公开(公告)号：US20140171639A1

公开(公告)日：2014-06-19

申请号：US14187677

申请日：2014-02-24

Applicant: AMGEN INC.

Inventor： Kaustav Biswas ,  James Brown ,  Jian J. Chen ,  Vijay Keshav Gore ,  Scott Harried ,  Daniel B. Horne ,  Matthew R. Kaller ,  Qingyian Liu ,  Vu Van Ma ,  Holger Monenschein ,  Thomas T. Nguyen ,  David J. St. Jean, JR. ,  Chester Chenguang Yuan ,  Wenge Zhong

IPC: C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D413/12 ,  C07D498/04 ,  C07D417/12 ,  C07D409/12 ,  C07D405/14 ,  C07D405/12 ,  C07D401/14 ,  C07D213/61

CPC classification number: C07D213/82 ,  C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

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.

Abstract translation: 式I的化合物可用作TRPM8的拮抗剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症，并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式I的化合物具有以下结构：其中本文提供变量的定义。

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：US09493459B2

公开(公告)日：2016-11-15

申请号：US15058023

申请日：2016-03-01

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Jian J. Chen ,  Michael J. Frohn ,  Matthew R. Kaller ,  Qingyian Liu ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Wenyuan Qian ,  Robert M. Rzasa ,  Wenge Zhong

IPC: C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  C07D401/14 ,  A61K31/497 ,  A61K45/06 ,  A61K31/517 ,  C07D403/14

CPC classification number: C07D471/04 ,  A61K31/497 ,  A61K31/517 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

公开(公告)号：US09096527B2

公开(公告)日：2015-08-04

申请号：US14187677

申请日：2014-02-24

Applicant: AMGEN INC.

Inventor： Kaustav Biswas ,  James Brown ,  Jian J. Chen ,  Vijay Keshav Gore ,  Scott Harried ,  Daniel B. Horne ,  Matthew R. Kaller ,  Qingyian Liu ,  Vu Van Ma ,  Holger Monenschein ,  Thomas T. Nguyen ,  David J. St. Jean, Jr. ,  Chester Chenguang Yuan ,  Wenge Zhong

IPC: C07D498/04 ,  C07D401/12 ,  C07D471/04 ,  C07D213/81 ,  C07D213/82 ,  C07D213/40 ,  C07D213/61 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

CPC classification number: C07D213/82 ,  C07D213/40 ,  C07D213/61 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

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.

Abstract translation: 式I的化合物可用作TRPM8的拮抗剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症，并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式I的化合物具有以下结构：其中本文提供变量的定义。

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：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：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：US10889581B2

公开(公告)日：2021-01-12

申请号：US16466199

申请日：2017-12-13

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Albert Amegadzie ,  Matthew P. Bourbeau ,  Jian J. Chen ,  Michael J. Frohn ,  Paul E. Harrington ,  Jonathan D. Low ,  Vu V. Ma ,  Thomas T. Nguyen ,  Alexander Pickrell ,  Corey Reeves

IPC: C07D471/14 ,  C07D417/14 ,  C07D417/10

Abstract: The present disclosure 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 A, R1, R2, R2′, R3, R4, and R5 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：US09376450B2

公开(公告)日：2016-06-28

申请号：US13892196

申请日：2013-05-10

Applicant: Amgen Inc.

Inventor： Jennifer R. Allen ,  Daniel B. Horne ,  Essa Hu Harrington ,  Matthew R. Kaller ,  Holger Monenschein ,  Thomas T. Nguyen ,  Andreas Reichelt ,  Robert M. Rzasa

IPC: C07D491/107 ,  C07D413/14 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04 ,  C07D487/10 ,  C07D401/04 ,  C07D401/06 ,  C07D405/14 ,  C07D405/04 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D409/14

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10

Abstract: Heteroaryloxyheterocyclyl 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, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.