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    Polymer-bound paclitaxel derivatives
    1.
    发明授权
    Polymer-bound paclitaxel derivatives 失效
    聚合物结合紫杉醇衍生物

    公开(公告)号：US5362831A

    公开(公告)日：1994-11-08

    申请号：US77065

    申请日：1993-06-16

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  A61K31/765 ,  C80F222/38

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式 ，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键 ，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， Ala，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-βAla，Phe-Ala-βAla，Leu-Phe-βAla，Leu-Gly-βAla ，Phe-Leu-Gly-β-Ala，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Glyβ Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，该化合物具有抗肿瘤活性并显示改善的水溶性和降低的毒性。 还描述了其制备方法和含有它们的药物组合物。

    Polymer-bound paclitaxel derivatives
    3.
    发明授权
    Polymer-bound paclitaxel derivatives 失效

    公开(公告)号：US5569720A

    公开(公告)日：1996-10-29

    申请号：US508210

    申请日：1995-07-27

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  C08F20/56 ,  C08F8/30 ,  C08F8/32

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

    Polymer-bound paclitaxel derivatives
    4.
    发明授权
    Polymer-bound paclitaxel derivatives 失效
    聚合物结合紫杉醇衍生物

    公开(公告)号：US5473055A

    公开(公告)日：1995-12-05

    申请号：US263832

    申请日：1994-06-22

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta.Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式 ，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键 ，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， βAla，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-Ala，Phe-Ala-Ala，Leu-Phe-βAla，Leu-Gly-β Ala，Phe-Leu-Gly-βAla，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Gly β-Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，这些化合物具有抗肿瘤活性， 。 还描述了其制备方法和含有它们的药物组合物。

    Mono and bis alkylamino-anthracyclines
    5.
    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。

    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
    9.
    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。