5,6,7,8-tetrahydropyrido¬2,3-d|pyrimidines

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 471/04 (2006.01) A61K 31/505 (2006.01) A61K 31/695 (2006.01) C07F 7/10 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2251813

Glutamic acid derivatives in which the amino group is substituted with a 2- amino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylalkyl-Z-carbonyl group, in which Z is a divalent, five-membered, nitrogen-containing heterocyclic ring system optionally containing a sulfur or nitrogen atom as a second hetero ring member, are antineoplastic agents. A typical embodiment is N-{3-[2-(2-amino-4- hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]-pyrazol-5- ylcarbonyl}-L-glutamic acid.

Les dérivés de l'acide glutamique, dans lesquels le groupe amino est substitué par un groupe 2-amino-5,6,7,8-tétrahydropyrido[2,3-d]pyrimidin-6-ylalkyl-Z-carbonyle dans lequel Z est un noyau hétérocyclique azoté divalent, à cinq chaînons, contenant éventuellement un atome de soufre ou d'azote, comme second chaînon dudit noyau, sont des agents antinéoplasiques. Une forme de réalisation typique est l'acide N-{3-[2-(2-amino-4-hydroxy-5,6,7,8-tétrahydripyridol[2,3-d]pyrimidin-6-yl(éthyl]-pyrazol-5-ylcarbonyl}-L-glutamique.

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