and a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim
40 words
A method of claim 9 wherein said compound is selected from the group consisting of: 6-carboxy-flavone, 6-carboxy-2'-isopropoxy-flavone, 6-carboxy-2'-methoxy-flavone, 6-carboxy-2'-ethoxy-flavone, 6-carboxy-2'-propoxy-flavone, 6-carboxy-2'-butoxy-flavone, 6-carboxy-2'-(2-methyl-propoxy)-flavone, 6-carboxy-2'-(1-methyl-propoxy)-flavone, 6-carboxy-2'-(2-ethoxy-ethoxy)-flavone, 6-carboxy-4'-(2-ethoxy-ethoxy)-flavone, 6-carboxy-2'-(2-hydroxy-ethoxy)-flavone, 6-carboxy-2'-(2-hydroxy-propoxy)-flavone, 6-carboxy-2'-(3-hydroxy-propoxy)-flavone, 6-carboxy-2'-(2,3-dihydroxy-propoxy)-flavone, 6-carboxy-2'-(2-hydroxy-butoxy)-flavone, 6-carboxy-2'-(2-hydroxy-2-methyl-propoxy)-flavone, 6-carboxy-2'-(2-hydroxy-2-methyl-butoxy)-flavone, 6-carboxy-2'-(2-hydroxy-3-methyl-butoxy)-flavone, 6-carboxy-4'-(2-hydroxy-propoxy)-flavone, and a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
25 words
A method of claim 9, wherein said allergic conditions are selected from the group consisting of bronchial asthma, allergic rhinitis, hay fever, urticaria and dermatosis.
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) | 1981-04-10 | 1981-10-10 | 1982-04-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-04-10 | 1985-10-10 | 1986-04-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-04-10 | 1989-10-10 | 1990-04-11 | $7700.00 | Window Closed / Lapsed |