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：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：US10202378B2

公开(公告)日：2019-02-12

申请号：US15658213

申请日：2017-07-24

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

Inventor： Marc Adler ,  Daniel J. Burdick ,  Terry Crawford ,  Martin Duplessis ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  F. Anthony Romero ,  Yong Tang ,  Vickie Hsiao-Wei Tsui ,  Shumei Wang

IPC: A61K31/506 ,  C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1-R6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.

公开(公告)号：US09855269B2

公开(公告)日：2018-01-02

申请号：US15454793

申请日：2017-03-09

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Nbdubaku ,  Lan Wang

IPC: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The invention provides a method of inhibiting angiogenesis in a patient by administering a compound of formula (I): wherein R1 R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US09382241B2

公开(公告)日：2016-07-05

申请号：US13906626

申请日：2013-05-31

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Terry Crawford ,  Seth F. Harris ,  Steven R. Magnuson ,  Chudi Ndubaku ,  Lan Wang

IPC: C07D471/04 ,  C07D239/94 ,  C07D403/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D239/95 ,  C07D413/12

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract translation: 本发明提供具有以下通式的新化合物：其中A，R 1，R 2和R 3如本文所定义，包括该化合物的组合物和使用该化合物的方法。

公开(公告)号：US10258603B2

公开(公告)日：2019-04-16

申请号：US15592012

申请日：2017-05-10

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Daniel J. Burdick ,  Alexandre Cote ,  Terry Crawford ,  Les A. Dakin ,  Vickie Hsiao-Wei Tsui ,  Michael Charles Hewitt ,  Yves LeBlanc ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  F. Anthony Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: A61K31/40 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, Rc, and Rd have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

公开(公告)号：US10150767B2

公开(公告)日：2018-12-11

申请号：US15592017

申请日：2017-05-10

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Daniel J. Burdick ,  Alexandre Cote ,  Terry Crawford ,  Les A. Dakin ,  Vickie Hsiao-Wei Tsui ,  Michael Charles Hewitt ,  Yves LeBlanc ,  Steven R. Magnuson ,  Christopher G. Nasveschuk ,  Anthony F. Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: C07D471/04 ,  A61K31/437 ,  C07D519/00 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  A61K45/06

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated 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：US09505767B2

公开(公告)日：2016-11-29

申请号：US14477566

申请日：2014-09-04

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

Inventor： Brian K. Albrecht ,  Steven F. Bellon ,  Victor S. Gehling ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Jun Liang ,  Steven R. Magnuson ,  Vickie Hsiao-Wei Tsui ,  Birong Zhang

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61N5/10

Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.

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。