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1. 发明申请

WO2009067767A2 TARGETED RADIOTHERAPY 审中-公开
标题翻译：目标放射治疗
公开(公告)号：WO2009067767A2
公开(公告)日：2009-06-04
申请号：PCT/BE2008/000099
申请日：2008-11-26
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , NI, Yicheng , VAN DE PUTTE, Marie , DE WITTE, Peter , VERBRUGGEN, Alfons , MARCHAL, Guy
发明人： NI, Yicheng , VAN DE PUTTE, Marie , DE WITTE, Peter , VERBRUGGEN, Alfons , MARCHAL, Guy
IPC分类号： A61K51/04 , A61P35/00
CPC分类号： A61K51/04
摘要： The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability. Examples of necrosis inducing therapies are for instance minimally invasive tumor ablations applied chemically by percutaneous injection of ethanol or acetic acid, or physically by cryotherapy, microwave, focused ultrasound, interstitial laser therapy and radio- frequency ablation (RFA); by chemotherapies using cytotoxic agents or vascular targeting agents (VTA); and by external or internal radiotherapies.
摘要翻译：本发明涉及一种治疗上标记的阴蒂龙酮或菲咯啉[1,10,9,8-吖庚因]二萘嵌苯-7,14-二酮化合物，其包含具有不稳定核的化学元素或同位素，并在其衰变期间发射辐射足以破坏用于靶向放射治疗的相邻细胞或组织的稳定形式，以增强已经进行坏死诱导的抗肿瘤治疗的温血动物的固化性。本发明的一个特别优点是可以通过一种单独或重复剂量的治疗性放射性标记的小分子坏死化学化合物治疗来补充对坏死诱导的抗肿瘤治疗如血管靶向剂（VTA）有抗性的活性边缘，以增强固化性。坏死诱导疗法的实例是例如通过经皮注射乙醇或乙酸而化学施用的微创肿瘤消融，或通过冷冻治疗，微波，聚焦超声，间质激光治疗和射频消融（RFA）物理化的微创肿瘤消融。通过使用细胞毒剂或血管靶向剂（VTA）的化疗; 以及外部或内部放射治疗。

2. 发明申请

WO2005009423A1 NECROSIS AVID TRACER AGENT 审中-公开
标题翻译： NECROSIS AVID追踪器代理
公开(公告)号：WO2005009423A1
公开(公告)日：2005-02-03
申请号：PCT/BE2004/000107
申请日：2004-07-23
申请人： K.U.LEUVEN RESEARCH AND DEVELOPMENT , NI, Yicheng , BORMANS, Guy , MARCHAL, Guy , VERBRUGGEN, Alfons
发明人： NI, Yicheng , BORMANS, Guy , MARCHAL, Guy , VERBRUGGEN, Alfons
IPC分类号： A61K31/122
CPC分类号： A61K31/122 , A61K51/0406
摘要： The present invention concerns to the use of phenanthro[1,10,9,8-opqra]perylene-7,14-dione derivatives, and more specifically hypericin or its derivatives, as necrosis or infarct specific agents. The phenanthro[1,10,9,8-opqra]perylene-7,14-dione derivatives can be labeled with a radionuclide, a radiopaque material or a material enhancing the effects magnetic resonance imaging.
摘要翻译：本发明涉及菲咯啉[1,10,9,8-opqra]苝-7,14-二酮衍生物，更具体地涉及金丝桃素或其衍生物作为坏死或梗死特异性试剂的用途。菲咯啉[1,10,9,8-opqra]苝-7,14-二酮衍生物可用放射性核素，不透射线材料或增强磁共振成像效果的材料进行标记。

