INHIBITORS OF DIPEPTIDYL-PEPTIDASE IV Russian patent published in 2006 - IPC C07D207/16 C07D277/06 C07D295/18 C07D401/12 C07D403/12 C07D417/06 C07D417/12 A61K31/425 A61P5/50 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention proposes compounds of the general formula (1): wherein X is chosen from sulfur atom and methylene group; X¹ is chosen from sulfur atom and methylene group; X² is chosen from oxygen (O), sulfur (S) atoms and methylene group; X³ means -NR⁵ or carbonyl group; R¹ means hydrogen atom or nitrile group; R and R³ are chosen independently from hydrogen atom (H) and (C₁-C₆)-alkyl; R⁴ means R^4A when X³ means -NR⁵ and R^4B when X³ means carbonyl group; R^4A is chosen from -R⁶R⁷NC(=O), -R⁶R⁷NC(=S), -R⁸(CH₂)_qC(=O), -R⁸(CH₂)_qC(=S), -R⁸(CH₂)_qSO₂ and -R⁸(CH₂)_qOC(=O); R^4B means -R⁶R⁷N; R⁵ means hydrogen atom (H); R⁶ and R⁷ are chosen independently from -R⁸(CH₂)_q, or they form in common -(CH₂)₂-Z¹-(CH₂)₂- or -CHR⁹-X²-CH₂-CHR¹⁰-; R⁸ is chosen from hydrogen atom (H), (C₁-C₄)-alkyl, cycloalkyl group condensed with benzene ring, acyl, dialkylcarbamoyl, dialkylamino-group, N-alkylpiperidyl, optionally substituted aryl, optionally substituted α-alkylbenzyl, optionally substituted aroyl, optionally substituted arylsulfonyl and optionally substituted heteroaryl representing monocyclic 5- and 6-membered ring aromatic group with one or two heteroatoms chosen from nitrogen, oxygen and sulfur atoms, and derivatives of abovementioned rings condensed with benzene; R⁹ and R¹⁰ are chosen independently from hydrogen atom (H), hydroxymethyl and cyanomethyl groups; Z¹ is chosen from -(CH₂)_r-, -O-, and -N((CH₂)_q)R⁸)-; Z² means optionally the substituted ortho-phenylene group; m = 1-3; n = 0-4; p = 2-5; q = 0-3, and r = 1 or 3. Proposed compounds are inhibitors of dipeptidyl-peptidase IV and can be used in preparing pharmaceutical compositions designated for treatment of different diseases, among them, diabetes mellitus of type 2.

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

22 cl, 8 tbl, 453 ex