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1. 发明申请

WO2010053751A1 HIGH AFFINITY HUMAN ANTIBODIES TO HUMAN IL-4 RECEPTOR 审中-公开
标题翻译：人类IL-4受体的高亲和力人体抗体
公开(公告)号：WO2010053751A1
公开(公告)日：2010-05-14
申请号：PCT/US2009/062168
申请日：2009-10-27
申请人： REGENERON PHARMACEUTICALS, INC. , MARTIN, Joel, H. , HUANG, Tammy, T. , FAIRHURST, Jeanette, L. , PAPADOPOULOS, Nicholas, J.
发明人： MARTIN, Joel, H. , HUANG, Tammy, T. , FAIRHURST, Jeanette, L. , PAPADOPOULOS, Nicholas, J.
IPC分类号： C07K16/28 , A61P37/08
CPC分类号： C07K16/2866 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2317/21 , C07K2317/76 , C07K2317/92
摘要： An isolated human antibody or antibody fragment thereof which binds to human interleukin-4 receptor alpha (hlL-4Rα) with high affinity (K0), capable of blocking hlL-4 and hlL-13 activity.
摘要翻译：以高亲和力（K0）结合能够阻断hIL-4和hIL-13活性的人白细胞介素-4受体α（hIL-4Ra）的分离的人抗体或其抗体片段。

2. 发明申请

WO2014159595A3 HUMAN ANTIBODIES TO NAV1.7 审中-公开
公开(公告)号：WO2014159595A3
公开(公告)日：2014-10-02
申请号：PCT/US2014/024336
申请日：2014-03-12
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： MACDONALD, Lynn , MURPHY, Andrew, J. , PAPADOPOULOS, Nicholas, J. , STAHL, Neil , ALESSANDRI-HABER, Nicole
IPC分类号： C07K16/28 , A61K39/395
摘要： The present invention provides antibodies that bind to the human voltage gated sodium channel designated Nav1.7 and methods of using same. According to certain embodiments of the invention, the antibodies are fully human antibodies that bind to human Nav1.7 (hNav1.7). The antibodies of the invention are useful for the treatment of diseases and disorders associated with one or more Nav1.7 biological activities, including the treatment of acute or chronic pain conditions, or inflammatory conditions.

3. 发明申请

WO2008019144A2 THREAPEUTIC METHODS FOR TREATING VASCULAR EYE DISORDERS WITH DLL4 ANTAGONISTS 审中-公开
标题翻译：用DLL4拮抗剂治疗血管性眼病的药物治疗方法
公开(公告)号：WO2008019144A2
公开(公告)日：2008-02-14
申请号：PCT/US2007/017546
申请日：2007-08-07
申请人： REGENERON PHARMACEUTICALS, INC. , WIEGAND, Stanley, J. , PAPADOPOULOS, Nicholas, J. , LOBOV, Ivan, B.
发明人： WIEGAND, Stanley, J. , PAPADOPOULOS, Nicholas, J. , LOBOV, Ivan, B.
IPC分类号： A61K39/39
CPC分类号： C07K16/2863 , A61K38/1709 , A61K2039/505 , C07K2317/76 , C07K2319/30
摘要： A therapeutic method for treating ischemic or vascular disorders by administering an agent capable of inhibiting human delta-like ligand 4 (DII4) activity to a subject in need thereof. Preferably, the agent is an anti-DII4 antibody or antibody fragment capable of inhibiting the binding of DII4 to a Notch receptor. In one embodiment, the ischemic or vascular disorder is ischemic injury, cerebral ischemia, cardiac ischemia, ischemic conditions affecting the limbs and other organs or tissues, arteriovenous malformations, wound healing, organ or tissue transplantation, placental insufficiency, arterial narrowing and occlusion, atherosclerosis, and systemic or pulmonary hypertension. In another embodiment, the disease treated is an eye disease or condition such as retinopathy of prematurity, ischemic retinopathy, retinal vein or artery occlusion, diabetic retinopathy, choroidal neovascularization, age related macular degeneration, corneal neovascularization, neovascular glaucoma or corneal transplantation.
摘要翻译：通过向需要的受试者施用能够抑制人类δ-样配体4（DII4）活性的试剂来治疗局部缺血或血管病症的治疗方法。优选地，该药剂是能够抑制Dll4与Notch受体结合的抗Dll4抗体或抗体片段。在一个实施方案中，缺血性或血管病症为局部缺血性损伤，脑缺血，心脏局部缺血，影响肢体和其他器官或组织的缺血性病症，动静脉畸形，伤口愈合，器官或组织移植，胎盘功能不全，动脉狭窄和闭塞，动脉粥样硬化，全身性或肺动脉高压。在另一个实施方案中，所治疗的疾病是眼疾或病症，例如早产儿视网膜病，缺血性视网膜病，视网膜静脉或动脉闭塞，糖尿病性视网膜病，脉络膜新血管生成，年龄相关性黄斑变性，角膜新血管生成，新生血管性青光眼或角膜移植。 p>

