GLUCOKINASE ACTIVATING AGENTS Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, medicine, endocrinology.

SUBSTANCE: invention relates to compounds representing amide of the formula (I):

wherein * means asymmetric carbon atom; R¹ and R² mean independently of one another hydrogen or halogen atom, amino-, hydroxyamino-, nitro-, cyano-, sulfonamido-group, (lower)-alkyl, -OR⁵, -C(O)OR⁵, perfluoro-(lower)-alkyl, (lower)-alkylthio-, perfluoro-(lower)-alkylthio-, (lower)-alkylsulfonyl-, perfluoro-(lower)-alkylsulfonyl-, or (lower)-alkylsulfinyl-group; R³ means cycloalkyl comprising from 3 to 7 carbon atoms, or (lower)-alkyl comprising from 2 to 4 carbon atoms; R⁴ means (O)NHR⁴⁰ or unsubstituted or monosubstituted five- or six-membered heteroaromatic ring bound by ring carbon atom with given amino-group wherein this five- or six-membered heteroaromatic ring comprises from 1 to 3 heteroatoms taken among sulfur, oxygen and nitrogen atoms and wherein one heteroatom represents nitrogen atom that is adjacent with connecting ring carbon atom; this monosubstituted heteroaromatic ring is monosubstituted by ring carbon atom that differs from adjacent atom with connecting carbon atom and substitute is taken among the following row including (lower)-alkyl, halogen atom, nitro-group, cyano-group, -(CH₂)_n-OR⁶, -(CH₂)_n-C(O)OR⁷, -(CH₂)_n-C(O)NHR⁶, -C(O)-C(O)OR⁸ and -(CH₂)_n-NHR⁶, or its pharmaceutically acceptable salts. These compounds are activators of glucokinase that enhance secretion of insulin in treatment of diabetes mellitus of type II.

EFFECT: valuable medicinal properties of compounds.

32 cl, 175 ex