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US 5,473,071 AGranted
Process for the preparation of fused pyridine compounds
AssigneeThe Trustees of Princeton University
InventorsEdward C. Taylor, Philip M. Harrington
Life of this patent
Estimating the term…
Abstract
Pyrido[2,3-d]pyrimidine compounds are prepared through the reaction of 2,4-diamino-6(1H)-pyrimidone and an activated derivative of a dialdehyde. A typical embodiment utilizes the dinitrile.
Claims15
A compound of the formula:
- ##STR11## wherein:
- R.sup.2 is hydrogen or a carboxylic acid protecting group;
- and
- R.sup.11 is hydrogen or an amino protecting group.
1 more element
A compound of the formula:
- ##STR12## wherein each of R.sup.2 and R.sup.3 is hydrogen or a carboxylic acid protecting group;
- and
- R.sup.11 is hydrogen or an amino protecting group.
A compound selected from the group consisting of
- (i) the (R,S)- and (S,S)-diastereomers of N-[4-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-ylmeth yl)benzoyl]-L-glutamic acid, and
- (ii) the pharmaceutically acceptable alkali metal, alkaline earth metal, non-toxic metal, ammonium and substituted ammonium salts thereof.
A compound of the formula:
- ##STR13## wherein:
- R.sup.2 is hydrogen or a carboxylic acid protecting group;
- and
- R.sup.11 is hydrogen or an amino protecting group.
1 more element
A compound of the general formula:
- ##STR14## wherein the ring A is a pyridine ring which may be hydrogenated, X is hydroxyl, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen, and --COOR.sup.5 and --COOR.sup.6 are independently a carboxyl group which may be esterified, or a salt thereof.
A compound of the formula:
- ##STR15## wherein:
- each of R.sup.2 and R.sup.3 is hydrogen or a carboxylic acid protecting group;
- and
- R.sup.11 is hydrogen or an amino protecting group.
1 more element
A compound selected from the group consisting of (i) the (R,S)- and (S,S)-diastereomers of N-(4-[3-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)p ropyl]benzoyl)-L-glutamic acid;
- and (ii) the pharmaceutically acceptable alkali metal, alkaline earth metal, non-toxic metal, ammonium and substituted ammonium salts thereof.
Dependencies are inferred from the claim text.