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Composition useful in the treatment of pathologies associated with e.g. hyperglycemia, diabetes, dyslipidemia, obesity, arterial hypertension, neuropathies, and nephropathies, comprises oxamate derivatives
Composition useful in the treatment of pathologies associated with e.g. hyperglycemia, diabetes, dyslipidemia, obesity, arterial hypertension, neuropathies, and nephropathies, comprises oxamate derivatives
Composition comprises oxamate derivatives containing substituted nitrogen heterocycle, their tautomeric forms, enantiomers, diastereoisomers, epimers or salts. Composition comprises oxamate derivatives containing substituted nitrogen heterocycle of formula (I), their tautomeric forms, enantiomers, diastereoisomers, epimers or salts. R, R1-R4 = H or 1-3C alkyl; X = O, S, CR5R5' or NR6; R5, R5' = H, OH, 1-5C alkyl, CO-R7 or 6-14C aryl (optionally substituted); R6 = 1-10C alkyl, 2-10C alkene, 6-14C aryl, 5-8 membered heterocyclic radical (comprising at least one of O, N or S) (all optionally substituted), H, R8-(CH2)m-C(=O)-(CH2)n or sulfonyl (optionally substituted by at least one T); T = 1-20C alkyl, perfluoroalkyl, 6-14C aryl, 5-8 membered cycloalkyl or 5-8 membered heterocyclic (comprising at least one O, N or S) or styryl (all optionally substituted); m, n = 0 or 1; R7 = OH, 1-5C alkyl, 1-5C alkoxy, 6-14C aryl or 6-14C aryloxy; R8 = 2-5C alkene, 5-8 membered cycloalkyl or cycloalkoxy, 6-14C aryl, 6-14C aryloxy, 5-8 membered heterocyclic or heteroaryloxy (containing at least one O, N or S) (all optionally substituted), H, OH, 1-5C alkoxy, 1-5C alkyl or NR9R'9; R9, R'9 = 1-5C alkyl, 6-14C aryl (both optionally substituted), H or COR7; R9+R'9 = 3-10 membered ring optionally containing at least one O, N or S. Provided that when X represents NR6 then R1 and R6 can together form a 3-10 membered ring optionally containing at least one O, N or S. Independent claims are also included for: (1) new oxamate derivatives of formula (I) (provided that when X is NR6, then R6 is other than phenyl (substituted in the para position by a methyl and in the meta position by a halogen), benzyl or beta -phenethyl radical; when X is O then R1-R4 other than H; and when X is CR5R'5 then R1-R5 and R'5 are other than H); and (2) preparation of (I).
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机译：组合物包含草酸盐衍生物，其包含取代的氮杂环，其互变异构形式，对映异构体，非对映异构体，差向异构体或盐。组合物包含草酸酯衍生物，其包含式（I）的取代的氮杂环，其互变异构形式，对映异构体，非对映异构体，差向异构体或盐。 R，R 1 -R 4 ＝ H或1-3C烷基; X ＝ O，S，CR 5 R 5'或NR 6; R 5，R 5'＝ H，OH，1-5C烷基，CO-R 7或6-14C芳基（任选取代）; R 6 ＝ 1-10C烷基，2-10C烯烃，6-14C芳基，5-8元杂环基（包含O，N或S中的至少一个）（全部任选取代），H，R 8 -（CH 2）m C（＝ O）-（CH 2）n或磺酰基（任选地被至少一个T取代）; T ＝ 1-20C烷基，全氟烷基，6-14C芳基，5-8元环烷基或5-8元杂环（包含至少一个O，N或S）或苯乙烯基（全部任选取代）; m，n = 0或1; R 7 ＝ OH，1-5C烷基，1-5C烷氧基，6-14C芳基或6-14C芳氧基; R 8 ＝ 2-5C烯烃，5-8元环烷基或环烷氧基，6-14C芳基，6-14C芳氧基，5-8元杂环或杂芳氧基（包含至少一个O，N或S）（全部任选地被取代） ），H，OH，1-5C烷氧基，1-5C烷基或NR 9 R'9; R 9，R′9 ＝ 1-5C的烷基，6-14C的芳基（均被取代），H或COR 7; R 9 + R′9 ＝ 3-10元环，其任选地包含至少一个O，N或S。条件是当X代表NR 6时，R 1和R 6可以一起形成一个3-10元环，可选地包含至少一个O，N或S。还包括以下方面的独立权利要求：（1）式（I）的新草酸酯衍生物（条件是当X为NR 6时，则R 6不同于苯基（在对位被甲基取代并且在间位被卤素取代），苄基或β-苯乙基;当X是O时，则R 1 -R 4不同于H;并且当X是CR 5 R'5，则R 1 -R 5和R'5不是H）; （2）制备（I）。
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