公开(公告)号：US10800780B2

公开(公告)日：2020-10-13

申请号：US16065397

申请日：2016-12-23

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Xingyu Lin ,  Po-wai Yuen ,  Rohan Mendonca ,  Brendan Parr ,  Richard Pastor ,  Zhonghua Pei ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Xiaokai Li ,  Roheeth Pavana ,  Hima Potturi ,  Venkata Velvadapu ,  Jesse Waldo ,  Zuhui Zhang ,  Guosheng Wu ,  Benjamin Douglas Sellers

IPC: A61K31/4188 ,  A61K31/407 ,  A61K31/4035 ,  C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61K45/06 ,  A61K38/16

Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

公开(公告)号：US20200002345A1

公开(公告)日：2020-01-02

申请号：US16561432

申请日：2019-09-05

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 ,  Christopher Hurley

IPC: C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

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.

公开(公告)号：US20150336962A1

公开(公告)日：2015-11-26

申请号：US14720323

申请日：2015-05-22

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-Wai Yuen

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

Abstract translation: 本文描述了式（00A）的化合物和用作Janus激酶抑制剂的方法。

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。