Affordable Access

Access to the full text

Issues Related to Patent Protecton of Darunavir and its Analogs

Authors
  • Goizman, M. S.1
  • Zotova, O. A.1
  • Kamalova, A. A.1
  • Popova, A. O.1
  • Shobolov, D. L.1
  • Korlyukov, A. A.2
  • Suponitskii, K. Yu.2
  • Shimanovskii, N. L.3
  • Zaitsev, S. A.4
  • Degterev, E. V.5
  • 1 Drug Technology Co., 2a Rabochaya St., Khimki, Moscow Oblast, 141400, Russia , Khimki (Russia)
  • 2 Russian Academy of Sciences, A. N. Nesmeyanov Institute of Organoelement Compounds, Moscow, 28 Vavilova St., 119334, Russia , Moscow (Russia)
  • 3 N. I. Pirogov State Medical University, 1 Ostrovityanova St., Moscow, 117997, Russia , Moscow (Russia)
  • 4 ZAO INFARMA Co., 79/4 Elizarovykh St., Tomsk, 834021, Russia , Tomsk (Russia)
  • 5 Folium Publishing, Moscow, 127411, Russia , Moscow (Russia)
Type
Published Article
Journal
Pharmaceutical Chemistry Journal
Publisher
Springer US
Publication Date
Sep 01, 2016
Volume
50
Issue
6
Pages
413–418
Identifiers
DOI: 10.1007/s11094-016-1461-7
Source
Springer Nature
Keywords
License
Yellow

Abstract

It is shown that prolongation of patent protection for the antiviral drug darunavir by patenting it again as darunavir ethanolate is illegal. The claims of the successor patent “Pseudopolymorphic forms of a HIV protease inhibitor,” WO 2003106461 A2, are analyzed and shown to be invalid from both scientific and ethical viewpoints. It is established that darunavir was initially used as its ethanolate. Darunavir is one of the best protease inhibitors of both types of HIV. Currently, not only darunavir ethanolate but also amorphous darunavir (unsolvated) are used as active pharmaceutical ingredients with INN darunavir. This was confirmed by x-ray diffraction studies. Justification for the orderly invalidation of this patent in the RF was given.

Report this publication

Statistics

Seen <100 times