NOVEL FORMS OF TELAPREVIR

摘要

The invention relates to an amorphous form of telaprevir, its preparation via novel crystalline Form C of telaprevir (also referred to as “crystalline Form C” or “Form C”), and telaprevir compositions comprising said amorphous form and Form C. Furthermore, the present invention relates to the use of said amorphous telaprevir, telaprevir composition and Form C of telaprevir for the preparation of medicaments such as anti-hepatitis C medicaments. Moreover, the present invention relates to pharmaceutical compositions and dosage forms comprising a pharmaceutically effective amount of said novel forms for use in treating patients suffering from hepatitis C virus.

主权项

1. A process for the preparation of an amorphous form of telaprevir of Formula 1comprising the steps of:
(i) providing a crystalline Form C of telaprevir having an X-ray powder diffraction pattern with peaks at 2-theta angles of 6.6±0.2 degrees 2theta, 7.0±0.2 degrees 2theta, 8.0±0.2 degrees 2theta, 8.9±0.2 degrees 2theta, 9.4±0.2 degrees 2theta, 17.6±0.2 degrees 2theta, when using Cu-Kα radiation, and (ii) converting said crystalline Form C of telaprevir into said amorphous form of telaprevir.