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N-AROILAMINES CYCLES AS ANTAGONISTS OF OREXIN RECEPTORS.

机译:N-谷胱甘肽循环作为食欲素受体的拮抗剂。

摘要

A compound of formula (I): in which: X is O, CR7R8, NH or a bond; R1 and R2 are both hydrogen, both optionally substituted (C1-4) alkyl, or together with the carbon to which they are attached form a cycloalkyl (C3-6) ring or a 4- to 6-membered heterocyclyl ring; R3 and R4 are both hydrogen, both optionally substituted (C1-4) alkyl, or together with the carbon to which they are attached form a cycloalkyl (C3-6) ring or a 4- to 6-membered heterocyclyl ring; R7 and R8 are both hydrogen, both optionally substituted (C1-4) alkyl, or together with the carbon to which they are attached form a cycloalkyl (C3-6) ring or a 4- to 6-membered heterocyclyl ring; with the proviso that a pair of R1 and R2, R3 and R4, R7 and R8 are both optionally substituted (C1-4) alkyl, or together with the carbon to which they are attached form a cycloalkyl (C3-6) ring or a 4 to 6-membered heterocyclyl ring, and the rest of the groups are hydrogen; R5 is hydrogen, optionally substituted (C1-4) alkyl, or (C1-4) alkyl optionally substituted CO; Ar1 is an optionally substituted aryl, an optionally substituted mono- or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; Ar2 represents phenyl, or a 5- or 6-membered heterocyclic group containing up to 3 heteroatoms selected from N, O and S, in which the phenyl or heterocyclyl group is substituted with R6 and other optional substituents; or Ar2 represents an optionally substituted bicyclic or bicyclic heteroaromatic group containing up to 4 heteroatoms selected from N, O and S; R6 represents hydrogen, optionally substituted (C1-4) alkoxy, halogen, cyano, optionally substituted (C1-6) alkyl, optionally substituted phenyl, or an optionally substituted 5 or 6 membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; or its pharmaceutically acceptable salt.
机译:式(I)的化合物:其中:X为O,CR 7 R 8,NH或键; R 1和R 2均为氢,均是任选取代的(C 1-4)烷基,或与它们所连接的碳一起形成环烷基(C 3-6)环或4至6元杂环基环; R3和R4都是氢,它们都是任选取代的(C1-4)烷基,或与它们相连的碳一起形成环烷基(C3-6)环或4-至6-元杂环基环; R7和R8都是氢,它们都是任选取代的(C1-4)烷基,或与它们相连的碳一起形成环烷基(C3-6)环或4-至6-元杂环基环;前提是一对R1和R2,R3和R4,R7和R8均为可选取代的(C1-4)烷基,或与它们连接的碳一起形成环烷基(C3-6)环或4至6元杂环基环,其余基团为氢; R5是氢,任选取代的(C1-4)烷基或(C1-4)烷基任选取代的CO; Ar 1是任选取代的芳基,是任选取代的单环或双环杂芳基,其含有至多3个选自N,O和S的杂原子; Ar 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元杂环基,其中苯基或杂环基被R 6和其他任选的取代基取代;或Ar 2表示任选取代的双环或双环杂芳族基团,其含有至多4个选自N,O和S的杂原子; R 6代表氢,含有至多4个选自N,O的杂原子的氢,任选取代的(C1-4)烷氧基,卤素,氰基,任选取代的(C1-6)烷基,任选取代的苯基或任选取代的5或6元杂环基。和S;或其药学上可接受的盐。

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