公开(公告)号：US20140171406A1

公开(公告)日：2014-06-19

申请号：US14187732

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: C07D487/04 ,  C07D401/14 ,  C07D401/12 ,  C07D213/82 ,  C07D413/12 ,  C07D471/04

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.

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：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：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：US11279712B2

公开(公告)日：2022-03-22

申请号：US16642441

申请日：2018-08-27

Applicant: AMGEN INC.

Inventor： Sean P. Brown ,  Yunxiao Li ,  Paul E. Harrington ,  Brian Alan Lanman ,  Jonathan D. Low ,  Ana Elena Minatti ,  Vu Van Ma ,  Kexue Li

IPC: C07D513/04 ,  C07D513/08 ,  C07D519/00 ,  A61P35/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7068

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stenoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US20150031668A1

公开(公告)日：2015-01-29

申请号：US14331426

申请日：2014-07-15

Applicant: AMGEN INC.

Inventor： Kaustav Biswas ,  Jian J. Chen ,  Vijay Keshav Gore ,  Scott Harried ,  Daniel B. Horne ,  Matthew R. Kaller ,  Vu Van Ma ,  Kelvin Sham ,  James Brown ,  Wenge Zhong ,  Thomas T. Nguyen

IPC: C07D491/052 ,  C07D498/04 ,  C07D471/04

CPC classification number: C07D491/052 ,  C07D471/04 ,  C07D498/04

Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors 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: 色甘酸化合物和式I的衍生物是TRPM8的有用抑制剂。 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：US11090304B2

公开(公告)日：2021-08-17

申请号：US16402538

申请日：2019-05-03

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：US11053226B2

公开(公告)日：2021-07-06

申请号：US16687546

申请日：2019-11-18

Applicant: Amgen Inc.

Inventor： Youngsook Shin ,  Victor J. Cee ,  Christopher M. Tegley ,  Brian Alan Lanman ,  Ryan Paul Wurz ,  Kevin C. Yang ,  Vu Van Ma ,  Daniel Erlanson ,  Joon Won Jeong ,  Raymond V. Fucini ,  Jeffrey Iwig

IPC: C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61P35/00

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.