Aryl, Heteroaryl, and Heterocyclic Compounds for Treatment of Complement Mediated Disorders
申请人:Achillion Pharmaceuticals, Inc.
公开号:US20150239895A1
公开(公告)日:2015-08-27
Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R
12
or R
13
on the A group is an aryl, heteroaryl or heterocycle (R
32
) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
本文提供了包含式I的补体因子D抑制剂的化合物、使用方法和制备过程,或其药学上可接受的盐或组合物,其中A组上的R12或R13是芳基、杂芳基或杂环(R32)。本文所描述的抑制剂针对因子D并在替代补体途径的早期和关键点上抑制或调节补体级联反应,并减少因子D调节经典和凝集素补体途径的能力。本文所描述的因子D抑制剂能够减少过度激活补体,这与某些自身免疫、炎症和神经退行性疾病、缺血再灌注损伤和癌症有关。