Treating symptoms of chronic pain of neuropathic or psychogenic origin, using 1-benzoyl-4-(pyridinylmethyl-aminomethyl)-piperidine derivatives having both symptomatic and curative analgesic action

摘要

The use of 1-benzoyl-4-(((pyridin-2-ylmethyl)-amino)-methyl)-piperidine derivatives (I) for treating the symptoms of chronic pain of neuropathic or psychogenic origin is new. The use of pyridine derivatives of formula (I), or their mineral or organic acid addition salts, is claimed in the production of medicaments for treating the symptoms of chronic pain of neuropathic or psychogenic origin. [Image] U : H; or may also be Me if V = W = H; V : H or Cl; or may also be Me if U = W = H; W : H or F; or may also be Me if U = V = H; X : H or F; Y : Cl or Me; Z : H, F, Cl or Me; A : H, F, Cl, 1-5C alkyl, fluoroalkyl (e.g. CH 2F, CHF 2, CF 3, CHFMe or CF 2Me), 3-5C cycloalkyl, optionally substituted 5-membered aromatic heterocyclyl containing 1-4 of N, O and/or S as heteroatom(s) (provided that not more than one O and/or S is present), OR 1, SR 1, NR 2R 3, azetidino, pyrrolidino or alkoxycarbonyl (preferably COOMe or COOEt); R 11-5C alkyl, CH 2F, CF 3 or 3-5C cycloalkyl; R 2, R 3H, 1-5C alkyl, CF 3 or cyclopropyl. ACTIVITY : Analgesic. In tests for activity against central neuropathic pain induced by spinal column lesions in rats (see Pain, 1996, 66, 279-286), (3-chloro-4-fluorophenyl)-(4-fluoro-(((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)-piperidin-1-yl)-methanone (Ia) was administered (as the fumarate) at a constant rate of 0.63 mg per day for 14 days using an implanted analgesic pump. Statistically significant analgesia was observed from day 10 of the treatment (demonstrating symptomatic analgesic action); and the analgesia remained at the same level from day 15 after cessation of the treatment for a further 14 days (demonstrating curative analgesic action). MECHANISM OF ACTION : 5-HT-1A receptor agonist.