首页> 外国专利> New 1-(N-substituted amidoalkyl) bicyclic uracil derivatives useful as medicaments for treating ischemia or reperfusion damage, are poly-(ADP-ribose)-synthetase inhibitors

New 1-(N-substituted amidoalkyl) bicyclic uracil derivatives useful as medicaments for treating ischemia or reperfusion damage, are poly-(ADP-ribose)-synthetase inhibitors

机译:新的1-(N-取代的酰胺基烷基)双环尿嘧啶衍生物可作为治疗缺血或再灌注损伤的药物,是聚-(ADP-核糖)合成酶抑制剂

摘要

1-(N-Substituted amidoalkyl) 5,6-fused bicyclic uracil derivatives (I) are new. 1-(N-Substituted amidoalkyl) 5,6-fused bicyclic uracil derivatives of formula (I) and their salts, hydrates, hydrated salts and solvates are new. A = J, CH2-J, J-CH2, CH=CHCH2, CH2CH=CH, CH2CH2-J, J-CH2CH2 or CH2-J-CH2; J = CH2, O or S; E, G = 1-6C alkylene or 3-8C cycloalkylene (optionally substituted by one or more of 1-4C alkoxy, OH or NH2); T = direct bond or CH2; U, V = direct bond or CC (sic); or 6-10C arylene or 5-7 membered heterocyclene (containing 1-3 of O, S and N as heteroatom(s)), both optionally substituted by 1-3 of NO2, CN, halo, R, 3-8C cycloalkyl, OR, CF2, OCHF2, OCF3, OH, NH2, NHR, N(R)2, COOR, SO2NH2, SO2R, SO2NHR, SO2N(R)2 or OCOR; W = direct bond, O, S, COO, OCO or NR4; R4 = H or R; X = O, S or NR5; Y1 = H and Y2 = OH; or Y1 + Y2 = =O, =S or =NR6; R5, R6 = H, R or CH2Ph; R1 = H, R (optionally substituted by one or more halo) or 3-8C cycloalkyl; R2 = H or COOR; R3 = 6-10C aryl or 5-13 membered heterocyclyl (containing 1-4 of O, S and N as heteroatom(s)), both optionally substituted by 1-3 of NO2, CN, halo, R, 3-8C cycloalkyl, OR, CF2, OCHF2, OCF3, OH, =O, NH2, NHR, N(R)2, CH2NHR, CH2N(R)2, COOR, SO2NH2, SO2R, SO2NHR, SO2N(R)2, OCOR or CH2R7; R7 = 5-7 membered heterocycle containing 1-3 of O, S and N as heteroatom(s); and R = 1-6C alkyl. An Independent claim is also included for the preparation of (I).
机译:1-(N-取代的酰胺烷基)5,6-稠合的双环尿嘧啶衍生物(I)是新的。式(I)的1-(N-取代的酰胺基烷基)5,6-稠合的双环尿嘧啶衍生物及其盐,水合物,水合盐和溶剂化物是新的。 A = J,CH2-J,J-CH2,CH = CHCH2,CH2CH = CH,CH2CH2-J,J-CH2CH2或CH2-J-CH2; J = CH2,O或S; E,G = 1-6C亚烷基或3-8C亚环烷基(任选地被1-4C烷氧基,OH或NH 2中的一个或多个取代); T =直接键或CH2; U,V =直接键或CC(原文如此);或6-10C亚芳基或5-7元杂环(含有1-3的O,S和N作为杂原子),二者均可选地被1-3的NO2,CN,卤素,R,3-8C环烷基取代,或CF2,OCHF2,OCF3,OH,NH2,NHR,N(R)2,COOR,SO2NH2,SO2R,SO2NHR,SO2N(R)2或OCOR; W =直接键,O,S,COO,OCO或NR4; R4 = H或R; X = O,S或NR5; Y1 = H,Y2 = OH;或者Y1 + Y2 = = O,= S或= NR6; R5,R6 = H,R或CH2Ph; R1 = H,R(任选地被一个或多个卤素取代)或3-8C环烷基; R2 = H或COOR; R3 = 6-10C芳基或5-13元杂环基(包含1-4的O,S和N作为杂原子),两者均可选地被1-3的NO2,CN,卤素,R,3-8C环烷基取代,或,CF2,OCHF2,OCF3,OH = O,NH2,NHR,N(R)2,CH2NHR,CH2N(R)2,COOR,SO2NH2,SO2R,SO2NHR,SO2N(R)2,OCOR或CH2R7; R7 = 5-7元杂环,含有1-3个O,S和N作为杂原子; R = 1-6C烷基。独立索赔也包括在准备(I)中。

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