PYRAZOLES AS 11-BETA-HSD-1 INHIBITORS Russian patent published in 2010 - IPC C07C13/615 C07D231/12 C07D231/16 C07D231/38 C07D401/04 C07D403/04 C07D407/14 C07D413/04 C07D417/04 A61K31/4155 A61P3/10 

Abstract RU 2402517 C2

FIELD: chemistry.

SUBSTANCE: invention relates to pyrrole derivatives of formula (I): , where R1 denotes hydrogen; R2 denotes adamantine which is unsubstituted or substituted with a hydroxy group or halogen; R3 denotes trifluoromethyl, pyrazole, triazole, piperidine, pyrrolidine, hydroxymethylpiperidine, benzylpiperazine, hydroxypyrrolidine, tert-butylpyrrolidine, hydroxyethylpiperazine, hydroxypiperidine or thiomorpholyl group; R4 denotes cyclopropyl, tert-butyl, -CH(CH3)2CH2OH, methyl, -CF3 or -(CH2)nCF3 group, where n equals 1 or 2; R5 denotes hydrogen or lower alkyl which is unsubstituted or substituted with a halogen, as well as pharmaceutically acceptable salts thereof.

EFFECT: compounds and pharmaceutical compositions containing said compounds can inhibit 11β-hydroxysteroid dehydrogenase of the form 1 (11-BETA-HSD-1) and can be used to treat diseases such as type II sugar diabetes type and metabolic syndrome.

17 cl, 99 ex, 1 tbl

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Authors

Anderson Kevin Uill'Jam

Fotui Nader

Dzhillespaj Pol

Gudnau Robert Alan Dzhr.(Us)

Guirtin Kevin Richard

Khejnes Nansi-Ehllen

Majers Majkl Pol

Pitraniko-Koul Sherri Linn

Tsi Lida

Rossman Pamela Lorin

Skott Natan Robert

Takkar Kshitij Chkhabilbkhaj

Tilli Dzhefferson Rajt

Chzhan Tsjan

Dates

2010-10-27Published

2007-03-12Filed