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1. 发明申请

WO2012040177A1 METHODS AND COMPOSITIONS FOR TREATMENT OF DIABETES AND DYSLIPIDEMIA 审中-公开
标题翻译：用于治疗糖尿病和DYSLIPIDEMIA的方法和组合物
公开(公告)号：WO2012040177A1
公开(公告)日：2012-03-29
申请号：PCT/US2011/052318
申请日：2011-09-20
申请人： KAREUS THERAPEUTICS, SA , KHANNA, Ish , PILLARISETTI, Sivaram
发明人： KHANNA, Ish , PILLARISETTI, Sivaram
IPC分类号： A61K31/225
CPC分类号： C07C311/51 , C07C31/27 , C07C43/115 , C07C53/132 , C07C61/12 , C07C61/15 , C07C69/608 , C07C69/74 , C07C233/58 , C07C233/60 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D257/04
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, NHSO 2 R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR' wherein R' is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n 1 and n 2 are independently selected from 0, 1, and 2. At least one of R 3 and R 4 and/or R 5 and R 6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO 2 . Additionally, when R 3 and R 4 or R 5 and R 6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L 1 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. R 2 is independently selected from hydrogen, alkoxy, hydroxy, alkyl, haloalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, cyano, or COR 7 , wherein R 7 is selected from hydroxy, alkyl, alkoxy, or amine, NHR', NHSO2R, or NHCOR. Y 1 is oxygen or hydrogen. Y 2 is optional, wherein when Y2 is present, Y 1 and Y 2 are hydrogen. When Y 2 is not present, Y 1 is a carbonyl group.
摘要翻译：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。

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