Compound reducing the functional activity of protease by inhibition of Human Immunodeficiency Association by its subunit containing such compounds and Pharmaceutical Compositions

摘要

1. u043du0435u043au043eu043du043au0443u0440u0435u043du0442u043du044bu0435 protease inhibitors of human immunodeficiency virus (hiv), u043eu0442u043bu0438u0447u0430u044eu0449u0438u0435u0441u00a0 that selectively block the u0434u0438u043cu0435u0440u0438u0437u0430u0446u0438u044e subunits of this enzyme.;2. connection for 1, u043eu0442u043bu0438u0447u0430u044eu0449u0435u0435u0441u00a0, blocking hiv protease u0434u0438u043cu0435u0440u0438u0437u0430u0446u0438u0438 subunits occurs through contact with u0440u0430u0441u0441u0442u043eu00a0u043du0438u0435 not more than 5 u0430u043du0433u0441u0442u0440u0435 one of al u043eu043cu043eu0432 u0441u043eu0435u0434u0438u043du0435u043du0438u00a0 u0445u043eu0442u00a0 with one of the atoms u0430u043cu0438u043du043eu043au0438u0441u043bu043eu0442u043du044bu0445 residues from the list of ASN98, u0440u043du043599, ASP29, ASP30, ARG8, GLY49, GLY51, GLY52 where u043du0443u043cu0435u0440u0430u0446u0438u00a0 dana in accordance with annex 1.;3. the connection to u043eu0442u043bu0438u0447u0430u044eu0449u0435u0435u0441u00a0 2, so that the u0434u0438u043cu0435u0440u0438u0437u0430u0446u0438u0438 hiv protease subunits occurs through changes u043au043eu043du0444u043eu0440u043cu0430u0446u0438u043eu043du043du044bu0445 subunits caused by through a contact at the u0440u0430u0441u0441u0442u043eu00a0u043du0438u0438 not more than 5 of one of the atoms u0445u043eu0442u00a0 compounds with one of the atoms u0430u043cu0438u043du043eu043au0438u0441u043bu043eu0442u043du044bu0445 residues from the list, where u043du0443u043cu0435u0440u0430u0446u0438u00a0 dana in u0441u043eu043eu0442u0432u0435u0442u0441u0442u0432u0438 and annex 1.;4. u0441u043eu0435u0434u0438u043du0435u043du0438u00a0 on p.2, u0445u0430u0440u0430u043au0442u0435u0440u0438u0437u0443u044eu0449u0438u0435u0441u00a0 formula (i), where r is the n2 - acetylthreoninamide (i - a) and 4 - [(ammocarbonyl) oxy] benzenammium (i - b).;5. u0441u043eu0435u0434u0438u043du0435u043du0438u00a0 on p.3, u0445u0430u0440u0430u043au0442u0435u0440u0438u0437u0443u044eu0449u0438u0435u0441u00a0 formulas (ii and iii) in which the radicals r to h, c1 and c6h5.;6. the on clause 5, u043eu0442u043bu0438u0447u0430u044eu0449u0435u0435u0441u00a0, efficiency u0434u0435u0439u0441u0442u0432u0438u00a0 u0434u043eu0441u0442u0438u0433u0430u0435u0442u0441u00a0 by u0441u043eu0447u0435u0442u0430u043du0438u00a0 grounds specified in u043f.u043f.2 and 3.;7. u0444u0430u0440u043cu0430u0446u0435u0432u0442u0438u0447u0435u0441u043au0430u00a0 u043au043eu043cu043fu043eu0437u0438u0446u0438u00a0 u0434u043bu00a0 u043bu0435u0447u0435u043du0438u00a0 acquired immunodeficiency syndrome, u0441u043eu0434u0435u0440u0436u0430u0449u0430u00a0 u0441u043eu0435u0434u0438u043du0435u043du0438u00a0 on u043fu043f.1 - 6 and u0444u0430u0440u043cu0430u0446u0435u0432u0442u0438u0447u0435u0441u043au0438 acceptable carrier.