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1. 发明申请

WO2009083804A2 IMPROVED FIBRONECTIN-BASED BINDING MOLECULES AND THEIR USE 审中-公开
标题翻译：改进的基于纤维蛋白的结合分子及其使用
公开(公告)号：WO2009083804A2
公开(公告)日：2009-07-09
申请号：PCT/IB2008/003962
申请日：2008-12-22
申请人： NOVARTIS AG , KOLBINGER, Frank , VINCENT, Karen, Jane , BRANNETTI, Barbara , EWERT, Stefan
发明人： KOLBINGER, Frank , VINCENT, Karen, Jane , BRANNETTI, Barbara , EWERT, Stefan
IPC分类号： A61K47/48
CPC分类号： A61K47/6835 , A61K47/60 , A61K47/643 , A61K47/644
摘要： The invention provides fibronectin-based binding molecules and methods for introducing donor CDRs into a fibronectin-based binding scaffold, in particular, Fn3. The fibronectin-based binding molecules of the invention may be further conjugated to another moiety, for example, Fc, anti-FcRn, HSA, anti-HSA, and PEG, for improved half life and stability, particularly in mammalian cells. The invention also provides methods for screening such molecules for binding to a target antigen as well as the manufacture and purification of a candidate binder.
摘要翻译：本发明提供基于纤连蛋白的结合分子和用于将供体CDR导入基于纤连蛋白的结合支架，特别是Fn3的方法。本发明的基于纤连蛋白的结合分子可以进一步缀合到另一部分，例如Fc，抗-FcRn，HSA，抗-HSA和PEG，以改善半衰期和稳定性，特别是在哺乳动物细胞中。本发明还提供筛选此类分子以结合靶抗原以及制备和纯化候选粘合剂的方法。

2. 发明申请

WO2016207858A1 FACTOR XI ANTIBODIES AND METHODS OF USE 审中-公开
标题翻译：因素XI抗体和使用方法
公开(公告)号：WO2016207858A1
公开(公告)日：2016-12-29
申请号：PCT/IB2016/053790
申请日：2016-06-24
申请人： NOVARTIS AG , EDER, Jorg , EWERT, Stefan , HASSIEPEN, Ulrich , KHDER, Yasser , MAYR, Lorenz M. , MELKKO, Samu , SCHIERING, Nikolaus
发明人： EDER, Jorg , EWERT, Stefan , HASSIEPEN, Ulrich , KHDER, Yasser , MAYR, Lorenz M. , MELKKO, Samu , SCHIERING, Nikolaus
IPC分类号： C07K16/36
CPC分类号： C07K16/40 , A61K2039/505 , C07K16/36 , C07K2317/21 , C07K2317/33 , C07K2317/34 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要： The present invention relates to monoclonal antibodies and antigen binding fragments thereof that bind to human Factor XI and activated Factor XI ("Factor XIa"), and pharmaceutical compositions and methods of treatment comprising the same.
摘要翻译：本发明涉及结合人因子XI和活化因子XI（“因子XIa”）的单克隆抗体及其抗原结合片段，以及包含其的药物组合物和治疗方法。

