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25 条记录 (耗时 0.017 秒)

    2-acyloxy-4-morpholinyl anthracyclines
    2.
    发明授权
    2-acyloxy-4-morpholinyl anthracyclines 失效
    2-酰氧基-4-吗啉基蒽环类

    公开(公告)号：US5510469A

    公开(公告)日：1996-04-23

    申请号：US987281

    申请日：1993-05-12

    申请人： Daniela Faiardi ,  Alberto Bargiotti ,  Antonino Suarato

    发明人： Daniela Faiardi ,  Alberto Bargiotti ,  Antonino Suarato

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/7042 ,  A61K31/7052 ,  A61P35/00 ,  C07H15/252 ,  C07H19/24 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Anthracycline glycosides of formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy; both R.sub.3 and R.sub.4 represent hydrogen or one of R.sub.3 and R.sub.4 is hydroxy and the other of R.sub.3 and R.sub.4 a represents hydrogen; R.sub.5 represents hydrogen atom or an acyl residue--COX in which X is a C.sub.1 -C.sub.8 linear or branched alkyl chain, an aryl, an aryl lower alkyl, or a 5- or 6-membered heteroaromatic group are anti-tumour agents.

    摘要翻译： PCT No.PCT / EP91 / 01506 Sec。 371日期：1993年5月12日 102（e）日期1993年5月12日PCT 1991年8月8日PCT PCT。 出版物WO92 / 04362 1992年3月19日。式1的蒽环糖苷：其中R1是氢或甲氧基; R2是氢或羟基; R3和R4分别代表氢或R3和R4之一是羟基，R3和R4中的另一个代表氢; R5表示氢原子或其中X为C1-C8直链或支链烷基链，芳基，芳基低级烷基或5或6元杂芳族基团的酰基残基-COX为抗肿瘤剂。

    Mono and bis alkylamino-anthracyclines
    3.
    发明授权
    Mono and bis alkylamino-anthracyclines 失效
    单和双烷基氨基蒽环类

    公开(公告)号：US5496808A

    公开(公告)日：1996-03-05

    申请号：US904650

    申请日：1992-06-26

    申请人： Alberto Bargiotti ,  Michele Caruso ,  Daniela Faiardi ,  Antonino Suarato ,  Nicola Mongelli

    发明人： Alberto Bargiotti ,  Michele Caruso ,  Daniela Faiardi ,  Antonino Suarato ,  Nicola Mongelli

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H20060101 ,  C07H15/252 ,  C07H15/24

    CPC分类号： A61K31/70 ,  C07H15/252

    摘要： An anthracycline glycoside of general formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy group, A and B both represent hydrogen or one of A and B is hydrogen and the other is hydroxy or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is C1-C4 alkyl or aryl optionally substituted by C1-C4 alkyl, nitro, amino, methoxy or halogen; R.sub.3 is a hydrogen atom or a group of formula 2 and R.sub.4 is a group of formula 2--(CH.sub.2).sub.n --X 2in which n is 2 or 3 and X is hydroxy group, a halogen or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is as defined above and with the proviso that if R.sub.2, X and A are an hydroxy group and R.sub.3 .dbd.H, n must be 3; or a pharmaceutically acceptable salt thereof.Compounds of the invention have activity as antitumor agents. Processes for their preparation and pharmaceutical composition containing them are also disclosed.

    摘要翻译： 通式1的蒽环类苷：oup; R2是氢或羟基，A和B都代表氢或A和B之一是氢，另一个是羟基或式-OSO 2 R 5基团，其中R 5是任选被C 1 -C 4烷基取代的C 1 -C 4烷基或芳基 ，硝基，氨基，甲氧基或卤素; R3是氢原子或式2的基团，R4是式2 - （CH2）nX2的基团，其中n是2或3，X是羟基，卤素或式-OSO2R5基团，其中R5 条件是如果R2，X和A是羟基，R3 = H，则n必须为3; 或其药学上可接受的盐。 本发明的化合物具有作为抗肿瘤剂的活性。 还公开了其制备方法和含有它们的药物组合物。

    3'-aziridino-anthracycline derivatives
    5.
    发明授权
    3'-aziridino-anthracycline derivatives 失效
    3'-氮丙啶基 - 蒽环类衍生物

    公开(公告)号：US5532218A

    公开(公告)日：1996-07-02

    申请号：US345450

    申请日：1994-11-21

    申请人： Alberto Bargiotti ,  Michele Caruso ,  Maria Grandi ,  Marina Ripamonti ,  Antonino Suarato

    发明人： Alberto Bargiotti ,  Michele Caruso ,  Maria Grandi ,  Marina Ripamonti ,  Antonino Suarato

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  C07H17/02 ,  C07H15/24

    CPC分类号： C07H15/252 ,  C07H17/02

    摘要： Anthracycline glycosides of general formula 1 and 2: ##STR1## wherein R.sub.1 is hydrogen or a methoxy group; R.sub.2 is hydrogen, a hydroxy group or represents an acyloxy residue of formula 3 --O--COR.sub.5 wherein R.sub.5 is a linear or branched C.sub.1 -C.sub.8 alkyl, an aryl group or a heterocyclic mono or bicyclic ring, each of which may be unsubstituted or substituted with (a) an amino group NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1 -C.sub.4 alkyl or (b) a carboxy group; R.sub.3 and R.sub.4 both represent hydrogen or one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy group or a group of formula --OSO.sub.2 R.sub.8 in which R.sub.8 may be a linear or branched alkyl group containing from 1 to 6 carbon atoms or an aryl group unsubstituted or substituted by 1 to 3 substituents each of which may independently be a linear or branched alkyl or alkoxy group of from 1 to 6 carbon atoms, a halogen atom or a nitro group; and pharmaceutically acceptable salts thereof; are active as antitumor agents.

    摘要翻译： 通式1和2的蒽环酸苷：其中R 1是氢或甲氧基; R2是氢，羟基或代表式3-COR5的酰氧基残基，其中R5是直链或支链C1-C8烷基，芳基或杂环单环或双环，其各自可以是未取代或取代的 与（a）氨基NR 6 R 7，其中R 6和R 7独立地是氢或C 1 -C 4烷基或（b）羧基; R 3和R 4均代表氢或R 3和R 4之一是氢，另一个是羟基或式-OSO 2 R 8基团，其中R 8可以是含有1至6个碳原子的直链或支链烷基或未取代的芳基 或被1〜3个取代基取代，各自可以独立地为具有1-6个碳原子的直链或支链烷基或烷氧基，卤素原子或硝基; 及其药学上可接受的盐; 作为抗肿瘤剂有活性。