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1. 发明申请

WO2011131659A3 BINDING DOMAINS 审中-公开
公开(公告)号：WO2011131659A3
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056220
申请日：2011-04-19
申请人： GLAXO GROUP LIMITED , DE WILDT, Rudolf, Maria , LIDDAMENT, Mark , RAMSAY, Nicola , SCHON, Oliver , STOOP, Adriaan, Allart
发明人： DE WILDT, Rudolf, Maria , LIDDAMENT, Mark , RAMSAY, Nicola , SCHON, Oliver , STOOP, Adriaan, Allart
IPC分类号： C07K16/00 , C07K16/18 , C07K16/22 , C07K16/24 , C07K16/30
摘要： The invention relates to amino acid residues within an immunoglobulin light chain amino acid sequence (V L ) which stabilize the monomeric state of the immunoglobulin single variable domain. In particular, but not exclusively, the invention describes a number of mutations that stabilize the monomeric state of DP к 9 framework V κ domain antibodies.

2. 发明申请

WO2011131659A2 BINDING DOMAINS 审中-公开
标题翻译：绑定域
公开(公告)号：WO2011131659A2
公开(公告)日：2011-10-27
申请号：PCT/EP2011056220
申请日：2011-04-19
申请人： GLAXO GROUP LTD , DE WILDT RUDOLF MARIA , LIDDAMENT MARK , RAMSAY NICOLA , SCHON OLIVER , STOOP ADRIAAN ALLART
发明人： DE WILDT RUDOLF MARIA , LIDDAMENT MARK , RAMSAY NICOLA , SCHON OLIVER , STOOP ADRIAAN ALLART
IPC分类号： C07K16/00 , C07K16/18 , C07K16/22 , C07K16/24 , C07K16/30
CPC分类号： C07K16/00 , C07K16/18 , C07K16/22 , C07K16/241 , C07K16/247 , C07K16/3007 , C07K2317/567 , C07K2317/569 , C07K2317/92
摘要： The invention relates to amino acid residues within an immunoglobulin light chain amino acid sequence (VL) which stabilize the monomeric state of the immunoglobulin single variable domain. In particular, but not exclusively, the invention describes a number of mutations that stabilize the monomeric state of DP?9 framework V? domain antibodies.
摘要翻译：本发明涉及稳定免疫球蛋白单可变结构域的单体状态的免疫球蛋白轻链氨基酸序列（VL）内的氨基酸残基。特别地但并非排他地，本发明描述了许多稳定DPα9框架Vβ的单体状态的突变。结构域抗体。

3. 发明申请

WO2011012609A3 ANTI - TGF - BETA RECEPTOR TYPE II SINGLE DOMAIN ANTIBODIES 审中-公开
标题翻译：抗TGF - β受体II型单个抗体
公开(公告)号：WO2011012609A3
公开(公告)日：2011-09-15
申请号：PCT/EP2010060867
申请日：2010-07-27
申请人： GLAXO GROUP LTD , DE WILDT RUDOLF MARIA , DIMECH CAROLINE J , HOLMES STEVE , STOOP ADRIAAN ALLART
发明人： DE WILDT RUDOLF MARIA , DIMECH CAROLINE J , HOLMES STEVE , STOOP ADRIAAN ALLART
IPC分类号： C07K16/28 , A61P27/02 , A61P43/00 , C07K16/40
CPC分类号： C07K16/2863 , C07K16/40 , C07K2317/21 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/76 , C07K2317/92
摘要： The invention provides an anti-TGFbetaRII immunoglobulin single variable domain. Suitably, an anti-TGFbetaRII immunoglobulin single variable domain in accordance with the invention is one which binds to TGFbetaRII with a dissociation constant (Kd) in the range of 10pM to 50nM, preferably 10pM to 10nM, preferably 250pM to 10nM. Isolated polypeptides comprising an amino acid sequence that is at least 70% identical to at least one amino acid sequence selected from the group of: SEQ ID NOs: 1 to 23, wherein said isolated polypeptide binds to TGFbetaRII are also provided. The invention also provides a polypeptide, ligand or pharmaceutical composition for treating a disease associated with TGFbeta signalling and suitably a disease selected from the group of: tissue fibrosis, such as pulmonary fibrosis, including idiopathic pulmonary fibrosis, liver fibrosis, including cirrhosis and chronic hepatitis, rheumatoid arthritis, ocular disorders, or fibrosis of the skin, including keloid of skin, and kidney such as nephritis, kidney fibrosis and nephrosclerosis, and a vascular condition, such as restenosis.
摘要翻译：本发明提供抗TGFbetaRII免疫球蛋白单可变结构域。适当地，根据本发明的抗TGFbetaRII免疫球蛋白单可变结构域是以解离常数（Kd）在10pM至50nM，优选10pM至10nM，优选250pM至10nM范围内结合TGFbetaRII的结合。分离的多肽包含与选自SEQ ID NO：1至23的至少一个氨基酸序列至少70％相同的氨基酸序列，其中所述分离的多肽与TGFbetaRII结合。本发明还提供了用于治疗与TGFbeta信号传导相关疾病的合适的多肽，配体或药物组合物，适当地选自以下组中的疾病：组织纤维化，例如肺纤维化，包括特发性肺纤维化，肝纤维化，包括肝硬化和慢性肝炎，类风湿性关节炎，眼部疾病或皮肤纤维化，包括皮肤瘢痕疙瘩，肾脏如肾炎，肾纤维化和肾硬化，以及血管病变，如再狭窄。

