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Claims for Patent: 3,878,217

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Claims for Patent: 3,878,217

Title: Alpha-aryl-4-substituted piperidinoalkanol derivatives
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 within this invention.
Inventor(s): Carr; Albert A. (Cincinnati, OH), Kinsolving; Richard (Cincinnati, OH)
Assignee: Richardson-Merrell Inc. (New York, NY)
Application Number:05/378,561
Patent Claims: 1. A compound selected from a base of the formula ##SPC6##

wherein R is selected from the group consisting of hydrogen or hydroxy; R.sup.1 is 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; and Z is selected from the group consisting of thienyl, phenyl, or substituted phenyl wherein the substituents on the substituted pheny 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 lower 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, or a saturated monocyclic heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, morpholino, or N-(lower)alkylpiperazino, or pharmaceutically acceptable acid addition salts thereof.

2. A compound of claim 1 where R is hydrogen.

3. A compound of claim 2 wherein n is 3.

4. A compound of claim 3 which is 4-(diphenylmethyl)-.alpha.-phenyl-1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

5. A compound of claim 3 which is 4-(diphenylmethyl)-.alpha.-(p-fluorophenyl)-1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

6. A compound of claim 1 wherein R is hydroxy.

7. A compound of claim 6 wherein n is 3.

8. A compound of claim 7 which is .alpha.-(p-fluorophenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-piperi dinebutanol or a pharmaceutically acceptable acid addition salt thereof.

9. A compound of claim 7 which is .alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-pi peridinebutanol or a pharmaceutically acceptable acid addition salt thereof.

10. A compound of claim 7 which is 4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-.alpha.-(2-thienyl)-1-piperidineb utanol or a pharmaceutically acceptable acid addition salt thereof.

11. A compound of claim 7 which is 4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-.alpha.-(p-piperidinophenyl)-1-pi peridinebutanol or a pharmaceutically acceptable acid addition salt thereof.

12. A compound of claim 7 which is 4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-.alpha.-(p-dimethylaminophenyl)-1 -piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

13. A compound of claim 6 wherein n is 1.

14. A compound of claim 13 which is .alpha.-(p-fluorophenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-piperi dineethanol or a pharmaceutically acceptable acid addition salt thereof.

15. A compound of claim 1 wherein R and R.sup.1 taken together form a second bond between the carbon atoms bearing R and R.sup.l.

16. A compound of claim 15 wherein n is 3.

17. A compound of claim 16 which is .alpha.-(p-bromophenyl)-4-(diphenylmethylene)-1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

18. A compound of claim 16 which is .alpha.-(p-fluorophenyl)-4-(diphenylmethylene)-1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

19. The compound (+)-.alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)- 1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.

20. The compound (-)-.alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)- 1-piperidinebutanol or a pharmaceutically acceptable acid addition salt thereof.
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