公开(公告)号：US11046680B1

公开(公告)日：2021-06-29

申请号：US16347910

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Xiaoqi Chen ,  Yinhong Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Jeffrey Deignan ,  Paul John Dransfield ,  Xiaohui Du ,  Zice Fu ,  James S. Harvey ,  Julie Anne Heath ,  Lars V. Heumann ,  Daniel B. Horne ,  Jonathan Houze ,  Matthew R. Kaller ,  Frank Kayser ,  Aarif Yusuf Khakoo ,  David J. Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Julio C. Medina ,  Jeffrey T. Mihalic ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Xiaodong Wang ,  Malgorzata Wanska ,  Kevin Yang ,  Wen-Chen Yeh

IPC: C07D417/14 ,  A61P9/00 ,  C07D401/14 ,  C07D403/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

公开(公告)号：US20170281625A1

公开(公告)日：2017-10-05

申请号：US15629567

申请日：2017-06-21

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Xiaoqi CHEN ,  Yinhong CHEN ,  Zice FU ,  Julie Anne HEATH ,  Daniel B. HORNE ,  Matthew R. KALLER ,  Aarif Yusuf KHAKOO ,  David John KOPECKY ,  Zhihua MA ,  Jeffrey T. MIHALIC ,  Gayathri SWAMINATH ,  Xiaodong WANG ,  Wen-Chen YEH

IPC: A61K31/506 ,  A61K45/06 ,  A61K31/497

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07C311/13 ,  C07D211/54 ,  C07D213/61 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D241/24 ,  C07D249/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.

公开(公告)号：US09656998B2

公开(公告)日：2017-05-23

申请号：US15298686

申请日：2016-10-20

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Xiaoqi Chen ,  Richard V. Connors ,  Jeffrey Deignan ,  Paul John Dransfield ,  Xiaohui Du ,  Zice Fu ,  Julie Anne Heath ,  Daniel B. Horne ,  Jonathan Houze ,  Matthew R. Kaller ,  David John Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Lawrence R. McGee ,  Julio C. Medina ,  Jeffrey T. Mihalic ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Xiaodong Wang ,  Kevin Yang ,  Mikkel V. Debenedetto ,  Robert P. Farrell ,  Simon J. Hedley ,  Ted C. Judd

IPC: C07D213/82 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K45/06 ,  C07B57/00 ,  C07B59/00 ,  C07D211/54 ,  C07D213/71 ,  C07D239/26 ,  C07D239/30 ,  C07D241/12 ,  C07D249/08 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/695

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07C311/13 ,  C07D211/54 ,  C07D213/61 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D241/24 ,  C07D249/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: Compounds of Formula V, salts thereof, tautomers thereof, and salts of the tautomers are useful intermediates in the synthesis of agonists of the APJ Receptor. Compounds of Formula V have the following structure: where the definitions of the variables are provided herein.

公开(公告)号：US09174992B2

公开(公告)日：2015-11-03

申请号：US13780557

申请日：2013-02-28

Applicant: Amgen Inc.

Inventor： Jennifer R. Allen ,  Albert Amegadzie ,  Kristin L. Andrews ,  James Brown ,  Jian J. Chen ,  Ning Chen ,  Essa Hu Harrington ,  Qingyian Liu ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Wenyuan Qian ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Chester Chenguang Yuan ,  Wenge Zhong

IPC: C07D419/14 ,  C07D419/12 ,  C07D487/04 ,  C07D498/04 ,  C07D473/00 ,  C07D471/04 ,  C07D513/04 ,  C07D417/12 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and 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, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.

Abstract translation: 式（I）的异双环化合物：或其药学上可接受的盐，互变异构体或立体异构体，以及含有它们的组合物，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，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症，亨廷顿舞蹈病等。

公开(公告)号：US11045484B2

公开(公告)日：2021-06-29

申请号：US16402589

申请日：2019-05-03

Applicant: Amgen Inc.

