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：US08952009B2

公开(公告)日：2015-02-10

申请号：US13958478

申请日：2013-08-02

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 ,  Wenge Zhong

IPC: C07D491/052 ,  C07D401/12 ,  C07D311/68 ,  C07D215/40 ,  C07D471/04 ,  C07D491/04

CPC classification number: C07D491/052 ,  C07D215/40 ,  C07D311/68 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04

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：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：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：US10344060B2

公开(公告)日：2019-07-09

申请号：US14773756

申请日：2014-03-12

Applicant: AMGEN INC.

Inventor： Justin K. Murray ,  Jerry Ryan Holder ,  Malgorzata Wanska ,  Christopher M. Tegley ,  James R. Falsey ,  Elizabeth M. Doherty ,  Leslie P. Miranda ,  Kaustav Biswas ,  Bin Wu ,  Kelvin Sham ,  Jason C. Long

IPC: C07K14/00 ,  C07K14/435 ,  C07K16/00 ,  C07K19/00 ,  C07K14/46 ,  C07K14/47 ,  A61K38/00 ,  A61K38/16 ,  A61K38/17 ,  A61K47/64 ,  A61K47/68

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

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。