Claims
- 1. A method of preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema of a mammal in need thereof comprising administration to the mammal of a prophylactically effective amount of a tricyclic compound of formula I
- wherein Z.sup.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 has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl; Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is 5-(1-alkyl)tetrazolyl or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl or carboxyl; or Z.sup.2 is a substituent in the 5-, 6-, 7-, or 8-position selected from the group consisting of Z.sup.1 as defined above, carboxyl, alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl or alkoxy wherein the "alkyl" moiety of each of the alkyl, alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms; and Z.sup.3 is carbonyl; or a pharmaceutically acceptable salt thereof.
- 2. A method as claimed in claim 1 wherein the tricyclic compound is of formula II ##STR4## wherein Z.sup.1 is a substituent in the 3-position and is 5-tetrazolyl and Z.sup.2 is a substituent in the 5-, 6-, 7-, or 8-position selected from carboxyl, 5-tetrazolyl, nitro, chloro, bromo, or alkyl having 1 to 3 carbon atoms; or a pharmaceutically acceptable salt thereof.
- 3. A method as claimed in claim 1 wherein the tricyclic compound is of formula V ##STR5## wherein Z.sup.3 is as defined in claim 1, Z.sup.1 is selected from the group consisting of 5-tetrazolyl and a 5-tetrazolyl salt and Z.sup.2 is selected from the group consisting of carboxyl, a pharmaceutically acceptable carboxylate salt, alkyl carboxylate having 1 to 6 carbon atoms in the alkyl moiety thereof, carboxamide optionally N-substituted by alkyl having 1 to 6 carbon atoms, 5-tetrazolyl, and a 5-tetrazolyl salt.
- 4. A method as claimed in claim 1 wherein the tricyclic compound is selected from the group consisting of 7-methyl-3-(5-tetrzolyl) thioxanthone-10,10-dioxide; and a pharmaceutically acceptable salt thereof.
- 5. A method as claimed in claim 4 wherein said salt is the sodium salt.
- 6. A method as claimed in claim 4 wherein said tricyclic compound or salt thereof is administered by the oral route.
- 7. A method as claimed in claim 6 wherein said tricyclic compound or salt thereof is administered at a dose of 1 to 50 mg. per kilogram body weight of said mammal.
- 8. A method as claimed in claim 7 wherein said allergic condition is allergic asthma.
- 9. A method as claimed in claim 7 wherein said allergic condition is hay fever.
- 10. A method as claimed in claim 1 wherein administration is effected by the pulmonary route.
- 11. A method as claimed in claim 10 wherein the tricyclic compound is administered as a powder having a particle size in the range of 0.5 to 7.mu..
- 12. A method as claimed in claim 11 wherein the tricyclic compound is administered at a dose of 5.mu. to 0.5 mg. per kilogram body weight of said mammal.
- 13. A method as claimed in claim 1 wherein administration is effected by the oral route.
- 14. A method as claimed in claim 13 wherein the tricyclic compound is administered at a dose of 1 to 50 mg. per kilogram body weight of said mammal.
- 15. A method as claimed in claim 1 wherein the tricyclic compound is of formula III ##STR6## wherein Z.sup.1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, 5-tetrazolyl salt, 5-(1-alkyl)tetrazolyl or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms, Z.sup.2 is hydrogen (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is carboxyl, 5-(1-alkyl)tetrazolyl, or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl, or Z.sup.2 is a substituent in the 5-, 6-, 7-, or 8-position and has the same values as the group Z.sup.1 as defined above or is alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkanoyl, alkyl or alkoxy wherein the "alkyl" moiety of each of the alkyl and alkoxy, have 1 to 6 carbon atoms and Z.sup.3 is carbonyl.
- 16. A method of preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema of a mammal in need thereof comprising administration to the mammal of a prophylactically effective amount of a tricyclic compound of formula XI wherein ##STR7## Z.sup.3 is carbonyl Z.sup.1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, a 5-tetrazolyl salt, 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 hydroxy, carboxyl and Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is 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 hydroxy, carboxyl or Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z.sup.1 as defined above or is alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl, or alkoxy wherein the "alkyl" moiety of each of the alkyl, alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms, carboxyl, a carboxylate salt, alkyl carboxylate wherein the alkyl moiety has 1 to 6 carbon atoms, or a carboxamide group optionally N-substituted by alkyl having 1 to 6 carbon atoms.
- 17. A method of preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema of a mammal in need thereof comprising administration to the mammal of a prophylactically effective amount of a tricyclic compound of formula XII ##STR8## wherein Z.sup.1 is a substitutent in the 3-position and is a 5-tetrazolyl or 5-tetrazolyl salt group; Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from the values of the group Z.sup.1 defined above or is alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl or alkoxy wherein the "alkyl" moiety of alkanoyl alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms or a carboxyl; and Z.sup.3 is carbonyl.
- 18. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective, non-toxic amount of a tricyclic compound of formula I ##STR9## wherein Z.sup.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 has 1 to 6 carbon atoms and are each optionally substituted by a hydroxyl; Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 3-position and is 5-(1-alkyl)tetrazolyl or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl or carboxyl; or Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z.sup.1 as defined above or is carboxyl, alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl or alkoxy wherein the "alkyl" moiety of each of the alkyl, alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms; and Z.sup.3 is carbonyl; or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier therefor.
- 19. A pharmaceutical composition as claimed in claim 18 wherein the pharmaceutically acceptable salt is selected from sodium, potassium, magnesium, calcium, or ammonium salts.
