公开(公告)号：US09302985B2

公开(公告)日：2016-04-05

申请号：US14101561

申请日：2013-12-10

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Olivier Rene ,  Monique Bodil van Niel ,  Stuart Ward

IPC: C07C311/21 ,  C07C311/41 ,  C07C311/16 ,  C07C311/29 ,  C07C311/46 ,  C07C311/44 ,  C07C317/14

CPC classification number: C07C311/21 ,  C07C311/16 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07C317/14

Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract translation: 式Ia或Ib化合物或其药学上可接受的盐，其中m，n，r，A，X1，X2，X3，X4，Y，Z，R1，R2，R3，R4，R5，R6，R7和 R8如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。

公开(公告)号：US20160024504A1

公开(公告)日：2016-01-28

申请号：US14776051

申请日：2014-03-14

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

Inventor： Brian K. Albrecht ,  Alexandre Cote ,  Terry Crawford ,  Benjamin Fauber ,  Hon-Ren Huang ,  Jose M. Lora ,  Steven Magnuson ,  Christopher G. Nasveschuk ,  Andres Salmeron ,  Robert J. Sims, III ,  Alexander M. Taylor

IPC: C12N15/113 ,  G01N33/50 ,  A61K31/444 ,  A61K31/437 ,  A61K31/496

CPC classification number: C12N15/113 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/713 ,  C07K14/4702 ,  C12N2310/14 ,  C12N2320/30 ,  G01N33/505 ,  G01N2333/52 ,  G01N2500/04 ,  G01N2500/10 ,  Y02A50/422

Abstract: The invention provides methods for treating Th2 cytokine-mediated diseases by inhibiting bromodomain function.

Abstract translation: 本发明提供了通过抑制溴结构域功能来治疗Th2细胞因子介导的疾病的方法。

公开(公告)号：US09216988B2

公开(公告)日：2015-12-22

申请号：US13717998

申请日：2012-12-18

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Olivier Rene

IPC: A61K31/495 ,  A61K31/496 ,  C07D295/26 ,  C07D295/135 ,  C07D295/185 ,  C07C311/13 ,  C07D491/107 ,  C07D309/14 ,  C07D405/04 ,  C07D241/08 ,  C07D241/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D207/12 ,  C07D207/14 ,  C07D211/46 ,  C07D211/58 ,  C07D305/06 ,  C07D305/08 ,  C07D265/30 ,  C07D267/14 ,  C07C311/10

CPC classification number: C07D491/107 ,  C07C311/13 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D207/14 ,  C07D211/46 ,  C07D211/58 ,  C07D241/04 ,  C07D241/08 ,  C07D265/30 ,  C07D267/14 ,  C07D295/135 ,  C07D295/185 ,  C07D295/26 ,  C07D305/06 ,  C07D305/08 ,  C07D309/14 ,  C07D405/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n，A，X1，X2，X3，X4，R1，R2，R3a，R3b，R4a和R4b如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。

公开(公告)号：US08912219B2

公开(公告)日：2014-12-16

申请号：US14210978

申请日：2014-03-14

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Olivier Rene ,  Monique Bodil van Niel ,  Stuart Ward

IPC: A61K31/445 ,  C07D211/96 ,  C07D285/36 ,  C07D295/185 ,  C07D417/12 ,  C07D285/16

CPC classification number: C07D417/12 ,  C07D211/96 ,  C07D285/16 ,  C07D285/36 ,  C07D295/185 ,  C07D401/12

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract translation: 其中m，n，p，q，r，A，X1，X2，X3，X4，X5，X6，Y，Z，G，R1a，R2a，R1b，R2b ，R3，R4，R5和R6如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。

公开(公告)号：US10259808B2

公开(公告)日：2019-04-16

申请号：US15847407

申请日：2017-12-19

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Emanuela Gancia ,  Tammy Ladduwahetty ,  David Vesey ,  Paul Winship ,  Olivier Rene

IPC: C07D417/12 ,  C07D417/14 ,  C07D417/10 ,  A61K31/541 ,  A61P19/02 ,  A61P17/06

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, Het, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.

公开(公告)号：US10131644B2

公开(公告)日：2018-11-20

申请号：US15199447

申请日：2016-06-30

Applicant: Genentech, Inc.

Inventor： Monique Bodil van Niel ,  Benjamin Fauber ,  Emanuela Gancia ,  Simon Gaines ,  Alberto Gobbi ,  Christopher Hurley ,  Tammy Ladduwahetty ,  Olivier Rene ,  David Vesey ,  Stuart Ward ,  Paul Winship

IPC: C07D279/02 ,  C07D417/10 ,  C07D417/12

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.

公开(公告)号：US09994551B2

公开(公告)日：2018-06-12

申请号：US15801178

申请日：2017-11-01

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Monique Bodil van Niel ,  Andrew Cridland ,  Christopher Hurley ,  Jonathan Killen ,  Stuart Ward ,  Paul Winship

IPC: C07D403/12 ,  C07D237/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D403/12 ,  C07D237/26 ,  C07D237/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US20170296550A1

公开(公告)日：2017-10-19

申请号：US14972597

申请日：2015-12-17

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Olivier Rene

IPC: A61K31/541 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

CPC classification number: A61K31/541 ,  C07D279/02 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, Ar, A, W, X1, X2, X3, X4, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

公开(公告)号：US09550771B2

公开(公告)日：2017-01-24

申请号：US14481991

申请日：2014-09-10

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Alberto Gobbi

IPC: C07D471/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Compounds of the formula I or II: or pharmaceutically acceptable salts thereof, wherein R1 is a group of formula (a), (b), (c); (d) or (e): and m, n, X, Y, R1, R2, R3, R4, Rb and Rc are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract translation: 并且m，n，X，Y，R 1，R 2，R 3，R 4，R b和R c如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。

公开(公告)号：US20160168141A1

公开(公告)日：2016-06-16

申请号：US15047523

申请日：2016-02-18

Applicant: Genentech, Inc.

Inventor： Benjamin Fauber ,  Alberto Gobbi ,  Olivier Rene ,  Monique Bodil van Niel ,  Emanuela Gancia ,  Simon Gaines ,  Tammy Ladduwahetty ,  David Vesey ,  Stuart Ward ,  Paul Winship

IPC: C07D417/10

CPC classification number: C07D417/10 ,  C07D279/02 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D491/107 ,  C07D491/113

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.