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Last Updated: April 26, 2024

Claims for Patent: 6,037,353


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Summary for Patent: 6,037,353
Title: Method of providing an antihistaminic effect in a hepatically impaired patient
Abstract:The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the 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 --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; or a pharmaceutically acceptable salt and individual isomers thereof.
Inventor(s): Woodward; James K. (Cincinnati, OH), Okerholm; Richard A. (West Chester, OH), Eller; Mark G. (Overland Park, KS), McNutt; Bruce E. (Olathe, KS)
Assignee: Hoechst Marion Roussel, Inc. (Bridgewater, NJ)
Application Number:08/397,542
Patent Claims: 1. A method of treating a histamine-mediated condition in a patient having impaired liver function due to disease or due to administration of a concomitant drug which inhibits normal liver metabolic function while avoiding cardiac events associated with the administration of terfenadine, said method comprising administering to said patient an effective antihistaminic amount of a compound of the formula ##STR3## 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 --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;

or a pharmaceutically acceptable salt and individual isomers thereof.

2. A method of claim 1 wherein R.sub.1 is hydroxy.

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

4. A method of claim 3 wherein A and B are both hydrogen.

5. A method of claim 1 wherein the compound is 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethyl-benzeneacetic acid.

6. A method of claim 1 wherein the compound is (R)-4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha. ,.alpha.-dimethyl-benzeneacetic acid.

7. A method of claim 1 wherein the compound is (S)-4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha. ,.alpha.-dimethyl-benzeneacetic acid.

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