公开(公告)号：US20070082872A1

公开(公告)日：2007-04-12

申请号：US10555352

申请日：2004-05-03

申请人： Kevin Pinney ,  Feng Wang ,  Mallinath Hadimani ,  Maria Mejia

发明人： Kevin Pinney ,  Feng Wang ,  Mallinath Hadimani ,  Maria Mejia

IPC分类号： A61K31/675 ,  C07F9/547 ,  A61K31/404 ,  C07D209/36

CPC分类号： C07D209/12 ,  C07F9/247 ,  C07F9/5728

摘要： Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin assembly. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

摘要翻译： 已经发现了三甲氧基苯基取代的吲哚配体，其表现出令人印象深刻的细胞毒性以及显着的抑制微管蛋白装配的能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外，作为前药的这些配体中的某些可以很好地证明是肿瘤选择性血管靶向化学治疗剂或具有导致选择性预防和/或破坏非恶性增殖血管的血管靶向活性。

公开(公告)号：US06849656B1

公开(公告)日：2005-02-01

申请号：US10070484

申请日：2000-09-15

申请人： Kevin Pinney ,  Feng Wang ,  Mallinath Hadimani

发明人： Kevin Pinney ,  Feng Wang ,  Mallinath Hadimani

IPC分类号： C07D209/12 ,  C07F9/24 ,  C07F9/572 ,  A61K31/404

CPC分类号： C07F9/247 ,  C07D209/12 ,  C07F9/5728

摘要： Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as prodrugs, may well prove to be tumor selective vascular targeting and destruction chemotherapeutic agents or to have anti-angiogenesis activity resulting in the selective prevention and/or destruction of tumor cell vasculature.

摘要翻译： 已经发现了三甲氧基苯基取代的吲哚配体，其表现出令人印象深刻的细胞毒性以及抑制微管蛋白聚合的显着能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外，作为前药的这些配体中的某些可以很好地证明是肿瘤选择性血管靶向和破坏化学治疗剂，或具有抗血管生成活性，导致选择性预防和/或破坏肿瘤细胞脉管系统。

公开(公告)号：US20060142252A1

公开(公告)日：2006-06-29

申请号：US11359095

申请日：2006-02-21

申请人： Kevin Pinney ,  Vani Mocharla ,  Zhi Chen ,  Charles Garner ,  Anjan Ghatak ,  Usha Ghatak ,  Mallinath Hadimani ,  Jimmy Kessler ,  James Dorsey ,  Klaus Edvardson ,  David Chaplin ,  Joseph Prezioso

发明人： Kevin Pinney ,  Vani Mocharla ,  Zhi Chen ,  Charles Garner ,  Anjan Ghatak ,  Usha Ghatak ,  Mallinath Hadimani ,  Jimmy Kessler ,  James Dorsey ,  Klaus Edvardson ,  David Chaplin ,  Joseph Prezioso

IPC分类号： A61K31/66 ,  A61K31/075

CPC分类号： C07C43/23 ,  A61K31/075 ,  A61K31/66 ,  C07C43/215 ,  C07C45/512 ,  C07C45/64 ,  C07C45/673 ,  C07C49/755 ,  C07C49/84 ,  C07C205/37 ,  C07C205/45 ,  C07C217/84 ,  C07C217/94 ,  C07C223/06 ,  C07C225/22 ,  C07C237/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07D307/80 ,  C07D307/81 ,  C07D333/56 ,  C07D333/64 ,  C07F9/12 ,  C07F9/18 ,  C07F9/247 ,  C07F9/65517 ,  C07F9/655354

摘要： A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

公开(公告)号：US20050065217A1

公开(公告)日：2005-03-24

申请号：US10861186

申请日：2004-06-04

申请人： Kevin Pinney ,  Feng Wang ,  Maria Mejia

发明人： Kevin Pinney ,  Feng Wang ,  Maria Mejia

IPC分类号： C07D209/12 ,  C07F9/24 ,  C07F9/572 ,  A61K31/16 ,  C07C235/20

CPC分类号： C07F9/247 ,  C07D209/12 ,  C07F9/5728

摘要： Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting and destruction chemotherapeutic agents or to have anti-angiogenesis activity resulting in the selective prevention and/or destruction of tumor cell vasculature.

