公开(公告)号：US20220395504A1

公开(公告)日：2022-12-15

申请号：US17363878

申请日：2021-06-30

Applicant: Amgen Inc.

Inventor： John Gordon ALLEN ,  Jennifer Rebecca ALLEN ,  Ana Elena MINATTI ,  Qiufen XUE ,  Ryan Paul WURZ ,  Christopher M. TEGLEY ,  Alexander J. PICKRELL ,  Thomas T. NGUYEN ,  Vu Van MA ,  Patricia LOPEZ ,  Longbin LIU ,  David John KOPECKY ,  Michael J. FROHN ,  Ning CHEN ,  Jian Jeffrey CHEN ,  Aaron C. SIEGMUND ,  Albert AMEGADZIE ,  Nuria A. TAMAYO ,  Shon BOOKER ,  Clifford GOODMAN ,  Mary WALTON ,  Nobuko NISHIMURA ,  Youngsook SHIN ,  Jonathan D. LOW ,  Victor J. CEE ,  Anthony B. REED ,  Hui-Ling WANG ,  Brian Alan LANMAN

IPC: A61K31/517 ,  A61P35/00 ,  A61K31/4985 ,  A61K39/395 ,  C07D403/04 ,  C07D471/04

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：US20200231601A1

公开(公告)日：2020-07-23

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 ,  C07D417/10 ,  A61P25/28

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：US20200207766A1

公开(公告)日：2020-07-02

申请号：US16817109

申请日：2020-03-12

Applicant: Amgen Inc.

Inventor： Brian Alan LANMAN ,  Shon BOOKER ,  Clifford GOODMAN ,  Anthony B. REED ,  Jonathan D. LOW ,  Hui-Ling WANG ,  Ning CHEN ,  Ana Elena MINATTI ,  Ryan WURZ ,  Victor J. CEE

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/519

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

公开(公告)号：US20190077801A1

公开(公告)日：2019-03-14

申请号：US16125359

申请日：2018-09-07

Applicant: Amgen Inc.

Inventor： Brian Alan LANMAN ,  Shon BOOKER ,  Clifford GOODMAN ,  Anthony B. REED ,  Jonathan D. LOW ,  Hui-Ling WANG ,  Ning CHEN ,  Ana Elena MINATTI ,  Ryan WURZ ,  Victor J. CEE

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/519

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：US20180222876A1

公开(公告)日：2018-08-09

申请号：US15749895

申请日：2016-08-04

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  James A. BROWN ,  Ning CHEN ,  Michael J. FROHN ,  Longbin LIU ,  Qingyian LIU ,  Liping H. PETTUS ,  Wenyuan QIAN ,  Corey M. REEVES ,  Aaron C. SIEGMUND

IPC: C07D279/08 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  C07D417/14 ,  C07D417/10 ,  C07D491/08 ,  C07F7/08 ,  C07D471/04 ,  C07D491/056 ,  C07D498/10 ,  C07D491/107

CPC classification number: C07D279/08 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D498/10 ,  C07F7/0812

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 of Formula I, independently, are defined herein. The invention 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, schizophrenia and other central nervous system conditions.

公开(公告)号：US20170035744A1

公开(公告)日：2017-02-09

申请号：US15298748

申请日：2016-10-20

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 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: A61K31/4439 ,  C07D239/30 ,  C07D241/18 ,  C07D213/61 ,  A61K31/695 ,  A61K31/444 ,  A61K31/497 ,  A61K31/437 ,  A61K31/501 ,  A61K45/06 ,  C07C311/13 ,  C07D241/12 ,  C07D239/34 ,  C07D295/16 ,  A61K31/506 ,  C07D239/26

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.