公开(公告)号：US11129832B2

公开(公告)日：2021-09-28

申请号：US16666273

申请日：2019-10-28

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Liting Dong ,  Kevin X. Chen ,  Paul Gibbons ,  Malcolm Huestis ,  Terry Kellar ,  Wen Liu ,  Changyou Ma ,  Joseph P. Lyssikatos ,  Alan G. Olivero ,  Snahel Patel ,  Daniel Shore ,  Michael Siu

IPC: C07D471/08 ,  A61K31/506 ,  A61K45/06 ,  A61K31/5386 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/55 ,  A61K35/30 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  A61K31/553 ,  C07D417/14 ,  C07D487/14 ,  C07D487/18 ,  A61K31/444

Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.

公开(公告)号：USRE47848E1

公开(公告)日：2020-02-11

申请号：US15902746

申请日：2018-02-22

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Alan G. Olivero ,  Snahel Patel ,  Michael Siu ,  Joseph Lyssikatos ,  Malcolm Huestis ,  Terry Kellar

IPC: A61K31/55 ,  C07D403/14 ,  A61K35/30 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  C07D471/08 ,  A61K45/06 ,  A61K31/5386 ,  C07D487/08 ,  C07D413/14 ,  C07D471/18 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/553 ,  A61K31/155

Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.

公开(公告)号：US20190322661A1

公开(公告)日：2019-10-24

申请号：US16438135

申请日：2019-06-11

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-wai Yuen

IPC: C07D471/04 ,  C07D487/04 ,  C07D403/14 ,  A61K31/519 ,  C07D519/00 ,  A61P11/06

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US20180265515A1

公开(公告)日：2018-09-20

申请号：US15986256

申请日：2018-05-22

Applicant: Genentech, Inc.

Inventor： Yun-Xing Cheng ,  Paul Gibbons ,  Terry Kellar ,  Wei Li ,  Rohan Mendonca ,  Po-wai Yuen ,  Mark Edward Zak ,  Lei Zhang

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.

公开(公告)号：US20180133219A1

公开(公告)日：2018-05-17

申请号：US15868301

申请日：2018-01-11

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Liting Dong ,  Kevin X. Chen ,  Paul Gibbons ,  Malcolm Huestis ,  Terry Kellar ,  Wen Liu ,  Changyou Ma ,  Joseph Lyssikatos ,  Alan Olivero ,  Snahel Patel ,  Daniel Shore ,  Michael Siu

IPC: A61K31/506 ,  A61K31/444 ,  A61K35/30 ,  C07D487/14 ,  A61K31/553 ,  C07D417/14 ,  C07D487/18 ,  A61K31/55 ,  C07D401/14 ,  A61K31/5377 ,  C07D495/08 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/5386 ,  A61K45/06 ,  C07D471/08 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08

CPC classification number: A61K31/506 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/553 ,  A61K35/30 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D471/18 ,  C07D487/08 ,  C07D487/14 ,  C07D487/18 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  A61K2300/00

Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.

公开(公告)号：US09604984B2

公开(公告)日：2017-03-28

申请号：US15139164

申请日：2016-04-26

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-Wei Yuen

IPC: C07D487/04 ,  A61K31/519 ,  A61P11/06 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US11731943B2

公开(公告)日：2023-08-22

申请号：US17177356

申请日：2021-02-17

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Mark Zak ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  F. Anthony Romero ,  Paul Gibbons ,  Guiling Zhao ,  Gregory Hamilton ,  Simon Charles Goodacre

IPC: C07D231/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/08 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D231/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/08 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: Compounds of Formula (I):




and salts thereof, and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US20210277024A1

公开(公告)日：2021-09-09

申请号：US17156384

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Terry Kellar ,  Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D519/00 ,  C07D471/04 ,  A61P37/04

Abstract: Naphthyridine compounds of formula (I). variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

公开(公告)号：US20210179564A1

公开(公告)日：2021-06-17

申请号：US17177356

申请日：2021-02-17

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Mark Zak ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  F. Anthony Romero ,  Paul Gibbons ,  Guiling Zhao ,  Gregory Hamilton ,  Simon Charles Goodacre

IPC: C07D231/40 ,  C07D401/14 ,  C07D401/04 ,  C07D403/08 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14

Abstract: Compounds of Formula (I): and salts thereof, and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US20190071404A1

公开(公告)日：2019-03-07

申请号：US16181228

申请日：2018-11-05

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Mark Zak ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  F. Anthony Romero ,  Paul Gibbons ,  Guiling Zhao ,  Gregory Hamilton ,  Simon Charles Goodacre

IPC: C07D231/40 ,  C07D401/04 ,  C07D405/04 ,  C07D403/08 ,  C07D409/14 ,  C07D401/14 ,  C07D405/12

Abstract: Compounds of Formula (I): and salts thereof, and methods of use as Janus kinase inhibitors are described herein.