摘要:
The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R represents "Het", or a group of formula (II), wherein "Het" represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R , R , and R independently represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R , R , and R independently represents (CH2)nR ; wherein R represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkyl-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR R , or "Het"; wherein n is 0, 1, 2, or 3; and R represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. "A" represents a ring of five to seven atoms fused with the benzo ring at the positions marked "a" and "b", and formed by the following bivalent radicals: a-NR -CH2-CH2-b; a-CH2-NR -CH2-b; a-CH2-CH2-NR -b; a-NR -CH2-CH2-CH2-b; a-CH2-NR -CH2-CH2-b; a-CH2-CH2-NR -CH2-b; a-CH2-CH2-CH2-NR -b; a-NR -CH2-CH2-CH2-CH2-b; a-CH2-NR -CH2-CH2-CH2-b; a-CH2-CH2-NR -CH2-CH2-b; a-CH2-CH2-CH2-NR -CH2-b; or a-CH2-CH2-CH2-CH2-NR -b; wherein R represents hydrogen, alkyl or CH2CH2OH; or a pharmaceutically acceptable salt thereof.
摘要(中):
本发明涉及能够拮抗兴奋性氨基酸如谷氨酸的作用的新的吲哚-2,3-二酮-3-肟衍生物。 更具体地,本发明的新的吲哚-2,3-二酮-3-肟衍生物可以由通式(I)描述,其中R 3表示“Het”,或式(II)的基团,其中“ Het“表示饱和或不饱和的4至7元单环杂环,R 31,R 32和R 33中的至少一个独立地表示氢,烷基或羟烷基,并且至少一个 R 31,R 32和R 33独立地表示(CH 2)n R 34; 其中R 34表示羟基,羧基,烷氧基羰基,烯氧基羰基,炔氧基羰基,环烷氧基羰基,环烷基 - 烷氧基羰基,芳氧基羰基,芳烷氧羰基,CONR 35 R 36或“Het”。 其中n为0,1,2或3; 并且R 5代表苯基,萘基,噻吩基或吡啶基,它们都可被取代。 “A”表示在标记为“a”和“b”的位置与苯并环稠合的5至7个原子的环,由以下二价基团形成:a-NR 6 -CH 2 -CH 2 -B; 一个-CH2-NR <6> -CH2-B; 一个-CH2-CH2-NR <6> -b; 一个-NR <6> -CH2-CH2-CH2-B; 一个-CH2-NR <6> -CH2-CH2-B; 一个-CH2-CH2-NR <6> -CH2-B; 一个-CH2-CH2-CH2-NR <6> -b; 一个-NR <6> -CH2-CH2-CH2-CH2-B; 一个-CH2-NR <6> -CH2-CH2-CH2-B; 一个-CH2-CH2-NR <6> -CH2-CH2-B; 一个-CH2-CH2-CH2-NR <6> -CH2-B; 或a-CH2-CH2-CH2-CH2-NR6-b; 其中R 6表示氢,烷基或CH 2 CH 2 OH; 或其药学上可接受的盐。