C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/12 (2006.01) A61K 31/44 (2006.01) A61K 38/04 (2006.01) A61K 38/55 (2006.01) C07C 279/14 (2006.01) C07D 235/18 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2475609
The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX- 2 induction modulating activities. wherein: A is -hydrogen, - (C1-C8) alkyl or - (C1-C8) alkyl substituted by hydroxy; B is - (Cl-C6) alkylguanidino, (C1-C6) alkyl (4-imidazolyl) , - (C1-C6) alkylamino, p-aminophenylalkyl (Cl-C6) -, p- guanidinophenylalkyl (C1-C6) - or 4-pyridinylalkyl (Cl-C6) -; D is - (CO) -, - (CO) - (C1-C6) alkylene or - (C1-C6) alkylene; E is a single bond or - (C1-C6) alkylene.
L'invention concerne de nouveaux dérivés d'acides aminés basiques de formule générale I, II et III, ainsi que leur préparation et leur utilisation dans le traitement de la douleur. Lesdits composés présentent des activités de modulation de l'induction de COX-2 et de potentialisation de la morphine, antinociceptives de type histogranine. Dans lesdites formules, A représente -hydrogène, - alkyle (C¿1?-C¿8?) ou - alkyle (C¿1?-C¿8?) substitué par hydroxy; B représente - alkylguanidino (C¿l?-C¿6?), (4-imidazolyl) alkyle (C¿1?-C¿6?), - alkylamino (C¿1?-C¿6?), p-aminophénylalkyle (C¿l?-C¿6?) -, p-guanidinophénylalkyle (C¿1?-C¿6?) - ou 4-pyridinylalkyle (C¿l?-C¿6?) -; D représente - (CO) -, - (CO) - (C¿1?-C¿6?) alkylène ou - alkylène (C¿1?-C¿6?); E représente une liaison simple ou - alkylène (C¿1?-C¿6?).
Bernatchez-Lemaire Irma
Le Hoang-Tanh
Lemaire Simon
Smart & Biggar
University Of Ottawa
LandOfFree
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