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US4025635A Expired / Lapsed US ⏱️ 0.0 years remaining

Cyclic sulphur compounds

Assignee: SmithKline Beecham Corp
•
Filing: 1973-09-05
•
Granted: 1977-05-24
•
Expires: 1993-09-05
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Abstract

Abstract Certain tricyclic sulphone compounds each of which is substituted in the 1-,2-,3- or 4-position by a carboxyl or (5-tetrazolyl) group and each of which is optionally substituted in the 5-,6-,7- or 8-position by a second carboxyl or (5-tetrazolyl) group or a substituent selected from cyano, halogen, nitro, alkyl, alkoxy, acyl, amino, acylamino, thioalkyl, alkylsulphinyl and alkylsulphonyl, as well as salts, and optionally substituted esters and amides of the carboxyl substituted compounds and alkyl derivatives of the tetrazolyl substituted compounds, are useful for the relief or prophylaxis of allergic conditions.

Inventors

  • 👤 Harold Francis Hodson
  • 👤 John Frederick Batchelor

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 13:28
CPC Classifications
C; C07; C07C; C07C317/00; C07C317/44; C07C323/00; C07C323/50; C07C323/62

Claims Analysis

Total Claims: 27
Claim 1
Independent Claim 55 words
The method of preventing the symptoms of an allergic condition of a mammal having an allergic condition which comprises administering to said mammal a prophylactically effective amount of a tricyclic compound: 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide; or a pharmaceutically acceptable salt thereof, said allergic condition being selected from the group consisting of asthma, allergic rhinitis, conjunctivitis, urticaria and eczema.
Claim 2
Independent Claim 55 words
The method of preventing the symptoms of an allergic condition of a mammal having an allergic condition which comprises administering to said mammal a prophylactically effective amount of a tricyclic compound: 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide; or a pharmaceutically acceptable salt thereof, said allergic condition being selected from the group consisting of asthma, allergic rhinitis, conjunctivitis, urticaria and eczema.
Claim 3
Dependent Claim 25 words
The method of claim 1 wherein the tricyclic compound is administered as a powder having a particle size in the range of 0.5 to 7μ.
Claim 4
Dependent Claim 25 words
The method of claim 2 wherein the tricyclic compound is administered at a dose of 5μg. to 0.5mg. per kilogram body weight of said mammal.
Claim 5
Dependent Claim 20 words
A method as claimed in claim 1 wherein said tricyclic compound or salt thereof is administered by the oral route.
Claim 6
Dependent Claim 30 words
A method as claimed in claim 4 wherein said tricyclic compound or salt thereof is administered at a dose of 1 to 50mg. per kilogram body weight of said mammal.
Claim 7
Dependent Claim 14 words
A method as claimed in claim 5 wherein said allergic condition is allergic asthma.
Claim 8
Dependent Claim 14 words
A method as claimed in claim 5 wherein said allergic condition is hay fever.
Claim 9
Independent Claim 56 words
The method of preventing the symptoms of allergic asthma effecting a mammal having allergic asthma comprising the administration to said mammal of a prophylactic dose of 10 to 40 mg. per kilogram body weight of said mammal of a tricyclic compound selected from the group consisting of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide and a pharmaceutically acceptable salt of said compound.
Claim 10
Independent Claim 56 words
The method of preventing the symptoms of allergic asthma effecting a mammal having allergic asthma comprising the administration to said mammal of a prophylactic dose of 10 to 40 mg. per kilogram body weight of said mammal of a tricyclic compound selected from the group consisting of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide and a pharmaceutically acceptable salt of said compound.
Claim 11
Dependent Claim 12 words
The method of claim 8 wherein said salt is a sodium salt.
Claim 12
Independent Claim 155 words
The method of preventing the symptoms of an allergic condition of a mammal having an allergic condition which comprises administering to said mammal a prophylactically effective amount of a tricyclic compound of formula I ##STR3## wherein the tricyclic compound of formula I Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, a 5-(1-alkyl) tetrazolyl group or a 5-(2-alkyl) tetrazolyl group in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by hydroxy; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position and has the same values as the group Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing from 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof: said allergic condition selected from the group consisting of asthma, allergic rhinitis, conjunctivitis, urticaria and eczema.
Claim 13
Independent Claim 155 words
The method of preventing the symptoms of an allergic condition of a mammal having an allergic condition which comprises administering to said mammal a prophylactically effective amount of a tricyclic compound of formula I ##STR3## wherein the tricyclic compound of formula I Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, a 5-(1-alkyl) tetrazolyl group or a 5-(2-alkyl) tetrazolyl group in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by hydroxy; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position and has the same values as the group Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing from 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof: said allergic condition selected from the group consisting of asthma, allergic rhinitis, conjunctivitis, urticaria and eczema.
