Reversal of multi-drug resistance by triphenyl-azacycloalkane derivatives
AssigneeMerrell Pharmaceuticals Inc.
InventorsJules Freedman, Sai P. Sunkara
Life of this patent
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Abstract
Certain triphenylpiperidines reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.
Claims4
A method of reversing multidrug resistance in a patient having a multidrug resistant tumor which comprises administering to the patient a nontoxic multidrug resistance reversing amount of a compound of the formula ##STR3## wherein Ph.sub.1 is a phenyl substituted with one or two (C.sub.1 -C.sub.4)alkoxy groups;
- Ph.sub.2, and Ph.sub.3 are each a phenyl group;
- n is an integer 2;
- m is an integer 1;
- and
- q is an integer of from 1 to 2;
- or an acid addition salt thereof.
A compound that is selected from the group consisting of
- 1-(3,4-Dimethoxyphenylacetyl)-2-(2,2-diphenylethyl)piperidine;
- 1-(3,4,5-trimethoxyphenylacetyl)-2-(2,2-diphenylethyl)piperidine;
- 1-(3,4-dichlorophenylacetyl)-2-(2,2-diphenylethyl)piperidine;
- 1-(3,4-dimethoxyphenylpropionyl)-2-(2,2-diphenylethyl)piperidine;
- 1-(3,4,5-trimethoxyphenylacetyl)-2-2,2-bis-(4-methylphenyl)ethyl!piperidin e;
- and
- 1-(2-methoxyphenylacetyl)-2-(2,2-diphenylethyl)piperidine.
Dependencies are inferred from the claim text.