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METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA
专利权人:
KAREUS THERAPEUTICS; SA
发明人:
KHANNA, Ish,PILLARISETTI, Sivaram
申请号:
USUS2011/052318
公开号:
WO2012/040177A1
申请日:
2011.09.20
申请国别(地区):
WO
年份:
2012
代理人:
摘要:
Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO2R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR wherein R is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy and n1 and n2 are independently selected from 0, 1, and 2. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally, when R3 and R4 or R5 and R6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl. R2 is independently selected from hydrogen, alkoxy, hydroxy, alkyl, haloalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, cyano, or COR7, wherein R7 is selected from hydroxy, alkyl, alkoxy, or amine, NHR, NHSO2R, or NHCOR. Y1 is oxygen or hydrogen. Y2 is optional, wherein when Y2 is present, Y1 and Y2 are hydrogen. When Y2 is not present, Y1 is a carbonyl group.La présente invention concerne de nouveaux composés de formule I, leurs stéréoisomères et/ou leurs sels pharmaceutiquement acceptables pour le traitement du diabète et de la dyslipidémie associée au diabète. Dans la forumle I R1 est choisi dans le groupe constitué dun hydroxy, un alcoxy, une amine, un alkyle, un halogénoalkyle, NHSO2R, ou NHCOR où R est choisi parmi un alkyle ou un cycloalkyle, NHR où R est un alkyle ou un cycloalkyle facultativement substitué par un hydroxy ou un alcoxy et n1 et n2 sont indépendamment choisis parmi 0, 1 et 2. Au moins lun de R3 et R4 et/ou R5 et R6 forment un anneau cyclique de 3 à 8 atomes de carbone conte
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