3. 发明申请

WO2008132152A1 NOVEL ANTIBODY MOLECULES AND NUCLEIC ACIDS BINDING TO FUNGAL STRESS PROTEIN HSP90 审中-公开
标题翻译：新型抗体分子和核酸结合真菌应激蛋白HSP90
公开(公告)号：WO2008132152A1
公开(公告)日：2008-11-06
申请号：PCT/EP2008/055037
申请日：2008-04-24
申请人： NOVARTIS AG , MASSACHUSETTS INSTITUTE OF TECHNOLOGY , CHENNAMSETTY, Naresh , EWERT, Stefan , HELK, Bernhard , TROUT, Bernhardt , WECHNER, Philipp
发明人： CHENNAMSETTY, Naresh , EWERT, Stefan , HELK, Bernhard , TROUT, Bernhardt , WECHNER, Philipp
IPC分类号： C07K16/14 , C07K16/18 , A61K39/395 , A61P31/00 , A61K35/00 , C12N15/10 , A61P37/06
CPC分类号： C07K16/14 , A61K2039/505 , C07K16/18 , C07K2317/622 , C07K2319/21
摘要： An scFv peptide comprising a V H domain and a V L domain linked by an amino acid spacer is disclosed. The V H domain comprises a sequence with at least 80% sequence identity to the sequence of SEQ ID NO. 64. The V L domain comprises a sequence with at least 80% sequence identity to the sequence of SEQ ID NO. 66. The scFv peptide comprises an additional feature selected from (a) to (e) and combinations thereof. (a) A substitution or deletion of an amino acid in the V H domain at a position corresponding to that selected from the group consisting of : I 29 , H 68 , N 85 , C 97 and combinations thereof. (b) A substitution or deletion of an amino acid in the V L domain at a position corresponding to that selected from the group consisting of : V 2 , V 3 , F 10 , F 14 , A 39 , N 76 and combinations thereof. (c) The amino acid spacer comprises the sequence (GGGGS) n wherein n is between 4 and 6. (d) The V H domain further comprises an N-terminal pelB signal sequence comprising the sequence of SEQ ID NO. 68 or a sequence having at least 80% sequence identity thereto. (e) The V L domain is located at the N-terminal end of the V H domain. (f) The substitution of the cysteine residue in the V H domain corresponding to position 28 with a serine residue.
摘要翻译：公开了包含由氨基酸间隔物连接的V H H结构域和V L L结构域的scFv肽。 V H结构域包含与SEQ ID NO：1的序列具有至少80％的序列同一性的序列。 V L区包含与SEQ ID NO：1的序列具有至少80％的序列同一性的序列。 scFv肽包含选自（a）至（e）的附加特征及其组合。（a）在对应于选自以下的位置的位置上的V H H区域中的氨基酸的取代或缺失：I 68 N，N 85，C 97，及其组合。（b）在对应于选自以下的位置的位置上的V L区域中的氨基酸的取代或缺失：V 2， 3，F 10，F 14，A 39，N 76和它们的组合。（c）氨基酸间隔物包含序列（GGGGS）N，其中n在4和6之间。（d）V H区还包含N末端pelB 信号序列，其包含SEQ ID NO： 68或与其具有至少80％序列同一性的序列。（e）V L领域位于V H领域的N末端。（f）用丝氨酸残基取代对应于位置28的V H H区中的半胱氨酸残基。

4. 发明申请

WO2011080050A3 CCL21 BINDING MOLECULES 审中-公开
公开(公告)号：WO2011080050A3
公开(公告)日：2011-07-07
申请号：PCT/EP2010/069430
申请日：2010-12-10
申请人： NOVARTIS AG , BARDROFF, Michael , EWERT, Stefan , JAEGER, Ute , JARAI, Gabor , KUNZ, Christian Carsten Silvester , WIESEHAN, Katja
发明人： BARDROFF, Michael , EWERT, Stefan , JAEGER, Ute , JARAI, Gabor , KUNZ, Christian Carsten Silvester , WIESEHAN, Katja
IPC分类号： C07K16/24
摘要： The present invention relates to binding molecules, in particular antibodies and immunoglobulins to human CCL21 (hCCL21) and their use in the treatment and/or prevention of human diseases and disorders, particularly those of a fibrotic nature. Pharmaceutical compositions, methods of manufacture and methods of treatment are also disclosed.

5. 发明申请

WO2008025499A1 VERFAHREN UND VORRICHTUNG 审中-公开
标题翻译：方法和装置
公开(公告)号：WO2008025499A1
公开(公告)日：2008-03-06
申请号：PCT/EP2007/007481
申请日：2007-08-27
申请人： SEW-EURODRIVE GMBH & CO. KG , EWERT, Stefan , STEINSDÖRFER, Andreas
发明人： EWERT, Stefan , STEINSDÖRFER, Andreas
IPC分类号： H02P5/46 , H02M3/158 , H02M7/493
CPC分类号： H02P5/46
摘要： Verfahren zur Bewegungssteuerung von Achsen, deren Antriebe zum Energieaustausch verbunden sind, insbesondere durch Verbindung von Zwischenkreisen der von den Antrieben jeweils umfassten Umrichter, wobei vor Beginn der Bewegung eine prädiktive Bestimmung des Bewegungsablaufes statt findet, wobei zuerst die zeitkritische Achse bestimmt wird, dann das Verfahrprofil der zeitkritischen Achse festgelegt wird, dann den möglichen Verfahrprofilen weiterer Achsen ein jeweiliger Gesamtenergieverbrauch zugeordnet wird, davon dasjenige Profil ausgewählt wird, zu welchem der kleinste Gesamtenergiebedarf gehört, dann die Bewegung ausgeführt wird.
摘要翻译：对于轴的运动控制过程中，驱动器是由驱动器的中间电路，每个包括逆变器，其中运动的序列的预测判定的移动开始之前发生，第一时间关键的轴被确定，则该横动的连接而连接于能量交换，特别是时间关键的轴被确定，然后进一步轴的可能的运动轮廓与相应的总的能量消耗，其中选择了一个简档，向其中最小的总能量需求属于，则移动进行关联。

