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    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives
    31.
    发明授权
    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives 失效
    用7-取代的喜树碱衍生物抑制肿瘤生长的方法

    公开(公告)号：US06306868B1

    公开(公告)日：2001-10-23

    申请号：US09643256

    申请日：2000-08-22

    申请人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    发明人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    IPC分类号： A61K31436

    CPC分类号： C07D491/22

    摘要： Compounds of formula (I), wherein: R1 is —CN, —CH(CN)—R4, —CH═C(CN)—R4, —CH2—CH(CN)—R4, —C(═NOH)—NH2, —C(═NH)—NH2, —CH═C(NO2)—R4, —CH(CN)—R5, —CH(CH2NO2)—R5; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R2 is hydrogen; R3 is hydrogen, OR6; R4 is hydrogen, C1-C6 linear or branched alkyl, CN, COOR7; R5 is hydrogen, OR8; R6 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl, (C6-C12) aryl (C2-C4) acyl, (C2-C4) acyl, amino (C1-C4) alkyl, amino (C2-C4) acyl, glycosyl; R7 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl; R8 has the same meanings of R6, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

    摘要翻译： 式（I）化合物，其中：R1是-CN，-CH（CN）-R4，-CH = C（CN）-R4，-CH2-CH（CN）-R4，-C（= NOH） ，-C（= NH）-NH 2，-CH = C（NO 2）-R 4，-CH（CN）-R 5，-CH（CH 2 NO 2） 5-四唑基，2-（4,5-二氢恶唑基），1,2,4-恶二唑啉-3-基-5-酮; R2是氢; R3是氢，OR6; R4是氢，C1-C6直链或支链烷基，CN，COOR7; R5是氢，OR8; R6是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ，（C 6 -C 12）芳基（C 2 -C 4）酰基，（C 2 -C 4）酰基，氨基（C 1 -C 4）烷基，氨基（C 2 -C 4）酰基，糖基; R7是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ; R8与R6具有相同的含义，独立于后者。 这些化合物作为拓扑异构酶I抑制剂是有活性的，可用作抗肿瘤药物。

    Camptothecin derivatives having antitumor activity
    32.
    发明授权
    Camptothecin derivatives having antitumor activity 有权
    喜树碱衍生物具有抗肿瘤活性

    公开(公告)号：US06242457B1

    公开(公告)日：2001-06-05

    申请号：US09507928

    申请日：2000-02-22

    申请人： Sergio Penco ,  Lucio Merlini ,  Paolo Carminati ,  Franco Zunino

    发明人： Sergio Penco ,  Lucio Merlini ,  Paolo Carminati ,  Franco Zunino

    IPC分类号： A61K314761

    CPC分类号： C07D491/22

    摘要： Camptothecin derivatives of camptothecin of formula (I) wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.

    摘要翻译： 公开了式（I）的喜树碱喜树碱衍生物，其中基团R 1，R 2和R 3如说明书中所定义。式（I）化合物具有抗肿瘤活性并具有良好的治疗指标。 还公开了式（I）化合物及其在制备用于治疗肿瘤，病毒感染和恶性疟原虫药物中的用途。

    3-aryl-glycidic ester derivatives
    35.
    发明授权
    3-aryl-glycidic ester derivatives 失效
    3-芳基 - 缩水甘油酯衍生物

    公开(公告)号：US5436235A

    公开(公告)日：1995-07-25

    申请号：US16980

    申请日：1993-02-12

    申请人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    发明人： Franco Buzzetti ,  Maria G. Brasca ,  Silvia Fustinoni ,  Sergio Penco

    IPC分类号： A61K31/335 ,  A61K31/336 ,  A61K31/40 ,  A61K31/47 ,  A61P9/00 ,  A61P35/00 ,  A61P43/00 ,  C07D303/48 ,  C07D405/04 ,  C07D27/56

    CPC分类号： C07D405/04 ,  C07D303/48

    摘要： The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.

    摘要翻译： 本发明涉及式为“IMAGE”的3-芳基 - 环氧乙烷衍生物，其中Ar为4'-喹啉或5'-喹啉; R和R 1各自独立地是氢或C 1 -C 6烷氧基; X和Y中的一个是氢，氰基，-COOR 2或-CONR 3 R 4，X和Y中的另一个是氰基，-COOR 2或-CONR 3 R 4，其中R 2是C 1 -C 6烷基，R 3和R 4各自独立地是氢或C 1 -C6烷基和其药学上可接受的盐，其可用于治疗作为酪氨酸激酶抑制剂，特别是作为抗增殖剂（通常作为抗癌剂）用于治疗牛皮癣和抑制动脉粥样硬化斑块发展。

    Anthracycline glycosides, use and compositions containing same
    37.
    发明授权
    Anthracycline glycosides, use and compositions containing same 失效
    蒽环类苷，用途和含有它们的组合物

    公开(公告)号：US4563444A

    公开(公告)日：1986-01-07

    申请号：US621681

    申请日：1984-06-18

    申请人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

    发明人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

    IPC分类号： C07H15/252 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252 ,  Y02P20/55

    摘要： Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.

    摘要翻译： 式（I）的蒽环酸糖苷其中R 1和R 2之一是氢，R 1和R 2中的另一个是羟基，R 3，R 4和R 5各自独立地选自氢和羟基，X 是氢或三氟乙酰基，条件是R 4和R 5不同时为羟基，如果R 3为羟基，则X为氢，其可用于治疗某些哺乳动物肿瘤通过将式（II）的糖苷配基缩合制备其中R 1和R 2如上所定义，具有合适的受保护的卤糖，之后除去保护基。

    9-Deoxy-9,10-epoxide-daunomycinone
    39.
    发明授权
    9-Deoxy-9,10-epoxide-daunomycinone 失效
    9-脱氧-9,10-环氧化物 - 道诺霉素酮

    公开(公告)号：US4229355A

    公开(公告)日：1980-10-21

    申请号：US33995

    申请日：1979-04-27

    申请人： Sergio Penco ,  Fausto Gozzi ,  Francesco Angelucci ,  Federico Arcamone

    发明人： Sergio Penco ,  Fausto Gozzi ,  Francesco Angelucci ,  Federico Arcamone

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07D303/32 ,  C07D319/08 ,  C07H15/252

    CPC分类号： C07H15/252 ,  C07D303/32 ,  C07D319/08 ,  Y10S514/908

    摘要： Compounds having the formula: ##STR1## wherein (a) whenR.sup.1 is --COCH.sub.3 or --COCH.sub.2 OH,R.sup.2 is --OH, R.sup.3 is --OCH.sub.3 and R.sup.4 is --H;(b) whenR.sup.2 is --COCH.sub.3 or --COCH.sub.2 OH;R.sup.1 is --OH, R.sup.3 is --H and R.sup.4 is --OCH.sub.3 ;and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyl daunorubicin, a known compound. The invention described herein was made in the course of work under a grant from the United States Department of Health, Education and Welfare.

    摘要翻译： 具有下式的化合物：其中（a）当R 1是-COCH 3或-COCH 2 OH时，R 2是-OH，R 3是-OCH 3，且R 4是-H; （b）当R 2为-COCH 3或-COCH 2 OH时; R1是-OH，R3是-H，R4是-OCH3; 并且其可用于治疗某些哺乳动物肿瘤，由已知化合物9,10-脱氢-N-三氟乙酰柔红霉素制备。 本文描述的发明是在美国卫生，教育和福利部授予的工作过程中作出的。