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Claims for Patent: 6,187,791

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Claims for Patent: 6,187,791

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: Merrell Pharmaceuticals Inc. (Bridgewater, NJ)
Application Number:09/481,404
Patent Claims: 1. A method of treating a histaminic-mediated condition in a patient in need thereof but susceptible to possible 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 enantiomers thereof.

2. A method of claim 1 wherein the compound is 4-[1-hydroxy-4-[4-(hydroxydiphenymethyl)-1-piperidinyl]butyl]-.alpha.,.alp ha.-dimethyl benzeneacetic acid.

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

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

5. A method of treating a histamine-mediated disease in a human while avoiding the concomitant liability of cardiac arrhythmias associated with the administration of terfenadine, comprising administering to said human a therapeutically effective amount of racemic terfenadine carboxylate or a pharmaceutically acceptable salt thereof.

6. The method of claim 5 wherein the amount of racemic terfenadine carboxylate administered is from about 20 mg to about 800 mg per day.

7. The method of claim 6 wherein the amount of racemic terfenadine carboxylate administered is from about 40 mg to about 360 mg per day.

8. The method of claim 5 wherein the amount of said racemic terfenadine carboxylate or pharmaceutically acceptable salt thereof is administered together with a pharmaceutically acceptable carrier.

9. In a method of providing an antihistaminic effect in a patient susceptible to QT prolongation and/or ventricular tachycardia when using terfenadine, the improvement which comprises administering to said patient an effective amount of a compound of the formula: ##STR4##

wherein

R.sub.1 is hydrogen or hydroxy;

R.sub.2 is hydrogen;

or R.sub.1 and R2 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 enantiomers thereof.
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