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Generated: June 22, 2017

DrugPatentWatch Database Preview

Claims for Patent: 6,399,632

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Claims for Patent: 6,399,632

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:09/663,343
Patent Claims: 1. A method of treating a histamine-mediated condition in a patient in whom terfenadine is not metabolized at the normal rate to the terfenadine acid metabolite, while avoiding the concomitant liability of cardiac arrhythmias associated with the administration of terfenadine, said method comprising administering to said patient an effective amount of the compound 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the amount of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof administered is from about 20 mg to about 800 mg per day.

3. The method of claim 2 wherein the amount of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof administered is from about 40 mg to about 360 mg per day.

4. The method of claim 1 wherein the 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof is administered together with a pharmaceutically acceptable carrier.

5. A method of treating a histamine-mediated condition in a patient in whom terfenadine is not metabolized at the normal rate to the terfenadine acid metabolite, comprising administering to said patient a therapeutically effective amount of the compound 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof.

6. The method of claim 5 wherein the amount of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof administered is from about 20 mg to about 800 mg per day.

7. The method of claim 6 wherein the amount of 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof administered is from about 40 mg to about 360 mg per day.

8. The method of claim 5 wherein the 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt is administered together with a pharmaceutically acceptable carrier.

9. In a method of providing an antihistaminic effect in a patient in whom terfenadine is not metabolized at the normal rate to the terfenadine acid metabolite and who is subject to QT prolongation and/or ventricular tachycardia when using terfenadine, the improvement which comprises administering an effective amount of the compound 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.al pha.-dimethylbenzeneacetic acid or a pharmaceutically acceptable salt thereof.

10. The method of obtaining an anti-histaminic effect in a human in need of such effect but who has also received a product which inhibits terfenadine metabolism, said method comprising administering to said human, an anti-histaminically effective amount of 4-[-1-hydroxy-4-[4-hydroxy-diphenylmethyl)-1-piperidinyl]butyl]-.alpha.,.a lpha.-dimethyl-benzene acetic acid.
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