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11 条记录 (耗时 0.016 秒)

    3'-aziridino-anthracycline derivatives
    1.
    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。

    Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds
    2.
    发明授权
    Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
    聚-4-氨基-2-羧基-1-甲基化合物的脲基衍生物

    公开(公告)号：US5420296A

    公开(公告)日：1995-05-30

    申请号：US66583

    申请日：1993-05-25

    申请人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    发明人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    IPC分类号： A61K31/40 ,  A61K31/7056 ,  A61P3/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D207/325 ,  C07D207/335 ,  C07D207/34 ,  C07D403/02 ,  C07D403/14

    CPC分类号： C07D207/34

    摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.

    摘要翻译： 本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n各自相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）r CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

    Synergistic antitumor composition containing a naphthalensulphonic acid derivative
    5.
    发明授权
    Synergistic antitumor composition containing a naphthalensulphonic acid derivative 失效
    含有萘磺酸衍生物的协同抗肿瘤组合物

    公开(公告)号：US06214860B1

    公开(公告)日：2001-04-10

    申请号：US09367853

    申请日：1999-08-30

    申请人： Francesco Sola ,  Maria Grandi

    发明人： Francesco Sola ,  Maria Grandi

    IPC分类号： A61K3140

    CPC分类号： A61K45/06

    摘要： A pharmaceutical composition for use in antineoplastic therapy in mammals, including humans, comprising a biologically active ureido compound of formula (I) wherein each of m and n, being the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a naphthyl group substituted by 1 to 3 sulfonic groups, or a pharmaceutically acceptable salt thereof, and an antineoplastic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite, an antineoplastic platinum coordination complex, an antineoplastic taxane compound, an antineoplastic ceramide compound, an antineoplastic distamycin compound, an antineoplastic epidophyllotoxin compound and an antineoplastic topoisomerase I inhibitor, and a pharmaceutically acceptable carrier or excipient, in amounts effective to produce a synergistic antineoplastic effect, is provided herein.

    摘要翻译： 一种用于哺乳动物（包括人）抗肿瘤治疗的药物组合物，其包含式（I）的生物活性脲基化合物，其中m和n相同，为1至3的整数; 并且相同的R基中的每一个是被1至3个磺酸基取代的萘基或其药学上可接受的盐，以及抗肿瘤剂，其选自抗肿瘤长春花生物碱，抗肿瘤抗生素， 抗肿瘤抗代谢物，抗肿瘤性铂配位络合物，抗肿瘤性紫杉烷化合物，抗肿瘤性神经酰胺化合物，抗肿瘤性霉素化合物，抗肿瘤性表鬼臼毒素化合物和抗肿瘤性拓扑异构酶I抑制剂以及药学上可接受的载体或赋形剂， 协同抗肿瘤作用。

    New ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds
    6.
    发明授权
    New ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
    聚-4-氨基-2-羧基-1-甲基化合物的新脲基衍生物

    公开(公告)号：US5593976A

    公开(公告)日：1997-01-14

    申请号：US426130

    申请日：1995-04-21

    申请人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    发明人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    IPC分类号： A61K31/40 ,  A61K31/7056 ,  A61P3/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D207/325 ,  C07D207/335 ,  C07D207/34 ,  C07D403/02 ,  C07D403/14

    CPC分类号： C07D207/34

    摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.8 CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2;and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.

    摘要翻译： 本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n各自相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）8 CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

    Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds
    8.
    发明授权
    Ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds 失效
    聚-4-氨基-2-羧基-1-甲基化合物的脲基衍生物

    公开(公告)号：US5260329A

    公开(公告)日：1993-11-09

    申请号：US752577

    申请日：1991-09-09

    申请人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    发明人： Nicola Mongelli ,  Giovanni Biasoli ,  Alfredo Paio ,  Maria Grandi ,  Marina Ciomei

    IPC分类号： A61K31/40 ,  A61K31/7056 ,  A61P3/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D207/325 ,  C07D207/335 ,  C07D207/34 ,  C07D403/02 ,  C07D403/14

    CPC分类号： C07D207/34

    摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which areuseful as angiogenesis inhibitors.

    摘要翻译： PCT No.PCT / EP91 / 00014 Sec。 371日期1991年9月9日 102（e）1991年9月9日PCT PCT 1991年1月7日PCT公布。 出版物WO91 / 10649 日期：1991年7月25日本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）r CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。

    Biologically active compounds
    10.
    发明授权
    Biologically active compounds 失效
    生物活性化合物

    公开(公告)号：US5571785A

    公开(公告)日：1996-11-05

    申请号：US351474

    申请日：1994-12-20

    申请人： Francesco Angelucci ,  Maria Grandi ,  Antonino Suarato

    发明人： Francesco Angelucci ,  Maria Grandi ,  Antonino Suarato

    IPC分类号： C07K17/08 ,  A61K47/48 ,  A61P35/00 ,  C07H15/24 ,  C07K5/107 ,  C07K9/00 ,  A61K38/16 ,  A61K31/70

    CPC分类号： A61K47/48176 ,  Y02P20/582

    摘要： The present invention provides polymer-bound anthracyclines of formula A which consists essentially of three units represented by formulae 1, 2 and 3: ##STR1## wherein: Gly represents glycine;n is 0 or 1;x is from 70 to 98 mol %,y is from 1 to 29 mol %,z is from 1 to 29 mol %,R.sub.1 is a C.sub.1 -C.sub.6 alkyl group substituted by one or more hydroxy groups;Y is an amino acid residue or a peptide spacer;[NH--D] is the residue of an anthracycline aminoglycoside [NH.sub.2 --D]; andZ is a hydroxy group or a residue of formula --NHR.sub.1 wherein R.sub.1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.

    摘要翻译： PCT No.PCT / EP94 / 01100 Sec。 371日期1994年12月20日第 102（e）1994年12月20日PCT PCT 1994年4月8日PCT公布。 第WO94 / 26311号公报 日期1994年11月24日本发明提供式A的聚合物键合蒽环类药物，其基本上由式1，2和3表示的三个单元组成：其中：Gly表示甘氨酸; n为0或1; x为70〜98摩尔％，y为1〜29摩尔％，z为1〜29摩尔％，R1为被一个或多个羟基取代的C1-C6烷基。 Y是氨基酸残基或肽间隔基; [NH-D]是蒽环类氨基糖苷[NH2-D]的残基; 并且Z是羟基或式-NHR1的残基，其中R 1如上所定义。 还提供了它们的制备方法和含有它们的药物组合物。