| 摘要 |
A NK-1 receptor antagonist or a pharmaceutically acceptable salt thereof is used in the manufacture of a medicament for treating or preventing a disorder selected from stroke, epilepsy, head trauma, spinal cord trauma, ischemic neuronal damage, cerebral ischemic damage from a stroke or vascular occlusion, excitotoxic neuronal damage and amyotrophic lateral sclerosis in a mammal. The NK-1 antagonist can be a substance P receptor antagonist. Examples of the NK-1 receptor antagonist are the compounds of formula Ia, Ib, Ic, Id or Ie or formulae XI to XXI. In the formulae depicted: A is phenyl, naphthyl, thienyl, quinolinyl or indolinyl with the side chain containing NR2R3 being attached to a carbon atom of A; AA is phenyl, naphthyl, thienyl, dihydroquinolinyl or indolinyl with the side chain containing NR2R3 being attached to a carbon atom of AA; AAA is phenyl, naphthyl, thienyl, dihydroquinolinyl or indolinyl with the side chain containing -CH2P'R3 being attached to a carbon atom of AAA; P' is NR2, O or S(O)q and q is 0 to 2; Q is SO2, NH, -N(alkyl)- or -N(alkyl)-SO2- and the group -N(alkyl)-SO2- is attached to AAA by the nitrogen and to X5 by the sulphur; W1 and W2 are independently H, halo, alkyl, S-alkyl, or optionally fluoro substituted alkoxy; X5 is an optionally substituted 4 to 6 membered heterocyclic ring containing one to three of S, N or O; X and Z are independently =CM-, -C(M)2-, -O-, S(O)q, -N(R4)-, =N- or -NH-; Y is -C(=O)-, -C(=NR4)-, -C(=S)-, =CM-, -C(M)2-, -O-, S(O)q, -N(R4)-, =N- or -NH-; Ar1 to Ar3 are independently optionally aryl or heteroaryl; and the rest of the variables are as defined in the specification.
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