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2- (Hetero) arylbenzimidazole and imidazopyridine derivatives as inhibitors of asparagine methyltransferase

机译:2-(杂)芳基苯并咪唑和咪唑并吡啶衍生物作为天冬酰胺甲基转移酶的抑制剂

摘要

Substituted benzimidazole and 3H-imidazo [4,5-b] pyridine or Formula I: [wherein X and Y are selected from (i) N and N respectively; and (ii) N and CR 4:; A 2 is 2 Or a C5 heteroarylene group containing 3 ring heteroatoms, wherein the bond to L1 and the bond to the center are β with respect to each other; L1 is (i) A1-O-CH2- (Ii) A1-CH2-O-A2; (iii) A1-C (= O) -NH-A2; (iv) A1-CH (OH) -A2; (v) A1-CH2-NH-C (= O) -A2; (vi) A1-S-CH2-A2; (vii) A1-CH2-S-A2; (viii) A1-CH2-A2; and (ix) A1-CH (CH3) -O -A2: selected; A1 is phenyl optionally substituted with F or CF3], their use as pharmaceuticals, especially in the treatment of cancer and abnormal hemoglobinosis
机译:取代的苯并咪唑和3H-咪唑并[4,5-b]吡啶或式I:[其中X和Y分别选自(i)N和N; (ii)N和CR 4: A 2为2或含有3个环杂原子的C 5杂亚芳基,其中与L 1的键和与中心的键相对于β。 L1是(i)A1-O-CH2-(Ii)A1-CH2-O-A2; (iii)A1-C(= O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(= O)-A2; (vi)A1-S-CH2-A2; (vii)A1-CH2-S-A2; (viii)A1-CH2-A2; (ix)A1-CH(CH3)-O -A2:已选择; A1是任选被F或CF3取代的苯基],其用作药物的用途,尤其是在治疗癌症和异常血红蛋白病中

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