Antiallergic cyclic sulphur compounds

Claim 3

A method as claimed in claim 1 wherein the tricyclic compound is of formula II ##STR4## wherein Z 1 is a substituent in the 3-position and is 5-tetrazolyl and Z 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.

Claim 4

A method as claimed in claim 1 wherein the tricyclic compound is of formula V ##STR5## wherein Z 3 is as defined in claim 1, Z 1 is selected from the group consisting of 5-tetrazolyl and a 5-tetrazolyl salt and Z 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.

Claim 5

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.

Claim 6

A method as claimed in claim 4 wherein said salt is the sodium salt.

Claim 7

A method as claimed in claim 4 wherein said tricyclic compound or salt thereof is administered by the oral route.

Claim 8

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.

Claim 9

A method as claimed in claim 7 wherein said allergic condition is allergic asthma.

Claim 10

A method as claimed in claim 7 wherein said allergic condition is hay fever.

Claim 11

A method as claimed in claim 1 wherein administration is effected by the pulmonary route.

Claim 12

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 7μ.

Claim 13

A method as claimed in claim 11 wherein the tricyclic compound is administered at a dose of 5μ to 0.5 mg. per kilogram body weight of said mammal.

Claim 14

A method as claimed in claim 1 wherein administration is effected by the oral route.

Claim 15

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.

Claim 16

A method as claimed in claim 1 wherein the tricyclic compound is of formula III ##STR6## wherein Z 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 2 is hydrogen (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 2 is 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 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 3 is carbonyl.

Claim 21

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 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 2 is hydrogen when (a) Z 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 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z 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 3 is carbonyl; or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier therefor.

Claim 22

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 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 2 is hydrogen when (a) Z 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 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z 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 3 is carbonyl; or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier therefor.

Claim 23

A pharmaceutical composition as claimed in claim 18 wherein the pharmaceutically acceptable salt is selected from sodium, potassium, magnesium, calcium, or ammonium salts.

Claim 24

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.

Claim 25

A composition as claimed in claim 20 wherein the composition is in the form of a tablet, capsule, lozenge or sachet.

Claim 26

A composition as claimed in claim 20 wherein the composition is in the form of a coated, moisture resistant tablet.

Claim 27

A composition as claimed in claim 20 wherein each discrete unit contains from 50 to 500 mg. of said tricyclic compound.

Claim 28

A pharmaceutical composition as claimed to claim 18 wherein said tricyclic compound is in the form of a powder suitable for pulmonary administration.

Claim 29

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.

Claim 30

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.

Claim 31

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 1 is a substituent in the 3-position and is 5-tetrazolyl and Z 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 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.

Claim 32

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 1 is a substituent in the 3-position and is 5-tetrazolyl and Z 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 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.

Claim 33

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 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 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 2 is a substituent in the 5-, 6-, 6- or 8-position and has the same values as the group Z 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 3 is carbonyl; in association with a pharmaceutically acceptable carrier therefor.

Claim 34

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 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 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 2 is a substituent in the 5-, 6-, 6- or 8-position and has the same values as the group Z 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 3 is carbonyl; in association with a pharmaceutically acceptable carrier therefor.

Claim 35

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 3 is carbonyl, Z 1 is selected from 5-tetrazolyl and a 5-tetrazolyl salt and Z 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.

Claim 36

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 3 is carbonyl, Z 1 is selected from 5-tetrazolyl and a 5-tetrazolyl salt and Z 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.

Claim 37

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.

Claim 38

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.

Claim 39

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 3 is carbonyl; Z 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 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the values of Z 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.

Claim 40

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 3 is carbonyl; Z 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 2 is hydrogen when (a) Z 1 is in the 1-, 2-, or 4-position and has the same meaning as above and (b) when Z 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 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the values of Z 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.

Claim 41

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 1 is a substituent in the 3-position and is a 5-tetrazolyl or 5-tetrazolyl salt; Z 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z 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 3 is carbonyl.

Claim 42

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 1 is a substituent in the 3-position and is a 5-tetrazolyl or 5-tetrazolyl salt; Z 2 is a substituent in the 5-, 6-, 7- or 8-position selected from the group consisting of Z 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 3 is carbonyl.