公开(公告)号：US20150329538A1

公开(公告)日：2015-11-19

申请号：US14380918

申请日：2013-02-27

Applicant: AMGEN INC.

Inventor： Victor CEE ,  Frank CHAVEZ, JR. ,  Jian J. CHEN ,  Essa Hu HARRINGTON ,  Bradley HERBERICH ,  Claire L.M. JACKSON ,  Brian A. LANMAN ,  Thomas T. NGUYEN ,  Mark H. NORMAN ,  Liping H. PETTUS ,  Anthony B. REED ,  Adrian L. SMITH ,  Nuria A. TAMAYO ,  Andrew TASKER ,  Hui-Ling WANG ,  Bin WU ,  Ryan WURZ

IPC: C07D471/04 ,  C07D401/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D487/04

Abstract: The invention relates to amide-containing compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Abstract translation: 本发明涉及式（1）的含酰胺化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

公开(公告)号：US20210108212A1

公开(公告)日：2021-04-15

申请号：US17080771

申请日：2020-10-26

Applicant: AMGEN INC.

Inventor： 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: C12N15/113 ,  A61P9/10 ,  A61P3/06 ,  C07K16/28

Abstract: 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.

公开(公告)号：US20190309306A1

公开(公告)日：2019-10-10

申请号：US16328221

申请日：2017-08-25

Applicant: AMGEN INC.

Inventor： 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: C12N15/113 ,  A61P3/06 ,  A61P9/10 ,  C07K16/28

Abstract: 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.

公开(公告)号：US20230078200A1

公开(公告)日：2023-03-16

申请号：US17783232

申请日：2020-12-08

Applicant: AMGEN INC.

Inventor： Bin WU ,  Michael OLLMANN ,  Oliver HOMANN ,  Yuan CHENG

IPC: C12N15/113 ,  A61P9/10

Abstract: The present invention relates to RNAi constructs for reducing expression of the LPA gene, which encodes apolipoprotein(a), a component of lipoprotein(a) (Lp(a)) particles. Methods of using such RNAi constructs to treat or prevent cardiovascular disease, such as coronary artery disease, peripheral artery disease, stroke, and myocardial infarction, and to reduce serum Lp(a) levels are also described.

公开(公告)号：US20250121056A1

公开(公告)日：2025-04-17

申请号：US18982197

申请日：2024-12-16

Applicant: AMGEN INC.

Inventor： Yuan CHENG ,  Chawita NETIROJJANAKUL ,  Jerry Ryan HOLDER ,  Bin WU ,  James R. FALSEY ,  Bradley J. HERBERICH ,  Kelvin SHAM ,  Leslie P. MIRANDA ,  Shu-Chen LU ,  Murielle M. VENIANT-ELLISON ,  Shanaka STANISLAUS ,  Junming YIE ,  Jing XU

IPC: A61K39/395 ,  A61K47/68 ,  A61P3/10 ,  C07K16/28

Abstract: 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.

公开(公告)号：US20210154318A1

公开(公告)日：2021-05-27

申请号：US17151045

申请日：2021-01-15

Applicant: Amgen Inc.

Inventor： 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: A61K47/68 ,  A61P3/10 ,  C07K16/28 ,  A61K39/395

Abstract: 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.

公开(公告)号：US20180311372A1

公开(公告)日：2018-11-01

申请号：US15872841

申请日：2018-01-16

Applicant: AMGEN INC.

Inventor： 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: A61K47/68 ,  C07K16/28 ,  A61P3/10

CPC classification number: C07K16/28 ,  A61K39/395 ,  A61P3/10

Abstract: 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.

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。