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：US09382257B2

公开(公告)日：2016-07-05

申请号：US14688724

申请日：2015-04-16

Applicant: Genentech, Inc.

Inventor： Daniel Burdick ,  Huifen Chen ,  Shumei Wang ,  Weiru Wang

IPC: A61K31/4985 ,  C07D231/10 ,  C07D241/38 ,  C07D487/04 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K45/06

Abstract: Compounds having the formula I wherein R1 and R2 are as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中R 1和R 2如本文所定义，是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：US20130096102A1

公开(公告)日：2013-04-18

申请号：US13712015

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Mark Chambers ,  Bryan K. Chan ,  Huifen Chen ,  Anthony Estrada ,  Janet Gunzner-Toste ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: C07D413/14 ,  C07D498/08 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D403/14 ,  C07D413/12 ,  C07D473/16 ,  C07D498/06 ,  C07D498/08

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 5，R 6和R 7如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

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：US09321761B2

公开(公告)日：2016-04-26

申请号：US14575018

申请日：2014-12-18

Applicant: GENENTECH, INC. ,  CURIS, INC.

Inventor： Janet L. Gunzner-Toste ,  Daniel Sutherlin ,  Mark S. Stanley ,  Liang Bao ,  Georgette M. Castanedo ,  Rebecca L. LaLonde ,  Shumei Wang ,  Mark E. Reynolds ,  Scott J. Savage ,  Kimberly Malesky ,  Michael S. Dina ,  Michael F. T. Koehler

IPC: C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07F9/58

CPC classification number: C07D213/16 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07F9/58

Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

Abstract translation: 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A，X，Y R1，R2，R3，R4，m和n如本文所述。

公开(公告)号：US10183009B2

公开(公告)日：2019-01-22

申请号：US15592013

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

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：US20180009805A1

公开(公告)日：2018-01-11

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 ,  Anthony F. Romero ,  Yong Tang ,  Vickie Hsiao-Wei Tsui ,  Shumei Wang

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

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  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：US20170342067A1

公开(公告)日：2017-11-30

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 ,  A61K45/06 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K45/06 ,  C07D519/00

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：US20170340605A1

公开(公告)日：2017-11-30

申请号：US15592013

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

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.