EP0360390A1 — Spirolactam derivatives

USPTO Abstract

These are described spirolactam derivatives of formulae (Ia) and (Ib) wherein R represents a hydrogen atom or a conventional nitrogen protecting group; R¹ represents a hydrogen atom or a conventional carboxyl protecting group or activating group; R² represents the side chain of any naturally occurring amino acid; m represents 1 or 2; n representss 1 or 2; the configuration at * may be (R) or (S) or a mixture thereof; with the proviso that when R represents the nitrogen protecting group R³-CO(O)- (where R³ represents (CH₃)₃C-), the group -CO₂R¹ represents the protected carboxy group -CO₂CH₃, m is 1 and n is 1 in the compounds of formula (Ib); R² may not represent an arylmethyl group; and solvates or acid addition salts thereof. These derivatives are of value in the preparation of spirolactam compounds which, depending on their stereochemistry, are either antagonists or agonists of substance P, and as such have a variety of therapeutic properties.