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1. 发明专利

JP2008546821A Compounds that regulate Vegf receptors, and use thereof 审中-公开
公开(公告)号：JP2008546821A
公开(公告)日：2008-12-25
申请号：JP2008518723
申请日：2006-06-29
申请人：イアッカリノ、グウィドIACCARINO, Guido , エディトリーエヴェンティソシエタアレスポンサビリタリミタータEditree Eventi S.R.L. , ダンドレイ、ルカドメニコD’ANDREA, Luca Domenico , トゥルコ、マリアカタリーナTURCO, Maria Caterina , トリマルコ、ブルノTRIMARCO, Bruno , ペドネ、カルロPEDONE, Carlo , レオン、ステファニアLEONE, Stefania , レオン、マリナLEONE, Marina , ロゼリ、パトリツィアROSELLI, Patrizia
发明人：グウィドイアッカリノ、 , ルカドメニコダンドレイ、 , マリアカタリーナトゥルコ、 , ブルノトリマルコ、 , カルロペドネ、 , アートゥローレオン、
IPC分类号： A61K38/00 , A61P1/04 , A61P9/00 , A61P9/10 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , C07K7/08
CPC分类号： A61K38/10 , G01N2333/475 , G01N2333/71
摘要：本発明は、血管内皮成長因子受容体に結合し血管新生反応を調節する化合物の使用に関する。受容体の認識に関与するＶＥＧＦアミノ酸領域１７−２５を模倣しそれにより血管新生プロセスを抑制または刺激する化合物を、ＶＥＧＦに依存する血管新生が過剰または不足していることを特徴とする疾患、例えば、慢性虚血、癌、増殖性網膜症およびリューマチ性関節炎、新しい血管の形成または再生の恩恵を受ける状況または状態の治療において、およびＶＥＧＦ受容体の過剰発現を呈する病変の診断において、またはＶＥＧＦ受容体活性化に依存する細胞経路を分析するための生化学的ツールとして用いることができる。

2. 发明专利

JP2009512643A Selective αvβ3 receptor peptide antagonist for the treatment and diagnostic applications 有权
公开(公告)号：JP2009512643A
公开(公告)日：2009-03-26
申请号：JP2008534912
申请日：2006-10-09
申请人：サヴィアーノ,ミケーレSAVIANO,Michele , ザッカロ,ラウラZACCARO,Laura , デル・ガット,アンナリタDEL GATTO,Annarita , ペドネ、カルロPEDONE, Carlo
发明人：サヴィアーノ，ミケーレ , ザッカロ，ラウラ , デル・ガット，アンナリタ , ペドーネ，カルロ
IPC分类号： C07K14/47 , A61K38/00 , A61K49/00 , A61K51/00 , A61P9/00 , A61P19/10 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00
CPC分类号： C07K7/64 , A61K38/00 , C07K14/46 , C07K14/745
摘要：本発明は、ｃ（ＲＧＤｆ［ＮＭｅ］Ｖ）との複合体におけるインテグリンα
ｖ β
３の結晶構造およびエキスタチンのＮＭＲ構造に基づいてデザインされた、α
ｖ β
３レセプターの新規なペプチドアンタゴニストに関する。これらのペプチドは、α
ｖ β
３レセプターの強力な且つ選択性アンタゴニストであり、そして新規な抗癌薬物としておよび／またはα
ｖ β
３ −ターゲティングされた治療およびイメージングのための適当なツールとしての新規な種類の診断非侵襲性トレーサーとして使用することができる。

3. 发明申请

WO2007042241A3 SELECTIVE ALFAVBETA3 RECEPTOR PEPTIDE ANTAGONIST FOR THERAPEUTIC AND DIAGNOSTIC APPLICATIONS 审中-公开
标题翻译：选择性ALFAVBETA3受体肽拮抗剂治疗和诊断应用
公开(公告)号：WO2007042241A3
公开(公告)日：2007-11-29
申请号：PCT/EP2006009733
申请日：2006-10-09
申请人： DEL GATTO ANNARITA , ZACCARO LAURA , PEDONE CARLO , SAVIANO MICHELE
发明人： DEL GATTO ANNARITA , ZACCARO LAURA , PEDONE CARLO , SAVIANO MICHELE
IPC分类号： C07K14/46 , A61P19/02 , A61P19/10 , A61P35/00
CPC分类号： C07K7/64 , A61K38/00 , C07K14/46 , C07K14/745
摘要： The present invention is related to new peptide antagonists of a v ß 3 receptor, designed on the basis of the crystal structure of integrin a v ß 3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the a v ß 3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for a v ß 3 -targeted therapy and imaging.
摘要翻译：本发明涉及基于整联蛋白的晶体结构设计的新的β3β受体的肽拮抗剂 3（3）与c（RGDf [NMe] V）的复合物和echistatin的NMR结构。这些肽是α3受体的有效和选择性拮抗剂，可用作新型抗癌药物和/或新型诊断性非侵入式示踪剂作为合适的工具用于靶向治疗和成像。

