公开(公告)号：US20180086720A1

公开(公告)日：2018-03-29

申请号：US15686028

申请日：2017-08-24

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

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

IPC: C07D237/20 ,  C07D401/12 ,  C07D401/04 ,  C07D487/04 ,  C07D403/04 ,  C07D487/08 ,  C07D498/10 ,  C07D471/10 ,  C07D403/14 ,  C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14 ,  C07D237/22 ,  C07D451/02 ,  C07D413/04

CPC classification number: C07D237/20 ,  A61K31/337 ,  A61K31/437 ,  A61K31/501 ,  A61K45/06 ,  C07D237/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D498/10 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. 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 BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.

公开(公告)号：US20170312292A1

公开(公告)日：2017-11-02

申请号：US15482581

申请日：2017-04-07

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

Inventor： Anthony F. Romero ,  Steven R. Magnuson ,  Richard Pastor ,  Vickie Hsiao-Wei Tsui ,  Jeremy Murray ,  Terry Crawford ,  Daniel J. Burdick ,  Brian K. Albrecht ,  Alexandre Cote ,  Alexander M. Taylor ,  Christopher G. Nasveschuck ,  Yves LeBlanc ,  Michael Charles Hewitt ,  Kwong Wah Lai ,  Kevin Chen

IPC: A61K31/55 ,  C07D403/04 ,  C07D243/24 ,  A61K31/5513 ,  C07D243/12 ,  C07D223/16 ,  C07D403/14 ,  C07D267/14

CPC classification number: A61K31/55 ,  A61K31/337 ,  A61K31/5513 ,  A61K45/06 ,  C07D223/16 ,  C07D243/12 ,  C07D243/24 ,  C07D267/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, 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) 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：US20140206702A1

公开(公告)日：2014-07-24

申请号：US14220409

申请日：2014-03-20

Applicant: Genentech, Inc.

Inventor： Yingjie Lai ,  Jun Liang ,  Steven R. Magnuson ,  Kirk D. Robarge ,  Vickie H. Tsui ,  Birong Zhang

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, Ra, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.

Abstract translation: 本发明提供式Ia-Ib的化合物，其立体异构体或其药学上可接受的盐，其中A，X，Ra，R 1，R 2，R 4，R 5和R 16如本文所定义，药物组合物包含式Ia-Ib的化合物和 药学上可接受的载体，佐剂或载体，以及在治疗中使用该化合物或组合物的方法。

公开(公告)号：US20140171408A1

公开(公告)日：2014-06-19

申请号：US14185700

申请日：2014-02-20

Applicant: Genentech, Inc.

Inventor： Toby Jonathan Blench ,  Charles Ellwood ,  Simon Charles Goodacre ,  Yingjie Lai ,  Jun Liang ,  Calum MacLeod ,  Steven R. Magnuson ,  Vickie Hsiao-Wei Tsui ,  Karen Williams ,  Birong Zhang

IPC: A61K31/5377 ,  C07D513/04 ,  A61K31/519 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506

CPC classification number: A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  C07D513/04

Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.

Abstract translation: 提供式I化合物，立体异构体，互变异构体，溶剂合物，前药和药学上可接受的盐，其中A，X，R 1，R 2，R 4和R 5在本文中定义，药物组合物包括式I化合物和药学上可接受的 载体，佐剂或载体，在治疗中使用化合物或组合物的方法，以及制备式I化合物的方法。

公开(公告)号：US10308614B2

公开(公告)日：2019-06-04

申请号：US15686028

申请日：2017-08-24

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

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

IPC: C07D237/20 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D498/10 ,  A61K31/50 ,  A61K31/51 ,  C07D401/12 ,  C07D237/22 ,  C07D417/14 ,  C07D413/12 ,  C07D451/02 ,  C07D487/04 ,  A61K45/06 ,  A61K31/337 ,  A61K31/437 ,  A61K31/501

Abstract: The present invention relates to compounds of formula (I): and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. 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 BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.

公开(公告)号：US10206931B2

公开(公告)日：2019-02-19

申请号：US15482581

申请日：2017-04-07

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

Inventor： F. Anthony Romero ,  Steven R. Magnuson ,  Richard Pastor ,  Vickie Hsiao-Wei Tsui ,  Jeremy Murray ,  Terry Crawford ,  Daniel J. Burdick ,  Brian K. Albrecht ,  Alexandre Cote ,  Alexander M. Taylor ,  Christopher G. Nasveschuck ,  Yves LeBlanc ,  Michael Charles Hewitt ,  Kwong Wah Lai ,  Kevin Chen

IPC: A61K31/551 ,  C07D243/12 ,  C07D403/04 ,  C07D403/14 ,  A61K31/55 ,  C07D223/16 ,  C07D267/14 ,  C07D401/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/10 ,  C07D243/24 ,  C07D471/04 ,  C07D495/04 ,  A61K45/06 ,  A61K31/337 ,  A61K31/5513

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, 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) 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：US20170340604A1

公开(公告)日：2017-11-30

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 ,  Anthony F. Romero ,  Yong Tang ,  Alexander M. Taylor ,  Shumei Wang

IPC: A61K31/40 ,  C07D471/04

CPC classification number: 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：US09592235B2

公开(公告)日：2017-03-14

申请号：US15184310

申请日：2016-06-16

Applicant: Genentech, Inc.

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

IPC: A61K31/551 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04 ,  C07D403/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D239/95 ,  C07D413/12 ,  A61K31/5377 ,  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 treating cancer 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.

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：US09586956B2

公开(公告)日：2017-03-07

申请号：US14448941

申请日：2014-07-31

Applicant: Genentech, Inc.

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

IPC: C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D413/04

CPC classification number: C07D471/04 ,  C07D217/22 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12

Abstract: The invention provides novel compounds having the general formula: wherein A, R1 and R2 are as described 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和R 2如本文所述，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：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.