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AZIRIDINYL-EPOTHILONE COMPOUNDS
专利权人:
发明人:
바이트, 그레고리 디.,리먼, 크리스토퍼 피.,블라호브, 아이온초 알.,승-훈, 김
申请号:
KR1020087031405
公开号:
KR1014139550000B1
申请日:
2007.05.25
申请国别(地区):
KR
年份:
2014
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.본 발명은 화학식 X를 갖는 아지리디닐 에포틸론 화합물 (본원에 보다 상세하게 기재되어 있음) 및/또는 이들의 제약상 허용되는 염 및/또는 용매화물에 관한 것이다. 이들 화합물은 암 치료에서 표적화된 약물 전달을 위한 컨쥬게이트, 특히 폴레이트의 제조에 사용될 수 있다.<;화학식 X>;
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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