公开(公告)号：US11034692B1

公开(公告)日：2021-06-15

申请号：US16542129

申请日：2019-08-15

申请人： Genentech, Inc.

发明人： Bryan Chan ,  Blake Daniels ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu

IPC分类号： C07D471/04 ,  A61K45/06 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K31/55

摘要： Naphthyridine compounds and their use as inhibitors of HPK1 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：US20170369510A1

公开(公告)日：2017-12-28

申请号：US15699095

申请日：2017-09-08

申请人： Genentech, Inc.

发明人： Anthony Estrada ,  Snahel Patel ,  Terry Kellar ,  Malcolm Huestis ,  Daniel Shore ,  Michael Siu

IPC分类号： C07D498/14 ,  A61K45/06 ,  A61K31/553 ,  C07D519/00 ,  A61K31/5383

CPC分类号： C07D498/14 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  C07D491/14 ,  C07D519/00

摘要： The invention relates to compounds of formula (I) and salts thereof: wherein ring A and R1-R2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.

公开(公告)号：US20150080367A1

公开(公告)日：2015-03-19

申请号：US14550528

申请日：2014-11-21

申请人： Genentech, Inc.

发明人： Frederick Cohen ,  Malcolm Huestis ,  Cuong Ly ,  Snahel Patel ,  Michael Siu ,  Xianrui Zhao

IPC分类号： C07D401/14 ,  C07D491/107 ,  C07D487/08 ,  C07D405/14

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D487/08 ,  C07D491/107

摘要： The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.

摘要翻译： 本发明提供式I化合物及其各种实施方案，以及包含式I化合物及其各种实施方案的组合物。 在式I化合物中，基团R 1，R 2，R 3，R 4，R 5，R 6，m，n和C连接的环具有如本文所述的含义。 本发明还提供使用式I化合物的方法和包含式I化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症。

公开(公告)号：US20240300927A1

公开(公告)日：2024-09-12

申请号：US18275655

申请日：2022-02-03

申请人： Genentech, Inc.

发明人： Jun Liang ,  Araz Jakalian ,  Michael John Lambrecht ,  Robin Larouche-Gauthier ,  Malcolm Huestis ,  Man Un Ung ,  Xiaojing Wang ,  Arun Yadav ,  Jason Robert Zbieg ,  Fabio Broccatelli

IPC分类号： C07D405/14 ,  A61K31/4439

CPC分类号： C07D405/14 ,  A61K31/4439

摘要： Various amide compounds that bind Cbl-B, including those that are selective for C-Cbl, and methods of making and using the same. Representative amide compounds include molecules falling within the following formulae:

公开(公告)号：US10010549B2

公开(公告)日：2018-07-03

申请号：US14927267

申请日：2015-10-29

申请人： Genentech, Inc.

发明人： 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分类号： A61K31/506 ,  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 ,  C07D471/08 ,  A61K45/06 ,  A61K31/5386 ,  A61K31/553 ,  C07D417/14 ,  C07D487/14 ,  C07D487/18 ,  A61K31/444

CPC分类号： 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

摘要： 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：US10407424B2

公开(公告)日：2019-09-10

申请号：US15942321

申请日：2018-03-30

申请人： Genentech, Inc.

发明人： Bryan Chan ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John Tellis ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Matthew W. Cartwright ,  Emanuela Gancia ,  Graham Jones ,  Blake Daniels ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Seward ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu ,  Baihua Hu ,  Aijun Lu ,  Joy Drobnick ,  Lewis Gazzard ,  Timothy Heffron ,  Malcolm Huestis ,  Jun Liang ,  Sushant Malhotra ,  Rohan Mendonca

IPC分类号： C07D471/04 ,  A61K31/55 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5383 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/551 ,  A61K45/06

摘要： Naphthyridine compounds and their use as inhibitors of HPK1 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：US10131675B2

公开(公告)日：2018-11-20

申请号：US15699095

申请日：2017-09-08

申请人： Genentech, Inc.

发明人： Anthony Estrada ,  Snahel Patel ,  Terry Kellar ,  Malcolm Huestis ,  Daniel Shore ,  Michael Siu

IPC分类号： C07D498/14 ,  C07D491/14 ,  C07D519/00 ,  A61K31/5383 ,  A61K45/06 ,  A61K31/553

摘要： The invention relates to compounds of formula (I) and salts thereof: wherein ring A and R1-R2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.

公开(公告)号：US09399636B2

公开(公告)日：2016-07-26

申请号：US14550528

申请日：2014-11-21

申请人： Genentech, Inc.

发明人： Frederick Cohen ,  Malcolm Huestis ,  Cuong Ly ,  Snahel Patel ,  Michael Siu ,  Xianrui Zhao

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D487/08 ,  C07D491/107

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D487/08 ,  C07D491/107

摘要： The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.

摘要翻译： 本发明提供式I化合物及其各种实施方案，以及包含式I化合物及其各种实施方案的组合物。 在式I化合物中，基团R 1，R 2，R 3，R 4，R 5，R 6，m，n和C连接的环具有如本文所述的含义。 本发明还提供使用式I化合物的方法和包含式I化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症。

公开(公告)号：US11129832B2

公开(公告)日：2021-09-28

申请号：US16666273

申请日：2019-10-28

申请人： Genentech, Inc.

发明人： 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分类号： 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

摘要： 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

申请人： Genentech, Inc.

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

IPC分类号： 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

摘要： 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.