公开(公告)号：US20130253186A1

公开(公告)日：2013-09-26

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 ,  C07D403/04 ,  C07D487/04 ,  C07D403/14 ,  C07D401/14 ,  C07D487/10 ,  C07D401/04 ,  C07D405/04 ,  C07D401/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04

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.

Abstract translation: 杂环氧基杂环基化合物和含有它们的组合物，以及这些化合物的制备方法。 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，亨廷顿舞蹈病，双相情感障碍，强迫症等。

公开(公告)号：US11224601B1

公开(公告)日：2022-01-18

申请号：US17029249

申请日：2020-09-23

Applicant: AMGEN INC.

Inventor： Paul E. Harrington ,  Kate Ashton ,  Sean P. Brown ,  Matthew R. Kaller ,  Todd J. Kohn ,  Brian Alan Lanman ,  Kexue Li ,  Yunxiao Li ,  Jonathan D. Low ,  Ana Elena Minatti ,  Alexander J. Pickrell ,  Markian M. Stec ,  Joshua Taygerly

IPC: A61K31/553 ,  A61P35/02 ,  A61P35/00 ,  C07D498/08

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 stereoisomer 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：US10821115B2

公开(公告)日：2020-11-03

申请号：US16783269

申请日：2020-02-06

Applicant: AMGEN INC.

Inventor： Paul E. Harrington ,  Kate Ashton ,  Sean P. Brown ,  Matthew R. Kaller ,  Todd J. Kohn ,  Brian Alan Lanman ,  Kexue Li ,  Yunxiao Li ,  Jonathan D. Low ,  Ana Elena Minatti ,  Alexander J. Pickrell ,  Markian M. Stec ,  Joshua Taygerly

IPC: A61K31/553 ,  A61P35/02 ,  A61P35/00 ,  C07D498/08

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 stereoisomer 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：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：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.

公开(公告)号：US09303028B2

公开(公告)日：2016-04-05

申请号：US14170146

申请日：2014-01-31

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

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.

Abstract translation: 式（I）的氮杂环丁烷和哌啶化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿舞蹈病，精神分裂症，双相障碍，强迫症等。

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：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.