VITE, GREGORY D.,LEAMON, CHRISTOPHER P.,VLAHOV, IONTCHO R.,SOONG-HOON, KIM
申请号：
HK09103805.0
公开号：
HK1124335B
申请日:
2009.04.23
申请国别(地区):
HK
年份:
2012
代理人:
摘要：
The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is &mdash；O&mdash；, &mdash；S&mdash；, or &mdash；NR7&mdash；； A is &mdash；(CR8R9)&mdash；(CH2)m&mdash；Z&mdash；wherein Z is &mdash；(CHR10)&mdash；, &mdash；C(&boxH；O)&mdash；, &mdash；C(&boxH；O)&mdash；C(&boxH；O)&mdash；, &mdash；OC(&boxH；O)&mdash；, &mdash；N(R11)C(&boxH；O)&mdash；, &mdash；SO2&mdash；, or &mdash；N(R11)SO2&mdash；； B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together 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 taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl； R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl； R6 is hydrogen, alkyl or substituted alkyl； R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl； and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.
