ISOQUINOLINE CARBOXAMIDES AND MEDICINAL AGENT BASED ON THEREOF FOR USING AS INHIBITORS OF HIV PROTEASE Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of isoquinoline carboxamide of the formula (I):

and to their pharmaceutically acceptable salts wherein R¹ means hydrogen atom, hydroxy-group or -NHR² wherein R² means alkyl, arylalkyl, heterocyclylalkyl that comprises one or some heteroatoms taken among nitrogen, oxygen and sulfur atoms, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, heterocyclylcarbonyl that comprises one or some heteroatoms taken among nitrogen, oxygen and sulfur atoms, arylalkylcarbonyl, heterocyclylalkylcarbonyl that comprises one or some heteroatoms taken among nitrogen and oxygen atoms, alkyloxycarbonyl, arylalkyloxycarbonyl, heterocyclylalkyloxycarbonyl that comprises one or some heteroatoms taken among nitrogen atom, heterocyclyl that comprises one or some heteroatoms taken among nitrogen and sulfur atoms, alkylsulfonyl, arylsulfonyl or the group of the formula:

R³ and R⁴ mean alkyl independently of one another; R⁵ means alkyl; or R⁴ and R⁵ in common with carbon and sulfur atoms to which they are bound form a heterocycle; R⁶ means alkyl; R¹³ means hydrogen atom or the group of the formula:

R¹⁵ means aryl under condition that if R³, R⁴ and R⁵ form methyl, R⁶ forms tert.-butyl then R¹³ means hydrogen atom, and if R¹⁵ means phenyl then R² doesn't mean benzyloxycarbonyl and 2-quinoline carbonyl (other values of radicals are given in cl. 1 of the invention claim). Also, invention relates to a medicinal agent based on these compounds used in treatment of HIV-mediated diseases. Invention provides preparing new compounds and a medicinal agent based on thereof in aims for treatment of HIV-mediated diseases.

EFFECT: valuable medicinal properties of compounds and medicinal agent.

14 cl, 11 tbl, 173 ex