公开(公告)号：US09573899B2

公开(公告)日：2017-02-21

申请号：US15074027

申请日：2016-03-18

Applicant: Genentech, Inc.

Inventor： Robert Blake ,  Paola Di Lello ,  Jason Drummond ,  Christine Johanna Heideker ,  Lorna Kategaya ,  Till Maurer ,  Jeremy M. Murray ,  Chudi Ndubaku ,  Richard Pastor ,  Lionel Rouge ,  Vickie Tsui ,  Ingrid E. Wertz ,  Kebing Yu

IPC: C07D213/02 ,  C07D213/73 ,  A61K31/44 ,  A61K45/06 ,  C07D409/04 ,  A61K31/4436 ,  A61K31/5355 ,  C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/4439 ,  C07D213/74 ,  C07D403/04

CPC classification number: C07D213/73 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K45/06 ,  C07D213/74 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

Abstract: 2-Aminopyridine compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for modulating USP7, and for treating cancer and immune disorders such as inflammation mediated by USP7. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供了式I的2-氨基吡啶化合物，以及可用于调节USP7的各种取代基，包括立体异构体，互变异构体和其药学上可接受的盐，以及用于治疗癌症和免疫病症如USP7介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US20160333011A1

公开(公告)日：2016-11-17

申请号：US15220087

申请日：2016-07-26

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diastereomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

公开(公告)号：US20150152117A1

公开(公告)日：2015-06-04

申请号：US14615873

申请日：2015-02-06

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US20140378449A1

公开(公告)日：2014-12-25

申请号：US14483485

申请日：2014-09-11

Applicant: Genentech, Inc.

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Wendy Liu

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2，R 3，R 4和R 5在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。