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1. 发明申请

WO2011003780A1 BI-SPECIFIC DIGOXIGENIN BINDING ANTIBODIES 审中-公开
标题翻译：双特异性抗体结合抗体
公开(公告)号：WO2011003780A1
公开(公告)日：2011-01-13
申请号：PCT/EP2010/059243
申请日：2010-06-30
申请人： F. HOFFMANN-LA ROCHE AG , BRAMLAGE, Birgit , BRINKMANN, Ulrich , CROASDALE, Rebecca , DILL, Simone , DORMEYER, Wilma , GEORGES, Guy , GROTE, Michael , HAAS, Alexander , HOFFMANN, Eike , ICKENSTEIN, Ludger Markus , JAHN-HOFMANN, Kerstin , JOHN, Matthias , METZ, Silke , MUNDIGL, Olaf , SCHEUER, Werner , STRACKE, Jan Olaf
发明人： BRAMLAGE, Birgit , BRINKMANN, Ulrich , CROASDALE, Rebecca , DILL, Simone , DORMEYER, Wilma , GEORGES, Guy , GROTE, Michael , HAAS, Alexander , HOFFMANN, Eike , ICKENSTEIN, Ludger Markus , JAHN-HOFMANN, Kerstin , JOHN, Matthias , METZ, Silke , MUNDIGL, Olaf , SCHEUER, Werner , STRACKE, Jan Olaf
IPC分类号： A61K39/395 , A61K47/48 , C07K16/16 , C07K16/28 , C07K16/32 , C07K16/44 , C07K16/46 , C12N15/113
CPC分类号： C07K16/44 , A61K31/704 , A61K39/39533 , A61K47/6879 , A61K47/6897 , A61K49/0045 , A61K49/0058 , A61K2039/505 , B82Y5/00 , C07K16/16 , C07K16/2803 , C07K16/2863 , C07K16/2896 , C07K16/32 , C07K2317/24 , C07K2317/31 , C07K2317/51 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/622 , C07K2317/77 , C07K2317/92 , C07K2319/30 , C12N15/111 , C12N15/1138 , C12N2310/14 , C12N2310/3513 , C12N2320/32 , A61K2300/00
摘要： This invention relates to bispecific antibodies and antibody fragments against a target protein and a hapten, wherein the hapten is PEG or biotin, most preferably digoxigenin, methods for their production, their use as a delivery platform for therapeutic or diagnostic agents, pharmaceutical 5 compositions containing said antibodies, and uses thereof.
摘要翻译：本发明涉及针对靶蛋白和半抗原的双特异性抗体和抗体片段，其中半抗原是PEG或生物素，最优选地高辛，其制备方法，它们作为治疗或诊断剂的递送平台的用途，含有所述抗体及其用途。

2. 发明申请

WO2011003557A1 A COMPLEX OF BI-SPECIFIC ANTIBODY AND DIGOXIGENIN CONJUGATED TO A THERAPEUTIC OR DIAGNOSTIC AGENT 审中-公开
标题翻译：复合物与特异性抗体和联合治疗或诊断代谢的二氢吉他宁
公开(公告)号：WO2011003557A1
公开(公告)日：2011-01-13
申请号：PCT/EP2010/004051
申请日：2010-07-05
申请人： F. HOFFMANN-LA ROCHE AG , BRINKMANN, Ulrich , CROASDALE, Rebecca , DORMEYER, Wilma , GEORGES, Guy , HAAS, Alexander , HOFFMANN, Eike , METZ, Silke , MUNDIGL, Olaf , SCHEUER, Werner , STRACKE, Jan Olaf
发明人： BRINKMANN, Ulrich , CROASDALE, Rebecca , DORMEYER, Wilma , GEORGES, Guy , HAAS, Alexander , HOFFMANN, Eike , METZ, Silke , MUNDIGL, Olaf , SCHEUER, Werner , STRACKE, Jan Olaf
IPC分类号： A61K39/395 , A61K47/48 , C07K16/16 , C07K16/28 , C07K16/32 , C07K16/44 , C07K16/46 , C12N15/113
CPC分类号： C07K16/44 , A61K31/704 , A61K39/39533 , A61K47/6879 , A61K47/6897 , A61K49/0045 , A61K49/0058 , A61K2039/505 , B82Y5/00 , C07K16/16 , C07K16/2803 , C07K16/2863 , C07K16/2896 , C07K16/32 , C07K2317/24 , C07K2317/31 , C07K2317/51 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/622 , C07K2317/77 , C07K2317/92 , C07K2319/30 , C12N15/111 , C12N15/1138 , C12N2310/14 , C12N2310/3513 , C12N2320/32 , A61K2300/00
摘要： The present invention relates to complexes of a) bi-specific antibodies and antibody fragments against a target protein and b) a digoxigenin conjugated to a therapeutic or diagnostic agent, methods for their production, their use as a delivery platform for therapeutic or diagnostic agents, pharmaceutical compositions containing said antibodies, and uses thereof.
摘要翻译：本发明涉及a）针对靶蛋白的双特异性抗体和抗体片段的复合物，和b）与治疗或诊断试剂缀合的地高辛，其生产方法，它们作为治疗或诊断试剂的递送平台的用途，含有所述抗体的药物组合物及其用途。

