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EP0325343A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

L-glutamic acid derivatives

Assignee: Eli Lilly and Co
•
Filing: 1989-01-05
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Granted: —
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Expires: 2009-01-05
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Abstract

Abstract Pyrimidin-5-yl derivatives of L-glutamic acid are anti-neoplastic agents. A typical embodiment is N-(4-[4-(2,4-diamino-6-hydroxypyrimidin-5-yl)-butyl]-­benzoyl)-L-glutamic acid.

Inventors

  • 👤 Edward C. Taylor
  • 👤 Philip M. Harrington
  • 👤 Chuan Shih

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 10:48
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/48; A; A61; A61P; A61P35/00; C07D239/50; C07D239/52; C07D239/54; C07D239/545

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 74 words
A compound of the formula: in which each of X and Y, independently of the other is hydroxy or amino; Z is 1,4-phenylene unsubstituted or substituted with one to four chlorine or fluorine atoms; cyclohexa-1,4-diyl; or a straight or branched chain alkylene group of 2 to 5 carbon atoms; n has a value of 2 to 6; and the configuration about the carbon atom desig­nated * is L; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim 74 words
A compound of the formula: in which each of X and Y, independently of the other is hydroxy or amino; Z is 1,4-phenylene unsubstituted or substituted with one to four chlorine or fluorine atoms; cyclohexa-1,4-diyl; or a straight or branched chain alkylene group of 2 to 5 carbon atoms; n has a value of 2 to 6; and the configuration about the carbon atom desig­nated * is L; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim 15 words
A compound according to claim 1 in which Y is amino and X is hydrogen.
Claim 4
Dependent Claim 14 words
A compound according to claim 1 in which both X and Y are hydroxy.
Claim 5
Dependent Claim 14 words
A compound according to claim 1 in which both X and Y are amino.
Claim 6
Dependent Claim 14 words
A compound according to claim 1 in which Z is 1,4-phenylene, cyclohexa-1,4-diyl; or tetramethylene.
Claim 7
Dependent Claim 11 words
A compound according to claim 2 in which Z is 1,4-phenylene.
Claim 8
Dependent Claim 11 words
A compound according to claim 2 in which Z is cyclohexa-1,4-diyl.
Claim 9
Dependent Claim 11 words
A compound according to claim 4 in which Z is tetramethylene.
Claim 10
Dependent Claim 15 words
A compound according to claim 1 in which -(C n H 2n )- is tetramethylene.
Claim 11
Dependent Claim 32 words
The method of combating neoplastic growth in a mammal which comprises administering to the mammal in a single or multiple dose regimen an effective amount of a compound according to claim 1.
Claim 12
Dependent Claim 47 words
A pharmaceutical composition for combating neoplastic growth in a mammal which comprises an amount of a compound according to claim 1 which upon admini­stration to the mammal in a single or multiple dose regimen is effective to combat said growth, in combina­tion with a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim 31 words
A compound according to claim 1 which has the formula: in which n has a value of 3 to 5 and the configuration about the carbon atom designated * is L.
Claim 14
Dependent Claim 10 words
The compound according to claim 12 which is N-(4-[4-(2,4-diamino-6-hydroxypyrimidin-5-yl)butyl]-­benzoyl)-L-glutamic acid.
Claim 15
Dependent Claim 32 words
The method of combating neoplastic growth in a mammal which comprises administering to the mammal in a single or multiple dose regimen an effective amount of a compound according to claim 12.
Claim 16
Dependent Claim 47 words
A pharmaceutical composition for combating neoplastic growth in a mammal which comprises an amount of a compound according to claim 12 which upon admini­stration to the mammal in a single or multiple dose regimen is effective to combat said growth, in combina­tion with a pharmaceutically acceptable carrier.

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