公开(公告)号：US10280149B2

公开(公告)日：2019-05-07

申请号：US15643808

申请日：2017-07-07

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Victor Gehling ,  Vickie Hsiao-Wei Tsui ,  James Richard Jr. Kiefer ,  Jun Liang ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Birong Zhang

IPC: C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D241/04 ,  C07D211/30

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20170283424A1

公开(公告)日：2017-10-05

申请号：US15627847

申请日：2017-06-20

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

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.

公开(公告)号：US20140309210A1

公开(公告)日：2014-10-16

申请号：US14178527

申请日：2014-02-12

Applicant: Genentech, Inc.

Inventor： Jason Burch ,  Richard A. Goldsmith ,  Daniel Fred Ortwine ,  Richard Pastor ,  Zhonghua Pei

IPC: C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D491/052 ,  C07D417/14 ,  C07D471/04 ,  C07D409/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052

Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.

Abstract translation: 式I的化合物：立体异构体或其药学上可接受的盐，其中X，X 1，X 2，X 3，R 1，R 2，R 3，R 4，R 5和R 6在本文中描述，包括化合物的组合物和制备和使用化合物的方法 用于治疗疾病。

公开(公告)号：US20140107099A1

公开(公告)日：2014-04-17

申请号：US14134150

申请日：2013-12-19

Applicant: Genentech, Inc.

Inventor： Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia 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 JAK kinase activity in a patient.

Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK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：US20140038939A1

公开(公告)日：2014-02-06

申请号：US14049458

申请日：2013-10-09

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: C07D487/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/437

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

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.

公开(公告)号：US20240150364A1

公开(公告)日：2024-05-09

申请号：US18507678

申请日：2023-11-13

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph 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 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

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.

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：US10155764B2

公开(公告)日：2018-12-18

申请号：US15449692

申请日：2017-03-03

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Martin Duplessis ,  Andrew Charles Good ,  Yves LeBlanc ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  Anthony F. Romero ,  Alexander M. Taylor

IPC: C07D487/04 ,  C07D403/12 ,  C07D401/12 ,  C07D237/32 ,  C07D471/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/55 ,  C07D237/34 ,  C07D405/12

Abstract: The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R1, R3, R4, R5, and each Re have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170334883A1

公开(公告)日：2017-11-23

申请号：US15449706

申请日：2017-03-03

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Martin Duplessis ,  Andrew Charles Good ,  Yves LeBlanc ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Richard Pastor ,  Anthony F. Romero ,  Alexander M. Taylor

IPC: C07D403/12 ,  C07D401/12 ,  C07D401/04 ,  C07D253/075 ,  A61K45/06 ,  C07D403/04 ,  A61K31/53

CPC classification number: C07D403/12 ,  A61K31/53 ,  A61K45/06 ,  A61P35/00 ,  C07D249/12 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.