US5114919A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Adjuncts in cancer chemotherapy
Assignee: Merck and Co Inc
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Filing: 1991-02-11
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Granted: 1992-05-19
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Expires: 2011-02-11
Abstract
Abstract Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.
Inventors
- 👤 John J. Baldwin
- 👤 David C. Remy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 16:45
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/10; C07D211/00; C07D211/04; C07D211/68; C07D211/70
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
64 words
A pharmaceutical composition useful in treating multidrug resistant tumor cells in a patient in need thereof which comprises a mixture of the compound which is selected from the group consisting of: (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; (+)-1-cyclopropylmethyl-4-(3-iodo-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; 4-amino-5-chloro-2-methoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; 3,4,5-trimethoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; and diethyl 1,4-dihydro-2,6-dimethyl-4-(5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)-pyridinedicarboxylate or pharmaceutically acceptable acid addition salt thereof, and an anticancer agent which is selected from the group consisting of: vinblastine, vincristine, dactinomycin, daunorubicin, doxorubicin or mithramycin.
Claim 2
Dependent Claim
64 words
A pharmaceutical composition useful in treating multidrug resistant tumor cells in a patient in need thereof which comprises a mixture of the compound which is selected from the group consisting of: (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; (+)-1-cyclopropylmethyl-4-(3-iodo-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; 4-amino-5-chloro-2-methoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; 3,4,5-trimethoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; and diethyl 1,4-dihydro-2,6-dimethyl-4-(5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)-pyridinedicarboxylate or pharmaceutically acceptable acid addition salt thereof, and an anticancer agent which is selected from the group consisting of: vinblastine, vincristine, dactinomycin, daunorubicin, doxorubicin or mithramycin.
Claim 3
Dependent Claim
16 words
A pharmaceutical composition of claim 1 wherein said compounds are present in a unitary dosage form.
Claim 4
Dependent Claim
61 words
A pharmaceutical composition of claim 1, wherein the weight ratio of the compound which is selected from the group consisting of: (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; (+)-1-cyclopropylmethyl-4-(3-iodo-5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidine; 4-amino-5-chloro-2-methoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; 3,4,5-trimethoxy-N-((5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)methyl)benzamide; and diethyl 1,4-dihydro-2,6-dimethyl-4-(5-(1-methyl-4-piperidinylidene)-5H-dibenzo[a,d]cyclohepten-3-yl)-pyridinedicarboxylate or pharmaceutically acceptable acid addition salt thereof, to an anticancer agent which is selected from the group consisting of: vinblastine, vincristine, dactinomycin, daunorubicin, doxorubicin or mithramycin ranges from about 1000:1 to about 1:1000.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-05-19 | 1995-11-18 | 1996-05-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-05-19 | 1999-11-18 | 2000-05-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-05-19 | 2003-11-18 | 2004-05-19 | $7700.00 | Window Closed / Lapsed |