NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS, PHARMACEUTICAL COMPOSITION COMPRISING THEREOF, THEIR USING IN PREPARING MEDICINAL AGENT FOR TREATMENT OF HIV-1, INTERMEDIATE COMPOUNDS FOR THEIR PREPARING Russian patent published in 2006 - IPC C07D405/12 C07D409/12 C07D413/12 C07D417/12 C07D311/94 C07C43/23 A61K31/4402 A61K31/35 A61K31/381 A61P31/18 

Abstract RU 2281284 C2

FIELD: organic chemistry, medicine, virology, pharmacy.

SUBSTANCE: invention relates to new non-nucleoside inhibitors of reverse transcriptase activity of the formula (1): wherein R1 represents oxygen atom (O), sulfur atom (S); R2 represents optionally substituted nitrogen-containing heterocycle wherein nitrogen atom is at position 2 relatively to the bond with (thio)urea; R3 represents hydrogen atom (H), (C1-C3)-alkyl; R4-R7 are chosen independently from hydrogen atom (H), (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, halogen-(C1-C6)-alkyl, (C1-C6)-alcanoyl, halogen-(C1-C6)-alcanoyl, (C1-C6)-alkoxy-, halogen-(C1-C6)-alkoxy-group, hydroxy-(C1-C)-alkyl, cyano-group, halogen atom, hydroxy-group; X represents group of the formula: -(CHR8)-D-(CHR8)m- wherein D represents -O or -S-; R8 represents hydrogen atom (H); n and m represent independently 0, 1 or 2, and to its pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition based on these compounds possessing inhibitory effect with respect to activity of HIV-1 reverse transcriptase, and to using these compounds in preparing medicinal agents used in treatment of HIV-1 and to intermediates compounds.

EFFECT: valuable medicinal and biochemical properties of compounds and composition.

45 cl, 1 tbl, 57 ex

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RU 2 281 284 C2

Authors

Lindstrem Stefan

Sal'Berg Krister

Vall'Berg Khans

Kaljanov Genadij

Oden Lurdes

Naehslund Lotta

Dates

2006-08-10Published

2002-03-04Filed