4. 发明申请

WO2007042241A2 SELECTIVE ALFAVBETA3 RECEPTOR PEPTIDE ANTAGONIST FOR THERAPEUTIC AND DIAGNOSTIC APPLICATIONS 审中-公开
标题翻译：选择性ALFAVBETA3受体肽拮抗剂用于治疗性和诊断性应用
公开(公告)号：WO2007042241A2
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009733
申请日：2006-10-09
申请人： DEL GATTO, Annarita , ZACCARO, Laura , PEDONE, Carlo , SAVIANO, Michele
发明人： DEL GATTO, Annarita , ZACCARO, Laura , PEDONE, Carlo , SAVIANO, Michele
CPC分类号： C07K7/64 , A61K38/00 , C07K14/46 , C07K14/745
摘要： The present invention is related to new peptide antagonists of α v β 3 receptor, designed on the basis of the crystal structure of integrin α v β 3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the α v β 3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for α v β 3 -targeted therapy and imaging.
摘要翻译：本发明涉及αVβ3受体的新型肽拮抗剂，其基于整联蛋白αβ的晶体结构设计，（RGDf [NMe] V）与echistatin的核磁共振结构进行了比较。这些肽是αvββ3受体的有效和选择性拮抗剂，并且可以用作新型抗癌药物和/或新一类诊断性非侵入性示踪剂作为合适的工具用于αvβ3靶向治疗和成像。

5. 发明申请

WO2012014046A3 SUPRAMOLECULAR AGGREGATES AS DRUG CARRIERS ON CELL EXPRESSING RECEPTORS FOR BRANCHED NEUROTENSIN 审中-公开
标题翻译：作为分泌型神经递质受体的细胞表达载体的分子聚集
公开(公告)号：WO2012014046A3
公开(公告)日：2012-04-19
申请号：PCT/IB2011001731
申请日：2011-07-27
申请人： TESAURO DIEGO , ACCARDO ANTONELLA , MORELLI GIANCARLO , PEDONE CARLO , FALCIANI CHIARA , PINI ALESSANDRO , BRACCI LUISA
发明人： TESAURO DIEGO , ACCARDO ANTONELLA , MORELLI GIANCARLO , PEDONE CARLO , FALCIANI CHIARA , PINI ALESSANDRO , BRACCI LUISA
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/543 , A61K47/60
摘要： The present invention relates to supramolecular aggregates (liposomes, vesicles, or micelles) for target selective drug delivery; more specifically it relates to supramolecular aggregates derivatized with Neurotensin peptide in a branched form and filled, in their inner compartment or in the phospholipid bilayer, with a pharmaceutical active principle such as a cytotoxic chemotherapeutic drug. The aggregates are selectively driven by the exposed branched bioactive peptides to specific receptors overexpressed in malignant cells.
摘要翻译：本发明涉及用于靶选择性药物递送的超分子聚集体（脂质体，囊泡或胶束）更具体地说，它涉及用分支形式的神经降压肽肽衍生的超分子聚集体，并在其内室或磷脂双层中用药物活性成分如细胞毒性化学治疗药物填充。聚集体由暴露的支链生物活性肽选择性地驱动到在恶性细胞中过度表达的特异性受体。

