| abstract |
The application discloses the substituted of formula (I) azole and thiazole compounds or pharmaceutically acceptable salts thereof, Wherein: R 1 is selected from alkyl, branched alkyl and substituted alkyl; R 2 is selected from hydrogen, alkyl and substituted alkyl; R 3 is selected from -L 1 -A 1 , wherein L 1 is selected from from -C(O)-, -C(S)-, -S(O)- and -S(O) 2 - and A 1 is selected from alkyl, substituted alkyl, alkoxy, substituted Alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, and NR 8 R 9 ; R 4 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, and substituted alkynyl, and optionally substituted pyrrolidinyl; or R 3 and R together with the nitrogen atom to which they are bonded form a 5 to 7 membered heterocycloalkyl or substituted heterocycloalkyl wherein optionally one carbon ring atom is selected from O, S or NR; X is O or S; R is selected from cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all of which may be optionally substituted by -(R 10 ) m , wherein R 10 is as defined herein, and m is 1 , 2, 3 or 4, and when m is 2, 3 or 4, each R 10 may be the same or different; R 7 is -L 2 -A 2 , wherein L 2 is C 1 -C 5 alkylene and A 2 is selected from aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, and substituted heterocycloalkyl. Compounds of formula (I) are useful in the treatment of KSP-mediated diseases, including cancer. |