公开(公告)号：US20170190662A1

公开(公告)日：2017-07-06

申请号：US15321335

申请日：2015-07-07

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe ANDREZ ,  Philippe BERGERON ,  Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Thilo FOCKEN ,  Wei GONG ,  Michael Edward GRIMWOOD ,  Abid HASAN ,  Ivan William HEMEON ,  Qi JIA ,  Brian SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D207/16 ,  C07C235/54 ,  C07D401/12 ,  C07D277/06 ,  C07D403/14 ,  C07D401/10 ,  C07D413/12 ,  C07D413/14 ,  C07D405/10 ,  C07D471/08

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2103/74 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/02 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D221/22 ,  C07D231/06 ,  C07D263/04 ,  C07D263/26 ,  C07D265/30 ,  C07D277/06 ,  C07D305/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/08

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

公开(公告)号：US20210214336A1

公开(公告)日：2021-07-15

申请号：US17056325

申请日：2019-05-21

Applicant: GENENTECH, INC.

Inventor： Steven MCKERRALL ,  Ramsay BEVERIDGE ,  Kwong Wah LAI ,  Philippe BERGERON

IPC: C07D401/12 ,  A61P17/04 ,  A61K9/00 ,  A61P29/00

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables Y1-Y6, X, Z, Z1, Z2, R2-R3, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions. The compounds have sodium channel blocking activity that are useful for treating sodium channel-mediated diseases, in particular for treating pain

公开(公告)号：US20190031607A1

公开(公告)日：2019-01-31

申请号：US16150070

申请日：2018-10-02

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe ANDREZ ,  Philippe BERGERON ,  Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Thilo FOCKEN ,  Wei GONG ,  Michael Edward GRIMWOOD ,  Abid HASAN ,  Ivan William HEMEON ,  Qi JIA ,  Brian Salvatore SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D207/16 ,  C07C235/52 ,  C07D209/02 ,  C07D401/10 ,  C07D205/04 ,  C07D207/22 ,  C07D211/20 ,  C07C235/42 ,  C07D211/38 ,  C07D409/06 ,  C07D265/30 ,  C07D413/12 ,  C07D263/26 ,  C07C235/54 ,  C07D417/12 ,  C07D305/08 ,  C07D213/69 ,  C07D403/04 ,  C07D231/06 ,  C07D209/52 ,  C07D221/22 ,  C07D209/54 ,  C07D403/12 ,  C07D211/60 ,  C07D207/10 ,  C07D401/12 ,  C07D471/08 ,  C07D413/14 ,  C07D207/08 ,  C07D405/10 ,  C07D403/14 ,  C07D451/02 ,  C07D401/14 ,  C07D263/04 ,  C07D277/06

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/02 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D221/22 ,  C07D231/06 ,  C07D263/04 ,  C07D263/26 ,  C07D265/30 ,  C07D277/06 ,  C07D305/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/08

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

公开(公告)号：US20240239766A1

公开(公告)日：2024-07-18

申请号：US18584298

申请日：2024-02-22

Applicant: Genentech, Inc.

Inventor： Steven John MCKERRALL ,  Daniel Fred ORTWINE ,  Philippe BERGERON ,  Ramsay BEVERIDGE ,  Elise GHIRO ,  Kwong Wah LAI ,  Guqin SHI

IPC: C07D401/12 ,  A61K31/454 ,  A61K31/506 ,  A61P17/04 ,  A61P29/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D401/12 ,  A61K31/454 ,  A61K31/506 ,  A61P17/04 ,  A61P29/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein Z1, Z2, R3-R8, RA, ring A, and n have the meanings described herein, and compositions containing such compounds and methods for using such compounds and compositions for the treatment of pain.

公开(公告)号：US20180265465A1

公开(公告)日：2018-09-20

申请号：US15988956

申请日：2018-05-24

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe ANDREZ ,  Philippe BERGERON ,  Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Thilo FOCKEN ,  Wei GONG ,  Michael Edward GRIMWOOD ,  Abid HASAN ,  Ivan William HEMEON ,  Qi JIA ,  Brian SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D207/16 ,  C07D277/06 ,  C07D413/14 ,  C07D413/12 ,  C07D401/10 ,  C07D471/08 ,  C07D401/12 ,  C07C235/54 ,  C07D405/10 ,  C07D403/14

CPC classification number: C07D207/16 ,  C07C235/42 ,  C07C235/52 ,  C07C235/54 ,  C07C2103/74 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/02 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D221/22 ,  C07D231/06 ,  C07D263/04 ,  C07D263/26 ,  C07D265/30 ,  C07D277/06 ,  C07D305/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/08

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

公开(公告)号：US20170088582A1

公开(公告)日：2017-03-30

申请号：US15312614

申请日：2015-05-19

Applicant: RQX PHARMACEUTICALS, INC. ,  GENENTECH, INC.

