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1. 发明申请

WO2011042398A1 IMMUNOGLOBULIN SINGLE VARIABLE DOMAIN DIRECTED AGAINST HUMAN CXCR4 AND OTHER CELL ASSOCIATED PROTEINS AND METHODS TO GENERATE THEM 审中-公开
标题翻译：免疫球蛋白针对人CXCR4和其他细胞相关蛋白的单一变异域及其生成方法
公开(公告)号：WO2011042398A1
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064766
申请日：2010-10-04
申请人： ABLYNX NV , BESTE, Gerald , STAELENS, Stephanie , VANLANDSCHOOT, Peter , PAJUELO, Maria Gonzalez , REVETS, Hilde Adi Pierrette , SCHOTTE, Peter , STALS, Hilde , BRIGE, Ann , DEWILDE, Maarten , STORTELERS, Catelijne
发明人： BESTE, Gerald , STAELENS, Stephanie , VANLANDSCHOOT, Peter , PAJUELO, Maria Gonzalez , REVETS, Hilde Adi Pierrette , SCHOTTE, Peter , STALS, Hilde , BRIGE, Ann , DEWILDE, Maarten , STORTELERS, Catelijne
IPC分类号： C07K16/28 , C07K16/00
CPC分类号： C07K16/2866 , C07K16/00 , C07K2317/22 , C07K2317/31 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/76 , C07K2317/92
摘要： The invention relates to immunoglobulin single variable domains directed against specific human CXCR4 epitopes (herein also referred to interchangeably as "compounds of the invention ", "amino acid sequences of the invention ", or "building blocks of the invention ") and polypeptides comprising them (herein also referred to as "polypeptides of the invention ", ''"'compounds of the invention ", or "constructs of the invention "). Furthermore, the present invention relates to nucleic acids encoding the compounds of the invention (also referred to herein as "nucleic acids of the invention" or '"nucleotide sequences of the invention")-, to methods for preparing the compounds of the invention; to host cells expressing or capable of expressing the compounds of the invention; to compositions, and in particular to pharmaceutical compositions, that comprise the compounds of the invention; and to uses of the compounds of the invention and the aforementioned nucleic acids, host cells and/or compositions, in particular for prophylactic, therapeutic or diagnostic purposes, such as the prophylactic, therapeutic or diagnostic purposes mentioned herein. The invention also relates to methods for generating immunoglobulin single variable domains against a target such as a cell-associated protein and constructs comprising said immunoglobulin single variable domains. The invention also provides immunoglobulin single variable domains obtainable by the methods of the invention. Specifically, the present invention relates to the generation of immunoglobulin single variable domains and constructs thereof by use of epitope walking with multimer libraries. More specifically, the present invention relates to the generation of immunoglobulin single variable domains derived from camelids directed against a particular epitope of a target, in particular against a target with multiple transmembrane spanning domains, including GPCRs and ion channels, by epitope walking with multimer libraries.
摘要翻译：本发明涉及针对特异性CXCR4表位的免疫球蛋白单可变结构域（本文还可以互换地称为“本发明的化合物”，“本发明的氨基酸序列”或“本发明的构建模块”）和包含它们的多肽（本文还称为“本发明的多肽”，“本发明的化合物”或“本发明的构建体”）。此外，本发明涉及编码本发明化合物的核酸（本文中也称为“本发明的核酸”或“本发明的核苷酸序列”） - 制备本发明化合物的方法; 宿主表达或能够表达本发明化合物的细胞; 包括本发明化合物的组合物，特别是药物组合物; 以及本发明化合物和上述核酸，宿主细胞和/或组合物的用途，特别是用于预防，治疗或诊断目的，例如本文提及的预防，治疗或诊断目的。本发明还涉及用于产生针对靶的免疫球蛋白单可变结构域的方法，例如细胞相关蛋白和包含所述免疫球蛋白单可变结构域的构建体。本发明还提供可通过本发明的方法获得的免疫球蛋白单可变结构域。具体而言，本发明涉及通过使用多聚体文库进行表位走路来产生免疫球蛋白单可变结构域及其构建体。更具体地说，本发明涉及通过用多聚体文库进行抗原表位的步骤来产生源自靶的特定表位的骆驼的免疫球蛋白单可变结构域，特别是针对具有多个跨膜跨越结构域（包括GPCR和离子通道）的靶。

