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1. 发明申请

WO2008075192A3 TARGETING AND THERAPEUTIC COMPOUNDS AND GAS-FILLED MICROVESICLES COMPRISING SAID COM OUNDS 审中-公开
公开(公告)号：WO2008075192A3
公开(公告)日：2008-06-26
申请号：PCT/IB2007/004018
申请日：2007-12-19
申请人： BRACCO INTERNATIONAL BV , SWENSON, Rolf , BUSSAT, Philippe , LAMY, Bernard , RAMALINGAM, Kondareddiar , POCHON, Sibylle
发明人： SWENSON, Rolf , BUSSAT, Philippe , LAMY, Bernard , RAMALINGAM, Kondareddiar , POCHON, Sibylle
IPC分类号： A61K49/00
摘要： New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein : M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.

2. 发明申请

WO2003074005A2 KDR AND VEGF/KDR BINDING PEPTIDES AND THEIR USE IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译： KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用
公开(公告)号：WO2003074005A2
公开(公告)日：2003-09-12
申请号：PCT/US2003/006731
申请日：2003-03-03
申请人： DYAX CORP. , BRACCO INTERNATIONAL B.V. , SATO, Aaron, K. , SEXTON, Daniel, J. , LADNER, Robert, C. , DRANSFIELD, Daniel, T. , SWENSON, Rolf, E. , MARINELLI, Edmund, R. , RAMALINGAM, Kondareddiar , NUNN, Adrian, D. , VON WRONSKI, Mathew, A. , SHRIVASTAVA, Ajay , POCHON, Sibylle , BUSSAT, Philippe , ARBOGAST, Christophe , PILLAI, Radhakrishna , FAN, Hong , LINDER, Karen, E. , SONG, Bo , NANJAPPAN, Palaniappa
发明人： SATO, Aaron, K. , SEXTON, Daniel, J. , LADNER, Robert, C. , DRANSFIELD, Daniel, T. , SWENSON, Rolf, E. , MARINELLI, Edmund, R. , RAMALINGAM, Kondareddiar , NUNN, Adrian, D. , VON WRONSKI, Mathew, A. , SHRIVASTAVA, Ajay , POCHON, Sibylle , BUSSAT, Philippe , ARBOGAST, Christophe , PILLAI, Radhakrishna , FAN, Hong , LINDER, Karen, E. , SONG, Bo , NANJAPPAN, Palaniappa
IPC分类号： A61K
CPC分类号： C07K7/08 , A61K38/00 , A61K49/223 , A61K51/088 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00 , Y02A50/411 , Y02A50/58
摘要： The present invention provides binding polypetides for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, Detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity (e.g., having a K D
摘要翻译：本发明提供了用于KDR或VEGF / KDR复合物的结合多肽，其在治疗，检测，分离或定位血管发生的任何地方具有多种用途是有利的。特别公开的是能够以高亲和力结合KDR或VEGF / KDR复合物的合成的，分离的多肽（例如具有KD <1微摩尔）。

3. 发明申请

WO2004065621A1 KDR AND VEGF/KDR BINDING PEPTIDES AND THEIR USE IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译： KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用
公开(公告)号：WO2004065621A1
公开(公告)日：2004-08-05
申请号：PCT/US2003/028787
申请日：2003-09-11
申请人： DYAX CORP. , BRACCO INTERNATIONAL B.V. , SATO, Aaron, K. , SEXTON, Daniel, J. , DRANSFIELD, Daniel, T. , LADNER, Robert, C. , ARBOGAST, Christophe , BUSSAT, Philippe , FAN, Hong , KHURANA, Sudha , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sibylle , RAMALINGAM, Kondareddiar , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A.
发明人： SATO, Aaron, K. , SEXTON, Daniel, J. , DRANSFIELD, Daniel, T. , LADNER, Robert, C. , ARBOGAST, Christophe , BUSSAT, Philippe , FAN, Hong , KHURANA, Sudha , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sibylle , RAMALINGAM, Kondareddiar , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A.
IPC分类号： C12Q1/00
CPC分类号： A61K49/221 , A61K38/00 , A61K47/62 , A61K49/223 , A61K51/088 , C07K7/08 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00 , Y02A50/411 , Y02A50/58
摘要： The present invention provides polypeptides, peptide dimer, and multimeric complexes comprising at least one binding moiety for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEFG/KDR complex with high affinity ( e.g ., having a K D
摘要翻译：本发明提供了包含用于KDR或VEGF / KDR复合物的至少一个结合部分的多肽，肽二聚体和多聚体复合物，其具有各种用途，无论何处治疗，检测，分离或定位血管发生都是有利的。特别公开的是能够以高亲和力（例如具有KD <1μM）结合KDR或VEFG / KDR复合物的合成，分离的多肽，以及包含这些多肽的二聚体和多聚体构建体。

