Pyrimidine carboxamide derivatives

摘要

The invention relates to a compound of the formula;;wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.

主权项

1. A pyrimidine carboxamide derivative compound of formula wherein R1 is 3,5-di-tert-butyl-4-hydroxyphenyl or 4,6-di-tert-butyl-5-hydroxypyrimidin-2-yl; R2 is H, alkyl, deuteroalkyl, carboxyalkyl, carboxy(amino)alkyl, aminoalkyl, aminocarbonylalkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, halo, thio, hydroxy, cyano, carboxy, carbamoyl, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, and alkoxy; if R1 is 4,6-di-tert-butyl-5-hydroxypyrimidin-2-yl, R2 is also amino; R3 is H, lower alkyl, deuteroalkyl, or halo(lower)alkyl; R4 is H, hydroxy, alkyl, deuteroalkyl, aminoalkyl, cyanoalkyl, haloalkyl, hydroxyalkyl, carboxyalkyl, alkoxyalkyl, lower alkoxy, deuteroalkoxy, or aryloxy; R5 is H, alkyl, deuteroalkyl, haloalkyl, hydroxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, aminosulfonylalkyl, carboxy(amino)alkyl, alkylcarbonylalkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, alkylsulfonyl, or arylsulfonyl.