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：US20210395313A1

公开(公告)日：2021-12-23

申请号：US16619874

申请日：2018-06-01

Applicant: AMGEN INC.

Inventor： Irwin CHEN ,  Su CHONG ,  Essa Hu HARRINGTON ,  Fang-Tsao HONG ,  Jason C. LONG ,  Leslie P. MIRANDA

IPC: C07K14/00 ,  A61P25/06

Abstract: 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.

公开(公告)号：US20220340911A1

公开(公告)日：2022-10-27

申请号：US17634708

申请日：2020-08-13

Applicant: AMGEN INC.

Inventor： Wei GU ,  Essa Hu HARRINGTON ,  Oliver HOMANN

IPC: C12N15/113 ,  C12N15/10 ,  A61K47/00

Abstract: The present invention relates to RNAi constructs for reducing expression of the SLC30A8 gene. Methods of using such RNAi constructs to treat or prevent disease, such as pre-diabetes or diabetes are also described.

公开(公告)号：US20160102075A1

公开(公告)日：2016-04-14

申请号：US14973491

申请日：2015-12-17

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Jian J. CHEN ,  Michael J. FROHN ,  Essa Hu HARRINGTON ,  Qingyian LIU ,  Alexander J. PICKRELL ,  Shannon RUMFELT ,  Robert M. RZASA ,  Wenge ZHONG

IPC: C07D401/14 ,  C07D409/14 ,  C07D403/14 ,  C07D491/107 ,  C07D487/10 ,  C07C53/18 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/08 ,  C07D487/08 ,  C07D471/04 ,  C07D491/056 ,  C07D513/04 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07C53/18 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D513/04

Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 式（I）的不饱和氮杂环化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，亨廷顿舞蹈病，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。