公开(公告)号：US09434732B2

公开(公告)日：2016-09-06

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: C07D471/02 ,  C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377

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：US20160158207A1

公开(公告)日：2016-06-09

申请号：US14952821

申请日：2015-11-25

Applicant: Constellation Pharmaceuticals, Inc. ,  Genentech, Inc.

Inventor： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC: A61K31/437 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/4709 ,  A61K31/498 ,  A61K45/06 ,  A61K31/55 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D471/04 ,  A61K31/506

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

Abstract translation: 本发明涉及式（I）或式（II）化合物及其盐，其中式（I）的R 1 -R 4和式（II）的R 1 -R 3具有本文定义的任何值，组合物 及其用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括包含式（II）的式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。

公开(公告)号：US20160024089A1

公开(公告)日：2016-01-28

申请号：US14878774

申请日：2015-10-08

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 ,  A61K31/437 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/506 ,  A61K45/06 ,  A61K31/496

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。

公开(公告)号：US20240132507A1

公开(公告)日：2024-04-25

申请号：US18496146

申请日：2023-10-27

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Zhonghua Pei ,  Brendan Parr ,  Wendy Liu ,  Richard Pastor ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Hima Potturi ,  Guoshen Wu ,  Xingyu Lin ,  Yanyan Chu ,  Po-wai Yuen

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; 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：US20220389020A1

公开(公告)日：2022-12-08

申请号：US17648045

申请日：2022-01-14

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：US20200216456A1

公开(公告)日：2020-07-09

申请号：US16626191

申请日：2018-06-28

Applicant: Genentech, Inc. ,  NewLink Genetics Corporation

Inventor： Zhonghua Pei ,  Brendan Parr ,  Wendy Liu ,  Richard Pastor ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Hima Potturi ,  Guoshen Wu ,  Xingyu Lin ,  Yanyan Chu ,  Powai Yuen

IPC: C07D487/04

Abstract: Presently provided are inhibitors of TD02 and IDOl and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; 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：US09763922B2

公开(公告)日：2017-09-19

申请号：US14952821

申请日：2015-11-25

Applicant: Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

Inventor： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC: A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  C07D471/04 ,  C07D519/00 ,  A61K45/06

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：US20160272588A1

公开(公告)日：2016-09-22

申请号：US15074027

申请日：2016-03-18

Applicant: Genentech, Inc.

Inventor： Robert Blake ,  Paola Di Lello ,  Jake 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: C07D213/73 ,  A61K45/06 ,  C07D409/04 ,  A61K31/4436 ,  C07D213/74 ,  C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/44 ,  A61K31/5355

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.

公开(公告)号：US11603373B2

公开(公告)日：2023-03-14

申请号：US16626219

申请日：2018-06-20

Applicant: Genentech, Inc.

Inventor： Zhonghua Pei ,  Richard Pastor ,  Lewis Gazzard ,  Brendan Parr ,  Wendy Liu ,  Rohan Mendonca ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D221/00 ,  C07D335/00 ,  C07D487/04 ,  C07D471/08 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00

Abstract: Presently provided are inhibitors of cellularly expressed TD02 and IDO1, and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; 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：US10358437B2

公开(公告)日：2019-07-23

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 ,  F. Anthony Romero ,  Alexander M. Taylor

IPC: C07D249/12 ,  C07D403/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  A61K31/53 ,  A61K31/4196 ,  A61P35/00 ,  C07D253/075 ,  A61K45/06

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.