Agents for potentiating the effects of antitumor agents and combating multiple drug resistance
AssigneeBurroughs Wellcome Co.
InventorAnn C. King
Life of this patent
Estimating the term…
Abstract
Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are dibenz[b,e]oxepins such as doxepin.
Claims20
A method of increasing the sensitivity of a tumor to an antineoplastic agent, which tumor is harbored in a subject and which tumor is resistant to said antineoplastic agent, comprising concurrently administering to said subject an antineoplastic agent and a potentiating agent, said potentiating agent comprising a compound of the formula:
- ##STR4## wherein:
- R.sub.1 is selected from the group consisting of --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 --, and --CH.sub.2 NH--;
- X is selected from the group consisting of hydrogen and halogen;
- Y is selected from the group consisting of hydrogen and halogen;
- n is from 0 to 3;
- each of p and q is from 1 to 4;
- and
- R.sub.2 and R.sub.3 are each independently selected from the group consisting of hydrogen and C.sub.1-4 alkyl, or together with the nitrogen atom form a nitrogen-containing heterocyclic ring having four to six ring members;
- or a pharmaceutically acceptable salt thereof, said potentiating agent being administered in an amount effective to increase the sensitivity of said tumor to said antineoplastic agent.
A pharmaceutical formulation comprising, in a pharmaceutically acceptable carrier, a tumor-inhibiting amount of an antineoplastic agent and a potentiating agent in an amount effective to enhance the efficacy of said antineoplatic agent, said potentiating agent comprising a compound of the formula:
- ##STR5## wherein:
- R.sub.1 is selected from the group consisting of --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 --, and --CH.sub.2 NH--;
- X is selected from the group consisting of hydrogen and halogen;
- Y is selected from the group consisting of hydrogen and halogen;
- n is from 0 to 3;
- each of p and q is from 1 to 4;
- and
- R.sub.2 and R.sub.3 are each independently selected from the group consisting of hydrogen and C.sub.1-4 alkyl, or together with the nitrogen atom form a nitrogen-containing heterocyclic ring having four to six ring members;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.