| abstract |
Compounds of the formula (I) or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein: R is heta; R1 is phenyl optionally substituted by one or more substituents; m is 1-4; Z is selected from: a) N(R3)(R4X) wherein X is NR?3R5, OR5, Oaryl1, Ohetb, Ohetc, aryl1, hetb or hetc¿; b) N(R3)Y wherein Y is aryl?1, hetb or hetc¿; and c) a 4-7 membered N containing saturated or partially saturated heterocycle said heterocycle attached to the alkylene link via said nitrogen atom, said heterocycle optionally containing an additional 1-3 groups, each independently selected from C=O, NH, S(O)¿p? and O; optionally, said heterocycle is: (i) spirofused with het?b¿, such that both rings share 1 atom; or (ii) optionally independently substituted by 1-3 groups; wherein R?3 and R6¿ are both independently selected from H and C¿1-6?alkyl; wherein R?4¿ is selected from C¿1-6? alkylene; wherein R?5¿ is selected from C(O)OR3, S(O)¿pR?3, S(O)¿p?aryl?1, C(O)R3¿, and C(O)NR?3R6; hetb¿ is a 4-7 membered heterocycle containing 1-3 heteroatoms, each independently selected from N, O and S, said N being optionally substituted with O, said ring optionally containing 1-2 C=O groups, said ring being saturated or partially saturated, said ring being optionally benzofused, said ring being optionally substituted by 1-3 substituents; heta and hetc are a 5-7 membered aromatic heterocycle containing 1-3 heteroatoms each independently selected from N, O and S, said ring being optionally benzofused, said ring system as a whole being optionally substituted by 1-3 substituents; aryl1 is phenyl or naphthyl, each being optionally substituted by 1-3 substituents; p is 0, 1 or 2; and n is 0-4; are useful in treating or preventing a condition for which an NK¿2? antagonist is efficacious. |