2. 发明申请

WO2011144749A1 BIOLOGICAL MATERIALS RELATED TO HER3 审中-公开
标题翻译：与其相关的生物材料3
公开(公告)号：WO2011144749A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/058295
申请日：2011-05-20
申请人： ABLYNX NV , MERCK PATENT GMBH , KNUEHL, Christine , HOCK, Bjoern , HOFMEISTER, Robert , BESTE, Gerald , REVETS, Hilde Adi Pierrette , VERDONCK, Frank Kamiel Delphina , CORNELIS, Sigrid Godelieve Victor
发明人： KNUEHL, Christine , HOCK, Bjoern , HOFMEISTER, Robert , BESTE, Gerald , REVETS, Hilde Adi Pierrette , VERDONCK, Frank Kamiel Delphina , CORNELIS, Sigrid Godelieve Victor
IPC分类号： C07K16/32 , C07K16/18 , C07K16/46 , A61K39/395 , A61P35/00
CPC分类号： C07K16/2863 , A61K2039/505 , A61P35/00 , C07K16/18 , C07K16/32 , C07K2317/22 , C07K2317/31 , C07K2317/33 , C07K2317/567 , C07K2317/569 , C07K2317/73 , C07K2317/76 , C07K2317/77 , C07K2317/92 , C07K2317/94
摘要： The present disclosure relates to amino acid sequences that are directed against (as defined herein) HER3, as well as to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consist of one or more such amino acid sequences (also referred to herein as "amino acid sequences of the invention", "compounds of the invention", and "polypeptides of the invention", respectively). The disclosure also relates to nucleic acids encoding such amino acid sequences and polypeptides (also referred to herein as "nucleic acids of the invention" or "nucleotide sequences of the invention"); to methods for 10 preparing such amino acid sequences and polypeptides; to host cells expressing or capable of expressing such amino acid sequences or polypeptides; to compositions, and in particular to pharmaceutical compositions, that comprise such amino acid sequences, polypeptides, nucleic acids and/or host cells; and to uses of such amino acid sequences or polypeptides, nucleic acids, host cells and/or compositions, in particular for prophylactic, therapeutic or diagnostic purposes, such as the prophylactic, therapeutic or diagnostic purposes mentioned herein.
摘要翻译：本公开涉及针对（如本文所定义）HER3以及包含或基本上由一个或多个这样的氨基酸序列组成的化合物或构建体，特别是蛋白质和多肽的氨基酸序列（也称为在本文中分别为“本发明的氨基酸序列”，“本发明的化合物”和“本发明的多肽”）。本公开还涉及编码这种氨基酸序列和多肽（本文中也称为“本发明的核酸”或“本发明的核苷酸序列”）的核酸; 涉及10种制备此类氨基酸序列和多肽的方法; 宿主表达或能够表达这种氨基酸序列或多肽的细胞; 包括这样的氨基酸序列，多肽，核酸和/或宿主细胞的组合物，特别是药物组合物; 以及这些氨基酸序列或多肽，核酸，宿主细胞和/或组合物的用途，特别是用于预防，治疗或诊断目的，例如本文提及的预防，治疗或诊断目的。

3. 发明申请

WO2012042026A1 BIOLOGICAL MATERIALS RELATED TO C-MET 审中-公开
标题翻译：与C-MET相关的生物材料
公开(公告)号：WO2012042026A1
公开(公告)日：2012-04-05
申请号：PCT/EP2011/067132
申请日：2011-09-30
申请人： ABLYNX NV , BESTE, Gerald , DENAYER, Tinneke , HERMANS, Guy , SZYROKI, Alexander , STEFFENSEN, Soren , VERVERKEN, Cedric Jozef Néotére
发明人： BESTE, Gerald , DENAYER, Tinneke , HERMANS, Guy , SZYROKI, Alexander , STEFFENSEN, Soren , VERVERKEN, Cedric Jozef Néotére
IPC分类号： C07K16/28
CPC分类号： C07K16/2863 , A61K2039/505 , C07K16/18 , C07K2317/22 , C07K2317/34 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/73 , C07K2317/76 , C07K2317/92 , C12Q1/6876 , G01N33/53
摘要： The present invention relates to biological materials related to c-Met possibly in combination with VEGF and/or EGFR, and more in particuiar to polypeptides, nucleic acids encoding such polypeptides; to methods for preparing such polypeptides; to host cells expressing or capable of expressing such polypeptides; to compositions and in particuiar to pharmaceutical compositions that comprise such polypeptides, for prophylactic, therapeutic or diagnostic purposes.
摘要翻译：本发明涉及与可能与VEGF和/或EGFR组合的c-Met相关的生物学材料，更具体地涉及多肽，编码这些多肽的核酸; 制备这种多肽的方法; 以宿主表达或能够表达这种多肽的细胞; 包括用于预防，治疗或诊断目的的包含这种多肽的药物组合物。

