公开(公告)号：US11766436B2

公开(公告)日：2023-09-26

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

CPC classification number: A61K31/517 ,  A61K31/4985 ,  A61K39/39558 ,  A61P35/00 ,  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：US11285156B2

公开(公告)日：2022-03-29

申请号：US16438349

申请日：2019-06-11

Applicant: Amgen Inc.

Inventor： John Gordon Allen ,  Brian Alan Lanman ,  Jian Chen ,  Anthony B. Reed ,  Victor J. Cee ,  Longbin Liu ,  Patricia Lopez ,  Ryan Paul Wurz ,  Thomas T. Nguyen ,  Shon Booker ,  Jennifer Rebecca Allen ,  Margaret Chu-Moyer ,  Albert Amegadzie ,  Ning Chen ,  Clifford Goodman ,  Jonathan D. Low ,  Vu Van Ma ,  Ana Elena Minatti ,  Nobuko Nishimura ,  Alexander J. Pickrell ,  Hui-Ling Wang ,  Youngsook Shin ,  Aaron C. Siegmund ,  Kevin C. Yang ,  Nuria A. Tamayo ,  Mary Walton ,  Qiufen Xue

IPC: A61K31/497 ,  C07D241/04 ,  A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

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.

公开(公告)号：US11020395B2

公开(公告)日：2021-06-01

申请号：US16347942

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： Yinhong Chen ,  Paul John Dransfield ,  James S. Harvey ,  Julie Anne Heath ,  Jonathan Houze ,  Aarif Yusuf Khakoo ,  David J. Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Nobuko Nishimura ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Wen-Chen Yeh ,  Philip Dean Ramsden

IPC: A61K31/506 ,  A61P9/04 ,  C07D403/12 ,  C07D405/14 ,  C07D401/14 ,  C07D413/04 ,  C07D403/14 ,  A61K31/4439 ,  C07D401/04 ,  A61K31/4196 ,  C07D249/14

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: (I) (II) where the definitions of the variables are provided herein.

公开(公告)号：US09751864B2

公开(公告)日：2017-09-05

申请号：US15298434

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

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 preparing compounds of Formula VI, salts thereof, tautomers thereof, or salts of the tautomers include cyclizing compounds of Formula V, salts thereof, tautomers thereof, or salts of the tautomers. Compounds of Formula VI and Formula V have the following structures: where the definitions of the variables are provided herein.

公开(公告)号：US20140235642A1

公开(公告)日：2014-08-21

申请号：US14263143

申请日：2014-04-28

Applicant: AMGEN INC.

Inventor： James Brown ,  Jian J. Chen ,  Vijay Keshav Gore ,  Scott Harried ,  Daniel B. Horne ,  Matthew R. Kaller ,  Qingyian Liu ,  Holger Monenschein ,  Thomas T. Nguyen ,  Nobuko Nishimura ,  Wenge Zhong

IPC: C07D213/53 ,  C07D401/14 ,  C07C275/30 ,  C07D413/12 ,  C07D409/12 ,  C07D401/12 ,  C07D405/12

CPC classification number: C07D213/53 ,  C07C275/30 ,  C07D213/40 ,  C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

公开(公告)号：US20130079303A1

公开(公告)日：2013-03-28

申请号：US13681230

申请日：2012-11-19

Applicant: Amgen Inc.

Inventor： Kristin L. ANDREWS ,  Yunxin Y. Bo ,  Shon Booker ,  Victor J. Cee ,  Noel D'Angelo ,  Bradley J. Herberich ,  Fang-Tsao Hong ,  Claire I.M. Jackson ,  Brian Alan Lanman ,  Hongyu Liao ,  Longbin Liu ,  Nobuko Nishimura ,  Mark H. Norman ,  Liping H. Pettus ,  Anthony B. Reed ,  Adrian Leonard Smith ,  Seifu Tadesse ,  Nuria A. Tamayo ,  Bin Wu ,  Ryan Wurz ,  Kevin C. Yang

IPC: C07D473/00 ,  C07D417/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/14

CPC classification number: C07D473/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。

公开(公告)号：US11905281B2

公开(公告)日：2024-02-20

申请号：US17031607

申请日：2020-09-24

Applicant: Amgen Inc.

Inventor： Brian Alan Lanman ,  Jian Chen ,  Anthony B. Reed ,  Victor J. Cee ,  Longbin Liu ,  David John Kopecky ,  Patricia Lopez ,  Ryan Paul Wurz ,  Thomas T. Nguyen ,  Shon Booker ,  Nobuko Nishimura ,  Youngsook Shin ,  Nuria A. Tamayo ,  John Gordon Allen ,  Jennifer Rebecca Allen

IPC: C07D471/04 ,  C07D213/82 ,  C07D417/04 ,  A61K38/07 ,  C07D487/08 ,  C07D417/12 ,  C07D513/04 ,  C07D487/10 ,  C07D487/04 ,  C07D401/04 ,  C07D239/80 ,  C07D401/14 ,  C07D237/34 ,  C07D403/04 ,  A61K31/496 ,  A61K31/416 ,  A61K31/55 ,  A61K31/454 ,  A61K31/519 ,  A61K31/502 ,  A61K31/517 ,  A61K31/5025 ,  A61P35/00 ,  A61K31/7068 ,  C07D275/04 ,  C07D475/00

CPC classification number: C07D417/04 ,  A61K31/416 ,  A61K31/454 ,  A61K31/496 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61K31/7068 ,  A61K38/07 ,  A61P35/00 ,  C07D237/34 ,  C07D239/80 ,  C07D275/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D417/12 ,  C07D471/04 ,  C07D475/00 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D513/04

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：US20180222895A1

公开(公告)日：2018-08-09

申请号：US15945852

申请日：2018-04-05

Applicant: AMGEN INC.

Inventor： Xiaoqi Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Mikkel V. Debenedetto ,  Paul John Dransfield ,  Zice Fu ,  James S. Harvey ,  Julie Anne Heath ,  Jonathan Houze ,  Ted C. Judd ,  David John Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Xiaodong Wang

IPC: C07D405/14 ,  C07D409/14 ,  C07D403/14 ,  C07D403/04 ,  C07D401/14 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/506 ,  A61K31/5383 ,  C07D498/04 ,  C07D405/04 ,  C07D471/04 ,  A61K31/497

CPC classification number: C07D405/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D471/04 ,  C07D498/04

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

公开(公告)号：US09611261B2

公开(公告)日：2017-04-04

申请号：US14932787

申请日：2015-11-04

Applicant: AMGEN INC.

Inventor： Ana Elena Minatti ,  Jonathan D. Low ,  Jennifer R. Allen ,  Albert Amegadzie ,  James Brown ,  Michael J. Frohn ,  Angel Guzman-Perez ,  Paul E. Harrington ,  Patricia Lopez ,  Vu Van Ma ,  Nobuko Nishimura ,  Wenyuan Qian ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Kelvin Sham ,  Adrian L. Smith ,  Ryan White ,  Qiufen Xue

IPC: C07D471/04 ,  C07D265/12 ,  C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D417/12 ,  C07D413/10 ,  C07D491/048 ,  C07D413/04

CPC classification number: C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

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, A8, each of Ra, Rb, R1, R2, R3 and R7 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 A-beta 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. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

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。