4. 发明申请

WO2004064595A2 MULTIVALENT CONSTRUCTS FOR THERAPEUTIC AND DIAGNOSTIC APPLICATIONS 审中-公开
标题翻译：用于治疗和诊断应用的多功能结构
公开(公告)号：WO2004064595A2
公开(公告)日：2004-08-05
申请号：PCT/US2003/028838
申请日：2003-09-11
申请人： BRACCO INTERNATIONAL BV , DYAX CORPORATION , ARBOGAST, Christophe , BUSSAT, Philippe , DRANSFIELD, Daniel, T. , FAN, Hong , LINDER, Karen , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sybille , RAMALINGAM, Kondareddiar , SATO, Aaron , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A. , WALKER, Sharon, Michele
发明人： ARBOGAST, Christophe , BUSSAT, Philippe , DRANSFIELD, Daniel, T. , FAN, Hong , LINDER, Karen , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sybille , RAMALINGAM, Kondareddiar , SATO, Aaron , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A. , WALKER, Sharon, Michele
IPC分类号： A61B
CPC分类号： C07K7/08 , A61K47/60 , A61K47/64 , C07K7/64
摘要： The invention provides compositions and methods for therapeutic and diagnostic applications.
摘要翻译：本发明提供用于治疗和诊断应用的组合物和方法。

5. 发明申请

WO2003084574A1 MULTIVALENT CONSTRUCTS FOR THERAPEUTIC AND DIAGNOSTIC APPLICATIONS 审中-公开
标题翻译：用于治疗和诊断应用的多功能结构
公开(公告)号：WO2003084574A1
公开(公告)日：2003-10-16
申请号：PCT/US2003/006656
申请日：2003-03-03
申请人： BRACCO INTERNATIONAL BV , DYAX CORP. , ARBOGAST, Christophe , BUSSAT, Philippe , DRANSFIELD, Daniel, T. , FAN, Hang , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sybille , RAMALINGAM, Kondareddiar , SATO, Aaron , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A. , WALKER, Sharon, Michele
发明人： ARBOGAST, Christophe , BUSSAT, Philippe , DRANSFIELD, Daniel, T. , FAN, Hang , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian , PILLAI, Radhakrishna , POCHON, Sybille , RAMALINGAM, Kondareddiar , SATO, Aaron , SHRIVASTAVA, Ajay , SONG, Bo , SWENSON, Rolf, E. , VON WRONSKI, Mathew, A. , WALKER, Sharon, Michele
IPC分类号： A61K51/00
CPC分类号： C07K7/08 , A61K47/60 , A61K47/64 , C07K7/64
摘要： The invention provides compositions and methods for therapeutic and diagnostic applications such as that shown in Figure 36.
摘要翻译：本发明提供了治疗和诊断应用的组合物和方法，如图36所示。

6. 发明申请

WO2009076388A3 TARGETING VECTOR-PHOSPHOLIPID CONJUGATES 审中-公开
公开(公告)号：WO2009076388A3
公开(公告)日：2009-06-18
申请号：PCT/US2008/086136
申请日：2008-12-10
申请人： BRACCO INTERNATIONAL B.V. , BUSSAT, Philippe , CHERKAOUI, Samir , FAN, Hong (Helen) , LAMY, Bernard , NANJAPPAN, Palaniappa , PILLAI, Radhakrishna, K. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
发明人： BUSSAT, Philippe , CHERKAOUI, Samir , FAN, Hong (Helen) , LAMY, Bernard , NANJAPPAN, Palaniappa , PILLAI, Radhakrishna, K. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
IPC分类号： A61K49/22 , A61B8/00 , C07K14/00
摘要： Peptide vectors having high KDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.

7. 发明申请

WO2008073458A2 FIBRIN-BINDING PEPTIDES AND CONJUGATES THEREOF 审中-公开
标题翻译：纤连蛋白结合肽及其缀合物
公开(公告)号：WO2008073458A2
公开(公告)日：2008-06-19
申请号：PCT/US2007/025403
申请日：2007-12-11
申请人： BRACCO IMAGING S.P.A. , BUSSAT, Philippe , LAMY, Bernard , MARINELLI, Edmund, R. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
发明人： BUSSAT, Philippe , LAMY, Bernard , MARINELLI, Edmund, R. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
IPC分类号： A61K51/08
CPC分类号： A61K49/14 , A61K49/0043 , A61K49/0056 , A61K49/085 , A61K49/124 , C07K7/06 , G01N33/532 , G01N33/574 , G01N33/86 , G01N2500/04
摘要： Fibrin-binding peptides having high binding affinity and excellent physical characteristics compared to previously known fibrin-binding peptides are provided. These fibrin-binding peptides may be conjugated to a detectable label or a therapeutic agent and used to detect and facilitate treatment of pathological conditions associated with the presence of fibrin such as thrombic, angiogenic and neoplastic conditions. These peptides may be used in imaging processes such as MRI, ultrasound and nuclear medicine imaging (e.g. PET, scintigraphic imaging., etc.). The peptides may also be used therapeutically. The present invention also provides processes and methods for making and using such peptides and conjugates thereof.
摘要翻译：提供了与先前已知的纤维蛋白结合肽相比具有高结合亲和力和优异的物理特性的纤连蛋白结合肽。这些纤维蛋白结合肽可以与可检测标记或治疗剂缀合，并用于检测和促进与纤维蛋白存在相关的病理状态如血栓形成，血管生成和肿瘤病症的治疗。这些肽可用于成像过程，如MRI，超声和核医学成像（例如PET，闪烁成像等）。这些肽也可以用于治疗。本发明还提供了制备和使用这种肽及其缀合物的方法和方法。

