申请人:——
公开号:US20040192673A1
公开(公告)日:2004-09-30
This invention relates to N-aroyl cyclic amine derivatives of formula (I): wherein: Y represents a bond, oxygen, or a group (CH
2
)
n
, wherein n represents 1, 2 or 3 m represents 1, 2 or 3; p represents 0 or 1; X is O,SC═O, SO
2
, or —CH═CH; Ar
1
is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar
2
represents phenyl or a 5- or 5-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R
1
and further optional substituents; or Ar
2
represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R
1
represents hydrogen, optionally substituted (C
1-4
)alkoxy, halo, cyano, optionally substituted (C
1-16
)alkyl, optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acceptable salt thereof; and their use as pharmaceuticals, specifically as orexin receptor antagonists.
本发明涉及式(I)的 N-芳酰基环胺衍生物: 式中.Y 代表键、氧或基团(CH
2
)
n
其中 n 代表 1、2 或 3 m 代表 1、2 或 3; p 代表 0 或 1; X 是 O、SC═O、SO
2
或 -CH═CH; Ar
1
是芳基,或含有最多 4 个选自 N、O 和 S 的杂原子的单环或双环杂芳基,其中任一杂芳基可被任选取代;Ar
2
代表苯基或含有多达 3 个选自 N、O 和 S 的杂原子的 5 元或 5 元杂环烷基,其中苯基或杂环烷基被 R
1
和其他任选取代基取代;或 Ar
2
代表一个被任选取代的双环芳香族或双环杂芳香族基团,其中最多含有 3 个选自 N、O 和 S 的杂原子; R
1
代表氢、任选取代的 (C
1-4
烷氧基、卤代、氰基、任选取代的(C
1-16
)烷基、任选取代的含有多达 4 个选自 N、O 和 S 的杂原子的 5 或 6 元杂环;或其药物可接受盐;以及它们作为药物的用途,特别是作为奥曲肽受体拮抗剂的用途。