公开(公告)号：US20150023988A1

公开(公告)日：2015-01-22

申请号：US14207445

申请日：2014-03-12

Applicant: AMGEN INC.

Inventor： Justin K. MURRAY ,  Jerry Ryan HOLDER ,  Malgorzata WANSKA ,  Christopher M. TEGLEY ,  James R. FALSEY ,  Elizabeth M. DOHERTY ,  Leslie P. MIRANDA

IPC: A61K47/48 ,  C07K16/00 ,  A61K38/17 ,  C07K14/435

CPC classification number: A61K47/48438 ,  A61K38/00 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K14/43518 ,  C07K14/705 ,  C07K16/44

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160067347A1

公开(公告)日：2016-03-10

申请号：US14654501

申请日：2013-12-17

Applicant: AMGEN INC.

Inventor： Jerry Ryan HOLDER ,  Gayathri SWAMINATH ,  Leslie P. MIRANDA ,  Jennifer ARAL ,  Elizabeth M. DOHERTY ,  Thomas NIXEY

IPC: A61K47/48 ,  A61K38/08 ,  C07K7/08 ,  A61K38/10

CPC classification number: A61K47/48215 ,  A61K38/08 ,  A61K38/10 ,  A61K47/60 ,  A61K47/6811 ,  C07K7/08 ,  C07K14/47 ,  C07K14/503

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160024159A1

公开(公告)日：2016-01-28

申请号：US14773756

申请日：2014-03-12

Applicant: AMGEN INC

Inventor： 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: C07K14/435 ,  A61K38/17 ,  A61K47/48

CPC classification number: C07K14/43518 ,  A61K38/00 ,  A61K38/16 ,  A61K38/1709 ,  A61K38/1767 ,  A61K47/643 ,  A61K47/6817 ,  C07K14/435 ,  C07K14/46 ,  C07K14/47

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20140005198A1

公开(公告)日：2014-01-02

申请号：US14012861

申请日：2013-08-28

Applicant: AMGEN INC.

Inventor： Adrian L. SMITH ,  Elizabeth M. DOHERTY ,  Qi HUANG ,  Gang LIU

IPC: C07D487/04 ,  C07D473/00

CPC classification number: C07D487/04 ,  C07D473/00

Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节Raf激酶活性的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。 该化合物具有通式I，其中A1，A2，A3，A4，A5，A6，A7，A8，A9，键B，X，环Z1和Z2，R1和R3各自定义。 本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。