US5731334A
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Method for treating cancer using taxoid onium salt prodrugs
Assignee: Scripps Research Institute
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Filing: 1995-10-27
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Granted: 1998-03-24
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Expires: 2015-10-27
Abstract
Abstract C-2'-methylpyridinium acetates (MPA)-taxol and C-2'-methylpyridinium acetates (MPA)-taxotere are prodrugs having good aqueous solubility, low toxiticity and high anti-minor activity. These prodrugs are administered to patients for treating minors. Adminstration may be by injection or infusion.
Inventors
- 👤 Wolfgang Wrasidlo
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 17:14
CPC Classifications
C; C07; C07D; C07D305/00; C07D305/14
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
124 words
A method for treating a mammal having a tumor or other cancer by administering an aqueous solution of a taxoid onium salt prodrug to the mammal by a route selected from the group consisting of injection and infusion, wherein the taxoid onium salt prodrug is represented by the following structure: ##STR5## wherein S - is selected from the group consisting of OA - , Cl - , Br - , I - , BF 4 - , ClO 4 - , ArSO 3 - , and AlkylSO 3 - , R 1 is selected from the group consisting of phenyl and tBuO, R 2 is selected from the group consisting of OAc and OH, and R 3 is represented by the following structure: ##STR6##
Claim 2
Independent Claim
124 words
A method for treating a mammal having a tumor or other cancer by administering an aqueous solution of a taxoid onium salt prodrug to the mammal by a route selected from the group consisting of injection and infusion, wherein the taxoid onium salt prodrug is represented by the following structure: ##STR5## wherein S - is selected from the group consisting of OA - , Cl - , Br - , I - , BF 4 - , ClO 4 - , ArSO 3 - , and AlkylSO 3 - , R 1 is selected from the group consisting of phenyl and tBuO, R 2 is selected from the group consisting of OAc and OH, and R 3 is represented by the following structure: ##STR6##
Claim 3
Dependent Claim
17 words
A method as described in claim 1 wherein the mammal is a human tumor or cancer patient.
Claim 4
Dependent Claim
20 words
A method as described in claim 1 wherein the mammal is sensitive and/or intolerant to a side effect of taxol.
Claim 5
Dependent Claim
20 words
A method as described in claim 1 wherein the method has a dosage range of approximately 50-300 mg/m 2 .
Claim 6
Dependent Claim
22 words
A method as described in claim 1 wherein the method has a dosage range of approximately 50 and 4,900 mg/m 2 .
Claim 7
Dependent Claim
22 words
A method as described in claim 1 wherein the method has a dosage range of approximately 50 and 21,000 mg/m 2 .
Claim 8
Dependent Claim
22 words
A method as described in claim 1 wherein the method has a dosage range of approximately 50 and 28,000 mg/m 2 .
Claim 9
Dependent Claim
19 words
A method as described in claim 7 wherein the tumor or other cancer is refractory and/or insensitive to taxol.
Claim 10
Dependent Claim
28 words
A method as described in claim 1 wherein S - is any counter ion classified as generally regarded as safe (GRAS) by the U.S. Food and Drug Administration.
Claim 11
Dependent Claim
21 words
A method as described in claim 1 wherein the taxoid onium salt prodrug is taxol-2'-MPA represented by the following structure: ##STR7##
Claim 12
Dependent Claim
21 words
A method as described in claim 1 wherein the taxoid onium salt prodrug is taxotere-2'-MPA represented by the following structure: ##STR8##
Claim 13
Dependent Claim
18 words
A method as described in claim 1 wherein the route of administration is by injection of a bolus.
Claim 14
Dependent Claim
15 words
A method as described in claim 1 wherein the route of administration is by infusion.
Claim 15
Dependent Claim
12 words
A method as described in claim 1 wherein the administration is intravenous.
Claim 16
Dependent Claim
12 words
A method as described in claim 1 wherein the administration is intraperitoneal.
Claim 17
Dependent Claim
12 words
A taxoid onium salt prodrug taxol-2'-MPA represented by the following structure: ##STR9##
Claim 18
Dependent Claim
12 words
A taxoid onium salt prodrug taxol-2'-MPA represented by the following structure: ##STR9##
Claim 19
Dependent Claim
12 words
A taxoid onium salt prodrug taxotere-2'-MPA represented by the following structure: ##STR10##
Claim 20
Dependent Claim
12 words
A taxoid onium salt prodrug taxotere-2'-MPA represented by the following structure: ##STR10##
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) | 2001-03-23 | 2001-09-22 | 2002-03-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2005-03-23 | 2005-09-22 | 2006-03-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2009-03-23 | 2009-09-22 | 2010-03-24 | $7700.00 | Window Closed / Lapsed |