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Claims for Patent: 3,965,257

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Claims for Patent: 3,965,257

Title: Compositions and methods for the treatment of the symptoms of histamine induced allergic reactions
Abstract:Novel compounds useful as antihistamine agents, antiallergy agents, and bronchodilators are represented by the following formula ##SPC1## Wherein R represents hydrogen or hydroxy; R.sup.1 represents hydrogen; or R and R.sup.1 taken together form a second bond between the carbon atoms bearing R and R.sup.1 ; n is a positive whole integer of from 1 to 3; Z represents thienyl, phenyl, or substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta, or para positions of the phenyl ring and are selected from halogen, a straight or branched lower alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, di(lower)alkylamino, or a saturated monocyclic heterocyclic group such as pyrrolidino, piperidino, morpholino, or N-(lower)alkylpiperazino. Pharmaceutically acceptable acid addition salts and individual optical isomers of compounds of the above formula are also included as a part of this invention.
Inventor(s): Carr; Albert A. (Cincinnati, OH), Kinsolving; C. Richard (Cincinnati, OH)
Assignee: Richardson-Merrell Inc. (Wilton, CT)
Application Number:05/437,161
Patent Claims: 1. A pharmaceutical composition in unit dosage form containing from about 1 to 5 milligrams of a compound of the formula ##SPC6##

wherein R is selected from the group consisting of hydrogen and hydroxy; n is a positive integer of from 1 to 3; and Z is selected from the group consisting of thienyl, phenyl, and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta, or para positions of the substituted phenyl ring and are selected from the group consisting of a halogen atom, a straight or branched alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, a di(lower)alkylamino group, and a saturated monocyclic heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, morpholino, and N-(lower)alkylpiperazino; and a pharmaceutically acceptable acid addition salt thereof and a significant amount of a pharmaceutically acceptable carrier.

2. A composition of claim 1 wherein R represents hydroxy and n is 3.

3. A composition of claim 2 wherein the compound is 4'-tert-butyl-4-[4-(.alpha.-hydrozy-.alpha.-phenylbenzyl)piperidino]butyro phenone or a pharmaceutically acceptable acid addition salt thereof.

4. A composition of claim 2 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'methoxybutyrophen one or a pharmaceutically acceptable acid addition salt thereof.

5. A composition of claim 2 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-1-(2-thienyl)-1-but anone or a pharmaceutically acceptable acid addition salt thereof.

6. A composition of claim 2 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'-piperidinobutyro phenone or a pharmaceutically acceptable acid addition salt thereof.

7. A composition of claim 2 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]butyrophenone or a pharmaceutically acceptable acid addition salt thereof.

8. A composition of claim 2 wherein the compound is 4'-fluoro-4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-butyrophe none or a pharmaceutically acceptable acid addition salt thereof.

9. A composition of claim 2 wherein the compound is 4'-ethyl-4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-butyrophen one or a pharmaceutically acceptable acid addition salt thereof.

10. A composition of claim 2 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'-methylbutyrophen one hydrochloride or a pharmaceutically acceptable acid addition salt thereof.

11. A composition of claim 1 wherein said composition is in the form of a solid.

12. A composition of claim 1 wherein said composition is in a form suitable for injection.

13. A composition of claim 1 wherein said composition is in the form of an aerosol.

14. A method of treating the symptoms of an allergic reaction due to histamine in a patient comprising administering to said patient from 0.01 to 20 milligrams per kilogram of body weight of the patient a compound of the formula: ##SPC7##

wherein R is selected from the group consisting of hydrogen and hydroxy; n is a positive integer of from 1 to 3; and Z is selected from the group consisting of thienyl, phenyl, and substituted phenyl wherein the substituents on the substituted phenyl amy be attached at the ortho, meta, or para positions of the substituted phenyl ring and are selected from the group consisting of a halogen atom, a straight or branched alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, a di(lower) alkylamino group, and a saturated monocyclic heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, morpholino, and N-(lower)alkylpiperazino; and a

16. A method of claim 15 wherein the compound is 4'-fluoro-2-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]acetopheno

18. A method of claim 17 wherein the compound is 4'-tert-butyl-4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]butyro

19. A method of claim 17 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'-methoxybutyrophe

20. A method of claim 17 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-1-(2-thienyl)-1-but

21. A method of claim 17 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'-piperidinobutyro

22. A method of claim 17 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]butyrophenone or a

23. A method of claim 17 wherein the compound is 4'-fluoro-4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino[-butyrophe

24. A method of claim 17 wherein the compound is 4'-ethyl-4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-butyrophen

25. A method of claim 17 wherein the compound is 4-[4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)piperidino]-4'-methylbutyrophen one hydrochloride or a pharmaceutically acceptable acid addition salt

26. A method of inducing bronchial dilation in a patient suffering from bronchial constriction comprising administering to said patient from 0.01 to 20 milligrams per kilogram of body weight of the patient of a compound of the formula ##SPC8##

wherein R is selected from the group consisting of hydrogen and hydroxy; n is a positive integer of from 1 to 3; and Z is selected from the group consisting of thienyl, phenyl, and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta, or para positions of the substituted phenyl ring and are selected from the group consisting of a halogen atom, a straight or branched alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, a di(lower)alkylamino group, and a saturated monocyclic heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, morpholino, and N-(lower)alkylpiperazino; and a

27. A method of claim 26 wherein R is hydroxy and n is equal to 3.
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