High penetration composition and uses thereof

US11135153B2 · kind B2 · utility

Assignee

• Techfields Pharma Co., Ltd. · CN

Inventors

• Chongxi Yu · Kensington, US
• Lina Xu · Beijing, CN

Key dates

• Filing date: Dec 15, 2016
• Grant date: Oct 5, 2021
• Expiry date: Dec 15, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C233/25
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for 4-aminophenol derivatives, which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes. For example, the HPPs can be locally delivered to an action site of a condition with a high concentration due to their ability of penetrating biological barriers and thus obviate the need for a systematic administration. For another example, the HPPs herein can be systematically administer to a biological subject and enter the general circulation with a faster rate.