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    • 8. 发明申请
    • METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA
    • 用于治疗糖尿病和DYSLIPIDEMIA的方法和组合物
    • US20140142178A1
    • 2014-05-22
    • US14148580
    • 2014-01-06
    • Ish KhannaSivaram Pillarisetti
    • Ish KhannaSivaram Pillarisetti
    • C07C311/51
    • C07C311/51C07C31/27C07C43/115C07C53/132C07C61/12C07C61/15C07C69/608C07C69/74C07C233/58C07C233/60C07C255/46C07C2601/02C07C2601/04C07C2601/08C07D257/04
    • 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.
    • 提供式I的新型化合物:其用于治疗糖尿病和糖尿病相关血脂异常的其立体异构体和/或药学上可接受的盐,其中R 1选自羟基,烷氧基,胺,烷基,卤代烷基,NHSO 2 R或NHCOR 其中R选自烷基或环烷基,NHR',其中R'是任选被羟基或烷氧基取代的烷基或环烷基; 并且n1和n2独立地选自0,1和2. R3和R4和/或R5和R6中的至少一个形成3-8个碳原子的环状环,任选地含有烷基,杂原子或官能团,例如 作为O,N,SO 2。 此外,当R3和R4或R5和R6不形成环时,它们可以独立地选自氢,烷基,支链烷基和环烷基。 L1是任选含有4至16个碳原子的直链脂族链。 该链可以任选地被烷基,支链烷基,环烷基或芳基取代一次或多次。 R 2独立地选自氢,烷氧基,羟基,烷基,卤代烷基,环烷基,杂环烷基,杂芳基,氰基或COR 7,其中R 7选自羟基,烷基,烷氧基或胺,NHR',NHSO 2 R或NHCOR。 Y1是氧或氢。 Y2是任选的,其中当存在Y2时,Y1和Y2是氢。 当不存在Y2时,Y1是羰基。