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吖丙啶基-埃坡黴素(EPOTHILONE)化合物
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
VITE, GREGORY D.,格列高里D. 维特,格列高里D. 維特,KIM, SOONG-HOON,胜镛 金,勝鏞 金,LEAMON, CHRISTOPHER P.,克里斯多夫P. 利蒙,VLAHOV, IONTCHO,汤丘 福拉和夫,湯丘 福拉和夫,格列高里D. 维特,格列高里D. 維特,胜镛 金,勝鏞 金,克里斯多夫P. 利蒙,汤丘 福拉和夫,湯丘 福拉和夫
申请号:
TW096118882
公开号:
TWI383985B
申请日:
2007.05.25
申请国别(地区):
TW
年份:
2013
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 -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-; B1is hydroxyl or cyano and R1is hydrogen or B1and R1are taken together to form a double bond; R2,R3, and R5are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2and R3may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6is hydrogen, alkyl or substituted alkyl; R7, R8, R9,R10, R11and R12are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13is aryl, substituted aryl, heteroaryl or substituted heteroaryl.本發明係關於具有下式如在本文中進一步描述之吖丙啶基-埃坡黴素化合物及/或其醫藥學上可接受之鹽及/或溶劑合物:其中K為-O-、-S-或-NR7-;A為-(CR8R9)-(CH2)m-Z-,其中Z為-(CHR10)-、-C(=O)-、-C(=O)-C(=O)-、-OC(=O)-、-N(R11)C(=O)-、-SO2-或-N(R11)SO2-;B1為羥基或氰基且R1為氫,或B1與R1一起形成一雙鍵;R2、R3及R5獨立地為氫、烷基、經取代之烷基、芳基或經取代之芳基;或R2與R3可與其所連接之碳一起形成視情況經取代之環烷基;R4為氫、烷基、烯基、經取代之烷基、經取代之烯基、芳基或經取代之芳基;R6為氫、烷基或經取代之烷基;R7、R8、R9、R10、R11及R12獨立地為氫、烷基、經取代之烷基、環烷基、經取代之環烷基、芳基、經取代之芳基、雜環烷基、經取代之雜環烷基、雜芳基或經取代之雜芳基;且R13為芳基、經取代之芳基、雜芳基或經取代之雜芳基。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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