Phosphonate compounds for treatment of complement mediated disorders

US9663543B2 · kind B2 · utility

Assignee

• Achillion Pharmaceuticals, Inc. · US

Inventors

• Jason Allan Wiles · Madison, US
• Akihiro Hashimoto · Branford, US
• Venkat Rao Gadhachanda · Hamden, US
• Godwin Pais · Hamden, US
• Qiuping Wang · Bethany, US
• Dawei Chen · Middletown, US
• Xiangzhu Wang · Madison, US
• Atul Agarwal · Hamden, US
• Milind Deshpande · Madison, US
• Avinash Phadke · Branford, US

Key dates

• Filing date: Feb 25, 2015
• Grant date: May 30, 2017
• Expiry date: Feb 25, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/05
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 R12 or R13 on the A group is a phosphonate (R32) 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.