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11. 发明申请

WO2015127158A1 METHODS, COMPOSITIONS AND KITS FOR CELL SPECIFIC MODULATION OF TARGET ANTIGENS 审中-公开
标题翻译：方法，组合物和用于细胞特异性调节靶抗原的试剂盒
公开(公告)号：WO2015127158A1
公开(公告)日：2015-08-27
申请号：PCT/US2015/016737
申请日：2015-02-20
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GROMADA, Jesper , SMITH, Eric , MURPHY, Andrew , PAPADOPOULOS, Nicholas , MARTIN, Joel , YANCOPOULOS, George , MACDONALD, Douglas , BUCKLER, David
IPC分类号： A61K39/00 , A61K39/395 , C07K16/02 , C07K16/30
CPC分类号： C07K16/32 , A61K39/39558 , A61K2039/507 , C07K16/28 , C07K16/2803 , C07K16/2818 , C07K16/283 , C07K16/2863 , C07K16/2866 , C07K16/2869 , C07K16/3069 , C07K2317/31 , C07K2317/622 , C07K2317/75
摘要： The present invention provides, inter alia, a method for cell-specific modulation of a target antigen. The method comprises contacting a target cell having the target antigen on the surface of the target cell with: (a) first multi-specific antigen-binding polypeptide comprising: (i) a cell-specific antigen binding domain (C1), (ii) a target antigen binding domain (T1); and (b) a second multi-specific antigen-binding polypeptide comprising: (i) a cell-specific antigen binding domain (C2), (ii) a target antigen binding domain (T2); wherein C1 and C2 interact with the same cell-specific antigen, and the cell-specific antigen and the target antigen are on the same target cell. Pharmaceutical compositions and kits thereof are also included in the present invention.
摘要翻译：本发明尤其提供了靶抗原的细胞特异性调节方法。该方法包括使靶细胞表面上具有目标抗原的靶细胞与（a）第一多特异性抗原结合多肽包含：（i）细胞特异性抗原结合结构域（C1），（ii）靶抗原结合结构域（T1）; （b）第二多特异性抗原结合多肽，其包含：（i）细胞特异性抗原结合结构域（C2），（ii）靶抗原结合结构域（T2）; 其中C1和C2与相同的细胞特异性抗原相互作用，细胞特异性抗原和靶抗原位于相同的靶细胞上。药物组合物及其试剂盒也包括在本发明中。

12. 发明申请

WO2019217591A1 ANTI-MSR1 ANTIBODIES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2019217591A1
公开(公告)日：2019-11-14
申请号：PCT/US2019/031383
申请日：2019-05-08
申请人： REGENERON PHARMACEUTICALS, INC. , KYRATSOUS, Christos , NITTOLI, Thomas , ZUMSTEG, Anna
发明人： KYRATSOUS, Christos , NITTOLI, Thomas , ZUMSTEG, Anna , GROMADA, Jesper , GUSAROVA, Viktoria , HAN, Amy , HAXHINASTO, Sokol , MURPHY, Andrew J. , OLSON, William , SLEEMAN, Matthew
IPC分类号： C07K16/28 , A61K47/68
摘要： Provided herein are antibodies and antigen-binding fragments that bind MSR1 and methods of use thereof. According to certain embodiments, the antibodies bind human MSR1 with high affinity. In certain embodiments, the antibodies bind MSR1 without blocking, or blocking less than 90%, of modified LDL binding to MSR1. In some embodiments, the antibodies bind cell surface expressed-MSR1 and are internalized. The antibodies of the invention may be fully human antibodies. The invention includes anti-MSR1 antibodies, or antigen-binding fragments thereof, conjugated to drugs or therapeutic compounds.

13. 发明申请

WO2019040471A9 METHODS OF TREATING UREA CYCLE DISORDERS BY INTERFERING WITH GLUCAGON RECEPTOR SIGNALING 审中-公开
公开(公告)号：WO2019040471A9
公开(公告)日：2019-02-28
申请号：PCT/US2018/047286
申请日：2018-08-21
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： OKAMOTO, Haruka , CHENG, Xiping , GROMADA, Jesper
IPC分类号： A61K38/26
摘要： Provided herein are methods of treating a subject with hyperammonemia or a urea cycle disorder. The methods comprise administering to a subject in need thereof a therapeutic amount of a glucagon signaling pathway inhibitor, such that ammonia levels are lowered or that amino acid metabolism enzymes are down-regulated, or a condition or disease characterized by hyperammonemia is mediated, or at least one symptom or complication associated with the condition or disease is alleviated or reduced in severity. The glucagon signaling pathway inhibitor can be a small molecule inhibitor of the signaling pathway, an antisense inhibitor of the signaling pathway, shRNA, siRNA, a GCG neutralizing monoclonal antibody, a GCGR antagonist, a peptide inhibitor of the signaling pathway, a DARPin, a Spiegelmer, an aptamer, engineered Fn type-III domains, etc. The therapeutic methods are useful for treating a human suffering from hyperammonemia or a urea cycle disorder.

