公开(公告)号：US20200010420A1

公开(公告)日：2020-01-09

申请号：US16574373

申请日：2019-09-18

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: C07D213/16 ,  C07F9/58 ,  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

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：US20180105504A1

公开(公告)日：2018-04-19

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

IPC: C07D277/52 ,  C07D239/69 ,  C07D285/08 ,  C07D417/12 ,  C07D213/76 ,  C07D401/12 ,  C07D403/12 ,  C07D261/16

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

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：US20220055977A1

公开(公告)日：2022-02-24

申请号：US17396283

申请日：2021-08-06

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Ivan William HEMEON ,  Brian 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 a method of treating a disease or condition in a mammal by administering a compound having the general formula I: or a pharmaceutically acceptable salt 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.

公开(公告)号：US20210155588A1

公开(公告)日：2021-05-27

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：US20200017469A1

公开(公告)日：2020-01-16

申请号：US16495802

申请日：2018-03-22

Applicant: GENENTECH, INC.

Inventor： Daniel SUTHERLIN ,  Steven MCKERRALL ,  Kwong Wah LAI

IPC: C07D401/14

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：US20170087136A1

公开(公告)日：2017-03-30

申请号：US15275131

申请日：2016-09-23

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: A61K31/445 ,  A61K31/4545 ,  A61K31/4523

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 variablesRA, RAA, subscipt 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.

公开(公告)号：US20150252038A1

公开(公告)日：2015-09-10

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: C07D453/02 ,  C07D205/04 ,  C07D401/06 ,  C07D403/12 ,  C07D401/12 ,  C07D211/42

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 compactions.

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：US20240116872A1

公开(公告)日：2024-04-11

申请号：US18381304

申请日：2023-10-18

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: 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

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：US20220081423A1

公开(公告)日：2022-03-17

申请号：US17331164

申请日：2021-05-26

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: C07D403/12 ,  C07D233/96 ,  C07D401/12 ,  A61P17/04 ,  C07D263/52 ,  C07D305/06 ,  C07D401/14 ,  A61K31/506 ,  A61K31/538 ,  C07D413/12 ,  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：US20190112264A1

公开(公告)日：2019-04-18

申请号：US16088417

申请日：2017-03-28

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 ,  C07D205/04 ,  C07D213/69 ,  C07D211/42 ,  C07D211/22 ,  C07D401/12 ,  A61P25/04

CPC classification number: C07C381/10 ,  A61P25/04 ,  C07D205/04 ,  C07D211/22 ,  C07D211/42 ,  C07D213/69 ,  C07D401/12

Abstract: The invention provides compounds having the general formula I: (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.