公开(公告)号：US10010549B2

公开(公告)日：2018-07-03

申请号：US14927267

申请日：2015-10-29

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

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：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。

公开(公告)号：US20170087137A1

公开(公告)日：2017-03-30

申请号：US15374047

申请日：2016-12-09

Applicant: Genentech, Inc.

Inventor： Anthony Estrada ,  Wen Liu ,  Snahel Patel ,  Michael Siu

IPC: A61K31/4439 ,  A61K31/437 ,  A61K31/4545

CPC classification number: A61K31/4439 ,  A61K31/437 ,  A61K31/4545 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.

公开(公告)号：US09365583B2

公开(公告)日：2016-06-14

申请号：US14576890

申请日：2014-12-19

Applicant: Genentech, Inc.

Inventor： Michael Siu ,  Anthony Estrada ,  Wen Liu ,  Joseph P. Lyssikatos ,  Snahel Patel ,  Guibai Liang ,  Kevin Chen

IPC: C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10 ,  C07D401/04

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/10

Abstract: The present invention provides for compounds of formula 0 and various embodiments thereof, and compositions comprising compounds of formula 0 and various embodiments thereof. In compounds of formula 0, the groups R1A, R1B, R1C, R1D, R2, R3, R4, R5 and R6 have the meaning as described herein. The present invention also provides for methods of using compounds of formula 0 and compositions comprising compounds of formula 0 as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Abstract translation: 本发明提供式0化合物及其各种实施方案，以及包含式0化合物及其各种实施方案的组合物。 在式0的化合物中，基团R1A，R1B，R1C，R1D，R2，R3，R4，R5和R6具有如本文所述的含义。 本发明还提供使用式0化合物和包含式0化合物的组合物作为DLK抑制剂并用于治疗神经变性疾病和病症的方法。

公开(公告)号：US11236046B2

公开(公告)日：2022-02-01

申请号：US16657102

申请日：2019-10-18

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D417/12 ,  C07D451/02 ,  C07D491/048 ,  C07D405/14

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II 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：US10028954B2

公开(公告)日：2018-07-24

申请号：US15041375

申请日：2016-02-11

Applicant: Genentech, Inc.

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

IPC: A61K31/506 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/444

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.

公开(公告)号：US20180118680A1

公开(公告)日：2018-05-03

申请号：US15851322

申请日：2017-12-21

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/14 ,  C07D417/12 ,  C07D403/12 ,  C07D451/02 ,  C07D405/14 ,  C07D401/14 ,  C07D491/048 ,  C07D401/12

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II 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：US20170369510A1

公开(公告)日：2017-12-28

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 ,  A61K45/06 ,  A61K31/553 ,  C07D519/00 ,  A61K31/5383

CPC classification number: C07D498/14 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  C07D491/14 ,  C07D519/00

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.