6. 发明申请

WO2003097697A2 IMMUNOGLOBULIN FRAMEWORKS WHICH DEMONSTRATE ENHANCED STABILITY IN THE INTRACELLULAR ENVIRONMENT AND METHODS OF IDENTIFYING SAME 审中-公开
标题翻译：阐明细胞内环境中增强稳定性的免疫球蛋白框架及其鉴别方法
公开(公告)号：WO2003097697A2
公开(公告)日：2003-11-27
申请号：PCT/EP2003/005324
申请日：2003-05-21
申请人： ESBATECH AG , TISSOT, Kathrin , EWERT, Stefan , AUF DER MAUR, Adrian , BARBERIS, Alcide , ESCHER, Dominik
发明人： TISSOT, Kathrin , EWERT, Stefan , AUF DER MAUR, Adrian , BARBERIS, Alcide , ESCHER, Dominik
IPC分类号： C07K16/18
CPC分类号： C07K16/00 , A61K48/00 , C07K2317/21 , C07K2317/55 , C07K2317/567 , C07K2317/622 , C07K2317/80 , C07K2317/82 , C07K2317/94 , G01N33/6857
摘要： Compositions are provided, which can be used as frameworks for the creation of very stable and soluble single-chain Fv antibody fragments. These frameworks have been selected for intracellular performance and are thus ideally suited for the creation of scFv antibody fragments or scFv antibody libraries for applications where stability and solubility are limiting factors for the performance of antibody fragments, such as in the reducing environment of a cell. Such frameworks can also be used to identify highly conserved residues and consensus sequences which demonstrate enhanced solubility and stability.
摘要翻译：提供组合物，其可用作产生非常稳定和可溶性单链Fv抗体片段的框架。这些框架已经被选择用于细胞内性能，因此理想地适用于产生scFv抗体片段或scFv抗体文库，用于其中稳定性和溶解度是抗体片段表现的限制因素，例如在细胞的还原环境中。此类框架还可用于鉴定高度保守的残基和共有序列，其表现出增强的溶解度和稳定性。

7. 发明申请

WO2009033309A1 HUMANIZED ANTIBODIES AGAINST THE ß-AMYLOYD PEPTIDE 审中-公开
标题翻译：抗人β抗原肽的抗体
公开(公告)号：WO2009033309A1
公开(公告)日：2009-03-19
申请号：PCT/CH2008/000382
申请日：2008-09-15
申请人： ESBATECH AG , UNIVERSITY OF ZURICH , EWERT, Stefan , AUF DER MAUR, Adrian , CATTEPOEL, Susann , NITSCH, Roger
发明人： EWERT, Stefan , AUF DER MAUR, Adrian , CATTEPOEL, Susann , NITSCH, Roger
IPC分类号： C07K16/18 , A61K39/395 , A61P25/28 , G01N33/53
CPC分类号： C07K16/18 , A61K2039/505 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/622
摘要： The invention discloses an isolated antibody that selectively binds to the C-terminal part of Abeta and is humanized or fully human. The antibody of the invention is capable of preventing oligomerisation of Abeta. Furthermore, a method of diagnosis comprising the steps of: (i) Labelling an antibody; (ii) Administering an effective dose of said antibody intranasally or systemically to a subject; and (iii) Detecting the concentration and/or presence of the labelled antibody in body parts of the subject is disclosed.
摘要翻译：本发明公开了一种分离的抗体，其选择性地结合Abeta的C-末端部分并且是人源化的或完全人的。本发明的抗体能够防止Aβ的低聚。此外，诊断方法包括以下步骤：（i）标记抗体; （ii）向受试者鼻内或全身施用有效剂量的所述抗体; 并且（iii）公开了检测受试者体内部分标记的抗体的浓度和/或存在。