4. 发明申请

WO2011012609A2 LIGANDS THAT BIND TGF-BETA RECEPTOR RII 审中-公开
标题翻译：结合TGF-β受体RII的配体
公开(公告)号：WO2011012609A2
公开(公告)日：2011-02-03
申请号：PCT/EP2010/060867
申请日：2010-07-27
申请人： GLAXO GROUP LIMITED , DE WILDT, Rudolf Maria , DIMECH, Caroline J , HOLMES, Steve , STOOP, Adriaan Allart
发明人： DE WILDT, Rudolf Maria , DIMECH, Caroline J , HOLMES, Steve , STOOP, Adriaan Allart
IPC分类号： C07K16/28
CPC分类号： C07K16/2863 , C07K16/40 , C07K2317/21 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/76 , C07K2317/92
摘要： The invention provides an anti-TGFbetaRII immunoglobulin single variable domain. Suitably, an anti-TGFbetaRII immunoglobulin single variable domain in accordance with the invention is one which binds to TGFbetaRII with a dissociation constant (Kd) in the range of 10pM to 50nM, preferably 10pM to 10nM, preferably 250pM to 10nM. Isolated polypeptides comprising an amino acid sequence that is at least 70% identical to at least one amino acid sequence selected from the group of: SEQ ID NOs: 1 to 23, wherein said isolated polypeptide binds to TGFbetaRII are also provided. The invention also provides a polypeptide, ligand or pharmaceutical composition for treating a disease associated with TGFbeta signalling and suitably a disease selected from the group of: tissue fibrosis, such as pulmonary fibrosis, including idiopathic pulmonary fibrosis, liver fibrosis, including cirrhosis and chronic hepatitis, rheumatoid arthritis, ocular disorders, or fibrosis of the skin, including keloid of skin, and kidney such as nephritis, kidney fibrosis and nephrosclerosis, and a vascular condition, such as restenosis.
摘要翻译：本发明提供抗TGFbetaRII免疫球蛋白单可变结构域。合适地，根据本发明的抗TGFbetaRII免疫球蛋白单可变结构域是以10pM至50nM，优选10pM至10nM，优选250pM至10nM范围内的解离常数（Kd）结合TGFβRII的结构域。分离的多肽包含与选自SEQ ID NO：1至23的至少一个氨基酸序列至少70％相同的氨基酸序列，其中所述分离的多肽与TGFbetaRII结合。本发明还提供了用于治疗与TGFbeta信号传导相关疾病的合适的多肽，配体或药物组合物，适当地选自以下组中的疾病：组织纤维化，例如肺纤维化，包括特发性肺纤维化，肝纤维化，包括肝硬化和慢性肝炎，类风湿性关节炎，眼部疾病或皮肤纤维化，包括皮肤瘢痕疙瘩和肾脏如肾炎，肾纤维化和肾硬化，以及血管病变，如再狭窄。

5. 发明申请

WO2009068649A3 ANTIGEN-BINDING CONSTRUCTS 审中-公开
公开(公告)号：WO2009068649A3
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066438
申请日：2008-11-28
申请人： GLAXO GROUP LIMITED , ASHMAN, Claire , BATUWANGALA, Thil , BURDEN, Michael, Neil , CLEGG, Stephanie, Jane , DE WILDT, Rudolf, Maria , ELLIS, Jonathan, Henry , HAMBLIN, Paul, Andrew , HUSSAIN, Farhana , JESPERS, Laurent , LEWIS, Alan , ORECCHIA, Martin, Anibal , SHAH, Radha , STEWARD, Michael
发明人： ASHMAN, Claire , BATUWANGALA, Thil , BURDEN, Michael, Neil , CLEGG, Stephanie, Jane , DE WILDT, Rudolf, Maria , ELLIS, Jonathan, Henry , HAMBLIN, Paul, Andrew , HUSSAIN, Farhana , JESPERS, Laurent , LEWIS, Alan , ORECCHIA, Martin, Anibal , SHAH, Radha , STEWARD, Michael
IPC分类号： C07K16/46 , A61K39/395 , A61P35/00 , A61P29/00 , C12N15/13 , C12N5/10 , C07K16/22 , C07K16/24 , C07K16/28 , C07K16/32
摘要： The invention relates to antigen-binding constructs comprising a protein scaffold which are linked to one or more epitope-binding domains wherein the antigen- binding construct has at least two antigen binding sites at least one of which is from an epitope binding domain and at least one of which is from a paired VH/VL domain, methods of making such constructs and uses thereof.

