VITE, GREGORY D.,LEAMON, CHRISTOPHER P.,VLAHOV, IONTCHO R.,KIM, SOONG-HOON
申请号:
CA2655668
公开号:
CA2655668C
申请日:
2007.05.25
申请国别(地区):
CA
年份:
2013
代理人:
摘要:
The present invention is directed to aziridinyl epothilone compounds asfurther described herein, and/or pharmaceutically-acceptable salts and/orsolvatesthereof having the following Formula:(see above formula)wherein K is -O-, -S-, or -NR7-; A is -(CR8R9)-(CH2)m-Z- wherein Z is--(CHR10)-, -C(=O)-, -C(=O)-C(=O)-, -OC(=O)-, -N(R11)C(=O)-, -SO2-, or--N(R11)SO2-; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 aretakentogether to form a double bond; R2, R3, and R5 are, independently, hydrogen,alkyl,substituted alkyl, aryl or substituted aryl; or R2 and R3 may be takentogether withthe carbon to which they are attached to form an optionally substitutedcycloalkyl;R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl,orsubstituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10,R11 andR12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl,substitutedcycloalkyl, aryl, substituted aryl, heterocycloalkyl, substitutedheterocycloalkyl,heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl,heteroaryl orsubstituted heteroaryl.