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5- (3-phenyl-3-oxo-propyl) -1H-tetrazole derivative

机译:5-(3-苯基-3-氧代丙基)-1H-四唑衍生物

摘要

PCT No. PCT/EP98/04032 Sec. 371 Date Dec. 30, 1999 Sec. 102(e) Date Dec. 30, 1999 PCT Filed Jun. 25, 1998 PCT Pub. No. WO99/02506 PCT Pub. Date Jan. 21, 19995-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, SOR4 or SO2R4 wherein R4 is C1-C6 alkyl, -N(R5R6) in which each of R5 and R6 is, independently, hydrogen, C1-C6 alkyl, formyl or C2-C6 acyl; R2 is hydrogen, C1-C6 alkyl, C1-C6 alkoxy, benzyl, phenyl; R3 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, benzyl, phenyl or a group -N(R7R8) in which each of R7 and R8 is, independently, hydrogen, C1-C4 alkyl, benzyl, phenyl, or one of R7 and R8 is hydrogen and the other is COR9 wherein R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, phenyl or a group -N(R10R11) in which R10 and R11 are, each independently, hydrogen or C1-C4 alkyl or, taken together, R2 and R3 form a carbocyclic C3-C6 ring; and pharmaceutically acceptable salts thereof have kynurenine-3-hydroxylase enzyme inhibitory activity.
机译:PCT号PCT / EP98 / 04032第二部分371日期1999年12月30日102(e)日期,1999年12月30日PCT,1998年6月25日提交,PCT Pub。 WO99 /​​ 02506 PCT公开号1999年1月21日发布,式(I)的5-(3-苯基-3-氧代丙基)-1H-四唑衍生物,其中R和R1相同或不同,为氢,卤素,羟基,三氟甲基,氰基,硝基,苯基,苄基,C1-C6烷基,C1-C6烷氧基,C1-C6烷硫基,SOR4或SO2R4(其中R4为C1-C6烷基),-N(R5R6),其中R5和R6各自独立地为:氢,C 1 -C 6烷基,甲酰基或C 2 -C 6酰基; R2是氢,C1-C6烷基,C1-C6烷氧基,苄基,苯基; R 3是氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,苄基,苯基或-N(R 7 R 8)基团,其中R 7和R 8各自独立地是氢,C 1 -C 4烷基,苄基,苯基或R7和R8之一为氢,另一个为COR9,其中R9为氢,C1-C4烷基,C1-C4烷氧基,苯基或-N(R10R11)基团,其中R10和R11分别独立地为氢或C1- C 4烷基或R 2和R 3一起形成碳环C 3 -C 6环;及其药学上可接受的盐具有犬尿氨酸-3-羟化酶抑制活性。

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