- 20. A composition as claimed in claim 18 wherein the composition is in the form of a discrete dosage unit each containing an effective antiallergic, nontoxic amount of said tricyclic compound.
- 21. A composition as claimed in claim 20 wherein the composition is in the form of a tablet, capsule, lozenge or sachet.
- 22. A composition as claimed in claim 20 wherein the composition is in the form of a coated, moisture resistant tablet.
- 23. A composition as claimed in claim 20 wherein each discrete unit contains from 50 to 500 mg. of said tricyclic compound.
- 24. A pharmaceutical composition as claimed to claim 18 wherein said tricyclic compound is in the form of a powder suitable for pulmonary administration.
- 25. A composition as claimed in claim 24 wherein the composition comprises a self-propelling aerosol composition in a sealed valved container in which said tricyclic compound is dispersed in a liquid propellant.
- 26. A pharmaceutical composition as claimed in claim 24 wherein said powdered tricyclic compound is incorporated in a capsule suitable for use in an inhalation device.
- 27. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of a tricyclic compound of formula (II) ##STR10## wherein Z.sup.1 is a substituent in the 3-position and is 5-tetrazolyl and Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is carboxyl, 4-(1-alkyl) tetrazolyl, or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl; and Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from carboxyl, 5-tetrazoyly, nitro, chloro, bromo, or alkyl having 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
- 28. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of a tricyclic compound of formula III ##STR11## wherein Z.sup.1 is a substituent in the 1-, 2-, 3-, or 4-position and is 5-tetrazolyl, a 5-tetrazolyl salt, a 5-(1-alkyl)tetrazolyl or a 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by carboxyl; Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is 5-(1-alkyl)tetrazolyl or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl, or Z.sup.2 is a substituent in the 5-, 6-, 6- or 8-position and has the same values as the group Z.sup.1 as defined above or is a carboxyl, a pharmaceutically acceptable carboxylate salt, a alkyl carboxylate wherein the alkyl moiety has 1 to 6, carbon atoms a carboxamide optionally N-substituted by alkyl having 1 to 6 carbon atoms alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl or alkoxy wherein the "alkyl" moiety of each of the alkyl, alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms; and Z.sup.3 is carbonyl; in association with a pharmaceutically acceptable carrier therefor.
- 29. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically non-toxic amount of a tricyclic compound of formula V ##STR12## wherein Z.sup.3 is carbonyl, Z.sup.1 is selected from 5-tetrazolyl and a 5-tetrazolyl salt and Z.sup.2 is selected from carboxyl, a pharmaceutically acceptable carboxylate salt, alkyl carboxylate having 1 to 6 carbon atoms in the alkyl moiety thereof, carboxamide optionally N-substituted by alkyl having 1 to 6 carbon atoms, 5-tetrazolyl, and a 5-tetrazolyl salt in association with a pharmaceutically acceptable carrier therefor.
- 30. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, conjunctivitis, urticaria or eczema comprising a prophylactically effective non-toxic amount of 7-methyl-3-(5-tetrazolyl) thioxanthone-10, 10-dioxide; or a pharmaceutically acceptable salt thereof; in association with a pharmaceutically acceptable carrier therefor.
- 31. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, comprising effective non-toxic amount of a tricyclic comound of formula X1 wherein ##STR13## Z.sup.3 is carbonyl; Z.sup.1 is a substituent in the 1-, 2-, 4-, or 4-position and is 5-tetrazolyl, a 5-tetrazolyl salt, 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, carboxyl; and Z.sup.2 is hydrogen when (a) Z.sup.1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z.sup.1 is in the 3-position and is 5-(1-alkyl)tetrazolyl or 5-(2-alkyl)tetrazolyl in which the alkyl has 1 to 6 carbon atoms and are each optionally substituted by hydroxyl; or Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from the values of Z.sup.1 as defined above or is alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl, or alkoxy wherein the "alkyl" moiety of each of the alkyl, alkoxy, thioalkyl, alkylsulphinyl and alkylsulphonyl groups has 1 to 6 carbon atoms, carboxyl, a carboxylate salt group, an alkyl carboxylate group wherein the alkyl moiety has 1 to 6 carbon atoms, or carboxamide optionally N-substituted by alkyl having 1 to 6 carbon atoms.
- 32. A pharmaceutical composition for use in preventing the symptoms of allergic conditions consisting of asthma, allergic rhinitis, uticaria, conjunctivitis or eczema comprising a prophylactically effective non-toxic amount of a tricyclic compound of formula XII ##STR14## wherein Z.sup.1 is a substituent in the 3-position and is a 5-tetrazolyl or 5-tetrazolyl salt; Z.sup.2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z.sup.1 defined above, alkylsulphonyl, alkylsulphinyl, thioalkyl, amino, nitro, cyano, halogen, alkyl or alkoxy wherein the "alkyl" moiety of alkoxy, alkyl, thioalkyl, alkylsulphinyl and alkylsulphonyl has 1 to 6 carbon atoms, and carboxyl, and Z.sup.3 is carbonyl.
Parent Case Info
This application is a continuation-in-part of U.S. Pat. Application Ser. No. 361,523 filed May 18, 1973, now U.S. Pat. No. 3,905,989, issued Sept. 16, 1975.
US Referenced Citations (13)
Non-Patent Literature Citations (1)
Entry |
Physicians Desk Reference (PDR), (1974), pp. 760-761. |