摘要翻译： 已经发现了三甲氧基苯基取代的吲哚配体，其表现出令人印象深刻的细胞毒性以及抑制微管蛋白聚合的显着能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外，作为前药的这些配体中的某些可能被证明是肿瘤选择性血管靶向和破坏化学治疗剂，或者具有导致选择性预防和/或破坏肿瘤细胞脉管系统的抗血管生成活性。

公开(公告)号：US20050245489A1

公开(公告)日：2005-11-03

申请号：US10837841

申请日：2004-05-03

申请人： Kevin Pinney ,  Phyllis Arthasary ,  Anupama Shirali ,  Klaus Edvardsen ,  David Chaplin

发明人： Kevin Pinney ,  Phyllis Arthasary ,  Anupama Shirali ,  Klaus Edvardsen ,  David Chaplin

IPC分类号： A61K31/353 ,  A61K31/665 ,  C07D311/04 ,  C07D311/12 ,  C07D311/16 ,  C07D311/18

CPC分类号： C07D311/18 ,  C07D311/12 ,  C07D311/16

摘要： Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

摘要翻译： 已经发现了三甲氧基苯基取代的吲哚配体，其表现出令人印象深刻的细胞毒性以及抑制微管蛋白聚合的显着能力。 这些化合物以及相关衍生物是用于治疗人类癌症的优异临床候选物。 此外，作为前药的这些配体中的某些可以很好地证明是肿瘤选择性血管靶向化学治疗剂或具有导致选择性预防和/或破坏非恶性增殖血管的血管靶向活性。

公开(公告)号：US20060035868A1

公开(公告)日：2006-02-16

申请号：US11183556

申请日：2005-07-18

申请人： David Chaplin ,  Charles Garner ,  Robert Kane ,  Kevin Pinney ,  Joseph Prezioso ,  Klaus Edvardsen

发明人： David Chaplin ,  Charles Garner ,  Robert Kane ,  Kevin Pinney ,  Joseph Prezioso ,  Klaus Edvardsen

IPC分类号： A61K31/66 ,  C07F9/12

CPC分类号： C07C43/23 ,  C07C45/63 ,  C07C47/575 ,  C07C205/37 ,  C07C207/04 ,  C07C217/84 ,  C07C237/04 ,  C07F9/12

摘要： Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

公开(公告)号：US20050272824A1

公开(公告)日：2005-12-08

申请号：US11089612

申请日：2005-03-25

申请人： Kevin Pinney ,  Hania Wehbe ,  Christopher Kearney

发明人： Kevin Pinney ,  Hania Wehbe ,  Christopher Kearney

IPC分类号： A61K31/075 ,  G01N33/574

CPC分类号： G01N33/57484

摘要： Methods and diagnostic kits for monitoring combretastatin resistance are provided.

摘要翻译： 提供了用于监测库里他汀耐药性的方法和诊断试剂盒。

公开(公告)号：US20060293394A1

公开(公告)日：2006-12-28

申请号：US11454074

申请日：2006-06-14

申请人： Kevin Pinney ,  Madhavi Sriram

发明人： Kevin Pinney ,  Madhavi Sriram

IPC分类号： A61K31/12 ,  A01N31/14 ,  C07C49/00 ,  C07C43/20

CPC分类号： C07C43/23 ,  C07C43/215 ,  C07C49/84 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12

摘要： Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

公开(公告)号：US20050245490A1

公开(公告)日：2005-11-03

申请号：US10851445

申请日：2004-05-21

申请人： Kevin Pinney ,  Phyllis Arthasary ,  Anupama Shirali ,  Klaus Edvardsen ,  David Chaplin

发明人： Kevin Pinney ,  Phyllis Arthasary ,  Anupama Shirali ,  Klaus Edvardsen ,  David Chaplin

IPC分类号： A61K31/35 ,  A61K31/353 ,  A61K31/665 ,  A61P35/00 ,  C07D311/58

CPC分类号： C07D311/58

摘要： Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.