公开(公告)号：US12208088B2

公开(公告)日：2025-01-28

申请号：US17204089

申请日：2021-03-17

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Craig Stivala ,  BinQing Wei ,  Bryan K. Chan ,  Timothy Heffron ,  Michael Lainchbury ,  Andrew Madin ,  Terry Aaron Panchal ,  Eileen Mary Seward ,  Toby Blench ,  Matthew W. Cartwright ,  Elsa Amandine Dechaux ,  Richard Elliott ,  Emanuela Gancia

IPC: A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D487/04 ,  C07D487/20 ,  C07D491/20 ,  C07D519/00

Abstract: Spirocyclic 2,3-dihydro-7-azaindole 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 spirocyclic 2,3-dihydro-7-azaindole compounds.

公开(公告)号：US20240368170A1

公开(公告)日：2024-11-07

申请号：US18769184

申请日：2024-07-10

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Michael Siu ,  Weiru Wang ,  BinQing Wei ,  Aihe Zhou ,  Bryan K. Chan ,  Lewis J. Gazzard ,  Timothy Heffron ,  Michael Lainchbury ,  Andrew Madin ,  Eileen Mary Seward ,  Matthew W. Cartwright ,  Emanuela Gancia ,  David Favor ,  Kin Chiu Fong ,  Andrew Good ,  Yonghan Hu

IPC: C07D487/04 ,  C07D237/28 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D417/04

Abstract: Cinnoline 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 cinnoline compounds.

公开(公告)号：US12084429B2

公开(公告)日：2024-09-10

申请号：US17644993

申请日：2021-12-17

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Jianfeng Xin ,  Steven Do ,  Jack Terrett

IPC: C07D401/04 ,  A61K9/00 ,  A61K31/517 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D471/14

CPC classification number: C07D401/14 ,  A61K9/0019 ,  A61K9/0053 ,  A61P35/00 ,  C07D405/14

Abstract: This invention pertains to fused ring compounds of Formula (I), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.

公开(公告)号：US09303043B2

公开(公告)日：2016-04-05

申请号：US14205634

申请日：2014-03-12

Applicant: Genentech, Inc.

Inventor： Remy Angelaud ,  Danial R. Beaudry ,  Diane E. Carrera ,  Sushant Malhotra ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D233/54 ,  C07D249/08 ,  C07D267/14 ,  C07D498/04

CPC classification number: C07D498/04

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract translation: 描述了制备具有以下结构的PI3K抑制剂GDC-0032，式I的方法：和用于制备I的中间体。

公开(公告)号：US20140275523A1

公开(公告)日：2014-09-18

申请号：US14205634

申请日：2014-03-12

Applicant: Genentech, Inc.

Inventor： Remy Angelaud ,  Danial R. Beaudry ,  Diane E. Carrera ,  Sushant Malhotra ,  Travis Remarchuk ,  Frederic St-Jean

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract translation: 描述了制备具有以下结构的PI3K抑制剂GDC-0032，式I的方法：和用于制备I的中间体。

公开(公告)号：US20250059163A1

公开(公告)日：2025-02-20

申请号：US18747054

申请日：2024-06-18

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Jianfeng Xin ,  Steven Do ,  Jack Terrett

IPC: C07D401/14 ,  A61K9/00 ,  A61P35/00 ,  C07D405/14

Abstract: This invention pertains to fused ring compounds of Formula (I), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.

公开(公告)号：US11661424B2

公开(公告)日：2023-05-30

申请号：US17102086

申请日：2020-11-23

Applicant: Genentech, Inc.

Inventor： Danial Beaudry ,  Theresa Cravillion ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Sushant Malhotra ,  Qingping Tian ,  Haiming Zhang ,  Alexander Gmehling ,  Alec Fettes ,  Stephan Bachmann

IPC: C07D487/04 ,  B01J31/24

CPC classification number: C07D487/04 ,  B01J31/2409 ,  B01J31/2414 ,  B01J2231/40 ,  B01J2531/824 ,  C07B2200/09

Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3′-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4′]bipyridinyl-2′-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.

公开(公告)号：US11236068B2

公开(公告)日：2022-02-01

申请号：US16679104

申请日：2019-11-08

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Jianfeng Xin ,  Steven Do ,  Jack Terrett

IPC: A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D471/04 ,  A61K9/00 ,  C07D405/14

Abstract: This invention pertains to fused ring compounds of Formula (I), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.

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：US20210253580A1

公开(公告)日：2021-08-19

申请号：US17156387

申请日：2021-01-22

Applicant: Genentech, Inc.

Inventor： Jun Liang ,  Sushant Malhotra ,  Rohan V. Mendonca ,  Naomi Rajapaksa ,  Michael Siu ,  Craig Stivala ,  John C. Tellis ,  BinQing Wei ,  Bryan K. Chan ,  Joy Alison Drobnick ,  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: C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  C07D487/14 ,  C07D498/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D498/04 ,  A61P37/04

Abstract: Isoquinoline 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 isoquinoline compounds.