Pyridyl aminothiazoles as potent Chk1 inhibitors: Optimization of cellular activity
摘要:
Translation of significant biochemical activity of pyridyl aminothiazole class of Chk1 inhibitors into functional CEA potency required analysis and adjustment of both physical properties and kinase selectivity profile of the series. The steps toward optimization of cellular potency included elimination of CDK7 activity, reduction of molecular weight and polar surface area and increase in lipophilicity of the molecules in the series. (C) 2012 Elsevier Ltd. All rights reserved.
Spiroisoquinoline compound, a method for preparing the same and an intermediate thereof
申请人:——
公开号:US20040106635A1
公开(公告)日:2004-06-03
The present invention provides a novel spiroistiquinoline derivative of the formula [I]: which has a small-conductance potassium channel (SK) blocking activity and is useful as a medicament, a method for preparing the same and an intermediate thereof.
1
Aminopyridine compounds and methods for the preparation and use thereof
申请人:Cortexyme, Inc.
公开号:US11059786B2
公开(公告)日:2021-07-13
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
本发明一般涉及针对牙龈卟啉单胞菌的治疗药物,包括其蛋白酶精氨酸龈脂酶A/B (Rgp),及其用于治疗与牙龈卟啉单胞菌感染相关的疾病,包括脑部疾病,如阿尔茨海默氏症。在某些实施方案中,本发明提供了本文所述的根据式 I 和式 III 的化合物及其药学上可接受的盐。
SPIROISOQUINOLINE COMPOUNDS, METHODS FOR THEIR PREPARATION AND INTERMEDIATES THEREOF
申请人:TANABE SEIYAKU CO., LTD.
公开号:EP1373247A2
公开(公告)日:2004-01-02
AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF
申请人:Cortexyme, Inc.
公开号:US20200148642A1
公开(公告)日:2020-05-14
The present invention relates generally to therapeutics targeting the bacterium
Porphyromonas gingivalis
, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with
P. gingivalis
infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
[EN] A SPIROISOQUINOLINE COMPOUND, A METHOD FOR PREPARING THE SAME AND AN INTERMEDIATE THEREOF<br/>[FR] COMPOSE DE SPIRO-ISOQUINOLINE, PROCEDE PERMETTANT SA PREPARATION, ET COMPOSE INTERMEDIAIRE
申请人:TANABE SEIYAKU CO
公开号:WO2002079189A2
公开(公告)日:2002-10-10
The present invention provides a novel spiroisoquinoline derivative of the formula [I]: which has a small-conductance potassium channel (SK) blocking activity and is useful as a medicament, a method for preparing the same and an intermediate thereof.