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5-membered heterocycles for the treatment of human diseases involving modulatorsof selectins

机译:用于治疗人类疾病的5元杂环,涉及选择素调节剂

摘要

Compounds of Formula (1) (where at least one of R1, R2 or R3 contains calcium binding moiety e.g. CO2H etc.) are disclosed. Where R1 is typically a moiety containing a terminal carboxylic acid group such as cinnamic acid or phenoxy acetic acid, R2 is typically a hydrophobic moiety such as functionalized alkyl chain or a functionalized aryl group, and R3 is typically a functionalized aryl group, are within the scope of this invention. These compounds exhibit inhibitory activity against P-, L- and E-selectin and are indicated in the treatment of human diseases involving P-, L- and E-selectin.
机译:公开了式(1)的化合物(其中R 1,R 2或R 3中的至少一个包含钙结合部分,例如CO 2 H等)。其中R 1典型地是包含末端羧酸基团的部分,例如肉桂酸或苯氧基乙酸,R 2典型地是疏水性部分,例如官能化的烷基链或官能化的芳基,并且R 3是通常官能化的芳基在本发明的范围内。这些化合物表现出对P-,L-和E-选择素的抑制活性,并在涉及P-,L-和E-选择素的人类疾病的治疗中得到指示。

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