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    • 9. 发明授权
    • Piperdines for use as orexin receptor antagonists
    • 用作食欲肽受体拮抗剂的Pi子
    • US06677354B2
    • 2004-01-13
    • US10311445
    • 2002-12-16
    • Clive Leslie BranchChristopher Norbert JohnsonGeoffrey StempKevin Thewlis
    • Clive Leslie BranchChristopher Norbert JohnsonGeoffrey StempKevin Thewlis
    • A61K314545
    • C07D401/06C07D211/26C07D401/10C07D405/06C07D405/10C07D405/14C07D409/14C07D413/10C07D413/14C07D417/06C07D417/14C07D471/04
    • Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 3 heteroatoms selected from N, O and S; or pharmaceutically acceptable salts thereof.
    • 公开了式(I)的化合物:其中:Y表示基团(CH 2)n,其中n表示0,1或2; R 1是苯基,萘基,含有至多3个选自杂原子的单或双环杂芳基 来自N,O和S; 或NR 3或R 4基团,其中R 3和R 4中的一个是氢或任选取代的(C 1-4)烷基,另一个是苯基,萘基或含有上述的单或双环杂芳基 至3个选自N,O和S的杂原子,或R 3和R 4与它们所连接的N原子一起形成具有任选稠合的苯环的5至7元环胺; 任何R 1可以任选被取代; R 2表示苯基或含有至多3个选自N,O和S的杂原子的5-或6-元杂芳基,其中苯基或杂芳基被取代 R 5和另外任选的取代基; 或R 2表示含有至多3个选自N,O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 5表示任选取代的(C 1-4)烷氧基,卤素,任选取代的(C1- 6)烷基,任选取代的苯基或含有至多3个选自N,O和S的杂原子的任选取代的5或6元杂环; 或其药学上可接受的盐。