LACTAMS AS TACHYKININ ANTAGONISTS

摘要

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 NR3R5, OR5, Oaryl1, Ohetb, Ohetc, aryl1, hetb or het c; b) N(R3)Y wherein Y is aryl1, hetb or hetc; and c) a 4-7 membered N containi ng saturated or partially saturated heterocycle said heterocycle attached to th e 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 an d O; optionally, said heterocycle is: (i) spirofused with hetb, such that both rings share 1 atom; or (ii) optionally independently substituted by 1-3 groups; wherein R3 and R6 are both independently selected from H and C1- 6alkyl; wherein R4 is selected from C1-6 alkylene; wherein R5 is selected fr om C(O)OR3, S(O)pR3, S(O)paryl1, C(O)R3, and C(O)NR3R6; 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 substitute d 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 optional ly 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; ar e useful in treating or preventing a condition for which an NK2 antagonist is efficacious.