8. 发明申请

WO2006131013A2 STABLE AND SOLUBLE ANTIBODIES INHIBITING TNFα 审中-公开
标题翻译：稳定和可溶性抗体抑制TNFa
公开(公告)号：WO2006131013A2
公开(公告)日：2006-12-14
申请号：PCT/CH2006/000300
申请日：2006-06-06
申请人： ESBATECH AG , EWERT, Stefan , BARBERIS, Alcide , URECH, David M. , AUF DER MAUR, Adrian , LICHTLEN, Peter
发明人： EWERT, Stefan , BARBERIS, Alcide , URECH, David M. , AUF DER MAUR, Adrian , LICHTLEN, Peter
IPC分类号： C07K16/24 , A61K39/395 , G01N33/53 , C12N15/13 , A61P37/00 , A61P29/00
CPC分类号： C07K16/241 , A61K2039/505 , C07K2317/14 , C07K2317/21 , C07K2317/24 , C07K2317/522 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/622 , C07K2317/76 , C07K2317/92 , C07K2317/94
摘要： The present invention relates to particularly stable and soluble scFv antibodies and Fab fragments specific for TNFα, which comprise specific light chain and heavy chain sequences that are optimized for stability, solubility, in vitro and in vivo binding of TNFα, and low immunogenicity. Said antibodies are designed for the diagnosis and/or treatment of TNFα-related disorders. The nucleic acids, vectors and host cells for expression of the recombinant antibodies of the invention, methods for isolating them and the use of said antibodies in medicine are also disclosed.
摘要翻译：本发明涉及特别稳定和可溶的scFv抗体和对TNFa特异性的Fab片段，其包含针对TNFa的稳定性，溶解性，体外和体内结合以及低免疫原性而优化的特异性轻链和重链序列。所述抗体被设计用于诊断和/或治疗TNFα相关疾病。还公开了用于表达本发明的重组抗体的核酸，载体和宿主细胞，用于分离它们的方法和所述抗体在医学中的用途。

9. 发明申请

WO2003008451A2 MODIFICATION OF HUMAN VARIABLE DOMAINS 审中-公开
标题翻译：人类可变域修改
公开(公告)号：WO2003008451A2
公开(公告)日：2003-01-30
申请号：PCT/EP2002/008094
申请日：2002-07-19
申请人： UNIVERSITÄT ZÜRICH , EWERT, Stefan , HUBER, Thomas , HONEGGER, Annemarie , PLÜCKTHUN, Andreas
发明人： EWERT, Stefan , HUBER, Thomas , HONEGGER, Annemarie , PLÜCKTHUN, Andreas
IPC分类号： C07K16/00
CPC分类号： C07K16/00 , C07K2317/21 , C07K2317/56 , C07K2317/622
摘要： The present invention relates to a method for the optimization of isolated human immunoglobulin variable heavy (V H ) and light (V L ) constructs.
摘要翻译：本发明涉及用于优化分离的人免疫球蛋白可变重（VH）和轻（VL）构建体的方法。

10. 发明申请

WO2003097697A3 IMMUNOGLOBULIN FRAMEWORKS WHICH DEMONSTRATE ENHANCED STABILITY IN THE INTRACELLULAR ENVIRONMENT AND METHODS OF IDENTIFYING SAME 审中-公开
公开(公告)号：WO2003097697A3
公开(公告)日：2003-11-27
申请号：PCT/EP2003/005324
申请日：2003-05-21
申请人： ESBATECH AG , TISSOT, Kathrin , EWERT, Stefan , AUF DER MAUR, Adrian , BARBERIS, Alcide , ESCHER, Dominik
发明人： TISSOT, Kathrin , EWERT, Stefan , AUF DER MAUR, Adrian , BARBERIS, Alcide , ESCHER, Dominik
IPC分类号： C07K16/18
摘要： Compositions are provided, which can be used as frameworks for the creation of very stable and soluble single-chain Fv antibody fragments. These frameworks have been selected for intracellular performance and are thus ideally suited for the creation of scFv antibody fragments or scFv antibody libraries for applications where stability and solubility are limiting factors for the performance of antibody fragments, such as in the reducing environment of a cell. Such frameworks can also be used to identify highly conserved residues and consensus sequences which demonstrate enhanced solubility and stability.

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