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1. 发明申请

US20160067347A1 APJ RECEPTOR AGONISTS AND USES THEREOF 审中-公开
标题翻译： APJ受体激素及其用途
公开(公告)号：US20160067347A1
公开(公告)日：2016-03-10
申请号：US14654501
申请日：2013-12-17
申请人： AMGEN INC.
发明人： Jerry Ryan HOLDER , Gayathri SWAMINATH , Leslie P. MIRANDA , Jennifer ARAL , Elizabeth M. DOHERTY , Thomas NIXEY
IPC分类号： A61K47/48 , A61K38/08 , C07K7/08 , A61K38/10
CPC分类号： A61K47/48215 , A61K38/08 , A61K38/10 , A61K47/60 , A61K47/6811 , C07K7/08 , C07K14/47 , C07K14/503
摘要： The application is directed to APJ receptor agonist analogs having increased stability relative to the wild type apelin-13 and methods of using the agonist analogs. The analogs can be used, inter alia, in cardiac disorders such as heart failure.
摘要翻译：该应用涉及相对于野生型apelin-13具有增加的稳定性的APJ受体激动剂类似物和使用激动剂类似物的方法。类似物尤其可用于心脏病，例如心力衰竭。

2. 发明申请

US20160000932A1 MODIFIED Fc MOLECULES 审中-公开
标题翻译：改良的Fc分子
公开(公告)号：US20160000932A1
公开(公告)日：2016-01-07
申请号：US14796502
申请日：2015-07-10
申请人： AMGEN INC.
发明人： Colin V. GEGG , Kenneth W. WALKER , Leslie P. MIRANDA , Fei XIONG
IPC分类号： A61K47/48 , C07K16/00 , A61K38/02 , C07K17/00
CPC分类号： A61K38/02 , A61K47/60 , A61K47/68 , A61K47/6817 , C07K16/00 , C07K17/00 , C07K2317/40 , C07K2317/52
摘要： Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.
摘要翻译：公开了制备药理活性化合物的方法，其中选择Fc结构域序列的至少一个内部缀合位点，其适于通过定义的缀合化学通过氨基酸残基的侧链与另外的功能部分缀合在共轭位点。用于缀合的合适的氨基酸残基可以在缀合位点处的天然Fc结构域中存在，或者可以通过插入（即天然Fc结构域中的氨基酸之间）或替换（即，除去氨基酸并用不同的氨基酸）。在后一种情况下，加入的氨基酸数不需要对应于从先前存在的Fc结构域去除的氨基酸的数目。该技术可用于生产含有它们的物质和药物组合物的有用组合物。还公开了编码本发明组合物的DNA，含有该DNA的表达载体和含有表达载体的宿主细胞。

3. 发明申请

US20210154318A1 METHOD OF TREATING OR AMELIORATING METABOLIC DISORDERS USING GLP-1 RECEPTOR AGONISTS CONJUGATED TO ANTAGONISTS FOR GASTRIC INHIBITORY PEPTIDE RECEPTOR (GIPR) 有权
公开(公告)号：US20210154318A1
公开(公告)日：2021-05-27
申请号：US17151045
申请日：2021-01-15
申请人： Amgen Inc.
发明人： Yuan CHENG , Chawita NETIROJJANAKUL , Jerry Ryan HOLDER , Bin WU , James R. FALSEY , Bradley J. HERBERICH , Kelvin SHAM , Leslie P. MIRANDA , Shu-Chen LU , Murielle VENIENT-ELLISON , Shanaka STANISLAUS , Junming YIE , Jing XU
IPC分类号： A61K47/68 , A61P3/10 , C07K16/28 , A61K39/395
摘要： Methods of treating metabolic diseases and disorders using a composition comprising an antigen binding protein specific for the GIPR polypeptide conjugated to a GLP-1 receptor agonist are provided. In various embodiments the metabolic disease or disorder is type 2 diabetes, obesity, dyslipidemia, elevated glucose levels, elevated insulin levels and diabetic nephropathy. In certain embodiments the composition comprises an antibody or functional fragment thereof comprising a cysteine at one or more conjugation site(s) wherein the GLP-1 receptor agonist is conjugated to the antibody or functional fragment thereof through the side-chain of the cysteine residue.

