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公开(公告)号：US5777104A
公开(公告)日：1998-07-07
申请号：US392744
申请日：1995-03-08
IPC分类号： A61K31/545 , C07D501/00
CPC分类号： C07D501/00 , A61K31/545
摘要： The present invention relates to the use of known cephem derivatives of the formula: ##STR1## wherein n is zero, one or two; R.sup.1 is hydrogen or an organic radical, R.sup.2 represents halo or an organic radical or R.sup.1 and R.sup.2 taken together with the C-2 carbon atom of the cephem nucleus constitute a carbocyclic or heterocyclyl group; R.sup.3 represents R.sup.2 as defined above or an organic radical, R.sup.4 is either R.sup.1 or an organic group, R.sup.5 is either R.sup.1 as defined above or halo or C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or C.sub.1 -C.sub.6 acylamino;R.sup.6 is R.sup.2 as defined above or an organic group, or a pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / EP94 / 02059 Sec。 371日期：1995年3月8日 102（e）1995年3月8日PCT PCT 1994年6月24日PCT公布。 公开号WO95 / 02603 日本1995年1月26日本发明涉及已知的头孢烯衍生物，其具有下式：IMA GE> en或有机基团，R 2表示卤素或有机基团，或者R 1和R 2与C-2碳原子一起 头孢烯核构成碳环或杂环基; R3表示如上所定义的R 2或有机基团，R 4为R 1或有机基团，R 5为如上定义的R 1或卤素或C 1 -C 6烷氧基，C 1 -C 6烷硫基或C 1 -C 6酰氨基; R6是如上定义的R2或有机基团，或其药学上可接受的盐。
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2.发明申请THERAPEUTIC COMBINATION COMPRISING A CDKS INHIBITOR AND AN ANTINEOPLASTIC AGENT 有权包含CDKS抑制剂和抗原药物的治疗组合公开(公告)号：US20110312909A1
公开(公告)日：2011-12-22
申请号：US13055541
申请日：2009-07-29
IPC分类号： A61K31/519 , A61K31/7068 , A61B19/02 , A61P35/00
CPC分类号： A61K31/7068 , A61K31/4745 , A61K31/495 , A61K31/513 , A61K31/519 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
摘要翻译： 本发明提供治疗组合，其包含（a）如说明书中所述的式（I）化合物和（b）一种或多种抗肿瘤剂，其选自烷基化或烷基化样试剂，抗代谢剂和拓扑异构酶 I抑制剂，其中活性成分在每种情况下以游离形式或以药学上可接受的盐或其任何水合物的形式存在。
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3.发明申请THERAPEUTIC COMBINATION COMPRISING A CDC7 INHIBITOR AND AN ANTI-NEOPLASTIC AGENT 有权包含CDC7抑制剂和抗神经药物的治疗组合公开(公告)号：US20120276093A1
公开(公告)日：2012-11-01
申请号：US13509625
申请日：2010-11-17
IPC分类号： A61K31/506 , A61K33/24 , A61K31/655 , A61K31/513 , A61K31/7068 , A61P35/00 , A61K31/704 , A61K31/7048 , A61K31/517 , A61K31/69 , A61K31/5377 , A61K39/395 , A61K31/519
CPC分类号： A61K45/06 , A61K31/40 , A61K31/495 , A61K31/506 , A61K2300/00
摘要： The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
摘要翻译： 本发明提供治疗组合，其包含（a）如说明书中所述的式（I）化合物和（b）一种或多种抗肿瘤剂，其选自烷基化或烷基化样试剂，抗代谢药 ，拓扑异构酶I抑制剂，拓扑异构酶11抑制剂，生长因子或生长因子受体的抑制剂，抗有丝分裂剂，蛋白酶体抑制剂，抗凋亡蛋白的抑制剂和针对细胞表面蛋白的抗体， 其中活性成分在每种情况下以虱子形式存在，或以药学上可接受的盐或其任何水合物的形式存在。
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4.发明申请Antitumor Combination Comprising Substituted Acryloyl Distamycin Derivatives and Antibodies Inhibiting Growth Factors or Their Receptors 审中-公开包含取代的丙烯酰基间质霉素衍生物和抑制生长因子或其受体的抗体的抗肿瘤组合公开(公告)号：US20090074757A1
公开(公告)日：2009-03-19
申请号：US11887998
申请日：2006-03-29
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K31/40 , A61K39/395 , A61K39/39533 , A61K39/39558 , C07K2317/24 , A61K2300/00
摘要： The present invention provides the combined use of acryloyl distamycin derivatives, in particular α-homo- and α-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, and an antibody inhibiting a growth factor or its receptor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
摘要翻译： 本发明提供丙烯酰基地霉素衍生物，特别是说明书所述的式（I）的α-均 - 和α-氯 - 丙烯酰基霉霉素衍生物和抑制生长因子或其受体的抗体的组合使用， 在治疗肿瘤。 还提供了所述组合在治疗或预防转移中或在通过抑制血管生成治疗肿瘤中的用途。
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公开(公告)号：US5700788A
公开(公告)日：1997-12-23
申请号：US535056
申请日：1995-10-30
