US5364843A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Agents for potentiating the effects of antitumor agents and combating multiple drug resistance
Assignee: SmithKline Beecham Corp
•
Filing: 1992-06-10
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Granted: 1994-11-15
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Expires: 2012-06-10
Abstract
Abstract Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are piperazinyl benzyl compounds such as 1-[α-(4-Chlorophenyl)-3-methoxybenzyl]-4-allylpiperazine dihydrochloride.
Inventors
- 👤 Ann C. King
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:15
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/06; C07D295/073; A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/395; A61K31/40; A61K31/435; A61K31/44; A61K31/495; A61K31/55; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/54; C07D213/55; C07D213/56; C07D295/08; C07D295/096; C07D295/14; C07D295/155; C07D313/00; C07D313/02; C07D313/06; C07D313/10; C07D313/12
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
140 words
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 1 is halogen; R 2 is selected from the class consisting of hydrogen, halogen, C 1-4 alkoxy, --OCH 2 C 6 H 5 , and --CH═CHCO 2 R, wherein R is C 1-4 alkyl; and R 3 is selected from the class consisting of C 1-4 alkyl, --CH 2 CH═CH 2 , and--CH 2 C 6 H 4 CH 3; 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
Independent Claim
140 words
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 1 is halogen; R 2 is selected from the class consisting of hydrogen, halogen, C 1-4 alkoxy, --OCH 2 C 6 H 5 , and --CH═CHCO 2 R, wherein R is C 1-4 alkyl; and R 3 is selected from the class consisting of C 1-4 alkyl, --CH 2 CH═CH 2 , and--CH 2 C 6 H 4 CH 3; 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 3
Dependent Claim
26 words
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 4
Dependent Claim
36 words
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 5
Dependent Claim
12 words
A method according to claim 1, wherein said tumor is an adenocarcinoma.
Claim 6
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-(3-Bromo-4'-chlorobenzhydryl)-4-methylpiperazine dihydrochloride.
Claim 7
Dependent Claim
13 words
A method according to claim 1, wherein said compound is (E)-Ethyl 3-(4-chloro-α-(4-methyl-l-piperazinyl)-benzyl)cinnamate dihydrochloride.
Claim 8
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-(3-Benzyloxy-4'-chlorobenzhydryl)-4-methylpiperazine dihydrochloride.
Claim 9
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-(3-Benzyloxy-4'-chlorobenzhydryl)-4-(3-methylbenzyl)piperazine dihydrochloride.
Claim 10
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-(2-Bromo-4'-chlorobenzhydryl)-4-methylpiperazine dihydrochloride.
Claim 11
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-(α-(4-Bromophenyl)-3-methoxybenzyl)-4-methylpiperazine dihydrochloride.
Claim 12
Dependent Claim
12 words
A method according to claim 1, wherein said compound is 1-[α-(4-Chlorophenyl)-3-methoxybenzyl]-4-allylpiperazine dihydrochloride.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-11-14 | 1998-05-16 | 1998-11-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-11-14 | 2002-05-16 | 2002-11-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-11-14 | 2006-05-16 | 2006-11-15 | $7700.00 | Window Closed / Lapsed |