发明授权
US5180722A 10,11-methylenedioxy-20(RS)-camptothecin and
10,11-methylenedioxy-20(S)-camptothecin analogs
失效
10,11-亚甲二氧基-20（RS） - 喜树碱和10,11-亚甲二氧基-20（S） - 喜树碱类似物
- 专利标题： 10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs
- 专利标题（中）： 10,11-亚甲二氧基-20（RS） - 喜树碱和10,11-亚甲二氧基-20（S） - 喜树碱类似物
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申请号： US581916申请日： 1990-09-13
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公开(公告)号： US5180722A公开(公告)日： 1993-01-19
- 发明人: Monroe E. Wall , Mansukh C. Wani , Allan W. Nicholas , Govindarajan Manikumar
- 申请人： Monroe E. Wall , Mansukh C. Wani , Allan W. Nicholas , Govindarajan Manikumar
- 申请人地址： NC Research Triangle Park
- 专利权人： Research Triangle Institute
- 当前专利权人： Research Triangle Institute
- 当前专利权人地址： NC Research Triangle Park
- 主分类号： C07D471/14
- IPC分类号： C07D471/14 ; C07D491/22
摘要：
A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH, S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl, CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.3 is a peptide unit containing 1-3 amino acid units bonded to the nitrogen through a peptide bond; NHCO--C.sub.2-8 -alkylene--X or NHCO--C.sub.2-8 -alkenylene--X, where X is COOH; CONR.sup.2 --(CH.sub.2).sub.n --NR.sup.2 R.sup.3, where n=1-10 and R.sup.2 and R.sup.3 are as defined above; NHCO--B--(CH.sub.2).sub.n --NR.sup.2 R.sup.3, where B=oxygen or NH, or ##STR2## where m+y=3-6, and salts thereof.
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