6. 发明申请

WO2007000347A2 COMPOUNDS MODULATING VEGF RECEPTOR AND USES THEREOF 审中-公开
标题翻译：化合物调节VEGF受体及其用途
公开(公告)号：WO2007000347A2
公开(公告)日：2007-01-04
申请号：PCT/EP2006/006314
申请日：2006-06-29
申请人： ROSELLI, Patrizia , LEONE, Marina , LEONE, Stefania , D'ANDREA, Luca, Domenico , PEDONE, Carlo , TRIMARCO, Bruno , IACCARINO, Guido , TURCO, Maria, Caterina
发明人： D'ANDREA, Luca, Domenico , PEDONE, Carlo , TRIMARCO, Bruno , IACCARINO, Guido , TURCO, Maria, Caterina
CPC分类号： A61K38/10 , G01N2333/475 , G01N2333/71
摘要： The present invention is related to the use of compounds which bind to the Vascular Endothelial Growth Factor Receptors and modulate the angiogenic response. The compounds, which mimic the VEGF amino acid region 17-25 involved in receptor recognition thereby inhibiting or stimulating the angiogenic process, can be used in the treatment of diseases characterized by excessive or defective angiogenesis VEGF-dependent, such as chronic ischemia, cancer, proliferative retinopathy and rheumatoid arthritis, states or conditions benefiting from the formation or regeneration of new vessels, as well as in the diagnosis of pathologies which present a overexpression of VEGF receptors or as biochemical tools to analyze the cellular pathways dependent on VEGF receptor activation.
摘要翻译：本发明涉及结合血管内皮生长因子受体并调节血管发生应答的化合物的用途。模仿参与受体识别的VEGF氨基酸区域17-25，从而抑制或刺激血管发生过程的化合物可用于治疗以血管生成过度或缺陷为特征的疾病VEGF依赖性，例如慢性缺血，癌症，增生性视网膜病变和类风湿关节炎，有利于新血管形成或再生的状态或状况，以及诊断出VEGF表达过表达的病理学或作为生物化学工具来分析依赖于VEGF受体活化的细胞途径。

7. 发明申请

WO2006128643A2 SUPRAMOLECULAR AGGREGATES CONTAINING CHELATING AGENTS AND BIOACTIVE PEPTIDES AS EFFECTIVE AND SELECTIVE DELIVERY TOOLS FOR DRUGS AND CONTRAST AGENTS IN MRI OR NUCLEAR MEDICINE 审中-公开
标题翻译：含有螯合剂和生物活性肽的分子聚集体作为药物和对比剂在MRI或核医学中的有效和选择性递送工具
公开(公告)号：WO2006128643A2
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005046
申请日：2006-05-26
申请人： ACCARDO, Antonella , TESAURO, Diego , PADUANO, Luigi , PEDONE, Carlo , ALOJ, Luigi , MORELLI, Giancarlo
发明人： ACCARDO, Antonella , TESAURO, Diego , PADUANO, Luigi , PEDONE, Carlo , ALOJ, Luigi , MORELLI, Giancarlo
CPC分类号： A61K51/1234 , A61K47/6907 , A61K47/6911 , A61K49/085 , A61K49/10 , A61K49/14 , A61K49/1812 , B82Y5/00
摘要： The invention relates to supramolecular aggregates obtained by coaggregation of two monomers: - a first monomer containing a paramagnetic or radioactive metal ion complexed by a chelating agent having a lipophilic moiety, - a second monomer containing a bioactive peptide linked to a lipophilic moiety through an organic spacer. The aggregates are selectively driven by the exposed bioactive peptide on a desired biological target. The aggregates (micelles, vesicles or liposomes) could entrap on their inner region or on their surface a pharmaceutical active principle (drug). The invention thus relates to target specific delivery of drugs and/or metal ions. The aggregates object of this invention could act as: i) selective vehicles of contrast agents for both Magnetic Resonance Imaging and Nuclear Medicine techniques; ii) selective vehicles for simultaneous delivery of a drug (in the inner compartment) and a contrast agent (on the aggregate surface, for its visualization); iii) selective delivery of a drug and a therapeutic active radionuclide such as a beta-emitting metal ion. The invention therefore provides compositions containing said aggregates for use as contrast agents, in nuclear medicine or MRI, for the selective delivery of drugs, and for simultaneous delivery of a drug and a metal ion.
摘要翻译：本发明涉及通过两个单体共聚获得的超分子聚集体： - 含有由具有亲油部分的螯合剂络合的顺磁性或放射性金属离子的第一单体， - 含有通过有机物与亲油部分连接的生物活性肽的第二单体间隔。聚集体由暴露的生物活性肽选择性地驱动在期望的生物靶上。聚集体（胶束，囊泡或脂质体）可以在其内部区域或其表面上捕获药物活性成分（药物）。因此，本发明涉及药物和/或金属离子的目标特异性递送。本发明的聚集体的目的可以用作：i）用于磁共振成像和核医学技术的造影剂的选择性载体; ii）用于同时递送药物（在内室中）和造影剂（在聚集体表面上用于其可视化）的选择性载体; iii）选择性递送药物和治疗性活性放射性核素，例如β发射金属离子。因此，本发明提供含有用作造影剂，核医学或MRI中的用于选择性递送药物以及用于同时递送药物和金属离子的所述聚集体的组合物。