Inventor： Ryan Paul Wurz ,  Victor J. Cee ,  Albert Amegadzie ,  Ning Chen ,  Brian Alan Lanman ,  Michael D. Bartberger

IPC: A61K31/675 ,  A61P35/00 ,  A61K31/167 ,  A61K31/553 ,  C07K16/30 ,  A61K45/06

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US11021493B2

公开(公告)日：2021-06-01

申请号：US16466207

申请日：2017-12-13

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Matthew P. Bourbeau ,  James A. Brown ,  Ning Chen ,  Michael J. Frohn ,  Zice Fu ,  Longbin Liu ,  Qingyian Liu ,  Liping H. Pettus ,  Wenyuan Qian ,  Corey Reeves ,  Aaron C. Siegmund

IPC: C07D513/08 ,  A61P25/28 ,  C07D417/10

Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2′, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.

公开(公告)号：US20160340336A1

公开(公告)日：2016-11-24

申请号：US15158174

申请日：2016-05-18

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Xiaoqi Chen ,  Yinhong Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Jeffrey Deignan ,  Paul John Dransfield ,  Xiaohui Du ,  Zice Fu ,  Julie Anne Heath ,  Daniel B. Horne ,  Jonathan Houze ,  Matthew R. Kaller ,  Aarif Yusuf Khakoo ,  David John Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Lawrence R. McGee ,  Julio C. Medina ,  Jeffrey T. Mihalic ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Xiaodong Wang ,  Kevin Yang ,  Wen-Chen Yeh ,  Mikkel V. Debenedetto ,  Robert P. Farrell ,  Simon J. Hedley ,  Ted C. Judd ,  Frank Kayser

IPC: C07D401/14 ,  C07D213/82 ,  C07D241/24 ,  C07D239/30 ,  C07D239/26 ,  C07D401/04 ,  A61K31/4439 ,  A61K31/506 ,  C07D413/14 ,  C07B59/00 ,  A61K31/497 ,  A61K31/513 ,  C07D471/04 ,  A61K31/444 ,  C07D417/14 ,  C07B57/00 ,  C07D405/14 ,  A61K31/501 ,  C07D249/08 ,  C07D241/12 ,  C07D213/71 ,  C07D211/54 ,  A61K45/06

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07C311/13 ,  C07D211/54 ,  C07D213/61 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D241/24 ,  C07D249/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

Abstract translation: 其中在这里提供变量的定义。

公开(公告)号：US08759532B2

公开(公告)日：2014-06-24

申请号：US13676826

申请日：2012-11-14

Applicant: AMGEN Inc.

Inventor： Jennifer R. Allen ,  Kaustav Biswas ,  Frank Chavez, Jr. ,  Ning Chen ,  Frenel Fils De Morin ,  James R. Falsey ,  Michael J. Frohn ,  Paul E. Harrington ,  Daniel B. Home ,  Essa Hu Harrington ,  Matthew R. Kaller ,  Roxanne K. Kunz ,  Holger Monenschein ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Andreas Reichelt ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Kelvin Sham ,  Guomin Yao

IPC: C07D239/02 ,  A61K31/397

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00

Abstract: Pyridine and pyrimidine compounds, and 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, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 吡啶和嘧啶化合物，以及含有它们的组合物，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，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

公开(公告)号：US20250059179A1

公开(公告)日：2025-02-20

申请号：US18696948

申请日：2022-04-28

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Ryan Paul Wurz ,  Wei Zhao ,  Xiaofen Li ,  Michael M. Yamano ,  Yunxiao Li ,  Ning Chen ,  Sebastian Leth-Petersen ,  Kexue Li ,  Liping Pettus ,  Rene Rahimoff ,  Primali Vasundera Navaratne ,  Huan Rui

IPC: C07D417/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: (I) wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US11096939B2

公开(公告)日：2021-08-24

申请号：US16428163

申请日：2019-05-31

Applicant: Amgen Inc.

Inventor： Shon Booker ,  John Gordon Allen ,  Brian Alan Lanman ,  Ryan Paul Wurz ,  Ning Chen ,  Victor J. Cee ,  Patricia Lopez ,  Aaron C. Siegmund ,  Michael D. Bartberger

IPC: C07D471/04 ,  A61K31/497 ,  C07K16/28

Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.