4. 发明申请

WO2004056874A2 NEUROPILIN-1 INHIBITORS 审中-公开
标题翻译：神经营养因子-1抑制剂
公开(公告)号：WO2004056874A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014756
申请日：2003-12-22
申请人： XERION PHARMACEUTICALS AG , TUFTS UNIVERSITY , UNGER, Christine, Margarete , BESTE, Gerald , ZEHETMEIER, Carolin , LAIN, Blanca , TORELLA, Claudia , NIEWÖHNER, Jens , JAY, Daniel, G. , EUSTACE, Brenda, K. , KNAUER, Roland , JENSEN, Kristian, Hobold
发明人： UNGER, Christine, Margarete , BESTE, Gerald , ZEHETMEIER, Carolin , LAIN, Blanca , TORELLA, Claudia , NIEWÖHNER, Jens , JAY, Daniel, G. , EUSTACE, Brenda, K. , KNAUER, Roland , JENSEN, Kristian, Hobold
IPC分类号： C07K16/28
CPC分类号： G01N33/57492 , A61K38/00 , A61K2039/505 , C07K16/28 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/565 , C07K2317/622 , C07K2317/76 , C12N15/1138 , C12N2310/14 , G01N2333/515 , G01N2500/00
摘要： The present invention relates to molecules interfering with the function of neuropilin-1 in the context of angiogenesis and the treatment of cancer. Molecules, polypeptides, antibodies, compositions and methods are provided that are useful for reducing, inhibiting or treating angiogenesis, the invasion of blood vessels into tumors, and/or the invasion or the metastatic potential of specific tumor cells. Additionally, a method is provided that allows identifying molecules, which interfere with the functionality of neuropilin-1. Furthermore, a method is provided that allows determining whether a naturally occuring tumor cell depends on functional neuropilin-1 for its invasiveness and/or metastatic potential.
摘要翻译：本发明涉及在血管生成和癌症治疗中干扰神经毡蛋白-1功能的分子。提供了用于减少，抑制或治疗血管生成，血管侵入肿瘤和/或特定肿瘤细胞的侵袭或转移潜能的分子，多肽，抗体，组合物和方法。此外，提供了一种方法，可以识别干扰神经毡蛋白-1功能的分子。此外，提供了一种方法，其允许确定自然发生的肿瘤细胞是否依赖于功能性神经毡蛋白-1的功能，因为它的侵袭性和/或转移潜能。

5. 发明申请

WO2004074324A2 MODULATION OF THE POLIOVIRUS RECEPTOR FUNCTION 审中-公开
标题翻译： POLOVIRUS受体功能的调节
公开(公告)号：WO2004074324A2
公开(公告)日：2004-09-02
申请号：PCT/EP2004/001637
申请日：2004-02-19
申请人： XERION PHARMACEUTICALS AG , TUFTS UNIVERSITY , UNGER, Christine, Margarete , BESTE, Gerald , ZEHETMEIER, Carolin , LAIN, Blanca , TORELLA, Claudia , JAY, Daniel, G. , EUSTACE, Brenda, K. , SLOAN, Kevin, Ernest
发明人： UNGER, Christine, Margarete , BESTE, Gerald , ZEHETMEIER, Carolin , LAIN, Blanca , TORELLA, Claudia , JAY, Daniel, G. , EUSTACE, Brenda, K. , SLOAN, Kevin, Ernest
IPC分类号： C07K16/28
CPC分类号： A61K38/17 , A61K2039/505 , C07K16/2896 , C07K2317/622 , Y02A50/466
摘要： The present invention relates to the identification, the isolation and the use of molecules interfering with the function(s) mediated by the poliovirus receptor (PVR) on cells. The molecules can be used for the treatment of cells having a metastatic potential, metastasis and cancer. Further methods are provided that are useful for identifying and isolating molecules which have the capacity to modulate PVR mediated adhesion or invasion potential of cells.
摘要翻译：本发明涉及干扰由脊髓灰质炎病毒受体（PVR）在细胞上介导的功能的分子的鉴定，分离和使用。该分子可用于治疗具有转移潜能，转移和癌症的细胞。提供了可用于鉴定和分离具有调节PVR介导的细胞粘附或侵袭潜能的能力的分子的其它方法。