4. 发明申请

WO2015112800A1 HUMAN ANTIBODIES TO PD-1 审中-公开
标题翻译：人体抗PD-1抗体
公开(公告)号：WO2015112800A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/012589
申请日：2015-01-23
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： PAPADOPOULOS, Nicholas, J. , MURPHY, Andrew, J. , THURSTON, Gavin , IOFFE, Ella , BUROVA, Elena
IPC分类号： C07K16/28
CPC分类号： A61N5/10 , A61K39/3955 , A61K45/06 , A61K2039/505 , A61K2039/545 , C07K16/2818 , C07K16/2827 , C07K2317/21 , C07K2317/31 , C07K2317/76 , C07K2317/92 , A61K2300/00
摘要： The present invention provides antibodies that bind to the T-cell co-inhibitor programmed death- 1 (PD-1 ) protein, and methods of use. In various embodiments of the invention, the antibodies are fully human antibodies that bind to PD-1. In certain embodiments, the present invention provides multi-specific antigen-binding molecules comprising a first binding specificity that binds to PD-1 and a second binding specificity that binds to an autoimmune tissue antigen, another T- cell co-inhibitor, an Fc receptor, or a T-cell receptor. In some embodiments, the antibodies of the invention are useful for inhibiting or neutralizing PD-1 activity, thus providing a means of treating a disease or disorder such as cancer or a chronic viral infection. In other embodiments, the antibodies are useful for enhancing or stimulating PD-1 activity, thus providing a means of treating, for example, an autoimmune disease or disorder.
摘要翻译：本发明提供结合T细胞共抑制剂程序性死亡-1（PD-1）蛋白的抗体及其使用方法。在本发明的各种实施方案中，抗体是与PD-1结合的完全人抗体。在某些实施方案中，本发明提供多特异性抗原结合分子，其包含结合PD-1的第一结合特异性和结合自身免疫组织抗原的第二结合特异性，另一T细胞共抑制剂，Fc受体，或T细胞受体。在一些实施方案中，本发明的抗体可用于抑制或中和PD-1活性，从而提供治疗诸如癌症或慢性病毒感染的疾病或病症的方法。在其它实施方案中，抗体可用于增强或刺激PD-1活性，从而提供治疗例如自身免疫疾病或病症的方法。

5. 发明申请

WO2008054606A3 HIGH AFFINITY HUMAN ANTIBODIES TO HUMAN IL-4 RECEPTOR 审中-公开
公开(公告)号：WO2008054606A3
公开(公告)日：2008-05-08
申请号：PCT/US2007/021210
申请日：2007-10-02
申请人： REGENERON PHARMACEUTICALS, INC. , STEVENS, Sean , HUANG, Tammy, T. , MARTIN, Joel, H. , FAIRHURST, Jeanette, L. , RAFIQUE, Ashique , TORRES, Marcela , POBURSKY, Kevin, J. , LEIDICH, Raymond, W. , WINDSOR, Joan, A. , MIKULKA, Warren, R. , AHRENS, Diana, M. , SHI, Ergang , PAPADOPOULOS, Nicholas, J.
发明人： STEVENS, Sean , HUANG, Tammy, T. , MARTIN, Joel, H. , FAIRHURST, Jeanette, L. , RAFIQUE, Ashique , TORRES, Marcela , POBURSKY, Kevin, J. , LEIDICH, Raymond, W. , WINDSOR, Joan, A. , MIKULKA, Warren, R. , AHRENS, Diana, M. , SHI, Ergang , PAPADOPOULOS, Nicholas, J.
IPC分类号： C07K16/28 , C12N15/13 , C12N5/12 , A61K39/395 , A61P37/00
摘要： An isolated human antibody or antibody fragment thereof which binds to human interleukin-4 receptor alpha (hlL-4Rα) with an affinity constant (K0) of less than 200 pM, as measured by surface plasmon resonance.

