公开(公告)号：US12083121B2

公开(公告)日：2024-09-10

申请号：US17579359

申请日：2022-01-19

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

CPC classification number: A61K31/519 ,  A61K31/551 ,  A61K39/39558 ,  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：US11993597B2

公开(公告)日：2024-05-28

申请号：US17692026

申请日：2022-03-10

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 ,  A61K31/519 ,  A61P35/00 ,  A61K31/7068 ,  A61K38/07

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61P35/00 ,  A61K31/7068 ,  A61K38/07 ,  A61K2300/00

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：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：US11306087B2

公开(公告)日：2022-04-19

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 ,  A61K31/7068 ,  A61K38/07

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：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：US10947223B2

公开(公告)日：2021-03-16

申请号：US16466211

申请日：2017-12-13

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Matthew P. Bourbeau ,  Ning Chen ,  Michael J. Frohn ,  Paul E. Harrington ,  Qingyian Liu ,  Corey Reeves

IPC: A61K31/535 ,  A61K31/536 ,  A61K31/537 ,  C07D265/08 ,  C07D265/12 ,  C07D265/30 ,  C07D413/10 ,  A61P25/28 ,  C07D413/14

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: (insert Formula I structure) wherein variables W, X, Y, 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 beta amyloid (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：US10058550B2

公开(公告)日：2018-08-28

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 ,  A61K31/497 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  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 ,  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：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：US09725469B2

公开(公告)日：2017-08-08

申请号：US14435516

申请日：2013-11-12

Applicant: Amgen Inc.

Inventor： Ryan White ,  Oleg Epstein ,  Jason B. Human ,  Xiao Mei Zheng ,  Yuan Cheng ,  Kelvin Sham ,  Qingyian Liu ,  Ning Chen

IPC: C07D491/052 ,  C07D513/10 ,  C07D519/00 ,  C07D498/10 ,  C07D498/20 ,  C07D311/80 ,  C07D513/20

CPC classification number: C07D519/00 ,  C07D311/80 ,  C07D491/052 ,  C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

公开(公告)号：US20130225552A1

公开(公告)日：2013-08-29

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: C07D487/04 ,  C07D513/04 ,  C07D471/04 ,  C07D498/04 ,  C07D473/00

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。