6. 发明申请

WO2011107507A1 BIPARATOPIC ABETA BINDING POLYPEPTIDES 审中-公开
标题翻译： BIPARATOPIC ABETA结合多糖
公开(公告)号：WO2011107507A1
公开(公告)日：2011-09-09
申请号：PCT/EP2011/053090
申请日：2011-03-02
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , PARK, John, E. , DORNER-CIOSSEK, Cornelia , HOERER, Stefan , KUSSMAUL, Lothar , LENTER, Martin , ZIMMERMANN, Katharina , BESTE, Gerald , LAEREMANS, Toon , MERCHIERS, Pascal , VERCAMMEN, Jo
发明人： PARK, John, E. , DORNER-CIOSSEK, Cornelia , HOERER, Stefan , KUSSMAUL, Lothar , LENTER, Martin , ZIMMERMANN, Katharina , BESTE, Gerald , LAEREMANS, Toon , MERCHIERS, Pascal , VERCAMMEN, Jo
IPC分类号： C07K16/18 , C07K16/46 , A61K39/395
CPC分类号： A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/18 , C07K16/28 , C07K2317/22 , C07K2317/24 , C07K2317/31 , C07K2317/34 , C07K2317/40 , C07K2317/55 , C07K2317/92 , C07K2317/94 , C07K2319/00
摘要： The invention relates to biparatopic A-beta binding polypeptides and, more specifically, to biparatopic A-beta binding polypeptides comprising at least two immunoglobulin single variable domains binding to different epitopes of A-beta. The invention also relates to specific sequences of such polypeptides, methods of their production, and methods of using them, including methods of treatment of diseases such as Alzheimer's Disease.
摘要翻译：本发明涉及双互补位A-β结合多肽，更具体地涉及包含结合至A-β的不同表位的至少两个免疫球蛋白单可变结构域的双互补位A-β结合多肽。本发明还涉及这种多肽的具体序列，其制备方法及其使用方法，包括治疗疾病如阿尔茨海默病的方法。

7. 发明申请

WO2004007717A1 PROTEOMIC SCREEN TO IDENTIFY DISEASE-RELATED BIOLOGICAL MOLECULES AND INHIBITORS THERETO 审中-公开
标题翻译：鉴定疾病相关生物分子和抑制剂的PROTEMIC筛选
公开(公告)号：WO2004007717A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007660
申请日：2003-07-15
申请人： XERION PHARMACEUTICALS AG , UNGER, Christine, Margarete , BESTE, Gerald , JENSEN, Kristian, H. , ZEHETMEIER, Carolin , KNAUER, Roland , GUELBENZU, Blanca, Lain , TORELLA, Claudia , ILAG, L., Leodevico
发明人： UNGER, Christine, Margarete , BESTE, Gerald , JENSEN, Kristian, H. , ZEHETMEIER, Carolin , KNAUER, Roland , GUELBENZU, Blanca, Lain , TORELLA, Claudia , ILAG, L., Leodevico
IPC分类号： C12N15/10
CPC分类号： C07K16/30 , A61K2039/505 , C07K14/70503 , C07K16/2896 , C07K2317/622 , C12N15/1037 , C40B40/02
摘要： The invention provides a new paradigm for a screening method by combining the biochemical approach of specific binding between a ligand and a target, e.g. an antibody and an antigen, with the genetic principle of a functional screen. The present invention demonstrates its utility for identifying novel disease-relevant proteins and inhibitory ligands, e.g. antibodies or antibody fragments, that may serve as therapeutic leads for a wide variety of diseases, whether the cause of the disease is derivable from a virus, a bacterium, a lower eukaryote or from a misregulation of the cells of the subject to be treated.
摘要翻译：本发明通过结合配体和靶标之间的特异性结合的生物化学方法，例如，提供了一种筛选方法的新范例。抗体和抗原，具有功能筛选的遗传学原理。本发明证明其用于鉴定新的疾病相关蛋白和抑制性配体，例如，抗体或抗体片段，其可以用作各种疾病的治疗引导，无论疾病的病因是源自病毒，细菌，低等真核生物还是来自待治疗对象的细胞的错配。