6. 发明申请

WO2005000895A2 VEGF TRAPS AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译： VEGF TRAPS及其治疗用途
公开(公告)号：WO2005000895A2
公开(公告)日：2005-01-06
申请号：PCT/US2004/021059
申请日：2004-06-29
申请人： REGENERON PHARMACEUTICALS, INC. , DALY, Thomas, J. , FANDL, James, P. , PAPADOPOULOS, Nicholas, J.
发明人： DALY, Thomas, J. , FANDL, James, P. , PAPADOPOULOS, Nicholas, J.
IPC分类号： C07K14/71
CPC分类号： C07K14/71 , A61K38/00 , C07K2319/00
摘要： Nucleic acid molecules and multimeric proteins capable of binding vascular endothelial growth factor (VEGF). VEGF traps are disclosed which are therapeutically useful for treating VEGF-associated conditions and diseases, and are specifically designed for local administration to specific organs, tissues, and/or cells.
摘要翻译：核酸分子和能够结合血管内皮生长因子（VEGF）的多聚体蛋白质。公开了VEGF治疗用于治疗VEGF相关病症和疾病的捕获剂，并且特别设计用于局部施用于特定器官，组织和/或细胞。

7. 发明申请

WO2014152195A1 IL-33 ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译： IL-33拮抗剂及其用途
公开(公告)号：WO2014152195A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027058
申请日：2014-03-14
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： MURPHY, Andrew, J. , PAPADOPOULOS, Nicholas, J. , ORENGO, Jamie
IPC分类号： A61K38/17 , C07K14/715
CPC分类号： C07K14/7155 , A61K38/00 , A61K39/3955 , A61K45/06 , C07K2319/30 , C07K2319/32 , C07K2319/735
摘要： The present invention provides interleukin-33 (IL-33) antagonists comprising one or more IL-33-binding domains and one or more multimerizing domains and methods of using the same. According to certain embodiments of the invention, the IL-33-binding domains can comprise anIL-33-binding portion of an ST2 protein and/or an extracellular portion of an I L-1 RAcP protein. The IL-33 antagonists of the invention are useful for the treatment of diseases and disorders associated with IL-33 signaling and/or IL-33 cellular expression, such as infectious diseases, inflammatory diseases, allergic diseases and fibrotic diseases.
摘要翻译：本发明提供包含一个或多个IL-33结合结构域和一个或多个多聚化结构域的白细胞介素-33（IL-33）拮抗剂及其使用方法。根据本发明的某些实施方案，IL-33结合结构域可以包含ST2蛋白的IL-33结合部分和/或I L-1 RAcP蛋白的细胞外部分。本发明的IL-33拮抗剂可用于治疗与IL-33信号传导和/或IL-33细胞表达相关的疾病和病症，例如感染性疾病，炎性疾病，过敏性疾病和纤维化疾病。

8. 发明申请

WO2014047231A1 ANTI-CD3 ANTIBODIES, BISPECIFIC ANTIGEN-BINDING MOLECULES THAT BIND CD3 AND CD20, AND USES THEREOF 审中-公开
标题翻译：抗CD3抗体，结合CD3和CD20的双重抗原结合分子及其用途
公开(公告)号：WO2014047231A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060511
申请日：2013-09-19
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： SMITH, Eric , PAPADOPOULOS, Nicholas, J.
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00
CPC分类号： C07K16/2809 , A61K2039/505 , C07K16/2887 , C07K2317/21 , C07K2317/31 , C07K2317/33 , C07K2317/35 , C07K2317/734 , C07K2317/74 , C07K2317/92
摘要： The present invention provides antibodies that bind to CD3 and methods of using the same. According to certain embodiments, the antibodies of the invention bind human CD3 with high affinity and induce human T cell proliferation. The invention includes antibodies that bind CD3 and induce T cell-mediated killing of tumor cells. According to certain embodiments, the present invention provides bispecific antigen-binding molecules comprising a first antigen-binding domain that specifically binds human CD3, and a second antigen-binding molecule that specifically binds human CD20. In certain embodiments, the bispecific antigen-binding molecules of the present invention are capable of inhibiting the growth of B-cell tumors expressing CD20. The antibodies and bispecific antigen-binding molecules of the invention are useful for the treatment of diseases and disorders in which an upregulated or induced targeted immune response is desired and/or therapeutically beneficial. For example, the antibodies of the invention are useful for the treatment of various cancers as well as other CD20-related diseases and disorders.
摘要翻译：本发明提供了结合CD3的抗体及其使用方法。根据某些实施方案，本发明的抗体以高亲和力结合人CD3，并诱导人T细胞增殖。本发明包括结合CD3并诱导T细胞介导的杀伤肿瘤细胞的抗体。根据某些实施方案，本发明提供包含特异性结合人CD3的第一抗原结合结构域和特异性结合人CD20的第二抗原结合分子的双特异性抗原结合分子。在某些实施方案中，本发明的双特异性抗原结合分子能够抑制表达CD20的B细胞肿瘤的生长。本发明的抗体和双特异性抗原结合分子可用于治疗其中期望和/或治疗有益的上调或诱导的靶向免疫应答的疾病和病症。例如，本发明的抗体可用于治疗各种癌症以及其它与CD20相关的疾病和病症。

