10,11-methylenedioxy-20(RS)-camptothecin and
10,11-methylenedioxy-20(S)-camptothecin analogs
    2.
    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

    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
    5.
    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

    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。

    10,11-methylenedioxy-20(RS)-camptothecin analogs
    6.
    发明授权
    10,11-methylenedioxy-20(RS)-camptothecin analogs 失效
    10,11-亚甲二氧基-20(RS)喜树碱类似物

    公开(公告)号:US5049668A

    公开(公告)日:1991-09-17

    申请号:US407749

    申请日:1989-09-15

    CPC分类号: C07D491/22

    摘要: A camptothecin analog having the structure shown below: ##STR1## wherein R is NO.sub.2, NH.sub.2, 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 or CONR.sup.2 --(CH.sub.2).sub.n --NR.sup.2 R.sup.3, n=1-10 and R.sup.2 and R.sup.3 are as defined above, NHCO--Z--(CH.sub.2).sub.n --NR.sup.2 R.sup.3, where z=oxygen or NH, or ##STR2## where m+y=3-6 and salts thereof.

    摘要翻译: 具有如下结构的喜树碱类似物:其中R是NO 2,NH 2,NHCOCHR 1 NR 2 R 3,其中R 1是α-氨基酸的侧链,R 2和R 3独立地是氢或低级烷基或R 3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为COOH或CONR2-(CH2)n -NR 2 R 3,n = 1-10,R 2和R 3如上所定义,NHCO-Z-(CH 2)n -NR 2 R 3,其中z =氧或NH,或其中m + y = 3-6及其盐 。