6. 发明申请

WO2009068649A2 ANTIGEN-BINDING CONSTRUCTS 审中-公开
标题翻译：抗原结构
公开(公告)号：WO2009068649A2
公开(公告)日：2009-06-04
申请号：PCT/EP2008066438
申请日：2008-11-28
申请人： GLAXO GROUP LTD , ASHMAN CLAIRE , BATUWANGALA THIL , BURDEN MICHAEL NEIL , CLEGG STEPHANIE JANE , DE WILDT RUDOLF MARIA , ELLIS JONATHAN HENRY , HAMBLIN PAUL ANDREW , HUSSAIN FARHANA , JESPERS LAURENT , LEWIS ALAN , ORECCHIA MARTIN ANIBAL , SHAH RADHA , STEWARD MICHAEL
发明人： ASHMAN CLAIRE , BATUWANGALA THIL , BURDEN MICHAEL NEIL , CLEGG STEPHANIE JANE , DE WILDT RUDOLF MARIA , ELLIS JONATHAN HENRY , HAMBLIN PAUL ANDREW , HUSSAIN FARHANA , JESPERS LAURENT , LEWIS ALAN , ORECCHIA MARTIN ANIBAL , SHAH RADHA , STEWARD MICHAEL
IPC分类号： C07K16/46 , A61K39/395 , A61P29/00 , A61P35/00 , C07K16/22 , C07K16/24 , C07K16/28 , C07K16/32 , C12N5/10 , C12N15/13
CPC分类号： C07K16/244 , C07K16/22 , C07K16/241 , C07K16/247 , C07K16/2863 , C07K16/2866 , C07K16/2887 , C07K16/32 , C07K16/468 , C07K2317/14 , C07K2317/31 , C07K2317/34 , C07K2317/51 , C07K2317/515 , C07K2317/569 , C07K2317/64 , C07K2317/732 , C07K2317/734 , C07K2317/76 , C07K2317/92 , C07K2318/20 , C07K2319/30
摘要： The invention relates to antigen-binding constructs comprising a protein scaffold which are linked to one or more epitope-binding domains wherein the antigen- binding construct has at least two antigen binding sites at least one of which is from an epitope binding domain and at least one of which is from a paired VH/VL domain, methods of making such constructs and uses thereof.
摘要翻译：本发明涉及包含与一个或多个表位结合结构域连接的蛋白质支架的抗原结合构建体，其中所述抗原结合构建体具有至少两个抗原结合位点，其中至少一个抗原结合位点来自表位结合结构域，并且至少其中一个来自配对的VH / VL结构域，制备此类构建体的方法及其用途。

7. 发明申请

WO2010046337A3 LIGANDS THAT HAVE BINDING SPECIFICITY FOR DC-SIGN 审中-公开
标题翻译：对DC-SIGN具有结合特异性的配体
公开(公告)号：WO2010046337A3
公开(公告)日：2010-07-01
申请号：PCT/EP2009063655
申请日：2009-10-19
申请人： DOMANTIS LTD , DE WILDT RUDOLF MARIA
发明人： DE WILDT RUDOLF MARIA
IPC分类号： C07K16/28
CPC分类号： C07K16/2851 , A61K2039/505 , C07K2317/21 , C07K2317/565 , C07K2317/569
摘要： The present invention provides an anti-dendritic cell-specific ICAM-3 grabbing non-integrin (DC-SIGN; CD209) immunoglobulin single variable domain. Polypeptides, ligands and compositions comprising such anti-DC-SIGN immunoglobulin single variable domains are also described along with nucleic acids encoding such immunoglobulins and vectors and host cells for expression. The invention further relates to uses, formulations, compositions and devices comprising such DC-SIGN-binding agents.
摘要翻译：本发明提供了抗树突细胞特异性ICAM-3捕获非整联蛋白（DC-SIGN; CD209）免疫球蛋白单可变结构域。还描述了包含此类抗DC-SIGN免疫球蛋白单可变结构域的多肽，配体和组合物以及编码此类免疫球蛋白和载体以及用于表达的宿主细胞的核酸。本发明还涉及包含这种DC-SIGN结合剂的用途，制剂，组合物和装置。

