# US 5,346,897 A · Agents for potentiating the effects of antitumor agents and combating multiple drug resistance

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- Number: US 5,346,897 A
- Document ID: US5346897A
- Status: Granted
- Kind: A
- Application number: 07/899,711
- Filed: 1992-06-10
- Granted: 1994-09-13
- Earliest claimed: 1990-06-18
- Assignees: Burroughs Wellcome Co.
- Inventors: Ann C. King
- Web page: https://patentgrep.com/patent/US5346897A

## CPC

- C07D 295/073: with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- A61K 31/335: having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- C07D 213/55: Acids; Esters
- C07D 213/56: Amides
- C07D 295/096: with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 295/155: with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 313/12: [b,e]-condensed
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are acrivastine esters and the pharmaceutically acceptable salts thereof.

## Claims

### Claim 1

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 ##STR2## wherein R is C.sub.1-4 alkyl, and the pharmaceutically acceptable salts thereof, said potentiating agent being administered in an amount effective to increase the sensitivity of said tumor to said antineoplastic agent.

### Claim 2 (depends on 1)

A method according to claim 1, wherein said antineoplastic agent is administered to said subject parenterally and said potentiating agent is administered to said subject parenterally.

### Claim 3 (depends on 1)

A method according to claim 1, wherein said antineoplastic agent is selected from the class consisting of vinca alkaloids, epipodophyllotoxins, anthracycline antibiotics, actinomycin D, plicamycin, puromycin, gramicidin D, taxol, colchicine, cytochalasin B, emetine, maytansine, and amsacrine.

### Claim 4 (depends on 1)

A method according to claim 1, wherein said tumor is an adenocarcinoma.

### Claim 5 (depends on 1)

A method according to claim 1, wherein R is ethyl.

### Claim 6

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 antineoplastic agent, said potentiating agent selected from the class consisting of ##STR3## wherein R is C.sub.1-4 alkyl, and the pharmaceutically acceptable salts thereof.

### Claim 7 (depends on 6)

A pharmaceutical formulation as claimed in claim 6, wherein said antineoplastic agent is selected from the class consisting of vinca alkaloids, epipodophyllotoxins, anthracycline antibiotics, actinomycin D, plicamycin, puromycin, gramicidin D, taxol, colchicine, cytochalasin B, emetine, maytansine, and amsacrine.

### Claim 8 (depends on 7)

A pharmaceutical formulation as claimed in claim 7, wherein R is ethyl.