4. 发明申请

US20160304570A1 POTENT AND SELECTIVE INHIBITORS OF NAV1.3 AND NAV1.7 有权
标题翻译： NAV1.3和NAV1.7的POTENT和选择性抑制剂
公开(公告)号：US20160304570A1
公开(公告)日：2016-10-20
申请号：US15134305
申请日：2016-04-20
申请人： AMGEN INC.
发明人： Justin K. MURRAY , Leslie P. MIRANDA , Stefan I. MCDONOUGH
IPC分类号： C07K14/435 , C07K16/44 , A61K47/48
CPC分类号： C07K14/43518 , A61K38/00 , A61K47/60 , A61K47/68 , A61K47/6817 , C07K14/00 , C07K16/44 , C07K2317/35 , C07K2317/76 , C07K2319/30
摘要： Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7 and/or NaV1.3. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.
摘要翻译：公开了包含分离的多肽的物质组合物，其是外周受限制的NaV1.7抑制剂。在一些公开的实施方案中，分离的多肽是NaV1.7和/或NaV1.3的抑制剂。其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。还公开了治疗或预防疼痛的方法。

5. 发明申请

US20150023988A1 POTENT AND SELECTIVE INHIBITORS OF NAV1.7 有权
标题翻译： NAV1.7的POTENT和选择性抑制剂
公开(公告)号：US20150023988A1
公开(公告)日：2015-01-22
申请号：US14207445
申请日：2014-03-12
申请人： AMGEN INC.
发明人： Justin K. MURRAY , Jerry Ryan HOLDER , Malgorzata WANSKA , Christopher M. TEGLEY , James R. FALSEY , Elizabeth M. DOHERTY , Leslie P. MIRANDA
IPC分类号： A61K47/48 , C07K16/00 , A61K38/17 , C07K14/435
CPC分类号： A61K47/48438 , A61K38/00 , A61K47/60 , A61K47/68 , A61K47/6817 , C07K14/43518 , C07K14/705 , C07K16/44
摘要： Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Nav1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Nav1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.
摘要翻译：公开了包含分离的多肽的物质组合物，其是外周限制的Nav1.7抑制剂。在一些公开的实施方案中，分离的多肽是Nav1.7的抑制剂。其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。还公开了治疗或预防疼痛的方法。

6. 发明申请

US20210261619A1 APELIN POLYPEPTIDES 有权
公开(公告)号：US20210261619A1
公开(公告)日：2021-08-26
申请号：US17160819
申请日：2021-01-28
申请人： AMGEN INC.
发明人： Jerry Ryan HOLDER , Gayathri SWAMINATH , Michael J. FROHN , Brian Alan LANMAN , Anthony B. REED , Leslie P. MIRANDA , John Gordon ALLEN , Alexander J. PICKRELL , Aaron C. SIEGMUND , Lewis D. PENNINGTON , Bryant YANG
IPC分类号： C07K7/08 , C07K14/47 , A61K47/54 , A61K47/60 , A61K38/10
摘要： The invention provides modified apelin polypeptides having increased stability, circulating half-life, and/or potency relative to the native apelin-13 polypeptide. Compositions comprising the modified apelin polypeptides and methods of using the polypeptides for treating cardiac disorders, such as heart failure, are also disclosed.

