Patent US5565478A successfully refreshed from Google Patents.
US5565478A
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Combination therapy using signal transduction inhibitors with paclitaxel and other taxane analogs
Assignee: United States Department of Health and Human Services
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Filing: 1994-03-14
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Granted: 1996-10-15
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Expires: 2014-03-14
Abstract
Abstract The present invention provides compositions and methods for the treatment of cancer in a subject wherein compounds of formula I defined herein in combination with paclitaxel or other modified taxane analogs provide enhanced anticancer effects over the effects achieved with the individual compounds.
Inventors
- 👤 Elise C. Kohn
- 👤 Eddie Reed
- 👤 Lance A. Liotta
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 16:53
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/41; A61K31/415
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
199 words
A pharmaceutical composition comprising, an effective amount of a first compound having formula I: Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12 (I) wherein: is an integer of from 0 to 4; Ar 11 and Ar 12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, halo-substituted phenyl, halo-substituted naphthyl; X is a linking moiety selected from the group consisting of O, S, SO 2 , CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Y is a nitrogen-containing heterocyclic moiety of formula II: ##STR5## wherein: A is a member selected from the group consisting of N and CH; R 1 is a member selected from the group consisting of hydrogen, --CONH 2 , --CONHR 3 , --CO2H, --CO 2 R 3 , and --SO 2 NH 2 , R 2 is a member selected from the group consisting of hydrogen, --NHCOC 6 H 5 , --NH 2 , --NHR 3 , --NC(R 3 ) 2 , --NHCOR 3 , and --NHCHO; and R 3 is lower alkyl of from 1 to 6 carbon atoms, and an effective amount of a second compound selected from the group consisting of paclitaxel, motere, and modified taxane analogs in a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim
199 words
A pharmaceutical composition comprising, an effective amount of a first compound having formula I: Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12 (I) wherein: is an integer of from 0 to 4; Ar 11 and Ar 12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, halo-substituted phenyl, halo-substituted naphthyl; X is a linking moiety selected from the group consisting of O, S, SO 2 , CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Y is a nitrogen-containing heterocyclic moiety of formula II: ##STR5## wherein: A is a member selected from the group consisting of N and CH; R 1 is a member selected from the group consisting of hydrogen, --CONH 2 , --CONHR 3 , --CO2H, --CO 2 R 3 , and --SO 2 NH 2 , R 2 is a member selected from the group consisting of hydrogen, --NHCOC 6 H 5 , --NH 2 , --NHR 3 , --NC(R 3 ) 2 , --NHCOR 3 , and --NHCHO; and R 3 is lower alkyl of from 1 to 6 carbon atoms, and an effective amount of a second compound selected from the group consisting of paclitaxel, motere, and modified taxane analogs in a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim
14 words
A composition in accordance with claim 1 wherein said first compound is 5-amino-1-(4-(4-chlorobenzoyl)-3,5-dichlorobenzyl)- 1,2,3-triazo-4-carboxamide.
Claim 4
Dependent Claim
19 words
A composition in accordance with claim 1 wherein said first compound is 5,amino-1-(4-(4-chlorobenzoyl)-3,5-dichlorobenzyl)-1,2,3-triazole-4-carboxamide and said second compound is paclitaxel.
Claim 5
Dependent Claim
24 words
A composition in accordance with claim 1 further comprising an antimycotic imidazole selected from the group consisting of ketoconazole, fluconazole, itraconazole, econazole and miconazole.
Claim 6
Independent Claim
230 words
A method for treating cancer in a subject, said cancer being selected from the group consisting of breast cancer, lung cancer, melanoma, and ovarian cancer, said method comprising: (i) administering to said subject an effective amount of a compound of formula I: Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12 (I) wherein: p is an integer of from 0 to 4; Ar 11 and Ar 12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, halo-substituted phenyl, halo-substituted naphthyl; X is a linking moiety selected from the group consisting of O, S, SO 2 , CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Y is a nitrogen-containing heterocyclic moiety of formula II: ##STR6## wherein: A is a member selected from the group consisting of N and CH; R 1 is a member selected from the group consisting of hydrogen, --CONH 2 , --CONHR 3 , --CO 2 H, --CO 2 R 3 , and --SO 2 NH 2 , R 2 is a member selected from the group consisting of hydrogen, --NHCOC 6 H 5 , --NH 2 , --NHR 3 , --N(R 3 ) 2 , --NHCOR 3 , and --NHCHO; and R 3 is lower alkyl of from 1 to 6 carbon atoms, and (ii) administering to said subject an effective amount of a second compound selected from the group consisting of paclitaxel, taxotere and modified taxane analogs.
Claim 7
Independent Claim
230 words
A method for treating cancer in a subject, said cancer being selected from the group consisting of breast cancer, lung cancer, melanoma, and ovarian cancer, said method comprising: (i) administering to said subject an effective amount of a compound of formula I: Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12 (I) wherein: p is an integer of from 0 to 4; Ar 11 and Ar 12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, halo-substituted phenyl, halo-substituted naphthyl; X is a linking moiety selected from the group consisting of O, S, SO 2 , CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Y is a nitrogen-containing heterocyclic moiety of formula II: ##STR6## wherein: A is a member selected from the group consisting of N and CH; R 1 is a member selected from the group consisting of hydrogen, --CONH 2 , --CONHR 3 , --CO 2 H, --CO 2 R 3 , and --SO 2 NH 2 , R 2 is a member selected from the group consisting of hydrogen, --NHCOC 6 H 5 , --NH 2 , --NHR 3 , --N(R 3 ) 2 , --NHCOR 3 , and --NHCHO; and R 3 is lower alkyl of from 1 to 6 carbon atoms, and (ii) administering to said subject an effective amount of a second compound selected from the group consisting of paclitaxel, taxotere and modified taxane analogs.
Claim 8
Dependent Claim
17 words
A method in accordance with claim 5 wherein step (i) is carded out prior to step (ii).
Claim 9
Dependent Claim
17 words
A method in accordance with claim 5 wherein step (ii) is carried out prior to step (i).
Claim 10
Dependent Claim
39 words
A method in accordance with claim 5 wherein said effective amount of said compound of step (i) is from the range of from about 50 mg/m 2 to about 500 mg/m 2 of body surface area of said subject.
Claim 11
Dependent Claim
72 words
A method in accordance with claim 5 wherein said effective amount of said compound of step (i) is from the range of from about 50 mg/m 2 to about 500 mg/m 2 of body surface area of said subject and said effective amount of said compound of step (ii) is selected from the range of from about 75 mg/m 2 to about 300 mg/m 2 of body surface area of said subject.
Claim 12
Dependent Claim
12 words
A method in accordance with claim 5 wherein said subject is human.
Claim 13
Dependent Claim
28 words
A method in accordance with claim 5 wherein said subject is human, said compound of step (i) is 5-amino-1-(4-(4-chlorobenzoyl)-3,5-dichlorobenzyl)- 1,2,3-triazole-4-carboxamide and said compound of step (ii) is paclitaxel.
Claim 14
Dependent Claim
14 words
A method in accordance with claim 5 wherein said first compound is administered orally.
Claim 15
Dependent Claim
16 words
A method in accordance with claim 5 wherein said second compound is administered by intravenous injection.
Claim 16
Dependent Claim
36 words
A method in accordance with claim 5 wherein said compounds of steps (i) and (ii) are administered in combination with a compound selected from the group consisting of G-CSF, an antimycotic imidazole, and a mixture thereof.
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