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。

公开(公告)号：US09212186B2

公开(公告)日：2015-12-15

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

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：US09212173B2

公开(公告)日：2015-12-15

申请号：US14531271

申请日：2014-11-03

Applicant: Genentech, Inc.

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

IPC: A61K31/506 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D407/14 ,  C07D405/14

CPC classification number: C07D403/12 ,  A61K31/506 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14

Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 作为LRRK2的调节剂的吡唑化合物，制备化合物的方法，以及使用该化合物治疗与LRRK2受体相关的疾病如帕金森病的方法。

公开(公告)号：US20150051238A1

公开(公告)日：2015-02-19

申请号：US14531271

申请日：2014-11-03

Applicant: Genentech, Inc.

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

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

CPC classification number: C07D403/12 ,  A61K31/506 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14

Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 作为LRRK2的调节剂的吡唑化合物，制备化合物的方法，以及使用该化合物治疗与LRRK2受体相关的疾病如帕金森病的方法。

公开(公告)号：US08802674B2

公开(公告)日：2014-08-12

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-Tate ,  Daniel Shore ,  Zachary Kevin Sweeney ,  Shumei Wang ,  Guiling Zhao

IPC: A61K31/535 ,  C07D413/14 ,  C07D498/06 ,  C07D473/16 ,  C07D403/14 ,  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：US08796296B2

公开(公告)日：2014-08-05

申请号：US13687429

申请日：2012-11-28

Applicant: Genentech, Inc.

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

IPC: A01N43/54 ,  A61K31/505 ,  A61K31/506 ,  C07D239/47 ,  C07D239/48

CPC classification number: A61K31/506 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/08

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 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A，X，R 1，R 2，R 3和R 4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：US20130156700A1

公开(公告)日：2013-06-20

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: C07D403/12 ,  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：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.

公开(公告)号：US08791130B2

公开(公告)日：2014-07-29

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: A01N43/54 ,  A61K31/505 ,  C07D239/47 ,  C07D239/48

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.

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。