14. 发明申请

WO2018094112A1 METHODS OF TREATING OBESITY WITH ANTI-ANGPTL8 ANTIBODIES 审中-公开
公开(公告)号：WO2018094112A1
公开(公告)日：2018-05-24
申请号：PCT/US2017/062103
申请日：2017-11-16
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GUSAROVA, Viktoria , GROMADA, Jesper , MURPHY, Andrew, J.
IPC分类号： C07K16/22 , A61K39/00 , A61P3/06
摘要： The present invention provides antibodies that bind to ANGPTL8 and methods of using the same. According to certain embodiments, the invention includes methods of using anti-ANGPTL8 antibodies that bind human ANGPTL8 with high affinity to treat obesity, reduce body fat, reduce body weight, increase energy expenditure, and increase HDL-C, in a subject.

15. 发明申请

WO2018044903A1 METHODS OF TREATING SEVERE INSULIN RESISTANCE BY INTERFERING WITH GLUCAGON RECEPTOR SIGNALING 审中-公开
标题翻译：干扰胰高血糖素受体信号通路干预治疗重度胰岛素抵抗的方法
公开(公告)号：WO2018044903A1
公开(公告)日：2018-03-08
申请号：PCT/US2017/049137
申请日：2017-08-29
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GROMADA, Jesper , OKAMOTO, Haruka , JASPERS, Stephen , HARP, Joyce
IPC分类号： A61K39/395 , A61K45/06 , C07K16/26 , C07K16/28 , A61P3/10
摘要： Provided herein are methods of treating a patient with severe insulin resistance. The methods comprise administering to a patient in need thereof a therapeutic amount of a GCG/GCGR signaling pathway inhibitor, such that blood glucose or beta-hydroxybutyrate levels are lowered or that the severe insulin resistance is mediated, or a condition or disease characterized by severe insulin resistance is mediated, or at least one symptom or complication associated with the condition or disease is alleviated or reduced in severity. The GCG/GCGR signaling pathway inhibitor can be a small molecule inhibitor of the signaling pathway, an antisense inhibitor of the signaling pathway, a GCG neutralizing monoclonal antibody, a GCGR antagonist, a peptide inhibitor of the signaling pathway, a DARPin, a Spiegelmer, an aptamer, engineered Fn type-III domains, etc. The therapeutic methods are useful for treating a human suffering from severe insulin resistance.
摘要翻译：本文提供治疗患有严重胰岛素抵抗的患者的方法。该方法包括向有需要的患者施用治疗量的GCG / GCGR信号传导通路抑制剂，从而降低血糖或β-羟基丁酸酯水平或者介导严重的胰岛素抵抗，或以严重为特征的病症或疾病介导胰岛素抵抗，或者至少一种与病症或疾病相关的症状或并发症在严重程度上得到缓解或减轻。 GCG / GCGR信号传导途径抑制剂可以是信号传导途径的小分子抑制剂，信号传导途径的反义抑制剂，GCG中和性单克隆抗体，GCGR拮抗剂，信号传导途径的肽抑制剂，DARPin，Spiegelmer，适体，工程Fn III型结构域等。治疗方法可用于治疗患有严重胰岛素抵抗的人。

16. 发明申请

WO2017136712A1 NON-HUMAN ANIMALS HAVING AN ENGINEERED ANGPTL8 GENE 审中-公开
标题翻译：具有工程ANGPTL8基因的非人动物
公开(公告)号：WO2017136712A1
公开(公告)日：2017-08-10
申请号：PCT/US2017/016487
申请日：2017-02-03
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GUSAROVA, Viktoria , MURPHY, Andrew J. , GROMADA, Jesper , GUO, Dayong
IPC分类号： C07K14/515 , A01K67/027 , A61K49/00 , C07K16/22 , A61K39/00
CPC分类号： A01K67/0278 , A01K2207/15 , A01K2217/072 , A01K2217/206 , A01K2227/10 , A01K2227/105 , A01K2267/0306 , A01K2267/0375 , A61K49/0008 , A61K2039/505 , C07K14/515 , C07K16/22
摘要： Non-human animals, and methods and compositions for making and using the same, are provided, wherein said non-human animals comprise a humanization of an Angiopoietin- like protein 8 ( ANGPTL8 ) gene. Said non-human animals may be described, in some embodiments, as having a genetic modification to an endogenous ANGPTL8 locus so that said non-human animals express a human ANGPTL8 polypeptide.
摘要翻译：提供了非人动物以及用于制备和使用它们的方法和组合物，其中所述非人动物包含血管生成素样蛋白8（ANGPTL8）的人源化，基因）。在一些实施方案中，所述非人动物可被描述为具有对内源ANGPTL8基因座的遗传修饰，使得所述非人动物表达人ANGPTL8多肽。

