FRAUNHOFER-GESELLSCHAFT ZUR FÖRDERUNG DER ANGEWANDTEN FORSCHUNG E.V.
发明人:
GEISSLINGER, Gerd,PARNHAM, Michael,BERNAU, Marc,NÜSING, Rolf Michael
申请号：
EPEP2016/076954
公开号：
WO2017/080989A1
申请日:
2016.11.08
申请国别(地区):
EP
年份:
2017
代理人:
摘要：
The present invention relates to a compound being an (R)-enantiomer of a compound according to the following formula (I), wherein Rl or R2 is a group selected from H, -CH3, -CH2CH3, -CH2CH2CH3, and CH2CH2CH2CH3 or can be taken together with another to give a cyclopropyl ring, a cyclobutyl ring, a cyclopentyl ring, or a cyclohexyl ring, R3 is a group selected from -COOH, -COOR6, -CONH2, -CONHR6, -CONR6R7, -CONHS02R6, -COO-(CH2)3-CH20H, -COO- (CH2)4-ON02, -COO-PhOCH3-C2H2-COO-(CH2)4-ON02, tetrazolyl, and a -COOH bioisostere, R4 or R5 is a group selected from -CI, -F, -Br, -I, -CF3, -OCF3, -SCF3, -OCH3, - OCH2CH3, -CN, -CH=CH2, -CH20H, and -N02, R6 or R7 is a group selected from -CH3, - CH2CH3, -CH2CH2CH3, and -CH2CH2CH2CH3, and m or n is an integer selected from 0, 1, 2, and 3, a nitro-variant of said compound, or pharmaceutically acceptable salts of said compound for use in preventing and/or treating diabetes in a subject in need thereof. Moreover, also encompassed by the invention is a composition comprising said compound, nitro-variant, or pharmaceutically acceptable salts and at least one additional therapeutic agent for prevention and/or treatment of diabetes.La présente invention concerne un composé qui est un énantiomère R d'un composé de formule (I) suivante, dans laquelle R1 ou R2 représente un groupe choisi parmi H, -CH3, -CH2CH3, -CH2CH2CH3 et -CH2CH2CH2CH3 ou qui peut former conjointement avec un autre groupe un cycle cyclopropyle, un cycle cyclobutyle, un cycle cyclopentyle ou un cycle cyclohexyle, R3 représente un groupe choisi parmi -COOH, -COOR6, -CONH2, -CONHR6, -CONR6R7, -CONHSO2R6, -COO-(CH2)3-CH2OH, -COO-(CH2)4-ONO2, -COO-PhOCH3-C2H2-COO-(CH2)4-ONO2, un groupe tétrazolyle et un bioisostère du groupe -COOH, R4 ou R5 représente un groupe choisi parmi -Cl, -F, -Br, -I, -CF3, -OCF3, -SCF3, -OCH3, -OCH2CH3, -CN, -CH=CH2, -CH2OH et -NO2, R6 ou R7 représente un groupe choisi parmi -CH3, -CH2CH3, -CH2CH2CH3 et -CH2CH2CH2CH3, et m ou n est un nombre entier
