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：US20200308161A1

公开(公告)日：2020-10-01

申请号：US16903020

申请日：2020-06-16

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: C07D413/14 ,  C07D473/30 ,  C07D471/04 ,  A61P29/00 ,  C07D513/04 ,  C07D487/04 ,  A61P25/00 ,  C07D498/04 ,  A61K31/427 ,  A61P23/00 ,  A61P11/00

Abstract: The invention relates to methods of using compounds formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

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：US12202824B2

公开(公告)日：2025-01-21

申请号：US17816855

申请日：2022-08-02

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: C07D413/14 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  A61P11/00 ,  A61P19/02 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D471/04 ,  C07D473/08 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20220135528A1

公开(公告)日：2022-05-05

申请号：US17644861

申请日：2021-12-17

Applicant: Genentech, Inc.

Inventor： Michael F.T. Koehler ,  Peter Andrew Smith ,  Dana Winter ,  Boubacar Sow ,  Claudio Sturino ,  Guillaume Pelletier ,  Jonathan Boudreault

IPC: C07D239/42 ,  A61K31/497 ,  A61K38/12 ,  A61K38/14 ,  C07D239/28 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/351 ,  A61P31/04 ,  A61K31/702 ,  A61K31/5377 ,  A61K31/545 ,  A61K31/165 ,  A61K45/06

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US11208387B2

公开(公告)日：2021-12-28

申请号：US16884679

申请日：2020-05-27

Applicant: Genentech, Inc.

Inventor： Michael F. T. Koehler ,  Peter Andrew Smith ,  Dana Winter ,  Boubacar Sow ,  Claudio Sturino ,  Guillaume Pelletier ,  Jonathan Boudreault

IPC: A61K31/505 ,  C07D239/28 ,  C07D239/42 ,  A61K45/06 ,  A61P31/04 ,  A61K31/702 ,  A61K31/4709 ,  A61K38/14 ,  A61K31/497 ,  A61K31/165 ,  A61K31/351 ,  A61K38/12 ,  A61K31/5377 ,  A61K31/545

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US11655245B2

公开(公告)日：2023-05-23

申请号：US16903020

申请日：2020-06-16

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D513/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D471/04 ,  C07D413/14

CPC classification number: C07D413/14 ,  A61K31/427 ,  A61P11/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The invention relates to methods of using compounds formula I:




and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20200377463A1

公开(公告)日：2020-12-03

申请号：US16884679

申请日：2020-05-27

Applicant: Genentech, Inc.

Inventor： Michael F.T. Koehler ,  Peter Andrew Smith ,  Dana Winter ,  Boubacar Sow ,  Claudio Sturino ,  Guillaume Pelletier ,  Jonathan Boudreault

IPC: C07D239/42 ,  A61K45/06 ,  A61K31/505 ,  A61P31/04 ,  A61K31/702 ,  A61K31/4709 ,  A61K31/545 ,  A61K38/14 ,  A61K31/497 ,  A61K31/165 ,  A61K31/351 ,  A61K38/12 ,  A61K31/5377 ,  C07D239/28

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US10710994B2

公开(公告)日：2020-07-14

申请号：US16355352

申请日：2019-03-15

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: A61P23/00 ,  A61P11/00 ,  A61P29/00 ,  A61P25/00 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D413/14 ,  C07D498/04 ,  C07D513/04 ,  A61K31/427

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20190284179A1

公开(公告)日：2019-09-19

申请号：US16355352

申请日：2019-03-15

Applicant: Genentech, Inc.

Inventor： Jack Alexander Terrett ,  Huifen Chen ,  Lea Constantineau-Forget ,  Robin Larouche-Gauthier ,  Luce Lépissier ,  Francis Beaumier ,  Martin Déry ,  Chantal Grand-Maître ,  Claudio Sturino ,  Matthew Volgraf ,  Elisia Villemure

IPC: C07D413/14 ,  C07D473/30 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  A61P25/00 ,  A61P29/00

Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.