CYCLOPENTYLACRYLAMIDE DERIVATIVE Russian patent published in 2015 - IPC C07D277/46 C07D213/75 C07D231/40 C07D241/20 C07D261/14 C07D277/82 C07D285/08 C07D405/04 C07D405/06 C07D405/12 C07D417/04 C07D417/12 C07D513/04 C07F9/6509 C07F9/6539 A61K31/415 A61K31/4155 A61K31/42 A61K31/426 A61K31/428 A61K31/433 A61K31/437 A61K31/44 A61K31/454 A61K31/496 A61K31/4965 A61K31/497 A61K31/5377 A61P3/10 A61P43/00 

Abstract RU 2565070 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by general formula or its pharmaceutically acceptable salt, in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy- C1-C6alkylsulphonyl group, and A is selected from group which includes: thiazolyl group, 1,2,4-thiadiazolyl group, pyrazolyl group, pyridyl group, pyrazinyl group, isooxazolyl group, benzothiazolyl group and thiazolo[5,4-b]pyridyl group, and A can be mono-substituted by substituent, selected from group, which includes halogen atom; C1-C6alkyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C6alkoxyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C3alkoxy-C1-C2alkoxyl groups; C1-C3alkoxycarbonyl-C1-C2alkoxyl groups; C1-C6alkylsulphanyl groups; C1-C6amino-alkylsulphanyl group, optionally substituted with C1-C3alkyl group; C1-C6alkylsulphanyl-C1-C6alcoxyl groups; phenyl group; 1,3-dipxolane, substituted with two C1-C6alkyl groups; piperazinesulphonyl is substituted with methyl group; 1,3-dioxolanemethyl, substituted with two methyl groups; piperazinemethyl, substituted with methyl group; tetrahydropyranyloxy-C1-C3alkoxy group; aminosulphonyl groups, optionally substituted with C1-C3alkyl group; C1-C6 hydroxyalkylsulphanyl groups; -(O)(CH2)C(O)O-C1-C6alkyl group; -C(O)O-C1-C6 alkyl group; as well as groups, represented by general formula -(CH2)mP(O)R4R5 (where R4 and R5 independently represent C1-C3alkoxyl group; m is integer number from 0 to 1). Compound of formula (1) is intended, as active ingredient, for production of pharmaceutical composition, which has effect for activation of glucokinase (GK) or hypoglycaemic action. Invention also relates to intermediate compounds, represented by formula in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy-C1-C6alkylsulphonyl group.

EFFECT: acrylamide compounds as glucokinase activator for treatment of diabetes.

21 cl, 38 tbl, 55 ex

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RU 2 565 070 C2

Authors

Fukuda Jasumichi

Asakhina Joshikazu

Takadoi Masanori

Jamamoto Masanori

Dates

2015-10-20Published

2009-04-27Filed