NOVEL MELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES

摘要

Novel melatonin ligands of Formula I:; ;or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR₈; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C₁-C₆ alkyl, C₃-C₆ cycloalkyl, and; ;R is selected from the group consisting of hydrogen, hydroxyl, —OCF₃, CF₃, C₁-C₈ alkyl, C₁-C₈ alkyloxy, C₁-C₈ alkylthio, halogen and —Z—(CH₂)_p-A; R₁ is selected from the group consisting of C₁-C₄ alkyl, C₃-C₆ cycloalkyl, CF₃, hydroxy-substituted C₁-C₄ alkyl, hydroxy-substituted C₃-C₆ cycloalkyl, and NHR₅, wherein R₅ is C₁-C₃ alkyl or C₃-C₆ cycloalkyl; R₂ is selected from the group consisting of: hydrogen, C₁-C₄ alkyl, C₁-C₄ alkyloxy, OCF₃, CF₃, hydroxyl, and halogen; R₃ is selected from the group consisting of hydrogen, C₁-C₄ alkyl, C₁-C₄ alkyloxy, OCF₃, CF₃, hydroxyl, and halogen; R and R₃ may be connected together to form an —O—(CH₂)_v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R₄ is selected from the group consisting of hydrogen, C₁-C₄ alkyl, C₁-C₄ alkyloxy, OCF₃, CF₃, hydroxyl, and halogen; R₆ is selected from the group consisting of hydrogen and C₁-C₆ alkyl; R₇ is selected from the group consisting of hydrogen, C₁-C₄ alkyl, C₁-C₄ alkyloxy, OCF₃, CF₃, hydroxyl, and halogen; and R₈ is selected from the group consisting of hydrogen and C₁-C₄ alkyl.