公开(公告)号：US11028075B2

公开(公告)日：2021-06-08

申请号：US16283451

申请日：2019-02-22

Applicant: GENENTECH, INC.

Inventor： Daniel Sutherlin ,  Steven McKerrall ,  Kwong Wah Lai ,  Zhiguo Liu ,  Wenfeng Liu ,  Ramsay Beveridge ,  Jean-Philippe Leclerc ,  Alexandre Lemire ,  Liang Zhao ,  Claudio Sturino

IPC: C07D413/12 ,  C07D403/12 ,  C07D233/96 ,  C07D401/12 ,  A61P17/04 ,  C07D263/52 ,  C07D305/06 ,  C07D401/14 ,  A61K31/506 ,  A61K31/538 ,  C07B59/00 ,  A61K31/63 ,  A61K45/06 ,  C07D239/69 ,  A61K31/505

Abstract: The invention provides benzene sulfonamides and pharmaceutically acceptable salt thereof that are useful as sodium channel blockers for the treatment of, for example, pain. The following compound is illustrative:

公开(公告)号：US10457654B2

公开(公告)日：2019-10-29

申请号：US15799771

申请日：2017-10-31

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Daniel Sutherlin ,  Steven McKerrall ,  Michael Scott Wilson ,  Kwong Wah Lai ,  Philippe Bergeron ,  Birong Zhang ,  Ramsay Beveridge ,  Jean-Philippe Leclerc ,  Alexandre Lemire ,  Liang Zhao ,  Claudio Sturino

IPC: C07D285/08 ,  C07D277/52 ,  C07D239/69 ,  C07D213/76 ,  C07D261/16 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/427 ,  A61P19/02 ,  A61P29/00

Abstract: The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1—Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US10179767B2

公开(公告)日：2019-01-15

申请号：US15161085

申请日：2016-05-20

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Abid Hasan ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Zhiguo Liu ,  Daniel F. Ortwine ,  Brian Safina ,  Daniel Sutherlin ,  Shaoyi Sun ,  Andrew D. White ,  Wei Gong ,  Alla Yurevna Zenova ,  Jiuxiang Zhu

IPC: A01N43/00 ,  A61K31/00 ,  C07D211/22 ,  C07D211/48 ,  C07D211/34 ,  C07D405/08 ,  C07D401/12 ,  C07D401/08 ,  C07D211/42 ,  C07D221/20 ,  C07D401/04 ,  C07D211/38 ,  C07D211/62

Abstract: The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US10793550B2

公开(公告)日：2020-10-06

申请号：US16495802

申请日：2018-03-22

Applicant: GENENTECH, INC.

Inventor： Daniel Sutherlin ,  Steven McKerrall ,  Kwong Wah Lai

IPC: C07D401/14 ,  C07D405/14 ,  A61P9/00 ,  A61P11/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/24

Abstract: The invention provides 4-piperidin-chroman-7-sulfonamide derivatives and salts thereof that are sodium channel modulators, as well as compositions containing such a compound or salt and therapeutic methods for using such a compound, salt, or composition.

公开(公告)号：US11203572B2

公开(公告)日：2021-12-21

申请号：US17011355

申请日：2020-09-03

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Steven McKerrall ,  Daniel Sutherlin

IPC: C07C381/10 ,  C07D401/12 ,  C07D205/04 ,  C07D211/22 ,  C07D211/42 ,  C07D213/69 ,  A61P25/04

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, ring B, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US09790183B2

公开(公告)日：2017-10-17

申请号：US15015586

申请日：2016-02-04

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: C07D213/16 ,  C07D401/12 ,  A61K31/44 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  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.

公开(公告)号：US09546164B2

公开(公告)日：2017-01-17

申请号：US14603273

申请日：2015-01-22

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe Andrez ,  Paul Robert Bichler ,  Chien-An Chen ,  Sultan Chowdhury ,  Shannon Marie Decker ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Ivan William Hemeon ,  Qi Jia ,  Jun Li ,  Zhiguo Liu ,  Daniel F. Ortwine ,  Brian Safina ,  Daniel Sutherlin ,  Tao Sheng ,  Shaoyi Sun ,  Andrew D. White ,  Michael Scott Wilson ,  Alla Yurevna Zenova ,  Jiuxiang Zhu

IPC: C07D211/32 ,  C07D211/54 ,  C07D233/68 ,  C07D453/02 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/495 ,  C07D237/08 ,  C07D241/04 ,  C07D205/04 ,  C07D207/12 ,  C07D211/42 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D487/08 ,  C07D265/30 ,  C07D211/60

CPC classification number: A61K31/445 ,  A61K31/337 ,  A61K31/397 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4412 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/495 ,  C07D205/04 ,  C07D207/12 ,  C07D211/22 ,  C07D211/32 ,  C07D211/42 ,  C07D211/54 ,  C07D211/60 ,  C07D233/68 ,  C07D237/08 ,  C07D241/04 ,  C07D265/30 ,  C07D305/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D453/02 ,  C07D487/08 ,  C07F7/0812

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract translation: 本发明提供具有通式I的化合物及其药学上可接受的盐，其中变量RA，RAA，下标n，环A，X2，L，下标m，X1，R1，R2，R3，R4，R5和RN 具有本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：US11130726B2

公开(公告)日：2021-09-28

申请号：US16685335

申请日：2019-11-15

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Ivan William Hemeon ,  Brian Salvatore Safina ,  Daniel Sutherlin

IPC: C07C62/38 ,  C07C62/34 ,  C07C229/48 ,  C07D211/22 ,  C07C317/44 ,  C07C323/61 ,  C07C69/757 ,  A61P25/00 ,  A61P29/00 ,  A61P17/04 ,  C07C313/04

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

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：US10787446B2

公开(公告)日：2020-09-29

申请号：US15939112

申请日：2018-03-28

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Philippe Bergeron ,  Kristen Burford ,  Sultan Chowdhury ,  Christoph Martin Dehnhardt ,  Thilo Focken ,  Michael Edward Grimwood ,  Abid Hasan ,  Kwong Wah Lai ,  Zhiguo Liu ,  Steven McKerrall ,  Teresa Phuongtram Nguyen ,  Brian Safina ,  Daniel Sutherlin ,  Tao Wang

IPC: C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  A61P17/04 ,  C07D401/12 ,  C07D491/107

Abstract: The invention provides a compound of formula: or a salt thereof, wherein the variables RAA, n, ring A, ring B, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and R9 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.