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    10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs
    5.
    发明授权
    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

    公开(公告)号：US5180722A

    公开(公告)日：1993-01-19

    申请号：US581916

    申请日：1990-09-13

    申请人： Monroe E. Wall ,  Mansukh C. Wani ,  Allan W. Nicholas ,  Govindarajan Manikumar

    发明人： Monroe E. Wall ,  Mansukh C. Wani ,  Allan W. Nicholas ,  Govindarajan Manikumar

    IPC分类号： C07D471/14 ,  C07D491/22

    CPC分类号： C07D471/14

    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.

    摘要翻译： 具有下述结构的喜树碱类似物：其中Z是H或C 1-8烷基，R是NO 2，NH 2，N 3，氢，卤素，COOH，OH，O-C 1-3烷基，SH， C 1-3烷基，CN，CH 2 NH 2，NH-C 1-3烷基，CH 2 -NH-C 1-3烷基，N（C 1-3烷基）2，CH 2 N（C 1-3烷基）2，O-， ，或S-CH 2 CH 2 N（CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 CH 2 N（CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 N（CH 2 CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 CH 2 N（CH 2 CH 2 CH 2 OH 2） 2，O-，NH-或S-CH2CH2N（C1-3烷基）2，O-，NH-或S-CH2CH2CH2N（C1-3烷基）2，CHO，C1-3烷基或NHCOCHR1NR2R3，其中R1是侧 α-氨基酸的链和R2和R3独立地是氢或低级烷基，或R3是含有通过肽键与氮键合的1-3个氨基酸单元的肽单元; NHCO-C2-8-亚烷基-X或NHCO-C2-8-亚烯基-X，其中X是COOH; CONR2-（CH2）n-NR2R3，其中n = 1-10，R2和R3如上定义; NHCO-B-（CH 2）n -NR 2 R 3，其中B =氧或NH，或其中m + y = 3-6的或其盐。

    Method of treating tumors with anti-tumor effective camptothecin compounds
    9.
    发明授权
    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

    公开(公告)号：US5340817A

    公开(公告)日：1994-08-23

    申请号：US899865

    申请日：1992-06-17

    申请人： Monroe E. Wall ,  Mansukh C. Wani ,  Allan W. Nicholas ,  Govindarajan Manikumar

    发明人： Monroe E. Wall ,  Mansukh C. Wani ,  Allan W. Nicholas ,  Govindarajan Manikumar

    IPC分类号： C07D491/22 ,  A61K31/44

    CPC分类号： 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 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.

    摘要翻译： 具有下述结构的喜树碱类似物：其中Z是H或C 1-8烷基，R是NO 2，NH 2，N 3，氢，卤素，COOH，OH，O-C 1-3烷基，SH， C 1-3烷基，CN，CH 2 NH 2，NH-C 1-3烷基，CH 2 -NH-C 1-3烷基，N（C 1-3烷基）2，CH 2 N（C 1-3烷基）2，O-， 或S-CH 2 CH 2 N（CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 CH 2 N（CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 N（CH 2 CH 2 CH 2 OH）2，O-，NH-或S-CH 2 CH 2 CH 2 N（CH 2 CH 2 OH 2） ，O-，NH-或S-CH2CH2N（C1-3烷基）2，O-，NH-或S-CH2CH2CH2N（C1-3烷基）2，CHO，C1-3烷基或NHCOCHR1NR2R3，其中R1是侧 - α-氨基酸的链和R2和R3独立地是氢或低级烷基或R3是含有通过肽键键合到氮的1-3个氨基酸单元的肽单元; NHCO-C2-8-亚烷基-X或NHCO-C2-8-亚烯基-X，其中X是COOH; CONR2-（CH2）n-NR2R3，其中n = 1-10，R2和R3如上定义; NHCO-B-（CH 2）n -NR 2 R 3，其中B =氧或NH，或其中m + y = 3-6的或其盐。 氨基辛酸化合物抑制酶拓扑异构酶I，可用于治疗肿瘤和白血病。