| abstract |
The benzazole derivatives of the formula Iao and their tautomers, their geometric isomers, their optically active forms as enantiomers, diastereoisomers and their racemates, as well as their pharmaceutically acceptable salts, wherein: X is O, S or NR0, wherein R0 is H or unsubstituted or substituted C1-C6alkyl; G is an unsubstituted or substituted pyrimidinyl group; R 1 is selected from the group consisting of or consisting of hydrogen, unsubstituted or substituted C 1 -C 6 -alkoxy, unsubstituted or substituted C 1 -C 6 -thioalkoxy, unsubstituted or substituted C 1 -C 6 -alkyl, unsubstituted or substituted C 2 -C 6 -alkenyl, unsubstituted or substituted C2-C6-alkynyl groups, primary, secondary or tertiary amino groups, aminoacyl, aminocarbonyl, unsubstituted or substituted C1-C6alkoxycarbonyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, carboxylic, sulfonyl, sulfo, hydroxy groups, halogens, and unsubstituted or substituted hydrazides; R2 is selected from the group consisting of or consisting of hydrogen, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted C1-C6-alkyl-aryl , unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted C1-C6-alkyl-heteroaryl groups, -C (O) -OR3, -C (O) -R3, -C (O) -NR3R3 ', or - (SO2) R3, wherein R3 and R3 'are independently selected from the group consisting of or consisting of hydrogen, unsubstituted or substituted C1-C6alkyl, unsubstituted or substituted C2-C6alkenyl, unsubstituted or substituted C2-C6alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted , unsubstituted or substituted C1-C6-alkyl-aryl, and unsubstituted or substituted C1-C6-alkyl-heteroaryl groups; wherein the term "substituted" means that said groups may be substituted with 1 to 5 substituents selected from the following groups: C1-C6-alkyl, C1-C6-alkyl-aryl, C1-C6-alkyl-heteroaryl, C2-C6-alkenyl, C2-C6-alkynyl groups, primary, secondary or tertiary amino groups, quaternary ammonium groups, acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, aryl, heteroaryl, carboxylic, cyano, halogen, hydroxy, mercapto, sulfon, sulfo thioalkoxy, trihalomethyl wherein said substitution may include situations in which adjacent substituents form a ring, thus forming lactams, lactones, cyclic anhydrides, acetals, thioacetales and amines; provided that if X is S and R1 and R2 are H, G cannot be any of the following pyrimidines: and further provided that if X is NH and R1 and R2 are H, G cannot be any of the following pyrimidines: and with the last condition that if X is N-CH3 and R1 and R2 are H, G cannot be any of the following pyrimidines: The patent contains another 25 patent z |