7. 发明申请

US20180311372A1 METHOD OF TREATING OR AMELIORATING METABOLIC DISORDERS USING GLP-1 RECEPTOR AGONISTS CONJUGATED TO ANTAGONISTS FOR GASTRIC INHIBITORY PEPTIDE RECEPTOR (GIPR) 审中-公开
公开(公告)号：US20180311372A1
公开(公告)日：2018-11-01
申请号：US15872841
申请日：2018-01-16
申请人： AMGEN INC.
发明人： Yuan CHENG , Chawita NETIROJJANAKUL , Jerry Ryan HOLDER , Bin WU , James R. FALSEY , Bradley J. HERBERICH , Kelvin SHAM , Leslie P. MIRANDA , Shu-Chen LU , Murielle VENIANT-ELLISON , Shanaka STANISLAUS , Junming YIE , Jing XU
IPC分类号： A61K47/68 , C07K16/28 , A61P3/10
CPC分类号： C07K16/28 , A61K39/395 , A61P3/10
摘要： Methods of treating metabolic diseases and disorders using a composition comprising an antigen binding protein specific for the GIPR polypeptide conjugated to a GLP-1 receptor agonist are provided. In various embodiments the metabolic disease or disorder is type 2 diabetes, obesity, dyslipidemia, elevated glucose levels, elevated insulin levels and diabetic nephropathy. In certain embodiments the composition comprises an antibody or functional fragment thereof comprising a cysteine at one or more conjugation site(s) wherein the GLP-1 receptor agonist is conjugated to the antibody or functional fragment thereof through the side-chain of the cysteine residue.

8. 发明申请

US20160024159A1 POTENT AND SELECTIVE INHIBITORS OF NAV1.7 审中-公开
标题翻译： NAV1.7的POTENT和选择性抑制剂
公开(公告)号：US20160024159A1
公开(公告)日：2016-01-28
申请号：US14773756
申请日：2014-03-12
申请人： AMGEN INC
发明人： Justin K. MURRAY , Jerry Ryan HOLDER , Malgorzata WANSKA , Christopher M. TEGLEY , James R. FALSEY , Elizabeth M. DOHERTY , Leslie P. MIRANDA , Kaustav BISWAS , Bin WU , Kelvin SHAM , Jason C. LONG
IPC分类号： C07K14/435 , A61K38/17 , A61K47/48
CPC分类号： C07K14/43518 , A61K38/00 , A61K38/16 , A61K38/1709 , A61K38/1767 , A61K47/643 , A61K47/6817 , C07K14/435 , C07K14/46 , C07K14/47
摘要： Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.
摘要翻译：公开了包含分离的多肽的物质组合物，其是外周受限制的NaV1.7抑制剂。在一些公开的实施方案中，分离的多肽是NaV1.7的抑制剂。其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。还公开了治疗或预防疼痛的方法。

9. 发明申请

US20210395313A1 PEPTIDE PAC1 ANTAGONISTS 有权
公开(公告)号：US20210395313A1
公开(公告)日：2021-12-23
申请号：US16619874
申请日：2018-06-01
申请人： AMGEN INC.
发明人： Irwin CHEN , Su CHONG , Essa Hu HARRINGTON , Fang-Tsao HONG , Jason C. LONG , Leslie P. MIRANDA
IPC分类号： C07K14/00 , A61P25/06
摘要： Novel peptides that bind to human PAC1 are provided. These peptides that are antagonists of PAC1 are useful in a number of PAC1 related disorders, including the treatment and/or prevention of headache disorders, including migraine, such as acute migraine.

10. 发明申请

US20210108212A1 RNAi Constructs for Inhibiting ASGR1 Expression and Methods of Use Thereof 有权
公开(公告)号：US20210108212A1
公开(公告)日：2021-04-15
申请号：US17080771
申请日：2020-10-26
申请人： AMGEN INC.
发明人： Michael OLLMANN , Yang LI , Jun ZHANG , Kaustav BISWAS , Oliver HOMANN , Leslie P. MIRANDA , Justin K. MURRAY , Bin WU , Oh Kyu YOON , John Gordon ALLEN , Chawita NETIROJJANAKUL , Yuan CHENG
IPC分类号： C12N15/113 , A61P9/10 , A61P3/06 , C07K16/28
摘要： The present invention relates to RNAi constructs for reducing expression of the ASGR1 gene. Methods of using such RNAi constructs to treat or prevent cardiovascular disease, such as coronary artery disease and myocardial infarction, and to reduce serum non-HDL cholesterol levels are also described.

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