3. 发明申请

WO2012025530A1 BISPECIFIC ANTIBODIES COMPRISING A DISULFIDE STABILIZED - FV FRAGMENT 审中-公开
标题翻译：包含稳定的稳定抗体 - FV片段
公开(公告)号：WO2012025530A1
公开(公告)日：2012-03-01
申请号：PCT/EP2011/064476
申请日：2011-08-23
申请人： F. HOFFMANN-LA ROCHE AG , BRINKMANN, Ulrich , HAAS, Alexander , METZ, Silke , SCHANZER, Juergen Michael
发明人： BRINKMANN, Ulrich , HAAS, Alexander , METZ, Silke , SCHANZER, Juergen Michael
IPC分类号： C07K16/00 , C07K16/32 , C07K16/28
CPC分类号： C07K16/468 , C07K16/00 , C07K16/2863 , C07K16/32 , C07K2317/31 , C07K2317/56 , C07K2317/624 , C07K2317/64 , C07K2319/00
摘要： The present invention relates to bispecific antibodies, methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
摘要翻译：本发明涉及双特异性抗体，其制备方法，含有所述抗体的药物组合物及其用途。

4. 发明申请

WO2011135040A1 FLUORESCENT ANTIBODY FUSION PROTEIN, ITS PRODUCTION AND USE 审中-公开
标题翻译：荧光抗体蛋白，其生产和使用
公开(公告)号：WO2011135040A1
公开(公告)日：2011-11-03
申请号：PCT/EP2011/056770
申请日：2011-04-28
申请人： F. HOFFMANN-LA ROCHE AG , BRINKMANN, Ulrich , HAAS, Alexander
发明人： BRINKMANN, Ulrich , HAAS, Alexander
IPC分类号： G01N33/533 , G01N33/58
CPC分类号： G01N33/582 , G01N33/533
摘要： Herein is reported a fusion protein comprising (a) a citrine moiety, which is either a single fluorescent citrine moiety or two corresponding fragments of a citrine moiety that upon combination form a fluorescent citrine moiety, and (b) an antibody fragment comprising at least a light chain variable domain and a heavy chain variable domain, wherein (i) the single fluorescent citrine moiety, or (ii) each of the corresponding fragments of the citrine moiety is linked to one terminus of the antibody fragment via a peptide bond independently of each other either directly or via a connector, and wherein each terminus of the antibody fragment is at most linked to one single functional citrine moiety or a fractional citrine moiety. Herein is also reported the use of the fusion protein for the fluorescence staining of cells, for high throughput fluorescence staining, for monitoring intracellular acidification, and for intracellular tracking.
摘要翻译：本文报道了融合蛋白，其包含（a）黄连素部分，其是组合形成荧光黄水晶部分的单一荧光黄水晶部分或黄水晶部分的两个对应片段，和（b）抗体片段，其包含至少一个轻链可变结构域和重链可变结构域，其中（i）单个荧光黄水晶部分，或（ii）所述黄水晶部分的每个相应片段通过肽键与抗体片段的一个末端连接，独立于每个另一个直接或通过连接器，并且其中抗体片段的每个末端最多连接到一个单一功能性的黄水晶部分或部分的黄水晶部分。本文还报道了使用融合蛋白进行细胞荧光染色，用于高通量荧光染色，用于监测细胞内酸化和细胞内追踪。

