公开(公告)号：US20160102075A1

公开(公告)日：2016-04-14

申请号：US14973491

申请日：2015-12-17

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Jian J. CHEN ,  Michael J. FROHN ,  Essa Hu HARRINGTON ,  Qingyian LIU ,  Alexander J. PICKRELL ,  Shannon RUMFELT ,  Robert M. RZASA ,  Wenge ZHONG

IPC: C07D401/14 ,  C07D409/14 ,  C07D403/14 ,  C07D491/107 ,  C07D487/10 ,  C07C53/18 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/08 ,  C07D487/08 ,  C07D471/04 ,  C07D491/056 ,  C07D513/04 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07C53/18 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D513/04

Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, 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, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 式（I）的不饱和氮杂环化合物：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。 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，亨廷顿舞蹈病，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。

公开(公告)号：US20140045855A1

公开(公告)日：2014-02-13

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

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：US20200231585A1

公开(公告)日：2020-07-23

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: 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：US20160176874A1

公开(公告)日：2016-06-23

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: C07D471/04 ,  C07D403/14 ,  C07D401/14

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：US20170267673A1

公开(公告)日：2017-09-21

申请号：US15354877

申请日：2016-11-17

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  James A. BROWN ,  Jian J. CHEN ,  Yuan CHENG ,  Michael J. FROHN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Longbin LIU ,  Qingyian LIU ,  Jonathan D. LOW ,  Vu Van MA ,  James R. MANNING ,  Ana Elena MINATTI ,  Thomas T. NGUYEN ,  Nobuko NISHIMURA ,  Mark H. NORMAN ,  Liping H. PETTUS ,  Alexander J. PICKRELL ,  Wenyuan QIAN ,  Shannon RUMFELT ,  Robert M. RZASA ,  Aaron C. SIEGMUND ,  Markian M. STEC ,  Ryan D. WHITE ,  Qiufen XUE

IPC: C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D279/08 ,  C07D417/04 ,  C07D513/10

CPC classification number: C07D417/12 ,  C07D279/08 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10

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, and 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：US20160046618A1

公开(公告)日：2016-02-18

申请号：US14819256

申请日：2015-08-05

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  James A. BROWN ,  Jian J. CHEN ,  Yuan CHENG ,  Michael J. FROHN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Longbin LIU ,  Qingyian LIU ,  Jonathan D. LOW ,  Vu Van MA ,  James MANNING ,  Ana Elena MINATTI ,  Thomas T. NGUYEN ,  Nobuko NISHIMURA ,  Mark H. NORMAN ,  Liping H. PETTUS ,  Alexander J. PICKRELL ,  Wenyuan QIAN ,  Shannon RUMFELT ,  Robert M. RZASA ,  Aaron C. SIEGMUND ,  Markian M. STEC ,  Ryan D. WHITE ,  Qiufen XUE

IPC: C07D417/12 ,  C07D471/04 ,  C07D513/10 ,  C07D417/14

CPC classification number: C07D417/12 ,  C07D279/08 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10

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, and 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.

Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。

公开(公告)号：US20150329538A1

公开(公告)日：2015-11-19

申请号：US14380918

申请日：2013-02-27

Applicant: AMGEN INC.

Inventor： Victor CEE ,  Frank CHAVEZ, JR. ,  Jian J. CHEN ,  Essa Hu HARRINGTON ,  Bradley HERBERICH ,  Claire L.M. JACKSON ,  Brian A. LANMAN ,  Thomas T. NGUYEN ,  Mark H. NORMAN ,  Liping H. PETTUS ,  Anthony B. REED ,  Adrian L. SMITH ,  Nuria A. TAMAYO ,  Andrew TASKER ,  Hui-Ling WANG ,  Bin WU ,  Ryan WURZ

IPC: C07D471/04 ,  C07D401/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D487/04

Abstract: The invention relates to amide-containing compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Abstract translation: 本发明涉及式（1）的含酰胺化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。