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39 条记录 (耗时 0.022 秒)

    Mono and bis alkylamino-anthracyclines
    1.
    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
    6.
    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。

    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis
    9.
    发明授权
    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis 失效
    氨基蒽环类衍生物及其在治疗淀粉样变性中的应用

    公开(公告)号：US06268362B1

    公开(公告)日：2001-07-31

    申请号：US09622921

    申请日：2000-09-07

    申请人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    发明人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    IPC分类号： A61K315377

    CPC分类号： C07D405/06 ,  C07D211/70

    摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

    摘要翻译： 式（1）的化合物，其中R 1表示氢，羟基，式OR 7的基团，其中R 7是C 1 -C 6烷基，C 2 -C 6烯基; R2代表氢，羟基，二乙基氨基，哌啶子基，四氢吡啶基或吗啉代，独立的R 3独立地代表氢或羟基，独立地，R 4和R 5独立地表示氢，羟基或与碳原子一起代表 羰基; 或R 3和R 4一起表示式（A）的基团，其中R 8和R 9表示C 1 -C 6烷基，R 5表示氢; R6代表氢或任选被甲基，甲氧基或卤素取代的苯基及其药物上可接受的盐，可用于治疗淀粉样变性。 还描述了制备方法和药物组合物。