发明授权
US5340817A Method of treating tumors with anti-tumor effective camptothecin
compounds
失效
用抗肿瘤活性喜树碱化合物治疗肿瘤的方法
- 专利标题： Method of treating tumors with anti-tumor effective camptothecin compounds
- 专利标题（中）： 用抗肿瘤活性喜树碱化合物治疗肿瘤的方法
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申请号： US899865申请日： 1992-06-17
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公开(公告)号： US5340817A公开(公告)日： 1994-08-23
- 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： C07D491/22
- IPC分类号： C07D491/22 ; A61K31/44
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 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. The campothecin compounds inhibit the enzyme topisomerase I and are useful in treating tumors and leukemia.