Pseudolaric acid-B derivatives, their preparation and pharmaceutical compositions

Pseudolaric acid-B derivatives having general formula (I):

• wherein
• (a) R1 is cyano, heterocyclyl, COXR′ or CON(R″)2, wherein X is O or NH, R′ is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R″ is independently alkyl, cycloalkyl or heterocyclicalkyl;
• (b) R2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl;
• and
• (c) R3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH2, hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl,
• Provided that pseudolaric acid A, pseudolaric acid B, pseudolaric acid C, pseudolaric acid C2, deacetoxyl pseudolaric acid A, deacetoxyl pseudolaric acid C2, methyl pseudolarate A, deacetoxyl methyl pseudolarate A, p-bromine phenacyl pseudolarate A, methyl pseudolarate B, p-bromine phenacyl pseudolarate B, methyl pseudolarate C, propyl pseudolate C, iso-propyl pseudolate C, 19-demethoxyl iso-propyl pseudolarate B, 19-demethoxyl iso-propyl pseudolarate C, 19-propyoxyl pseudolarate B, 19-propoxyl pseudolaric acid C, 19-butoxyl pseudolaric acid B, and 19-butoxyl pseudolaric acid C are excluded.