8. 发明申请

WO2010046338A1 COMPOSITION FOR TARGETING DENDRITIC CELLS 审中-公开
标题翻译：用于靶向细胞的组合物
公开(公告)号：WO2010046338A1
公开(公告)日：2010-04-29
申请号：PCT/EP2009/063656
申请日：2009-10-19
申请人： DOMANTIS LIMITED , LIPOTEK PTY LTD , ALTIN, Joseph , ATMOSUKARTO, Ines , DE WILDT, Rudolf, Maria , PARISH, Christopher , PRICE, Jason
发明人： ALTIN, Joseph , ATMOSUKARTO, Ines , DE WILDT, Rudolf, Maria , PARISH, Christopher , PRICE, Jason
IPC分类号： A61K9/127 , A61K39/00 , A61P35/00 , A61P37/04
CPC分类号： A61K39/3955 , A61K38/217 , A61K39/0011 , A61K2039/55516 , A61K2039/55555 , A61K2039/6018 , C07K14/4748 , C07K16/2851 , C07K2317/22 , C07K2317/569
摘要： The present invention relates to a composition for targeting dendritic cells. In particular, the present invention relates to a composition comprising: a) one or more antigens; b) an anti-DC-SIGN immunoglobulin single variable domain; and c) a carrier which carries a) and b). The invention further relates to formulations, compositions and devices comprising such anti-DC-SIGN molecules and their use as a medicament and in the treatment of cancer, suitably melanoma.
摘要翻译：本发明涉及用于靶向树突状细胞的组合物。特别地，本发明涉及一种组合物，其包含：a）一种或多种抗原; b）抗DC-SIGN免疫球蛋白单可变区; 和c）承载a）和b）的载体。本发明进一步涉及包含这种抗DC-SIGN分子的制剂，组合物和装置及其作为药物的用途，以及用于治疗癌症，适当地为黑素瘤。

9. 发明申请

WO2010046337A2 LIGANDS THAT HAVE BINDING SPECIFICITY FOR DC-SIGN 审中-公开
标题翻译：对于DC-SIGN具有绑定特性的配置
公开(公告)号：WO2010046337A2
公开(公告)日：2010-04-29
申请号：PCT/EP2009/063655
申请日：2009-10-19
申请人： DOMANTIS LIMITED , DE WILDT, Rudolf, Maria
发明人： DE WILDT, Rudolf, Maria
IPC分类号： C07K16/28
CPC分类号： C07K16/2851 , A61K2039/505 , C07K2317/21 , C07K2317/565 , C07K2317/569
摘要： The present invention provides an anti-dendritic cell-specific ICAM-3 grabbing non-integrin (DC-SIGN; CD209) immunoglobulin single variable domain. Polypeptides, ligands and compositions comprising such anti-DC-SIGN immunoglobulin single variable domains are also described along with nucleic acids encoding such immunoglobulins and vectors and host cells for expression. The invention further relates to uses, formulations, compositions and devices comprising such DC-SIGN-binding agents.
摘要翻译：本发明提供抗树突状细胞特异性ICAM-3抓取非整联蛋白（DC-SIGN; CD209）免疫球蛋白单可变结构域。还描述了包含这种抗DC-SIGN免疫球蛋白单可变结构域的多肽，配体和组合以及编码这种免疫球蛋白的核酸和用于表达的宿主细胞。本发明还涉及包含这种DC-SIGN结合剂的用途，制剂，组合物和装置。

10. 发明申请

WO2009138413A1 SINGLE DOMAIN ANTIBODIES THAT BIND IL-13 审中-公开
标题翻译：绑定IL-13的单一抗体
公开(公告)号：WO2009138413A1
公开(公告)日：2009-11-19
申请号：PCT/EP2009/055745
申请日：2009-05-13
申请人： DOMANTIS LIMITED , DE SILVA, Inusha , DE WILDT, Rudolf, Maria , DIMECH, Caroline, J , PUPECKA, Malgorzata , SPARKS, Catherine, A
发明人： DE SILVA, Inusha , DE WILDT, Rudolf, Maria , DIMECH, Caroline, J , PUPECKA, Malgorzata , SPARKS, Catherine, A
IPC分类号： C07K16/24 , A61P11/06 , A61P37/08
CPC分类号： C07K16/244 , A61K2039/505 , C07K2317/569
摘要： Disclosed are ligands that have binding specificity for interleukin-13 (TL-13), or for IL-4 and IL-13. Also disclosed are methods of using these ligands. In particular, the use of these ligands for treating allergic asthma is described.
摘要翻译：公开了对白细胞介素-13（TL-13）或IL-4和IL-13具有结合特异性的配体。还公开了使用这些配体的方法。特别地，描述了这些配体用于治疗过敏性哮喘的用途。

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