4-substituted piperidine analogs and their use as subtype...

Details 4-substituted piperidine analogs and their use as subtype... 4-substituted piperidine analogs and their use as subtype...

C - Chemistry, Metallurgy

07

D

C07D 211/14 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 211/18 (2006.01) C07D 211/40 (2006.01) C07D 211/42 (2006.01) C07D 211/44 (2006.01) C07D 211/46 (2006.01) C07D 211/52 (2006.01) C07D 211/54 (2006.01) C07D 211/58 (2006.01) C07D 211/70 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/00 (2006.01) C07D 405/06 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 471

Patent

CA 2240038

Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

Cette invention concerne des analogues de pipéridine à substitution en position 4, des compositions pharmaceutiques contenant ces derniers ainsi que le procédé d'utilisation desdits analogues de pipéridine à substitution en position 4 en tant qu'antagonistes sélectivement actifs contre les sous-types du récepteur de N-méthyl-D-aspartate (NMDA) pour traiter des états pathologiques tels que l'attaque, l'ischémie cérébrale, le traumatisme du système nerveux central, l'hypoglycémie, l'anxiété, les convulsions, la perte d'audition induite par les antibiotiques aminoglucosides, les maux de tête migraineux, le glaucome, la rétinite à cytomégalovirus, la douleur chronique, la tolérance aux opioïdes ou le sevrage des opioïdes ou bien des maladies neurodégénératives telles que le lathyrisme, la maladie d'Alzheimer, la maladie de Parkinson et la maladie de Huntington. Cette invention concerne également de nouveaux procédés de préparation d'analogues de pipéridine à substitution en position 4 et de nouveaux intermédiaires desdits analogues de pipéridine à substitution en position 4.

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