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1. 发明申请

WO2011051217A1 STABLE ANTI-TNFR1 POLYPEPTIDES, ANTIBODY VARIABLE DOMAINS & ANTAGONISTS 审中-公开
标题翻译：稳定的抗TNFR1多肽，抗体可变域和拮抗剂
公开(公告)号：WO2011051217A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066046
申请日：2010-10-25
申请人： GLAXO GROUP LIMITED , DE SILVA, Inusha , SEPP, Armin , STOOP, Adriaan Allart
发明人： DE SILVA, Inusha , SEPP, Armin , STOOP, Adriaan Allart
IPC分类号： A61K39/395 , C07K16/18 , C07K16/28 , C07K16/46
CPC分类号： C07K16/2866 , A61K39/39591 , C07K16/18 , C07K16/2878 , C07K2317/21 , C07K2317/31 , C07K2317/569 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/00
摘要： The invention relates to storage-stable anti-TNFR1 antibody single variable domains (d Abs), antagonists and multispecific ligands, as well as methods and uses of these. The anti-TNFR1 polypeptides, antibody single variable domains (d Abs), antagonists and multispecific ligands are useful for treating and/or preventing inflammatory disease, such as arthritis or COPD, as well as for pulmonary administration, oral administration, delivery to the lung and delivery to the GI tract of a patient.
摘要翻译：本发明涉及储存稳定的抗TNFR1抗体单可变结构域（d Abs），拮抗剂和多特异性配体，以及它们的方法和用途。抗TNFR1多肽，抗体单可变结构域（d Abs），拮抗剂和多特异性配体可用于治疗和/或预防炎性疾病如关节炎或COPD，以及肺部给药，口服给药，输送至肺部并输送到患者的胃肠道。

2. 发明申请

WO2011006914A2 ANTAGONISTS, USES & METHODS FOR PARTIALLY INHIBITING TNFR1 审中-公开
标题翻译：拮抗剂，部分抑制TNFR1的用途和方法
公开(公告)号：WO2011006914A2
公开(公告)日：2011-01-20
申请号：PCT/EP2010/060111
申请日：2010-07-14
申请人： GLAXO GROUP LIMITED , STOOP, Adriaan Allart
发明人： STOOP, Adriaan Allart
IPC分类号： A61K39/00
CPC分类号： C07K16/18 , A61K2039/505 , C07K16/2878 , C07K2317/33 , C07K2317/34 , C07K2317/40 , C07K2317/565 , C07K2317/569 , C07K2317/76 , C07K2317/90 , C07K2317/92 , C07K2317/94 , C07K2319/00
摘要： The present invention relates to anti-Tumor Necrosis Factor 1 (TNFR1, p55, CD120a, P60, TNF receptor superfamily member 1A, TNFRSF1A) antagonists for partially inhibiting TNFR1 useful for the treatment and/or prevention of TNFR1- mediated diseases or conditions such as arthritis, psoriasis, Crohn's disease, COPD, lung inflammatory conditions and asthma. The invention further relates to methods, uses, formulations, compositions and devices comprising or using such anti-TNFR1 antagonists.
摘要翻译：本发明涉及用于部分抑制TNFR1的抗肿瘤坏死因子1（TNFR1，p55，CD120a，P60，TNF受体超家族成员1A，TNFRSF1A）拮抗剂，其用于治疗和/或预防TNFR1-介导的疾病或病症如关节炎，牛皮癣，克罗恩病，COPD，肺炎症状况和哮喘。本发明还涉及包含或使用这种抗TNFR1拮抗剂的方法，用途，制剂，组合物和装置。

3. 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。

4. 发明公开

EP2453920A2 ANTAGONISTS, USES & METHODS FOR PARTIALLY INHIBITING TNFR1 审中-公开
标题翻译：拮抗剂，用途和方法类偏TNFR1抑制
公开(公告)号：EP2453920A2
公开(公告)日：2012-05-23
申请号：EP10737010.8
申请日：2010-07-14
申请人： Glaxo Group Limited
发明人： STOOP, Adriaan Allart
IPC分类号： A61K39/395 , A61P29/00 , A61P37/00 , C07K16/18 , C07K16/28
CPC分类号： C07K16/18 , A61K2039/505 , C07K16/2878 , C07K2317/33 , C07K2317/34 , C07K2317/40 , C07K2317/565 , C07K2317/569 , C07K2317/76 , C07K2317/90 , C07K2317/92 , C07K2317/94 , C07K2319/00
摘要： The present invention relates to anti-Tumor Necrosis Factor 1 (TNFR1, p55, CD120a, P60, TNF receptor superfamily member 1A, TNFRSF1A) antagonists for partially inhibiting TNFR1 useful for the treatment and/or prevention of TNFR1- mediated diseases or conditions such as arthritis, psoriasis, Crohn's disease, COPD, lung inflammatory conditions and asthma. The invention further relates to methods, uses, formulations, compositions and devices comprising or using such anti-TNFR1 antagonists.

5. 发明公开

EP2459593A2 ANTI-TGF-BETA RECEPTOR TYPE II SINGLE DOMAIN ANTIBODIES 审中-公开
标题翻译：对TGF-β受体II型单域抗体
公开(公告)号：EP2459593A2
公开(公告)日：2012-06-06
申请号：EP10735014.2
申请日：2010-07-27
申请人： Glaxo Group Limited
发明人： DE WILDT, Rudolf Maria , DIMECH, Caroline J , HOLMES, Steve , STOOP, Adriaan Allart
IPC分类号： C07K16/28 , C07K16/40 , A61P27/02 , A61P43/00
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.

6. 发明授权

EP2493504B1 STABLE ANTI-TNFR1 POLYPEPTIDES, ANTIBODY VARIABLE DOMAINS AND ANTAGONISTS 有权
标题翻译：稳定的防TNFR1多肽，抗体可变结构域和拮抗剂
公开(公告)号：EP2493504B1
公开(公告)日：2015-10-07
申请号：EP10774177.9
申请日：2010-10-25
申请人： Glaxo Group Limited
发明人： DE SILVA, Inusha , SEPP, Armin , STOOP, Adriaan Allart
IPC分类号： A61K39/395 , C07K16/18 , C07K16/28 , C07K16/46
CPC分类号： C07K16/2866 , A61K39/39591 , C07K16/18 , C07K16/2878 , C07K2317/21 , C07K2317/31 , C07K2317/569 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/00

7. 发明公开

EP2493504A1 STABLE ANTI-TNFR1 POLYPEPTIDES, ANTIBODY VARIABLE DOMAINS&ANTAGONISTS 有权
标题翻译：稳定的防TNFR1多肽，抗体可变结构域和拮抗剂
公开(公告)号：EP2493504A1
公开(公告)日：2012-09-05
申请号：EP10774177.9
申请日：2010-10-25
申请人： Glaxo Group Limited
发明人： DE SILVA, Inusha , SEPP, Armin , STOOP, Adriaan Allart
IPC分类号： A61K39/395 , C07K16/18 , C07K16/28 , C07K16/46
CPC分类号： C07K16/2866 , A61K39/39591 , C07K16/18 , C07K16/2878 , C07K2317/21 , C07K2317/31 , C07K2317/569 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/00
摘要： The invention relates to storage-stable anti-TNFR1 antibody single variable domains (d Abs), antagonists and multispecific ligands, as well as methods and uses of these. The anti-TNFR1 polypeptides, antibody single variable domains (d Abs), antagonists and multispecific ligands are useful for treating and/or preventing inflammatory disease, such as arthritis or COPD, as well as for pulmonary administration, oral administration, delivery to the lung and delivery to the GI tract of a patient.

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