HETEROCICLIC DERIVATIVES (INDOL-3-IL), AS CB1 CANNABINOID RECEPTOR AGONISTS.

摘要

A heterocyclic (indole-3-yl) derivative having the general Formula I (See formula) where A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CR; R is H or (C1-4) alkyl; or R, when present in X2 or X3, together with R3 can form a 5-8 member ring; R1 is a saturated carbocyclic ring of 5 to 8 members, which eventually contains a heteroatom selected from O and S; R2 is H, CH3 or CH2-CH3; or R2 joins together with R7 to form a 6-membered ring, which eventually contains a heteroatom selected from O and S, and whose heteroatom binds to position 7 of the indole ring; R3 and R4 are independently H, (C1-6) alkyl or (C3-7) cycloalkyl, the alkyl groups being optionally substituted with OH, C1-4 alkyloxy, C1-4 alkylthio, C1-4 alkylsulfonyl , CN or halogen; or R3, together with R4 and the N to which they are attached, form a 4-8 membered ring that eventually contains another heteroatom selected from O and S, and which is optionally substituted with OH, (C1-4) alkyl, alkyloxy ( C1-4), (C1-4) alkyloxy (C1-4) alkyl or halogen; or R3, together with R5, forms a 4-8 membered ring that eventually contains another heteroatom selected from O and S, and which is optionally substituted with OH, (C1-4) alkyl, (C1-4) alkyloxy, ( C1-4) (C1-4) alkyl or halogen; or R3, together with R, when present in X2 or X3, forms a 5-8 member ring; R5 is H or (C1-4) alkyl; or R5, together with R3, forms a 4-8 membered ring that eventually contains another heteroatom selected from O and S, and which is optionally substituted with OH, (C1-4) alkyl, (C1-4) alkyloxy, ( C1-4) (C1-4) alkyl or halogen; R5 '' is H or (C1-4) alkyl; R6 represents 1-3 substituents independently selected from H, (C1-4) alkyl, (C1-4) alkyloxy, CN and halogen; R7 is H, (C1-4) alkyl, (C1-4) alkyloxy, CN or halogen; or R7 joins R2 to form a 6-membered ring, which eventually contains another heteroatom selected from O and S, and whose heteroatom binds to position 7 of the indole ring; or a pharmaceutically acceptable salt thereof.