3. 发明申请

WO2009067767A3 TARGETED RADIOTHERAPY 审中-公开
标题翻译：目标放射治疗
公开(公告)号：WO2009067767A3
公开(公告)日：2010-01-21
申请号：PCT/BE2008000099
申请日：2008-11-26
申请人： UNIV LEUVEN KATH , NI YICHENG , VAN DE PUTTE MARIE , DE WITTE PETER , VERBRUGGEN ALFONS , MARCHAL GUY
发明人： NI YICHENG , VAN DE PUTTE MARIE , DE WITTE PETER , VERBRUGGEN ALFONS , MARCHAL GUY
IPC分类号： A61K51/04 , A61P35/00
CPC分类号： A61K51/04
摘要： The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability. Examples of necrosis inducing therapies are for instance minimally invasive tumor ablations applied chemically by percutaneous injection of ethanol or acetic acid, or physically by cryotherapy, microwave, focused ultrasound, interstitial laser therapy and radio- frequency ablation (RFA); by chemotherapies using cytotoxic agents or vascular targeting agents (VTA); and by external or internal radiotherapies.
摘要翻译：本发明涉及一种治疗上标记的阴蒂龙酮或菲咯啉[1,10,9,8-吖庚因]二萘嵌苯-7,14-二酮化合物，其包含具有不稳定核的化学元素或同位素，并在其衰变期间发射辐射足以破坏用于靶向放射治疗的相邻细胞或组织的稳定形式，以增强已经进行坏死诱导的抗肿瘤治疗的温血动物的固化性。本发明的一个特别优点是可以通过一种单独或重复剂量的治疗性放射性标记的小分子坏死化学化合物治疗来补充对坏死诱导的抗肿瘤治疗如血管靶向剂（VTA）有抗性的活性边缘，以增强固化性。坏死诱导疗法的实例是例如通过经皮注射乙醇或乙酸而化学施用的微创肿瘤消融，或通过冷冻治疗，微波，聚焦超声，间质激光治疗和射频消融（RFA）物理化的微创肿瘤消融。通过使用细胞毒剂或血管靶向剂（VTA）的化疗; 以及外部或内部放射治疗。

4. 发明申请

WO1995031219A1 THE USE OF PORPHYRIN-COMPLEX OR EXPANDED PORPHYRIN-COMPLEX COMPOUNDS AS LOCALIZATION DIAGNOSTICUM FOR INFARCTION OR NECROSIS 审中-公开
标题翻译：使用PORPHYRIN复合物或扩展的PORPHYRIN复合化合物作为局部化诊断用于感染或NECROSIS
公开(公告)号：WO1995031219A1
公开(公告)日：1995-11-23
申请号：PCT/EP1995001762
申请日：1995-05-10
申请人： K.U. LEUVEN RESEARCH & DEVELOPMENT , MARCHAL, Guy, Jacques, Felix , NI, Yicheng
发明人： K.U. LEUVEN RESEARCH & DEVELOPMENT
IPC分类号： A61K49/00
CPC分类号： A61K51/0485 , A61K49/06 , A61K2123/00
摘要： The invention relates to the use of porphyrin-complex or expanded porphyrin-complex compounds for the manufacture of a diagnosticum for the localization of an infarction and of a necrosis, wherein the infarction or necrosis may comprise an infarction of heart, kidney, intestine, lung, and/or brain, and wherein the porphyrin-complex compound may be Gd-MP and/or Mn-TPP. Gd-MP: Bis-Gd-DTPA-{Mesoporphyrin-IX-13, 17-bis[2-oxo-4,7,10,10-tetra-(carboxylatomethyl)-1,4,7,10-tetraazadecyl]-13, 17-diamide}, bis sodium salt of formula (A); Mn-TPP: Manganese-(III)-{Tetrakis-[3]-(carboxylatomethoxy-phenyl)-porphyrin}-acetate, tetra sodium salt of formula (B).
摘要翻译：本发明涉及卟啉复合物或膨胀卟啉 - 络合物化合物在制造用于梗死和坏死定位的诊断物中的用途，其中梗死或坏死可包括心脏，肾脏，肠，肺的梗死，和/或脑，并且其中所述卟啉 - 络合物可以是Gd-MP和/或Mn-TPP。 Gd-MP：Bis-Gd-DTPA- {卟啉Ⅸ-13,17-双[2-氧代-4,7,10,10-四 - （羧基甲基）-1,4,7,10-四氮杂] 13，17-二酰胺}，式（A）的双钠盐; Mn-TPP：锰 - （III） - {四 - [3] - （羧基甲氧基 - 苯基） - 卟啉}乙酸酯，式（B）的四钠盐。

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