Agents for potentiating the effects of antitumor agents and combating multiple drug resistance
AssigneeBurroughs Wellcome Co.
InventorAnn C. King
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Abstract
Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are 2-(aminoethylamino) pyridines such as (E)-3-(6-(N-(2-Dimethylaminoethyl)-4-methoxybenzylamino)-2-pyridyl)acrylic acid.
Claims10
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 selected from the class consisting of ##STR3## wherein:
- R.sub.1 is selected from the class consisting of halogen, --COOH, --CH.dbd.CH--COOH, --CH.sub.2 COOH, or --(CH.sub.2).sub.2 COOH;
- R.sub.2 is selected from the class consisting of hydrogen, halogen, C.sub.1-4 alkoxy and C.sub.1-4 alkyl;
- and
- R.sub.3 and R.sub.4 are the same or different and are selected from the class consisting of hydrogen and C.sub.1-4 alkyl, or NR.sub.3 R.sub.4 is pyrrolidino;
- and the pharmaceutically acceptable salts thereof, said potentiating agent being provided 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 antineoplatic agent and a potentiating agent in an amount effective to enhance the efficacy of said antineoplastic agent, said potentiating agent selected from the class consisting of ##STR4## wherein:
- R.sub.1 is selected from the class consisting of halogen, --COOH, --CH.dbd.CH--COOH, --CH.sub.2 COOH, or --(CH.sub.2).sub.2 COOH;
- R.sub.2 is selected from the class consisting of hydrogen, halogen, C.sub.1-4 alkoxy and C.sub.1-4 alkyl;
- and
- R.sub.3 and R.sub.4 are the same or different and are selected from the class consisting of hydrogen and C.sub.1-4 alkyl, or NR.sub.3 R.sub.4 is pyrrolidino;
- and the pharmaceutically acceptable salts thereof, said potentiating agent being provided in an amount effective to increase the sensitivity of said tumor to said antineoplastic agent.
Dependencies are inferred from the claim text.