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use of imidazole derivatives for the treatment of angiotensin receptors at1 and complaints which are involved in at2 these compounds, their production, use as medicinesand pharmaceutical compositions containing it
use of imidazole derivatives for the treatment of angiotensin receptors at1 and complaints which are involved in at2 these compounds, their production, use as medicinesand pharmaceutical compositions containing it
Use of tetra-substd. imidazole derivs. of formula (I), their enantiomers and diastereomers and their acid and base addn. salts, to treat disorders arising from abnormal stimulation of angiotensin II receptors AT1 and AT2, is new. R1 = 1-6C alkyl, alkylthio, alkoxy, aryl, arylthio, aryloxy or aryl(1-6C)alkyl; R2 = -S-R, -O-R, -C(OH)(R)-COOH; halo; or -C(=O)Z; R = 1-8C alkyl, 2-8C alkenyl, 3-6C cycloalkyl or aryl (all opt. substd.); Z = OH, alkoxy or carboxy; R3 = carboxy, acyl halo, 1-8C alkyl, 2-8C alkenyl or alkylthio, aryl, aryl(1-6C)alkyl or aryl(2-6C)alkenyl; R4 = -(CH2)ml-COOR14, -(CH2)ml-CONHR14, -(CH2)ml-CN, -SO2-NH-SO2-R14, -NH-SO2-R14, -PO3R14, SO2NHSO2NR14R15, -SO2NHSO2N(-CH2-CH2-)2D, -SO2-W-R14, etc.; m1 = 0-4; D = O or S; W = -NR15-, -NH-CO-, -NH-CO-O-, -N=CH-N-R15-, or -NH-CO-NR15-; R14, R15 = H, 1-8C alkyl, 2-8C alkenyl, 3-6C cycloalkyl or aryl; or NR14R15 = pyrrolyl, pyrrolinyl, pyrrolidinyl, piperazinyl, alkylpiperazinyl, phenylpiperazinyl, morpholinyl or indolinyl; alkyl radicals are opt. interrupted by one or more heteroatoms (O, N or S); S atoms are opt. oxidised to sulphone or sulphoxide.
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机译:使用四取代。咪唑衍生物。式(I)的通式,其对映异构体和非对映异构体以及其酸和碱加成基。用于治疗由于血管紧张素II受体AT1和AT2异常刺激而引起的疾病的新型盐是新的。 R1 = 1-6C烷基,烷硫基,烷氧基,芳基,芳硫基,芳氧基或芳基(1-6C)烷基; R 2 = -S-R,-O-R,-C(OH)(R)-COOH;光环;或-C(= O)Z; R = 1-8C烷基,2-8C链烯基,3-6C环烷基或芳基(全部选择)。 Z = OH,烷氧基或羧基; R3 =羧基,酰基卤,1-8C烷基,2-8C烯基或烷硫基,芳基,芳基(1-6C)烷基或芳基(2-6C)烯基; R4 =-(CH2)ml-COOR14,-(CH2)ml-CONHR14,-(CH2)ml-CN,-SO2-NH-SO2-R14,-NH-SO2-R14,-PO3R14,SO2NHSO2NR14R15,-SO2NHSO2N( -CH2-CH2-)2D,-SO2-W-R14等; m1 = 0-4; D = O或S; W = -NR15-,-NH-CO-,-NH-CO-O-,-N = CH-N-R15-或-NH-CO-NR15-; R14,R15 = H,1-8C烷基,2-8C烯基,3-6C环烷基或芳基;或NR14R15 =吡咯基,吡咯烷基,吡咯烷基,哌嗪基,烷基哌嗪基,苯基哌嗪基,吗啉基或吲哚基;或烷基是优选的。被一个或多个杂原子(O,N或S)打断;选择S原子。氧化成砜或亚砜。
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