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Benzoxazine derivatives and benzothiazine derivatives having nos-inhibitory and antioxidant properties

机译:具有Nos抑制和抗氧化性能的苯并恶嗪衍生物和苯并噻嗪衍生物

摘要

The invention relates to compounds of formula (I) and to the tautomeric and isomeric forms and salts thereof, wherein: X represents O or S; R1 represents -(CHR9)n-NR7-A-NR8-B, -(CHR9)n-NR8-B or -(CHR9)n-B; R2 represents hydrogen or R1 and R2, together with two adjacent carbon atoms, form a 5-, 6-, 7- or 8-member ring, which is monocyclic or bicyclic, saturated or unsaturated, and in which 1 or 2 CH2 groups can be replaced by oxygen or carbonyl, and which is substituted by -(CHR9)r-NR7-A-NR8-B, -(CHR9)n-B or -(CHR9)r-NR8-B; R3 represents hydrogen or NR15R16; R4 represents hydrogen or acyl; R5 and R6, independent of one another, represent hydrogen, C3-7 cycloalkyl, phenyl, C1-6 alkyl, C2-6 alkenyl radicals or C2-6 alkynyl radicals, which can each be substituted by halogen, OH, O-C1-6 alkyl, SH, S-C1-6 alkyl, NR15R16, 5- or 6-member heteroaryl with 1-3 N, O or S atoms, phenyl or C3-7 cycloalkyl; A represents a straight-chain or branched C1-6 alkylene or -(CH2)p-Q-(CH2)q-, and; B represents (II) or (III). The invention also relates to the method for preparing said compounds and to their use in medicaments.
机译:本发明涉及式(I)化合物及其互变异构和异构形式及其盐,其中:X代表O或S; R 1代表-(CHR 9)n-NR 7 -A-NR 8 -B,-(CHR 9)n-NR 8-B或-(CHR 9 )nB; R 2代表氢或R 1和R 2与两个相邻的碳原子一起形成5、6、7或8元环,其为单环或双环,饱和或不饱和的,并且其中1或2个CH 2基团可以被氧或羰基取代,并且被-(CHR 9)r-NR 7 -A-NR 8 -B,-(CHR 9)取代)nB或-(CHR 9)r -NR 8 -B; R 3代表氢或NR 15 R 16; R 4代表氢或酰基; R 5和R 6彼此独立地表示氢,C 3-7环烷基,苯基,C 1-6烷基,C 2-6烯基或C 2-6炔基,它们各自可以被卤素取代, OH,O-C1-6烷基,SH,S-C1-6烷基,NR 15 R 16,具有1-3个N,O或S原子的5或6元杂芳基,苯基或C3-7环烷基A表示直链或支链的C 1-6亚烷基或-(CH 2)p -Q-(CH 2)q-,和; B代表(II)或(III)。本发明还涉及制备所述化合物的方法及其在药物中的用途。

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