Claim 14
Independent Claim 129 words
The method of preventing the symptoms or asthma or allergic rhinitis in a mammal having astham or allergic rhinitis which comprises administering to said mammal a phophylactically effective amount of a compound of formula I ##STR4## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl) tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z 1 as defined above is is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof.
Claim 15
Independent Claim 129 words
The method of preventing the symptoms or asthma or allergic rhinitis in a mammal having astham or allergic rhinitis which comprises administering to said mammal a phophylactically effective amount of a compound of formula I ##STR4## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl) tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z 1 as defined above is is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof.
Claim 16
Independent Claim 44 words
The method of preventing the symptoms of asthma or allergic rhinitis in a mammal having asthma or allergic rhinitis which comprises administering in a form for oral or pulmonary administration a prophylactically effective amount of the compound 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof.
Claim 17
Independent Claim 44 words
The method of preventing the symptoms of asthma or allergic rhinitis in a mammal having asthma or allergic rhinitis which comprises administering in a form for oral or pulmonary administration a prophylactically effective amount of the compound 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim 41 words
A pharmaceutical composition for the prevention of the symptoms of asthma or allergic rhinitis and which is in a form for oral or pulmonary administration which comprises a prophylactically effective amount of the compound 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof.
Claim 19
Dependent Claim 41 words
A pharmaceutical composition for the prevention of the symptoms of asthma or allergic rhinitis and which is in a form for oral or pulmonary administration which comprises a prophylactically effective amount of the compound 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim 132 words
A pharmaceutical composition for use in the prevention of the symptoms of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of a tricyclic compound of formula I ##STR5## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl)tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
Claim 21
Dependent Claim 132 words
A pharmaceutical composition for use in the prevention of the symptoms of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of a tricyclic compound of formula I ##STR5## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl)tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
Claim 22
Dependent Claim 132 words
A pharmaceutical composition for the prevention of the symptoms of asthma or allergic rhinitis comprising an effective asthma or allergic rhinitis prophylactic amount of a tricyclic compound of formula I ##STR6## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl) tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the groups Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
Claim 23
Dependent Claim 132 words
A pharmaceutical composition for the prevention of the symptoms of asthma or allergic rhinitis comprising an effective asthma or allergic rhinitis prophylactic amount of a tricyclic compound of formula I ##STR6## wherein Z 1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl) tetrazolyl, in which the alkyl groups have 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl group; Z 2 is hydrogen or a substituent in the 5-, 6-, 7- or 8-position selected from the values of the groups Z 1 as defined above or is halogen, or an alkyl or alkoxy group each containing 1 to 6 carbon atoms; and Z 3 is oxygen; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
Claim 24
Dependent Claim 39 words
A pharmaceutical composition for use in preventing the symptoms of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier therefor.
Claim 25
Dependent Claim 39 words
A pharmaceutical composition for use in preventing the symptoms of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier therefor.
Claim 26
Dependent Claim 58 words
A tablet for use in preventing the symptoms of an allergic condition being selected from the group consisting of asthma, allergic rhinitis, conjuntivitis, urticaria and eczema and said tablet containing as an active ingredient from 50 to 500 mg. of a tricyclic compound selected from the group consisting of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide; and a pharmaceutically acceptable salt of said compound.
Claim 27
Dependent Claim 58 words
A tablet for use in preventing the symptoms of an allergic condition being selected from the group consisting of asthma, allergic rhinitis, conjuntivitis, urticaria and eczema and said tablet containing as an active ingredient from 50 to 500 mg. of a tricyclic compound selected from the group consisting of 2-(5-tetrazolyl)phenoxathiin-10,10-dioxide; and a pharmaceutically acceptable salt of said compound.

References Cited (Backward Citations)

US3706768A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-05-23 1980-11-22 1981-05-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-05-23 1984-11-22 1985-05-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-05-23 1988-11-22 1989-05-24 $7700.00 Window Closed / Lapsed

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