5. 发明申请

WO2011157715A1 CELL-PENETRATING PEPTIDES AND USES THEROF 审中-公开
标题翻译：细胞穿刺肽及其用途
公开(公告)号：WO2011157715A1
公开(公告)日：2011-12-22
申请号：PCT/EP2011/059856
申请日：2011-06-14
申请人： F. HOFFMANN-LA ROCHE AG , BRINKMANN, Ulrich , HAAS, Alexander , MAISEL, Daniela
发明人： BRINKMANN, Ulrich , HAAS, Alexander , MAISEL, Daniela
IPC分类号： A61K47/48 , C07K14/00
CPC分类号： C07K14/47 , A61K47/6455 , C07K1/1075 , C07K1/1077 , C07K14/00 , C07K14/435
摘要： The present invention relates to the use of a peptide molecule capable of being internalized into a cell for the transformation or transfection of one or more cells with one or more nucleic acid molecules, wherein the peptide molecule (a) has a length of at least 10, preferably of at least 15 amino acid residues; (b) comprises in its primary amino acid sequence at least 25%, preferably at least 30% positively charged amino acid residues; and (c) is internalized into a cell with an efficacy being at least 80%, preferably at least 90% of the internalization efficacy of the TAT peptide having the amino acid sequence GRKKRRQRRRPPQ. The invention is also directed to the use of a composition comprising at least one such peptide being attached to one or more nucleic acid molecules for the transformation or transfection of one or more cells with the one or more nucleic acid molecules, wherein the attachment is accomplished by a linkage selected from the group consisting of a covalent linkage and a non-covalent linkage. Finally, the invention concerns the use of such peptide or such composition in the prevention and/or treatment of a condition selected from the group consisting of cancer, immune diseases, cardiovascular diseases, neuronal diseases, infections, and inflammatory diseases.
摘要翻译：本发明涉及能够内化于细胞以用于用一种或多种核酸分子转化或转染一种或多种细胞的肽分子的用途，其中肽分子（a）的长度至少为10 ，优选至少15个氨基酸残基; （b）在其主要氨基酸序列中包含至少25％，优选至少30％带正电荷的氨基酸残基; 并且（c）被内化到细胞中，其功效为具有氨基酸序列GRKKRRQRRRPPQ的TAT肽的内在功效的至少80％，优选至少90％。本发明还涉及包含至少一种这样的肽的组合物在一个或多个核酸分子上的用途，用于与一个或多个核酸分子转化或转染一种或多种细胞，其中所述附着被完成通过选自共价键和非共价键的键。最后，本发明涉及这种肽或这种组合物在预防和/或治疗选自癌症，免疫疾病，心血管疾病，神经元疾病，感染和炎性疾病的病症中的用途。

6. 发明申请

WO2011157713A2 CELL-PENETRATING PEPTIDES AND USES THEROF 审中-公开
标题翻译：细胞穿刺肽及其用途
公开(公告)号：WO2011157713A2
公开(公告)日：2011-12-22
申请号：PCT/EP2011/059853
申请日：2011-06-14
申请人： F. HOFFMANN-LA ROCHE AG , BRINKMANN, Ulrich , HAAS, Alexander , MAISEL, Daniela
发明人： BRINKMANN, Ulrich , HAAS, Alexander , MAISEL, Daniela
IPC分类号： A61K47/48
CPC分类号： C07K14/47 , A61K47/6455 , C07K1/1075 , C07K1/1077 , C07K14/00 , C07K14/435
摘要： The present invention relates to a peptide molecule capable of being internalized into a cell, wherein the peptide molecule (a) has a length of at least 10, preferably of at least 15 amino acid residues; (b) comprises in its primary amino acid sequence at least 25%, preferably at least 30% positively charged amino acid residues; and (c) is internalized into a cell with an efficacy being at least 80%, preferably at least 90% of the internalization efficacy of the TAT peptide having the amino acid sequence GRKKRRQRRRPPQ. The invention is also directed to a corresponding nucleic acid molecule encoding such peptide as well as to a composition comprising at least one such peptide being attached to any one of the group consisting of one or more nucleic acid molecules, one or more peptides or proteins, one or more small molecules, and one or more nanoparticles, wherein the attachment is accomplished by a linkage selected from the group consisting of a covalent linkage and a non-covalent linkage. Furthermore, the invention relates to a method of detecting the internalization behavior of such peptide or such composition, comprising (a) administering the peptide or composition to one or more cells; and (b) detecting the internalization of the peptide or composition. Finally, the invention concerns the use of such peptide or such composition for the transformation or transfection of one or more cells as well as in the prevention and/or treatment of a condition selected from the group consisting of cancer, immune diseases, cardiovascular diseases, neuronal diseases, infections, and inflammatory diseases.
摘要翻译：本发明涉及能够内化到细胞中的肽分子，其中肽分子（a）的长度至少为10，优选至少15个氨基酸残基; （b）在其主要氨基酸序列中包含至少25％，优选至少30％带正电荷的氨基酸残基; 并且（c）被内化成细胞，其功效为具有氨基酸序列GRKKRRQRRRPPQ的TAT肽的内在功效的至少80％，优选至少90％。本发明还涉及编码这种肽的相应核酸分子以及包含至少一种这样的肽的组合物，其连接到由一种或多种核酸分子，一种或多种肽或蛋白质组成的组中的任何一种，一种或多种小分子和一种或多种纳米颗粒，其中所述连接通过选自共价键和非共价键的键进行。此外，本发明涉及检测这种肽或这种组合物的内化行为的方法，其包括（a）将肽或组合物施用于一种或多种细胞; 和（b）检测肽或组合物的内在化。最后，本发明涉及这样的肽或这种组合物用于转化或转染一种或多种细胞以及预防和/或治疗选自以下的病症：癌症，免疫疾病，心血管疾病，神经元疾病，感染和炎性疾病。