17. 发明申请

WO2015148708A1 FGF21 RECEPTOR AGONISTS AND USES THEREOF 审中-公开
标题翻译： FGF21受体激动剂及其用途
公开(公告)号：WO2015148708A1
公开(公告)日：2015-10-01
申请号：PCT/US2015/022548
申请日：2015-03-25
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： YANCOPOULOS, George D. , MURPHY, Andrew J. , GROMADA, Jesper , BUCKLER, David R. , KANG, Kihwa
IPC分类号： C07K16/22 , C07K16/28
CPC分类号： C07K16/2863 , A61K38/00 , A61K2039/505 , C07K14/50 , C07K16/22 , C07K16/40 , C07K2317/31 , C07K2317/33 , C07K2317/52 , C07K2317/524 , C07K2317/526 , C07K2317/56 , C07K2317/565 , C07K2317/622 , C07K2317/75 , C07K2317/92 , C07K2319/75 , C12Y302/01031
摘要： The present invention provides agonists of FGF21 signaling. In particular, the present invention provides FGF21 receptor (FGF21R) agonists that are capable of simultaneously binding βKlotho (KLB) and/or FGFR1c to mimic the signaling activity of FGF21. The present invention also provides anti-FGF21 and anti-KLB/FGFR1c antibodies and antigen-binding fragments thereof. Also provided are methods of treating various metabolic disorders by administering the FGF21R agonists and/or anti-FGF21 antibodies to a subject in need thereof.
摘要翻译：本发明提供FGF21信号传导的激动剂。特别地，本发明提供能够同时结合βKlotho（KLB）和/或FGFR1c以模拟FGF21的信号传导活性的FGF21受体（FGF21R）激动剂。本发明还提供抗FGF21和抗KLB / FGFR1c抗体及其抗原结合片段。还提供了通过向有需要的受试者施用FGF21R激动剂和/或抗FGF21抗体来治疗各种代谢紊乱的方法。

18. 发明申请

WO2020106780A1 BIS-OCTAHYDROPHENANTHRENE CARBOXAMIDE DERIVATIVES AND PROTEIN CONJUGATES THEREOF FOR USE AS LXR AGONISTS 审中-公开
公开(公告)号：WO2020106780A1
公开(公告)日：2020-05-28
申请号：PCT/US2019/062302
申请日：2019-11-19
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GROMADA, Jesper , GUSAROVA, Viktoria , HAN, Amy , HAXHINASTO, Sokol , MURPHY, Andrew, J. , OLSON, William , SLEEMAN, Matthew
IPC分类号： C07D233/64 , A61K47/68 , A61K47/69 , C07C233/90 , C07D249/16 , C07H17/02 , C07K5/06 , C07K5/08
摘要： Provided herein are compounds or payloads, linker-payloads, antibody-drug conjugates, and compositions, and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.

19. 发明申请

WO2020086406A2 ANTI-NPR1 ANTIBODIES AND USES THEREOF 审中-公开
公开(公告)号：WO2020086406A2
公开(公告)日：2020-04-30
申请号：PCT/US2019/057033
申请日：2019-10-18
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： DUNN, Michael , SU, Jia , MASTAITIS, Jason , GROMADA, Jesper , MORTON, Lori
IPC分类号： C07K16/28 , A61K39/395 , A61P9/12
摘要： The present invention provides monoclonal antibodies that bind to the natriuretic peptide receptor 1 (NPR1) protein, and methods of use thereof. In various embodiments of the invention, the antibodies are fully human antibodies that bind to NPR1. In some embodiments, the antibodies of the invention are useful for activating NPR1 activity, thus providing a means of treating or preventing a disease, disorder or condition associated with NPR1 in humans.

20. 发明申请

WO2019126194A1 ANGPTL8 ASSAY AND USES THEREOF 审中-公开
公开(公告)号：WO2019126194A1
公开(公告)日：2019-06-27
申请号：PCT/US2018/066266
申请日：2018-12-18
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： GUSAROVA, Viktoria , GROMADA, Jesper , MURPHY, Andrew J.
IPC分类号： G01N33/74
CPC分类号： G01N33/74 , G01N2800/044
摘要： The present invention provides ELISA-based methods for detecting and/or quantifying ANGPTL8 in biological samples using anti-ANGPTL8 antibodies.

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