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NEW Pyrrole Inhibitors of S-Nitrozoglutathione Reductase as Therapeutic Agents

机译:S-硝基谷胱甘肽还原酶的新型吡咯抑制剂作为治疗药物

摘要

1. The compound of formula I or its pharmaceutically acceptable salts:! ! where Ar is selected from the group consisting of phenyl and thiophenyl; ! R1 is selected from the group consisting of unsubstituted imidazolyl, substituted imidazolyl, chloro, bromo, fluoro, hydroxy and methoxy; ! R2 is selected from the group consisting of hydrogen, methyl, chloro, fluoro, hydroxy, methoxy, ethoxy, propoxy, carbamoyl, dimethylamino, amino, formamido and trifluoromethyl; and! X is selected from the group consisting of CO and SO2. ! 2. The compound according to claim 1, where R1 is selected from the group consisting of unsubstituted imidazolyl and substituted imidazolyl. ! 3. The compound of claim 2, wherein the substituted imidazolyl group is substituted with C1-C6 alkyl. ! 4. The compound according to claim 2, where ArR1R2 is selected from the group consisting of:! ; ; ; ! ; ! where R3 is selected from H, methyl and ethyl. ! 5. The compound according to claim 2, selected from the group consisting of the following compounds:! 3- (5- (4- (1H-imidazol-1-yl) phenyl) -1- (4-carbamoyl-2-methylphenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (5- (5- (1H-imidazol-1-yl) thiophen-2-yl) -1- (4-carbamoyl-2-methylphenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (1- (4-carbamoyl-2-methylphenyl) -5- (4- (2-methyl-1H-imidazol-1-yl) phenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (1- (4-carbamoyl-2-methylphenyl) -5- (4- (4-methyl-1H-imidazol-1-yl) phenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (1- (4-carbamoyl-2-methylphenyl) -5- (4- (2-ethyl-1H-imidazol-1-yl) phenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (5- (4- (1H-imidazol-1-yl) thiophen-2-yl) -1- (4-carbamoyl-2-methylphenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (1- (4-carbamoyl-2-methylphenyl) -5- (5- (2-methyl-1H-imidazol-1-yl) thiophen-2-yl) -1H-pyrrole-2-yl) propanoic acid ; ! 3- (1- (4-carbamoyl-2-methylphenyl) -5- (3-fluoro-4- (1H-imidazol-1-yl) phenyl) -1H-pyrrol-2-yl) propanoic acid; ! 3- (
机译:1.式I化合物或其药学上可接受的盐: !其中Ar选自苯基和苯硫基; ! R1选自未取代的咪唑基,取代的咪唑基,氯,溴,氟,羟基和甲氧基; ! R2选自氢,甲基,氯,氟,羟基,甲氧基,乙氧基,丙氧基,氨基甲酰基,二甲氨基,氨基,甲酰胺基和三氟甲基。和! X选自CO和SO 2。 ! 2.根据权利要求1的化合物,其中R1选自未取代的咪唑基和取代的咪唑基。 ! 3.权利要求2的化合物,其中所述取代的咪唑基被C1-C6烷基取代。 ! 4.根据权利要求2的化合物,其中ArR1R2选自: ; ; ; ! ; !其中R 3选自H,甲基和乙基。 ! 5.根据权利要求2所述的化合物,其选自以下化合物: 3-(5-(4-(4-(1H-咪唑-1-基)苯基))-1-(4-氨基甲酰基-2-甲基苯基)-1H-吡咯-2-基)丙酸; ! 3-(5-(5-(5-(1H-咪唑-1-基)噻吩-2-基)-1-(4-氨基甲酰基-2-甲基苯基)-1H-吡咯-2-基)丙酸; ! 3-(1-(4-氨基甲酰基-2-甲基苯基)-5-(4-(2-甲基-1H-咪唑-1-基)苯基)-1H-吡咯-2-基)丙酸; ! 3-(1-(4-氨基甲酰基-2-甲基苯基)-5-(4-(4-甲基-1H-咪唑-1-基)苯基)-1H-吡咯-2-基)丙酸; ! 3-(1-(4-氨基甲酰基-2-甲基苯基)-5-(4-(2-乙基-1H-咪唑-1-基)苯基)-1H-吡咯-2-基)丙酸; ! 3-(5-(4-(4-(1H-咪唑-1-基)噻吩-2-基)-1-(4-氨基甲酰基-2-甲基苯基)-1H-吡咯-2-基)丙酸; ! 3-(1-(4-氨基甲酰基-2-甲基苯基)-5-(5-(5-(2-甲基-1H-咪唑-1-基)噻吩-2-基)-1H-吡咯-2-基)丙酸; ! 3-(1-(4-氨基甲酰基-2-甲基苯基)-5-(3-氟-4-(1H-咪唑-1-基)苯基)-1H-吡咯-2-基)丙酸; ! 3-(

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