公开(公告)号：US20180133219A1

公开(公告)日：2018-05-17

申请号：US15868301

申请日：2018-01-11

Applicant: Genentech, Inc.

Inventor： 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: A61K31/506 ,  A61K31/444 ,  A61K35/30 ,  C07D487/14 ,  A61K31/553 ,  C07D417/14 ,  C07D487/18 ,  A61K31/55 ,  C07D401/14 ,  A61K31/5377 ,  C07D495/08 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/5386 ,  A61K45/06 ,  C07D471/08 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08

CPC classification number: 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

Abstract: 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：US09266862B2

公开(公告)日：2016-02-23

申请号：US14267011

申请日：2014-05-01

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Alan G. Olivero ,  Snahel Patel ,  Michael Siu

IPC: C07D403/14 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K35/30 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D471/18 ,  C07D487/08 ,  C07D491/08 ,  C07D495/08 ,  C07D519/00 ,  C07D471/08 ,  A61K45/06 ,  A61K31/5386

CPC classification number: 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

Abstract: 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.

Abstract translation: 本发明提供式I化合物及其实施方案及其盐用于治疗疾病（如神经变性疾病）。 式中的R 1，R 2，R 3，X 1，X 2，A和Cy变量均具有如本文所定义的含义。

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：US10766878B2

公开(公告)日：2020-09-08

申请号：US16247995

申请日：2019-01-15

Applicant: Genentech, Inc.

Inventor： Baihua Hu ,  Vishal Verma ,  Matthew Volgraf ,  Anthony Estrada ,  Joseph Lyssikatos

IPC: C07D403/04 ,  C07D401/04 ,  C07D231/12 ,  C07D237/08 ,  C07D213/61 ,  C07D231/16 ,  C07D231/20 ,  C07D239/26

Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US10131675B2

公开(公告)日：2018-11-20

申请号：US15699095

申请日：2017-09-08

Applicant: Genentech, Inc.

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

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

Abstract: 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.