公开(公告)号：US20150087585A1

公开(公告)日：2015-03-26

申请号：US14384508

申请日：2013-03-26

Applicant: Pfizer Inc.

Inventor： Kay Ahn ,  Markus Boehm ,  Shawn Cabral ,  Philip A. Carpino ,  Kentaro Futatsugi ,  David Hepworth ,  Daniel W. Kung ,  Suvi Orr ,  Jian Wang

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  A61K31/437 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

Abstract translation: 抑制二酰基甘油酰基转移酶2（DGAT2）活性的式I的嘌呤衍生物，3H-咪唑并[4,5-b]嘧啶和1H-咪唑并[4,5-d]吡嗪及其在治疗疾病中的用途 本文描述了与动物相连的动物。

公开(公告)号：US09296745B2

公开(公告)日：2016-03-29

申请号：US14384508

申请日：2013-03-26

Applicant: Pfizer Inc.

Inventor： Kay Ahn ,  Markus Boehm ,  Shawn Cabral ,  Philip A. Carpino ,  Kentaro Futatsugi ,  David Hepworth ,  Daniel W. Kung ,  Suvi Orr ,  Jian Wang

IPC: C07D471/04 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

Abstract translation: 抑制二酰基甘油酰基转移酶2（DGAT2）活性的式I的嘌呤衍生物，3H-咪唑并[4,5-b]嘧啶和1H-咪唑并[4,5-d]吡嗪及其在治疗疾病中的用途 本文描述了与动物相连的动物。

公开(公告)号：US20140080756A1

公开(公告)日：2014-03-20

申请号：US14083275

申请日：2013-11-18

Applicant: Pfizer Inc.

Inventor： Samit K. Bhattacharya ,  Kimberly O. Cameron ,  Dilinie P. Fernando ,  Kim F. McClure ,  Daniel W. Kung ,  Allyn T. Londregan ,  Suvi T.M. Orr

IPC: C07D471/10 ,  A61K31/506 ,  A61K31/53 ,  A61K31/435 ,  A61K31/497 ,  C07D491/056 ,  C07D513/04 ,  A61K45/06

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K45/06 ,  C07D491/056 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention provides a compound of Formula (I) a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.

Abstract translation: 本发明提供了其作为Ghrelin拮抗剂或反向激动剂的其中R 1，R 2，R a，L，Z，Z 1和Z 2如本文所定义的药用盐的式（I）化合物; 其药物组合物; 以及治疗由Ghrelin受体的拮抗作用介导的疾病，病症或病症的方法。