公开(公告)号：US20220370420A1

公开(公告)日：2022-11-24

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 ,  A61K45/06 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  C07D487/20 ,  C07D471/20 ,  A61K31/5377 ,  A61K31/444 ,  A61K31/496 ,  A61K31/513 ,  A61K31/4985

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：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：US20150051201A1

公开(公告)日：2015-02-19

申请号：US14531349

申请日：2014-11-03

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Bryan K. Chan ,  Jennafer Dotson ,  Anthony Estrada ,  Timothy Heffron ,  Joseph Lyssikatos ,  Zachary Sweeney

IPC: C07D487/04 ,  C07D498/04 ,  C07D498/20 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/506 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D498/04 ,  C07D498/20

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中X，R 1，R 2，R 3和A如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US20130158057A1

公开(公告)日：2013-06-20

申请号：US13687421

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Mark Chambers ,  Bryan K. Chan ,  Anthony Estrada ,  Zachary Kevin Sweeney

IPC: C07D417/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/12 ,  C07D413/12

CPC classification number: A61K31/505 ,  C07D239/47 ,  C07D239/48 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

公开(公告)号：US20130096102A1

公开(公告)日：2013-04-18

申请号：US13712015

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Mark Chambers ,  Bryan K. Chan ,  Huifen Chen ,  Anthony Estrada ,  Janet Gunzner-Toste ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: C07D413/14 ,  C07D498/08 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D403/14 ,  C07D413/12 ,  C07D473/16 ,  C07D498/06 ,  C07D498/08

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 5，R 6和R 7如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US20220073520A1

公开(公告)日：2022-03-10

申请号：US17213362

申请日：2021-03-26

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 ,  C07D403/04 ,  C07D401/04 ,  C07D405/14 ,  C07D237/28 ,  C07D401/14 ,  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：US09145402B2

公开(公告)日：2015-09-29

申请号：US13687411

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Mark Chambers ,  Bryan K. Chan ,  Anthony Estrada ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Huifen Chen

IPC: A61K31/535 ,  A61K31/505 ,  C07D413/10 ,  C07D413/12 ,  C07D239/02 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D239/42 ,  C07D405/12 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D413/12 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中m，n。 X，R 1，R 2，R 3，R 4和R 5如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US09139566B2

公开(公告)日：2015-09-22

申请号：US13687441

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Zachary Kevin Sweeney ,  Bryan K. Chan ,  Anthony Estrada

IPC: A61K51/00 ,  A61M36/14 ,  C07D403/12 ,  A61K51/04 ,  C07D239/48

CPC classification number: C07D403/12 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  C07D239/48

Abstract: A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the compound includes at least one C11 or F18 label thereon; allowing the compound to penetrate into the tissue of the subject; and collecting a PET image of the CNS or brain tissue of the subject.

Abstract translation: 一种用于受试者组织中LRRK2的正电子发射断层摄影（PET）成像的方法，所述方法包括：向受试者施用式I，式II或式III化合物或其药学上可接受的盐，其中所述化合物包括 在其上至少有一个C11或F18标签; 允许化合物渗透到受试者的组织中; 并收集受试者的CNS或脑组织的PET图像。

公开(公告)号：US08809331B2

公开(公告)日：2014-08-19

申请号：US13687437

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Daniel Jon Burdick ,  Mark Chambers ,  Bryan K. Chan ,  Huifen Chen ,  Anthony Estrada ,  Janet L. Gunzner-Toste ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: A61K31/535

CPC classification number: C07D498/18 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08 ,  C07D498/10

Abstract: Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I的具体化合物或其药学上可接受的盐，其中m，X，R 1，R 2，R 3，R 5，R 6和R 7如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。