8. 发明申请

WO2004081037A1 INHIBITORS OF EXTRACELLULAR HSP90 审中-公开
标题翻译：细胞HSP90抑制剂
公开(公告)号：WO2004081037A1
公开(公告)日：2004-09-23
申请号：PCT/EP2004/002422
申请日：2004-03-09
申请人： TUFTS UNIVERSITY , XERION PHARMACEUTICALS AG , JAY, Daniel, G. , EUSTACE, Brenda, K. , SAKURAI, Takashi , BESTE, Gerald
发明人： JAY, Daniel, G. , EUSTACE, Brenda, K. , SAKURAI, Takashi , BESTE, Gerald
IPC分类号： C07K14/47
CPC分类号： G01N33/5029 , A61K31/00 , A61K31/37 , A61K49/0004 , A61K2039/505 , C07K16/18 , C07K16/30 , C07K2317/622 , C07K2317/76 , G01N33/5008 , G01N33/5011 , G01N33/5091
摘要： The present invention describes the inhibitors of extracellular Hsp90. The inhibition of extracellular Hsp90 leads to a reduction of the invasiveness of the tumor cells. Furthermore, the invention relates to the use of molecules inhibiting extracellular Hsp90 function for the manufacture of a medicament for the treatment or prevention of invasion and/or metastatic potential of cancer cells.
摘要翻译：本发明描述了细胞外Hsp90的抑制剂。细胞外Hsp90的抑制导致肿瘤细胞侵袭性的降低。此外，本发明涉及抑制胞外Hsp90功能的分子在制备用于治疗或预防癌细胞的侵袭和/或转移潜力的药物中的用途。

9. 发明申请

WO2004007550A1 MCAM INHIBITORS 审中-公开
标题翻译： MCAM抑制剂
公开(公告)号：WO2004007550A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007661
申请日：2003-07-15
申请人： XERION PHARMACEUTICALS AG , UNGER, Christine, Margarete , ZEHETMEIER, Carolin , TORELLA, Claudia , NIEWÖHNER, Jens , AHRENS, Bianca , BESTE, Gerald
发明人： UNGER, Christine, Margarete , ZEHETMEIER, Carolin , TORELLA, Claudia , NIEWÖHNER, Jens , AHRENS, Bianca , BESTE, Gerald
IPC分类号： C07K14/705
CPC分类号： C07K16/30 , A61K2039/505 , C07K14/70503 , C07K16/2896 , C07K2317/622 , C12N15/1037 , C40B40/02
摘要： The present invention relates to polypeptides inhibiting the function of MCAM in naturally occurring tumor cells and their use, and the use of other molecules inhibiting MCAM function, for the treatment of cancers, particularly for reducing the invasiveness, proliferation, adhesion and/or the metastatic potential of specific cancer cells. Furthermore, a method is provided that allows determining whether a naturally occurring tumor cell depends on functional MCAM for its invasiveness, adhesiveness, proliferation and/or its metastatic potential. Finally, a method is provided that allows identifying an antibody or an antibody fragment capable of inhibiting invasiveness, proliferation or adhesiveness of tumor cells.
摘要翻译：本发明涉及在天然存在的肿瘤细胞中抑制MCAM功能的多肽及其用途以及抑制MCAM功能的其它分子用于治疗癌症，特别是用于降低侵袭性，增殖，粘附和/或转移的功能特定癌细胞的潜力。此外，提供了一种方法，其允许确定天然存在的肿瘤细胞是否依赖于功能性MCAM对其侵袭性，粘附性，增殖和/或其转移潜力。最后，提供了一种能够鉴定能够抑制肿瘤细胞侵袭，增殖或粘附的抗体或抗体片段的方法。

10. 发明申请

WO2018220225A1 AGGRECAN BINDING IMMUNOGLOBULINS 审中-公开
公开(公告)号：WO2018220225A1
公开(公告)日：2018-12-06
申请号：PCT/EP2018/064608
申请日：2018-06-04
申请人： ABLYNX NV , MERCK PATENT GMBH
发明人： STEFFENSEN, Soren , BESTE, Gerald , HERMANS, Guy , GÜHRING, Hans , LADEL, Christoph , TOLEIKIS, Lars
IPC分类号： C07K16/18 , C07K16/40 , C07K16/46 , A61K39/395 , A61P19/02
摘要： The present invention relates to immunoglobulins that specifically bind Aggrecan and more in particular to polypeptides, nucleic acids encoding such polypeptides; to methods for preparing such polypeptides; to compositions and in particular to pharmaceutical compositions that comprise such polypeptides, for prophylactic, therapeutic or diagnostic purposes. In particular, the immunoglobulins of the present invention inhibit the activity of Aggrecan.

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