9. 发明申请

WO2014028354A1 ANTI-PCSK9 ANTIBODIES WITH PH-DEPENDENT BINDING CHARACTERISTICS 审中-公开
标题翻译：具有PH依赖性结合特征的抗PCSK9抗体
公开(公告)号：WO2014028354A1
公开(公告)日：2014-02-20
申请号：PCT/US2013/054456
申请日：2013-08-12
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： YANCOPOULOS, George, D. , PAPADOPOULOS, Nicholas, J. , MURPHY, Andrew, J. , STAHL, Neil
IPC分类号： C07K16/40 , A61K39/395 , A61P3/06
CPC分类号： C07K16/40 , A61K2039/505 , C07K2317/21 , C07K2317/565 , C07K2317/76 , C07K2317/92 , C07K2317/94
摘要： The present disclosure provides antibodies and antigen-binding fragments thereof that specifically bind proprotein convertase subtilisin/kexin-9 (PCSK9) with greater affinity at neutral pH than at acidic pH. The antibodies disclosed herein may possess one or more amino acid changes as compared to antibodies that do not exhibit pH-dependent binding properties. For example, the present disclosure includes anti-PCSK9 antibodies which possess one or more histidine substitutions in one or more complementarity determining regions. The antibodies disclosed herein, with pH-dependent binding properties, remain in circulation and exhibit cholesterol lowering activity for prolonged periods of time in animal subjects as compared to anti-PCSK9 antibodies that do not exhibit pH-dependent binding properties. The antibodies disclosed herein are therefore useful for treating diseases and disorders related to elevated HDL cholesterol, wherein the antibodiesdisclosed herein can be administered to a patient at a lower dose and/or with less frequent dosing as compared to antibodies that do not exhibit pH- dependent binding properties.
摘要翻译：本公开提供了在中性pH下比在酸性pH下以更高的亲和力特异性结合前蛋白转化酶枯草杆菌蛋白酶/ kexin-9（PCSK9）的抗体及其抗原结合片段。与不显示pH依赖性结合特性的抗体相比，本文公开的抗体可具有一个或多个氨基酸变化。例如，本公开内容包括在一个或多个互补决定区域中具有一个或多个组氨酸取代的抗PCSK9抗体。与不具有pH依赖性结合性质的抗PCSK9抗体相比，具有pH依赖性结合特性的本文公开的抗体在动物受试者中保持循环并显示长时间的胆固醇降低活性。因此，本文公开的抗体可用于治疗与升高的HDL胆固醇相关的疾病和病症，其中本文所公开的抗体可以以不显示pH依赖性的抗体与较低剂量和/或以较不频繁的给药相比施用于患者绑定属性。

10. 发明申请

WO2008076379A8 HUMAN ANTIBODIES TO HUMAN DELTA LIKE LIGAND 4 审中-公开
公开(公告)号：WO2008076379A8
公开(公告)日：2008-06-26
申请号：PCT/US2007/025653
申请日：2007-12-14
申请人： REGENERON PHARMACEUTICALS, INC. , PAPADOPOULOS, Nicholas, J. , MARTIN, Joel, H. , SMITH, Eric , NOGUERA-TROISE, Irene , THURSTON, Gavin
发明人： PAPADOPOULOS, Nicholas, J. , MARTIN, Joel, H. , SMITH, Eric , NOGUERA-TROISE, Irene , THURSTON, Gavin
IPC分类号： C07K16/18 , A61K39/395 , A61P35/00
摘要： An isolated human antibody or a fragment of a human antibody which specifically binds to human delta-like ligand 4 (hDII4) and blocks hDII4 binding to a Notch receptor. The human anti- hDII4 antibody or antibody fragment binds hDII4 with an affinity of ≤ 500 pM, as measured by surface plasmon resonance.

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