The present invention relates to compounds comprising an oxazoline or thiazoline moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, (I), wherein A1 is CH C(CH3) or N; R1 is hydrogen or halogen; R2 is (II); A2 is O or S; R3 is hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy; R4 is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or —O—(CH2)n-NR12aR each CH2 in —O—(CH2)n-NR12aR12b being optionally substituted by one or two C1-4 alkyl; R5 is hydrogen or —O—(CH2)m—NR13aR13b, each CH2 in —O—(CH2)m—NR13aR13b being optionally substituted by one or two C1-4 alkyl, and at least one of R4 and R5 should be a —O—(CH2)n-NR12/13aR12/13b group.
本发明涉及具有氧唑啉或
噻唑啉基团的化合物,制备它们的方法,包含所述化合物的制药组合物以及其作为H3受体
配体的用途,其中A1是CH、C(
CH3)或N;R1是氢或卤素;R2是(II);A2是O或S;R3是氢、卤素、C1-4烷基或C1-4烷氧基;R4是氢、卤素、C1-4烷基、C1-4烷氧基、三
氟甲基或—O—(
CH2)n-NR12aR,其中—O—( )n-NR12aR12b中的每个 可以选择性地由一个或两个C1-4烷基取代;R5是氢或—O—( )m—NR13aR13b,其中—O—( )m—NR13aR13b中的每个 可以选择性地由一个或两个C1-4烷基取代,且R4和R5中至少有一个应为—O—( )n-NR12/13aR12/13b基团。