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公开(公告)号：US5175182A
公开(公告)日：1992-12-29
申请号：US613490
申请日：1990-11-05
IPC分类号： A61K31/00 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/495 , A61K31/787 , A61P35/00 , C07D207/34 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D207/34
摘要： The invention relates to acryloyl substituted pyrrole derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, --CN, --NO.sub.2, C.sub.1 -C.sub.4 alkyl, or a group ##STR2## R.sub.3 is hydrogen, halogen, --CN, or --NO.sub.2 ; each R.sub.4 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;A is a bond, a group ##STR3## or a group --NH--Het--CO--, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; andB is a group ##STR4## in which m is 1, 2 or 3 and each R.sub.5 is, independently, a C.sub.1 -C.sub.4 alkyl group, and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.
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2.发明授权
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。
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公开(公告)号：US5534539A
公开(公告)日：1996-07-09
申请号：US489621
申请日：1995-06-12
IPC分类号： A61K31/40 , A61K31/475 , A61K31/505 , A61K31/675 , A61K31/70 , A61K31/785 , A61K38/04 , A61P17/00 , A61P27/02 , A61P29/00 , A61P35/00 , C07D207/34 , A61K31/395
CPC分类号： C07D207/34 , A61K31/40 , A61K31/475 , A61K31/505 , A61K31/675 , A61K31/70 , A61K31/785 , A61K38/04
摘要： The invention relates to the use of compounds of formula (I) ##STR1## 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 pharmaceutically acceptable salts thereof, in the preparation of a medicament for use in preventing and/or treating the metastatic spread of tumors.
摘要翻译： 本发明涉及式（I）化合物（I）的用途，其中m和n各自相同，为1〜3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在制备用于预防和/或治疗肿瘤转移性扩散的药物中的用途。
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公开(公告)号：US5362831A
公开(公告)日：1994-11-08
申请号：US77065
申请日：1993-06-16
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。 -
5.发明授权Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents 有权丙烯酰取代的雷霉霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途公开(公告)号：US06482920B1
公开(公告)日：2002-11-19
申请号：US09147573
申请日：1999-01-22
申请人： Paolo Cozzi , Italo Beria , Giovanni Biasoli , Marina Caldarelli , Laura Capolongo , Cristina Franzetti
发明人： Paolo Cozzi , Italo Beria , Giovanni Biasoli , Marina Caldarelli , Laura Capolongo , Cristina Franzetti
IPC分类号： C07K508
CPC分类号： C07D207/34
摘要： The present invention relates to acrylol substituted distamycin derivatives, to pharmaceutical compositions comprising such derivatives as well as their use in methods of treating humans and animals, particularly as anti-tumor agents.
摘要翻译： 本发明涉及丙烯酰取代的雷霉霉素衍生物，包含这些衍生物的药物组合物以及它们在治疗人和动物，特别是作为抗肿瘤剂的方法中的用途。
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公开(公告)号：US5719265A
公开(公告)日：1998-02-17
申请号：US508209
申请日：1995-07-27
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 , A61K38/04
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##
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; 0〜9.9摩尔％的由式 表示的单元 -
公开(公告)号：US5569720A
公开(公告)日：1996-10-29
申请号：US508210
申请日：1995-07-27
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.
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8.发明授权
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。
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9.发明授权
公开(公告)号：US5596105A
公开(公告)日：1997-01-21
申请号：US372872
申请日：1995-01-13
IPC分类号： A61K31/40 , A61P31/12 , A61P31/18 , C07D207/34 , C07D207/36
CPC分类号： C07D207/34
摘要： The invention relates to naphthalenesulfonic-pyrrolecarboxamido compounds of formula ##STR1## wherein n is zero or an integer of 1 to 3; R is a sulfonic acid residue; m is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, which are active as antiviral agents, in particular against Human Immunodeficiency Virus
摘要翻译： 本发明涉及式（I）+（其中n为0或1〜3的整数）的萘磺酰 - 吡咯酰胺化合物。 R是磺酸残基; m为1〜3的整数，或其药学上可接受的盐，其作为抗病毒剂具有活性，特别是针对人类免疫缺陷病毒
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公开(公告)号：US5473055A
公开(公告)日：1995-12-05
申请号：US263832
申请日：1994-06-22
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。
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