1-HYDROXYIMINO-3-PHENYL-PROPANES Russian patent published in 2016 - IPC C07C251/48 C07C249/08 C07D213/53 C07D213/64 C07D215/12 C07D241/12 C07D241/18 C07D239/26 C07D401/12 C07D409/12 C07D413/12 C07D417/06 C07D495/10 A61K31/15 A61K31/44 A61K31/4412 A61K31/4433 A61K31/4436 A61K31/4439 A61K31/444 A61K31/4545 A61K31/4709 A61K31/497 A61K31/506 A61K31/5377 A61P3/10 A61P1/00 A61P9/10 A61P11/00 A61P13/12 A61P19/02 A61P25/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 1-hydroxyimino-3-phenyl-propane derivatives of formula I, wherein R¹ represents -(CH₂)_m-phenyl, m is equal to 0, and phenyl is substituted by 1-3 groups independently specified in C_1-7-alkyl or hydroxy, or -(CH₂)_n-heteroaryl, wherein n is equal to 0 or 1, and heteroaryl is specified in pyridine, 1H-pyridin-2-one, 1-oxy-pyridine, 1H-pyrimidin-2-one, quinoline and pyrazine, and is ubsubstituted or substituted by 1-3 groups specified in the patent claim; R² represents hydrogen or C_1-7-alkyl, or when R⁴ represents hydrogen, R² represents phenyl optionally substituted by C_1-7-alkyl; R³ represents hydrogen; R⁵ represents hydrogen or hydroxy; or R³ and R⁵ are substituted by a double bond; R⁴ is specified in a group consisting of C_1-7-alkyl, C_3-7-cycloalkyl, C_2-7-alkenyl, halogen-C_1-7-alky, optionally substituted phenyl, optionally substituted phenyl-C_1-7-alkyl, 5-9-merous heteroaryl containing 1-2 heteroatoms specified in N and S optionally substituted by C_1-7-alkyl or oxo, and piperidinyl optionally substituted by C_1-7-alkyl, or R⁴ and R⁵ together with a carbon atom to which they are attached, form a C_3-7-cycloalkyl ring; R⁶ represents hydrogen halogen; or R⁴ and R⁶ together with a carbon atom to which they are attached, form a cyclic group G , wherein m represents 0 or 2; R⁷ - R⁹ are those as specified in the patent claim; R¹⁰ is specified in hydrogen, halogen and C_1-7-alkyl; or their pharmaceutically acceptable salts. The invention also refers to specific compounds specified in cl. 19 of the patent claim, a method for producing the compounds I, a pharmaceutical composition, a method of treating diabetes and using the compounds for producing a medicinal agent.

EFFECT: 1-hydroxyimino-3-phenyl-propane derivatives possessing GPBAR1 agonist activity and effective in treating diabetes.

26 cl, 516 ex