1,2,3,4-tetrahydro-6-substituted-4-aryl(or heterocyclo)...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/22 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01)

Patent

CA 1275410

Abstract 1,2,3,4-TETRAHYDRO-6-SUBSTITUTED-4- ARYL(OR HETEROCYCLO)-3-SUBSTITUTED-2-THIOXO (OR OXO)-5-PYRIMIDINECARBOXYLIC ACIDS AND ESTERS Cardiovascular activity is exhibited by compounds having the formula Image and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur; R1 is alkyl, cycloalkyl, alkenyl, alkynyl, aryl -(CH2)n-Y2, -(CH2)p-Y3, halo substituted alkyl, or -?-Y4; R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, -(CH2)n-Y1, or halo substituted alkyl; R3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, -(CH2)n-Y2, -(CH2)p-Y3, or halo substituted alkyl; R4 is aryl or heterocyclo; Y1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH2)m-O-, mercapto, alkylthio, aryl-(CH2)m-S-, amino, substituted amino, carbamoyl, (substituted amino)-?-, heterocyclo-(CH2)m-?-, carboxyl, alkoxycarbonyl, alkyl-?-, aryl-(CH2)m-?-, alkyl-?-O- or aryl-(CH2)m-?-O-; Y2 is cycloalkyl, aryl, heterocyclo, carbamoyl, (substituted amino)-?-, carboxyl, alkoxycarbonyl, alkyl-?-, aryl-(CH2)m-?- or heterocyclo-(CH2)m-?-; Y3 is hydroxyl, alkoxy, aryl-(CH2)m-O-, mercapto, alkylthio, aryl-(CH2)m-S-, alkyl-C-O-, aryl-(CH2)m-?-O-, amino, or substituted amino; Y4 is alkyl, cycloalkyl, aryl, heterocyclo, -(CH2)n-Y1 or halo substituted alkyl; m is 0 or an integer of 1 to 6; n is an integer of 1 to 6; and p is an integer of 2 to 6.

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