8. 发明公开

EP1926494A2 AGONISTIC AND ANTAGONISTIC PEPTIDE MIMETICS OF THE VEGF ALPHA-HELIX BINDING REGION FOR USE IN THERAPY 审中-公开
标题翻译：肽激动剂和拮抗剂VEGFα-螺旋物质结合区域在治疗中的
公开(公告)号：EP1926494A2
公开(公告)日：2008-06-04
申请号：EP06754625.9
申请日：2006-06-29
申请人： Pedone, Carlo , D'Andrea, Luca Domenico , Leone, Stefania , Leone, Marina , Roselli, Patrizia , Turco, Maria Caterina , Iaccarino, Guido , Trimarco, Bruno , EDITREE S.R.L.
发明人： D'ANDREA, Luca Domenico , PEDONE, Carlo , TRIMARCO, Bruno , IACCARINO, Guido , TURCO, Maria Caterina
IPC分类号： A61K38/04
CPC分类号： A61K38/10 , G01N2333/475 , G01N2333/71
摘要： The present invention is related to the use of compounds which bind to the Vascular Endothelial Growth Factor Receptors and modulate the angiogenic response. The compounds, which mimic the VEGF amino acid region 17-25 involved in receptor recognition thereby inhibiting or stimulating the angiogenic process, can be used in the treatment of diseases characterized by excessive or defective angiogenesis VEGF-dependent, such as chronic ischemia, cancer, proliferative retinopathy and rheumatoid arthritis, states or conditions benefiting from the formation or regeneration of new vessels, as well as in the diagnosis of pathologies which present a overexpression of VEGF receptors or as biochemical tools to analyze the cellular pathways dependent on VEGF receptor activation.

9. 发明申请

WO2006131249A3 METHOD FOR SEQUENCING NUCLEIC ACIDS AND ANALOGUES THEREOF 审中-公开
标题翻译：用于测序核酸的方法及其类似物
公开(公告)号：WO2006131249A3
公开(公告)日：2007-06-21
申请号：PCT/EP2006005188
申请日：2006-05-31
申请人： BIONUCLEON S R L , BUCCI ENRICO , MOCCIA MARIA , MUSUMECI DOMENICA , PEDONE CARLO , ROVIELLO GIOVANNI , SAPIO ROBERTO , VALENTE MARGHERITA
发明人： BUCCI ENRICO , MOCCIA MARIA , MUSUMECI DOMENICA , PEDONE CARLO , ROVIELLO GIOVANNI , SAPIO ROBERTO , VALENTE MARGHERITA
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6869
摘要： A method is for determining the sequence of a nucleic acid, analogue or fragment thereof, based on the determination of the Tm or of physico-chemical parameters associated to the Tm of the duplex generated by repeated annealings of probes to the nucleic acid.
摘要翻译：一种方法是基于通过将探针重复退火至该核酸而产生的双链体Tm的相关的Tm或与其相关的物理化学参数的确定来确定核酸，其类似物或片段的序列。

10. 发明申请

WO2006008775A2 METHOD FOR IDENTIFYING AGENTS MODULATING THE METABOLISM OF STEROID MOLECULES AND AGENTS IDENTIFIED BY THE METHOD 审中-公开
标题翻译：鉴定调节类固醇分子代谢的药剂和方法鉴定的方法
公开(公告)号：WO2006008775A2
公开(公告)日：2006-01-26
申请号：PCT/IT2005/000403
申请日：2005-07-15
申请人： ISTITUTO BIOCHIMICO NAZIONALE SAVIO s.r.l. , D'ANDREA, Luca , PEDONE, Carlo , ABRESCIA, Paolo
发明人： D'ANDREA, Luca , PEDONE, Carlo , ABRESCIA, Paolo
IPC分类号： G01N33/53
CPC分类号： G01N33/92 , G01N2500/02
摘要： Method to identify an agent modulating the reverse cholesterol transport or the metabolism of steroid molecules consisting of incubating the above agent with Hpt, in conditions allowing the formation of a bond between the two molecules, so that an agent-Hpt complex can be formed; verifying that the agent-Hpt complex binds Hb, with a binding constant essentially comparable to that of free Hpt; verifying that the agent-Hpt complex essentially inhibits Hpt, in the form linked to the agent, in binding HDL; verifying that the agent-Hpt complex essentially inhibits the negative effect of Hpt on the enzyme LCAT.
摘要翻译：鉴定调节胆固醇逆向转运或代谢类固醇分子的试剂的方法，所述方法包括在允许在两个分子之间形成键的条件下孵育上述试剂与Hpt，使得试剂可以形成复合体; 验证试剂-Hpt复合物以与游离Hpt基本上相当的结合常数结合Hb; 验证试剂-Hpt复合物基本上以与试剂连接的形式抑制Hpt与HDL的结合; 验证试剂-Hpt复合物基本上抑制Hpt对酶LCAT的负面影响。

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