公开(公告)号：US11760744B2

公开(公告)日：2023-09-19

申请号：US16642824

申请日：2019-08-15

申请人： Genentech, Inc.

发明人： Aijun Lu ,  Sushant Malhotra ,  Alan G. Olivero ,  Cheng Shao ,  Yamin Zhang ,  Steven Do

IPC分类号： C07D401/04 ,  C07D239/94 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D413/12 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D239/94 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D413/12 ,  C07D471/04

摘要： Provided are fused ring compounds of Formula (I), Formula (II), or Formula (III), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods treatment by their administration.

公开(公告)号：US11566003B2

公开(公告)日：2023-01-31

申请号：US16921297

申请日：2020-07-06

申请人： Genentech, Inc.

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

IPC分类号： C07D217/22 ,  A61K31/549 ,  A61P35/00 ,  A61K45/06 ,  C07D401/04 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/501 ,  C07D471/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K31/4985 ,  C07D401/14 ,  C07D487/04 ,  A61K31/551 ,  C07D498/04 ,  A61K31/5383 ,  C07D405/14 ,  C07D519/00 ,  C07D498/14 ,  C07D513/04 ,  A61K31/554 ,  A61K31/55 ,  A61K31/472 ,  C07D409/14 ,  C07D491/04 ,  C07D487/14

摘要： Isoquinoline compounds 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.

公开(公告)号：US20220073520A1

公开(公告)日：2022-03-10

申请号：US17213362

申请日：2021-03-26

申请人： Genentech, Inc.

发明人： 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分类号： C07D487/04 ,  C07D403/04 ,  C07D401/04 ,  C07D405/14 ,  C07D237/28 ,  C07D401/14 ,  C07D417/04

摘要： 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：US20160311817A1

公开(公告)日：2016-10-27

申请号：US15202911

申请日：2016-07-06

申请人： Genentech, Inc.

发明人： Benjamin Fauber ,  Olivier Rene ,  Sushant Malhotra ,  Herbert Yajima

IPC分类号： C07D417/14 ,  C07D417/04

CPC分类号： C07D417/14 ,  C07D417/04 ,  C07D417/10

摘要： Compounds of the formula I or a pharmaceutical salt thereof, wherein m, n, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

摘要翻译： 或其药物盐，其中m，n，q，r，A，W，X1，X2，X3，X4，Y，Z，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10 和R 11如本文所定义。 还公开了制备化合物和使用该化合物治疗炎性疾病如关节炎的方法。

公开(公告)号：US12084429B2

公开(公告)日：2024-09-10

申请号：US17644993

申请日：2021-12-17

申请人： Genentech, Inc.

发明人： Sushant Malhotra ,  Jianfeng Xin ,  Steven Do ,  Jack Terrett

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

CPC分类号： C07D401/14 ,  A61K9/0019 ,  A61K9/0053 ,  A61P35/00 ,  C07D405/14

摘要： 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

申请人： Genentech, Inc.

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

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

CPC分类号： C07D498/04

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

摘要翻译： 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

申请人： Genentech, Inc.

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

IPC分类号： C07D498/04

CPC分类号： C07D498/04

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

摘要翻译： 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：US20230002345A1

公开(公告)日：2023-01-05

申请号：US16642824

申请日：2019-08-15

申请人： Genentech, Inc.

发明人： Aijun LU ,  Sushant Malhotra ,  Alan G. Olivero ,  Cheng Shao ,  Yamin Zhang ,  Steven Do

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D239/94 ,  C07D405/04 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14 ,  C07D413/12 ,  C07D471/04

摘要： Provided are fused ring compounds of Formula (I), Formula (II), or Formula (III), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods treatment by their administration.

公开(公告)号：US20210163417A1

公开(公告)日：2021-06-03

申请号：US16921297

申请日：2020-07-06

申请人： Genentech, Inc.

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

IPC分类号： C07D217/22 ,  A61K31/549 ,  A61P35/00 ,  A61K45/06 ,  C07D401/04 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/501 ,  C07D471/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K31/4985 ,  C07D401/14 ,  C07D487/04 ,  A61K31/551 ,  C07D498/04 ,  A61K31/5383 ,  C07D405/14 ,  C07D519/00 ,  C07D498/14 ,  C07D513/04 ,  A61K31/554 ,  A61K31/55 ,  A61K31/472 ,  C07D409/14 ,  C07D491/04 ,  C07D487/14

摘要： Isoquinoline compounds 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.

公开(公告)号：US10882864B2

公开(公告)日：2021-01-05

申请号：US16460889

申请日：2019-07-02

申请人： Genentech, Inc.

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

IPC分类号： C07D487/04 ,  B01J31/24

摘要： 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.