IPC分类号： A61K31/675 , A61P9/00 , A61P29/00 , A61P31/12 , A61P31/18 , A61P33/02 , A61P37/06 , C07F9/38 , C07F9/40 , C07F9/572
CPC分类号： C07F9/5722
摘要： Subject of the present invention are new ureido derivatives of naphthalenephosphonic acids having the following formula (I) ##STR1## wherein each of m and n, which are the same, is an integer of 1 to 4; each of p and q, which are the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a free or esterified phosphonic acid group; and the pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / EP95 / 00444 Sec。 371 1995年10月30日第 102（e）1995年10月30日日期PCT提交1995年2月8日PCT公布。 公开号WO95 / 23806 日本1995年9月8日本发明的目的是具有下式（I）的萘膦酸的新脲基衍生物，其中相同的m和n是1的整数， 到4; p和q各自相同，为1〜3的整数， 相同的R基团是游离的或酯化的膦酸基团; 及其药学上可接受的盐。
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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。 -
公开(公告)号：US08946226B2
公开(公告)日：2015-02-03
申请号：US13055533
申请日：2009-07-28
IPC分类号： A61K45/06 , A61K31/4188 , A61K31/519
CPC分类号： A61K31/519 , A61K31/4188 , A61K45/06 , A61K2300/00
摘要： The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
摘要翻译： 本发明提供了能够跨越血脑屏障用于治疗恶性胶质瘤，特别是胶质母细胞瘤的低分子量ATP竞争性CDK抑制剂。 化合物可以与一种或多种选自细胞毒性或细胞抑制剂和电离辐射剂的药物一起施用。
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公开(公告)号：US20110190311A1
公开(公告)日：2011-08-04
申请号：US13055533
申请日：2009-07-28
IPC分类号： C07D471/04 , A61K31/496 , A61P35/00
CPC分类号： A61K31/519 , A61K31/4188 , A61K45/06 , A61K2300/00
摘要： The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
摘要翻译： 本发明提供了能够跨越血脑屏障用于治疗恶性胶质瘤，特别是胶质母细胞瘤的低分子量ATP竞争性CDK抑制剂。 化合物可以与一种或多种选自细胞毒性或细胞抑制剂和电离辐射剂的药物一起施用。
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9.发明申请Combinations Comprising a CDK Inhibitor and a Growth Factor Antibody or Anti-Mitotic 有权包含CDK抑制剂和生长因子抗体或抗有丝分裂的组合公开(公告)号：US20090017025A1
公开(公告)日：2009-01-15
申请号：US12278530
申请日：2007-02-02
IPC分类号： A61K39/395 , A61K31/496 , A61P35/00
CPC分类号： A61K39/395 , A61K31/337 , A61K31/519 , A61K39/39558 , A61K2300/00
摘要： The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piper-azin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.
摘要翻译： 本发明提供了包含本说明书中阐述的式（I）化合物A或其药学上可接受的盐和抑制生长因子或其受体的抗体和/或抗有丝分裂剂或其衍生物或前药的组合 ，可用于治疗肿瘤。 化合物A的化学名称是8- [4-（4-甲基 - 哌嗪-1-基） - 苯基氨基] -1,4,4-三甲基-4,5-二氢-1H-吡唑并[4,3 -h]喹唑啉-3-甲酸甲基酰胺。
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10.发明申请Fluoro linkers and their use as linkers for enzyme-activated drug conjugates 审中-公开氟接头及其作为酶活化药物偶联物的接头的用途公开(公告)号：US20050107543A1
公开(公告)日：2005-05-19
申请号：US10486477
申请日：2002-07-29
申请人： Francesco Angelucci , Antonino Suarato , Michele Caruso , Alessandra Scolaro , Enrico Pesenti , Daniela Faiardi
发明人： Francesco Angelucci , Antonino Suarato , Michele Caruso , Alessandra Scolaro , Enrico Pesenti , Daniela Faiardi
IPC分类号： C07D491/22 , A61K38/00 , A61K47/48 , A61P35/00 , A61P35/02 , C07C271/22 , C07D207/46 , C07D209/48 , C07K5/10 , C07K7/06 , C07F7/02 , C08G63/48 , C08G63/91
CPC分类号： C07C271/22 , Y02P20/55
摘要： The present invention provides compounds or formula (1) R1—HN—CH2—CF2—(CH2)l—CR3R4—CO—R2, wherein: l is 0, 1 or 2, R1 is a labile amino protecting group, R2 is hydroxy group or the residue or an activated ester or halogen atom; R3 and R4 are independently hydrogen atom or C1-C4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.
摘要翻译： 本发明提供化合物或式（1）R 1 -HN-CH 2 -CF 2 - （CH 2） 其中：l是0,1或2，其中：l是0,1或2，其中：l是0,1或2， 或2，R 1是不稳定的氨基保护基团，R 2是羟基或残基或活化的酯或卤素原子; R 3和R 4独立地是氢原子或C 1 -C 4烷基链。 还提供了它们的制备和基于这些接头的水溶性缀合物，具有选择性的抗癌活性。
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