8. 发明申请

WO2007067979A2 TARGETING VECTOR-PHOSPHOLIPID CONJUGATES 审中-公开
标题翻译：靶向载体 - 磷脂结合体
公开(公告)号：WO2007067979A2
公开(公告)日：2007-06-14
申请号：PCT/US2006/061793
申请日：2006-12-08
申请人： BRACCO INTERNATIONAL B.V. , BUSSAT, Philippe , CHERKAOUI, Samir , FAN, Hong (Helen) , LAMY, Bernard , NANJAPPAN, Palaniappa , PILLAI, Radhakrishna, K. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
发明人： BUSSAT, Philippe , CHERKAOUI, Samir , FAN, Hong (Helen) , LAMY, Bernard , NANJAPPAN, Palaniappa , PILLAI, Radhakrishna, K. , POCHON, Sibylle , SONG, Bo , SWENSON, Rolf, E.
IPC分类号： A61K38/10 , C07K7/08
CPC分类号： C07K14/00 , A61K47/544 , A61K49/223 , Y02A50/58
摘要： Peptide vectors having high KLDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.
摘要翻译：提供了具有高KLDR结合亲和力的肽载体和用于制备此类载体的方法。肽载体可以与磷脂结合并包含在超声造影剂组合物中。这样的超声造影剂在治疗和诊断方法中是特别有用的，例如在成像含KDR组织和评估和治疗与肿瘤病症相关的血管生成过程中。本发明还提供大规模生产高纯度二聚体和单体肽磷脂共轭物以及用于形成缀合物的前体材料的方法。本发明还提供了大规模生产含有非常低水平的TFA的高纯度肽磷脂缀合物的方法。

9. 发明申请

WO2012020030A1 TARGETED GAS-FILLED MICROVESICLES 审中-公开
标题翻译：目标气体填充微波
公开(公告)号：WO2012020030A1
公开(公告)日：2012-02-16
申请号：PCT/EP2011/063720
申请日：2011-08-09
申请人： BRACCO SUISSE SA , BETTINGER, Thierry , BUSSAT, Philippe , LAMY, Bernard , CHERKAOUI, Samir , GUILBERT-BRIGGER, Irene
发明人： BETTINGER, Thierry , BUSSAT, Philippe , LAMY, Bernard , CHERKAOUI, Samir , GUILBERT-BRIGGER, Irene
IPC分类号： A61K49/22
CPC分类号： A61K49/223 , A61K38/178 , A61K49/221 , A61K49/222 , A61K49/227
摘要： Gas-filled microvesicles associated with a polypeptide comprising a sequence of amino acids, said sequence exhibiting binding affinity for selectins, particularly p-selectin. The gas-filled microvesicles can be used in ultrasound imaging.
摘要翻译：与包含氨基酸序列的多肽相关的充气微泡，所述序列对选择素特别是对选择素具有结合亲合力。充气微泡可用于超声成像。

10. 发明申请

WO2006018433A1 GAS-FILLED MICROVESICLES COMPOSITION FOR CONTRAST IMAGING 审中-公开
标题翻译：用于对比成像的气体填充微晶组合物
公开(公告)号：WO2006018433A1
公开(公告)日：2006-02-23
申请号：PCT/EP2005/054041
申请日：2005-08-17
申请人： BRACCO RESEARCH SA , BUSSAT, Philippe , FRINKING, Peter , GUILLOT, Christian , SCHNEIDER, Michel
发明人： BUSSAT, Philippe , FRINKING, Peter , GUILLOT, Christian , SCHNEIDER, Michel
IPC分类号： A61K49/22
CPC分类号： A61K49/223
摘要： The present invention relates to a new composition comprising gas-filled microvesicles for contrast imaging which are particularly suitable for providing an effective echo response to at least two selected ultrasound waves having different frequencies. Said composition preferably comprises at least two different preparations of gas-filled microvesicles having respective peaks of non-linear echographic response differing by at least 2 MHz to each other, and preferably have respective size distributions with different median sizes. In particular, said preparations preferably have size distributions with respective D V50 values differing from each other by at least 0.5 μm, more preferably at least 1.0 μm. Alternatively, said composition has a volume size distribution showing a value of Bowley skewness of 0.16 or higher. According to a preferred embodiment, at least 95% of the total volume of gas contained in said microvesicles, calculated on the population of microvesicles up to a diameter of 10 μm, is contained in microvesicles having a diameter of 8 micron or less.
摘要翻译：本发明涉及一种新的组合物，其包括用于造影成像的充气微泡，其特别适合于向具有不同频率的至少两个选定的超声波提供有效的回波响应。所述组合物优选包含气体填充微泡的至少两种不同制剂，其具有彼此相差至少2MHz的非线性回波影响响应的各个峰，并且优选具有不同中值大小的相应尺寸分布。特别地，所述制剂优选具有各自的D

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