US5344932A
Expired / Lapsed
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N-(pyrrolo(2,3-d)pyrimidin-3-ylacyl)-glutamic acid derivatives
Assignee: Princeton University
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Filing: 1991-03-22
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Granted: 1994-09-06
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Expires: 2011-03-22
Abstract
Abstract N-(Acyl)glutamic acid derivatives in which the acyl group is substituted with 4-hydroxypyrrolo[2,3-d]-pyrimidin-3-yl group are antineoplastic agents. A typical embodiment is N-[4-(2-{4-hydroxy-6-aminopyrrolo-[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-glutamic acid.
Inventors
- 👤 Edward C. Taylor
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:49
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07D; C07D487/00; C07D487/02; C07D487/04; A; A61; A61P; A61P35/00; A61P35/02; A61P43/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y02P20/582
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
60 words
A compound of the formula: ##STR14## in which: R 1 is --OH or --NH 2 ; R 2 is hydrogen or a pharmaceutically acceptable cation: R 3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R 4 is hydrogen, or methyl; R 5 is amino; and the configuration about the carbon atom designated * is S.
Claim 2
Dependent Claim
60 words
A compound of the formula: ##STR14## in which: R 1 is --OH or --NH 2 ; R 2 is hydrogen or a pharmaceutically acceptable cation: R 3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R 4 is hydrogen, or methyl; R 5 is amino; and the configuration about the carbon atom designated * is S.
Claim 3
Dependent Claim
20 words
A compound according to claim 1 wherein R 1 is --OH; R 3 is 1,4-phenylene, and R 4 is hydrogen.
Claim 4
Dependent Claim
10 words
The compound according to claim 1 which is N-{4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benzoyl}-L-glutamic acid.
Claim 5
Dependent Claim
10 words
The compound according to claim 1 which is N-{4-[1-hydroxy-3-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)prop-2-yl]benzoyl}glutamic acid.
Claim 6
Dependent Claim
10 words
The compound according to claim 1 which is N-{2-fluoro-4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benzoyl}-L-glutamic acid.
Claim 7
Dependent Claim
10 words
The compound according to claim 1 which is N-{3-fluoro-4-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]benzoyl}-L-glutamic acid.
Claim 8
Dependent Claim
72 words
A compound of the formula: ##STR15## in which: R 1 is --OH or --NH 2 ; R 2' is hydrogen, a pharmaceutically acceptable cation, or a carboxy protecting group: R 3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R 4' is hydrogen, or methyl; R 5' is amino or amino substituted with an amino protecting group; and the configuration about the carbon atom designated * is S.
Claim 9
Dependent Claim
72 words
A compound of the formula: ##STR15## in which: R 1 is --OH or --NH 2 ; R 2' is hydrogen, a pharmaceutically acceptable cation, or a carboxy protecting group: R 3 is 1,4-phenylene unsubstituted or substituted with chloro, fluoro, methyl, methoxy, or trifluoromethyl; R 4' is hydrogen, or methyl; R 5' is amino or amino substituted with an amino protecting group; and the configuration about the carbon atom designated * is S.
References Cited (Backward Citations)
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