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BENZOXAZOLE, BENZTHIAZOLE AND BENZIMIDAZOLE ACID DERIVATIVES AND THEIR USE AS HEPARANASE INHIBITORS

机译:苯并恶唑,苯并噻唑和苯并咪唑酸衍生物及其作为肝素酶抑制剂的用途

摘要

Compounds of formula (I): wherein R1, R2 and R3 are independently, hydrogen, halogen, CF3, OR6, NR7R8, NR8COR10, NR8SO2R10 or C1-6 alkyl optionally substituted by hydroxy, C1-6 alkoxy or NR7R8; R4 is NR8CONR8R9, NR8COR9, NR8SO2R9, or W-CONR8R9, where W is a bond, C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene; and R5 is Formula (A) methods for their synthesis, pharmaceutical compositions comprising them and their use in medicine, in particular for the treatment of cancer.
机译:式(I)的化合物:其中R 1,R 2和R 3独立地为氢,卤素,CF 3,OR 6,NR 7 R 8,NR 8 COR 10,NR 8 SO 2 R 10或任选被羟基,C 1-6烷氧基或NR 7 R 8取代的C 1-6烷基; R 4是NR 8 CONR 8 R 9,NR 8 COR 9,NR 8 SO 2 R 9或W-CONR 8 R 9,其中W是键,C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基; R 5是用于合成的式(A)方法,包含它们的药物组合物及其在医学中的用途,特别是用于治疗癌症。

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