7. 发明申请

WO2019202399A8 ANTIBODIES FOR CHELATED RADIONUCLIDES AND CLEARING AGENTS 审中-公开
公开(公告)号：WO2019202399A8
公开(公告)日：2019-10-24
申请号：PCT/IB2019/000521
申请日：2019-04-16
申请人： HOFFMANN-LA ROCHE INC. , ORANO MED SAS , F. HOFFMANN-LA ROCHE AG
发明人： TORGUE, Julien , JUREK, Paul , ROJAS-QUIJANO, Federico , KIEFER, Garry E. , FREYTAG, Olivier , GERDES, Christian , KLEIN, Christian , UMANA, Pablo , HAAS, Alexander , FROST, Sofia , SAIDI, Amal , NAYAK, Tapan
IPC分类号： A61K39/395 , A61K31/28 , C07K16/28 , C07K16/30 , C07K16/32 , C07K16/44 , A61K47/68 , A61P35/00 , A61K51/04
摘要： The present application relates to antibodies which bind specifically to chelated radionuclides, including bispecific antibodies, It further relates to the use of such bispecific antibodies in applications such as radioimmunoimaging and radioimmunotherapy. It additionally relates to clearing agents and useful in such methods.

8. 发明申请

WO2022008688A1 ANTIBODIES WHICH BIND TO CANCER CELLS AND TARGET RADIONUCLIDES TO SAID CELLS 审中-公开
公开(公告)号：WO2022008688A1
公开(公告)日：2022-01-13
申请号：PCT/EP2021/069072
申请日：2021-07-08
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： HAAS, Alexander , IMHOF-JUNG, Sabine , KLEIN, Christian , FROST, Sofia
IPC分类号： C07K16/30 , C07K16/44 , A61K51/04 , A61P35/00
摘要： The present invention relates to a set of antibodies which bind to antigens on target cells and which target radionuclides to said cells, and to methods of using the same. The antibodies each comprising a Fab binding to the target antigen fused at the C-terminus of the VH to the N-terminus of the Fc and a VH or VL binding to a radiolabelled compound. The VH or VL are fused at the C-terminus to the N- terrminus of the Fc. VH and VL form an antigen binding site when the antibody binds via the scFv to the target antigen.

9. 发明申请

WO2013174873A1 MULTISPECIFIC ANTIBODIES 审中-公开
标题翻译：多重抗体
公开(公告)号：WO2013174873A1
公开(公告)日：2013-11-28
申请号：PCT/EP2013/060529
申请日：2013-05-22
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMAN-LA ROCHE INC.
发明人： CASTOLDI, Raffaella , HAAS, Alexander , KLEIN, Christian , SCHAEFER, Wolfgang , SUSTMANN, Claudio
IPC分类号： C07K16/46 , C07K16/32 , C07K16/28 , C07K16/22 , A61K39/395
CPC分类号： C07K16/32 , A61K39/39558 , A61K2039/505 , C07K16/22 , C07K16/2863 , C07K16/468 , C07K2317/31 , C07K2317/41 , C07K2317/51 , C07K2317/515 , C07K2317/66 , C07K2317/92 , C07K2319/70
摘要： The present invention relates to bivalent, multispecific antibodies, especially bivalent, trispecific antibodies which bind to human HER1, human HER2, and human HER3, their manufacture and use.
摘要翻译：本发明涉及结合人HER1，人HER2和人HER3的二价，多特异性抗体，特别是二价三特异性抗体，其制备和用途。

10. 发明申请

WO2020141109A1 METHOD FOR THE SELECTION OF CELLS BASED ON CRISPR/CAS-CONTROLLED INTEGRATION OF A DETECTABLE TAG TO A TARGET PROTEIN 审中-公开
公开(公告)号：WO2020141109A1
公开(公告)日：2020-07-09
申请号：PCT/EP2019/086666
申请日：2019-12-20
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： HAAS, Alexander
IPC分类号： C12N15/11 , C12N15/90 , C12N15/65
摘要： Herein is reported a method for providing cells that express a fusion protein from a marker protein and a cell-endogenous target protein, consisting of the steps a) transfecting the cells i) with a Cas9-encoding plasmid additionally containing a nucleic acid which is resistant to a first selection agent, ii) with a circular donor plasmid containing a first nucleic acid which confers resistance to a second selection reagent, and a second nucleic acid which encodes the marker protein and which is flanked 3' and 5' by nucleic acids homologous to the integration site in the cell, iii) a suitable synthetic crRNA, and iv) a suitable synthetic tracrRNA, b) cultivating the cells in the presence of the first and the second selection reagent, and c) selecting cells which under the conditions of step b) carry out cell division, and thereby providing/producing cells that express a fusion protein of a marker protein and a cell- endogenous target protein.

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