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：US20140288043A1

公开(公告)日：2014-09-25

申请号：US13847409

申请日：2013-03-19

Applicant: Genentech, Inc.

Inventor： Bryan Chan ,  Anthony Estrada ,  Daniel Shore ,  Zachary Sweeney

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: A first aspect of the invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted, and wherein X1, X2, X3 and X4 are as defined herein. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).

Abstract translation: 本发明的第一方面涉及式（1A）或（1B）化合物或其药学上可接受的盐，其中R1是选自烷基，单环杂环烷基，双环杂环烷基和环烷基的基团，其各自任选被取代 ，并且其中X1，X2，X3和X4如本文所定义。 其它方面涉及药物组合物，治疗用途和制备式（1A）和（1B）化合物的方法。

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：US20130225557A1

公开(公告)日：2013-08-29

申请号：US13854635

申请日：2013-04-01

Applicant: Genentech, Inc.

Inventor： Georgette Castanedo ,  Bryan Chan ,  Matthew C. Lucas ,  Brian Safina ,  Daniel P. Sutherlin ,  Zachary Sweeney

IPC: C07D471/04 ,  C07D491/107

CPC classification number: C07D471/04 ,  C07D491/107

Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。