Inventor： Tucker Curran ROBERTS ,  Peter Andrew SMITH ,  Robert I. HIGUCHI ,  Prasuna PARASELLI ,  Philippe BERGERON ,  Michael F.T. KOEHLER ,  Huiyong HU ,  Jacob Bradley SCHWARZ ,  Cuong LY ,  James CRAWFORD

IPC: C07K5/103 ,  A61K38/07 ,  A61K38/06 ,  C07K7/06 ,  A61K38/08 ,  A61K45/06 ,  C07K5/083

CPC classification number: C07K5/101 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4196 ,  A61K31/43 ,  A61K31/431 ,  A61K31/496 ,  A61K31/545 ,  A61K31/546 ,  A61K38/00 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K45/06 ,  C07K5/0202 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/1008 ,  C07K5/1013 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  Y02A50/401 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/483 ,  A61K2300/00 ,  A61L2300/00

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 peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US20250115576A1

公开(公告)日：2025-04-10

申请号：US18985502

申请日：2024-12-18

Applicant: Genentech, Inc.

Inventor： Steven MCKERRALL ,  Ramsay BEVERIDGE ,  Kwong Wah LAI ,  Philippe BERGERON

IPC: C07D401/12 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D413/12

Abstract: The invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables Y1-Y6, X, Z, Z1, Z2, R2-R3, 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：US20240228463A1

公开(公告)日：2024-07-11

申请号：US18584311

申请日：2024-02-22

Applicant: Genentech, Inc.

Inventor： Marc KSCHONSAK ,  Steven John MCKERRALL ,  Daniel Fred ORTWINE ,  Jian Mehr-Dean PAYANDEH ,  Benjamin Douglas SELLERS ,  John C. TELLIS ,  Matthew VOLGRAF ,  Philippe BERGERON ,  Claudio CIFERRI ,  Peter Scott DRAGOVICH

IPC: C07D401/12 ,  A61K31/18 ,  A61P25/04 ,  C07C311/51 ,  C07D211/96 ,  C07D277/44 ,  C07D277/82 ,  C07D295/26 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D401/12 ,  A61K31/18 ,  A61P25/04 ,  C07C311/51 ,  C07D211/96 ,  C07D277/44 ,  C07D277/82 ,  C07D295/26 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The invention provides compounds of formulae I, II, IIa, and III:




and pharmaceutically acceptable salts thereof, as well as compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US20210171516A1

公开(公告)日：2021-06-10

申请号：US17031348

申请日：2020-09-24

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 Salvatore SAFINA ,  Daniel SUTHERLIN ,  Tao WANG

IPC: C07D417/12 ,  C07D417/14 ,  A61P17/04 ,  C07D401/12 ,  C07D405/14 ,  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.

公开(公告)号：US20210078947A1

公开(公告)日：2021-03-18

申请号：US16702286

申请日：2019-12-03

Applicant: GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Jean-Christophe ANDREZ ,  Philippe BERGERON ,  Paul Robert BICHLER ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Thilo FOCKEN ,  Wei GONG ,  Michael Edward GRIMWOOD ,  Abid HASAN ,  Ivan William HEMEON ,  Qi JIA ,  Brian Salvatore SAFINA ,  Shaoyi SUN ,  Michael Scott WILSON ,  Alla Yurevna ZENOVA

IPC: C07D207/16 ,  C07D403/12 ,  C07D413/14 ,  C07D221/22 ,  C07D401/12 ,  C07D413/12 ,  C07C235/52 ,  C07D205/04 ,  C07D277/06 ,  C07D209/02 ,  C07D305/08 ,  C07D401/14 ,  C07D231/06 ,  C07D403/04 ,  C07D403/14 ,  C07D409/06 ,  C07D417/12 ,  C07D451/02 ,  C07D263/04 ,  C07D263/26 ,  C07C235/42 ,  C07C235/54 ,  C07D265/30 ,  C07D207/08 ,  C07D207/10 ,  C07D207/22 ,  C07D209/52 ,  C07D209/54 ,  C07D211/20 ,  C07D211/38 ,  C07D211/60 ,  C07D213/69 ,  C07D401/10 ,  C07D405/10 ,  C07D471/08

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