Substituted pyridopyrimidines as antihypertensives

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2119692

Abstract This invention relates to substituted pyridopyrimidinones of general formula (I): I Image wherein n is 0 to 3; R1 and R2 are, independently, H, C1-C6alkyl, hydroxy(C1-C6alkyl), formyl, carbonyl(C1-C6alkyl), carboxy, or carboxy(C1-C6alkyl); R3 and R4 are, independently, H, C1-C6alkyl, or hydroxy; R3a and R4a are H, or one of -CR3R3a and -CR4R4a is a carbonyl group; with the proviso that at least one of the groups R1 and R2 must be hydroxy(C1- C6alkyl), formyl, carbonyl(C1-C6alkyl), carboxy, or carboxy(C1-C6alkyl); or at least one of R3 and R4 must be hydroxy; or ons of -CR3R3a and -CR4R4a must be a carbonyl group;; Ar1 is Image , Image , or Image ; wherein W is H, C1-C6alkyl, halogen, hydroxy, or C1-C6alkoxy; Ar2 is Image , Image , Image , or Image ; wherein X is CO2H, CN, or Image ; wherein R5 is H, CH3, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; or a tautomer of said compound, or a pharmaceutically acceptable salt of said compound or tautomer. The compounds of Formula I are useful for treating hypertension and congestive heart failure. Also disclosed are pharmaceutical compositions containing compounds of Formula I and a pharmaceutically acceptable carrier and methods for production of the compounds of Formula I.

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