4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine derivatives

Claim 2

A compound selected from the group consisting of: (i) 4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]-pyrimidines of the formula: ##STR7## wherein: R 1 is hydrogen, methyl, or ethyl; and the configuration about the carbon atom designated * is L; (ii) the tautomeric forms thereof; and (iii) the pharmaceutically acceptable alkali metal, alkaline earth, non-toxic metal, ammonium, and substituted ammonium salts thereof.

Claim 3

The compound according to claim 1 wherein R 1 is hydrogen.

Claim 4

The (S,S) diastereoisomer of the compound according to claim 2 and having the following absolute configuration: ##STR8##

Claim 5

The (R,S) diastereoisomer of the compound according to claim 2 and having the following absolute configuration: ##STR9##

Claim 6

The compound according to claim 1 wherein R 1 is methyl.

Claim 7

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 8

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 9

A compound selected from the group consisting of: (i) 4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidines of the formula: ##STR10## wherein R 1 is hydrogen, methyl, or ethyl; R 2 and R 3 are the same or different carboxylic acid protecting group selected from the group consisting of alkyl of 1 to 6 carbon atoms, unsubstituted or substituted with one or more of phenyl, halo, or alkoxy; and silyl; R 4 is an amino protecting group selected from the group consisting of alkanoyl or alkoxycarbonyl of 2 to 6 carbon atoms, unsubstituted or substituted with one or more phenyl, halo, or alkoxy; benzoyl; and 4-nitrobenzoyloxycarbonyl; and the configuration about the carbon atom designated * is L; and (ii) the tautomeric forms thereof.

Claim 10

A compound selected from the group consisting of: (i) 4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidines of the formula: ##STR10## wherein R 1 is hydrogen, methyl, or ethyl; R 2 and R 3 are the same or different carboxylic acid protecting group selected from the group consisting of alkyl of 1 to 6 carbon atoms, unsubstituted or substituted with one or more of phenyl, halo, or alkoxy; and silyl; R 4 is an amino protecting group selected from the group consisting of alkanoyl or alkoxycarbonyl of 2 to 6 carbon atoms, unsubstituted or substituted with one or more phenyl, halo, or alkoxy; benzoyl; and 4-nitrobenzoyloxycarbonyl; and the configuration about the carbon atom designated * is L; and (ii) the tautomeric forms thereof.

Claim 11

A compound according to claim 8 wherein each of R 2 and R 3 is alkyl of 1 to 6 carbon atoms and R 4 is alkanoyl of 2 to 6 carbon atoms.

Claim 12

The compound according to claim 9 in which R 1 is hydrogen, each of R 2 and R 3 is ethyl, and R 4 is acetyl or pivaloyl.