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Claims for Patent: 4,254,129

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Claims for Patent: 4,254,129

Title: Piperidine derivatives
Abstract:Novel compounds of the following formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is an integer of from 1 to 5; R.sub.3 is --CH.sub.3, --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; and each of A and B is hydrogen or hydroxy; with the provisos that at least one of A or B is hydrogen and one of A or B is other than hydrogen when R.sub.3 is --CH.sub.3 ; and pharmaceutically acceptable salts thereof.
Inventor(s): Carr; Albert A. (Cincinnati, OH), Dolfini; Joseph E. (Cincinnati, OH), Wright; George J. (Richmond, VA)
Assignee: Richardson-Merrell Inc. (Wilton, CT)
Application Number:06/028,813
Patent Claims: 1. A compound of the formula ##STR13## wherein R.sub.1 represents hydrogen or hydroxy; R.sub.2 represents hydrogen; or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ; n is an integer of from 1 to 5; R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A and B is hydrogen or hydroxy; with the proviso that at least one of A or B is hydrogen; and pharmaceutically acceptable salts and individual optical isomers thereof.

2. A compound of claim 1 wherein R.sub.1 is hydrogen or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2.

3. A compound of claim 2 wherein n is 3 or 4.

4. A compound of claim 2 wherein R.sub.3 is --COOalkyl.

5. A compound of claim 2 wherein R.sub.3 is --COOH.

6. A compound of claim 1 of the formula ##STR14## wherein R.sub.4 is hydroxy and R.sub.5 is hydrogen, or R.sub.4 and R.sub.5 taken together form a second bond between the carbon atoms beraing R.sub.4 and R.sub.5 ; n is the integer 3; and R.sub.3 is --COOH or a pharmaceuticaly acceptable salt thereof.

7. A compound of claim 1 which is ethyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-.alpha.,.al pha.-dimethylbenzene acetate or a pharmaceutically acceptable salt thereof.

8. A compound of claim 1 which is 4-[4-[-4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-.alpha.,.a lpha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof.

9. A compound of claim 1 which is 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-.alpha.,.al pha.-dimethyl-(3-hydroxybenzene)acetic acid or a pharmaceutically acceptable salt thereof.

10. A pharmaceutical composition in unit dosage form comprising an effective antiallergic amount of a compound of claim 1 and a significant amount of a pharmaceutically acceptable carrier.

11. A method of treating allergic reactions in a patient in need thereof which comprises administering to said patient an effective amount of a compound of claim 1.
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