US2017145015A1PendingUtilityA1

(r)-pirlindole and its pharmaceutically acceptable salts for use in medicine

Assignee: TECNIMEDE SOC TECNICO-MEDICINAL S APriority: May 9, 2014Filed: May 9, 2014Published: May 25, 2017
Est. expiryMay 9, 2034(~7.8 yrs left)· nominal 20-yr term from priority
A61P 25/04A61P 25/00C07D 487/04A61K 9/2054A61K 9/2018A61K 45/06A61K 9/2095A61K 31/4985C07B 2200/07A61K 31/403A61K 2300/00
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Claims

Abstract

(R)-pirlindole or its pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising the same for use in the therapeutic treatment and prevention of pain.

Claims

exact text as granted — not AI-modified
1 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use in the therapeutic treatment or prevention of pain. 
     
     
         2 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1 , characterized in that the (R)-pirlindole is enantiomerically pure. 
     
     
         3 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1 , in a combination therapy with at least one additional analgesic agent. 
     
     
         4 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof, for use according to  claim 3 , wherein the combination therapy includes a fixed-dose combination therapy or a separate combination therapy selected from sequential or simultaneous administration of active agents. 
     
     
         5 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof, for use according to  claim 3  for potentiating the effects of the at least one additional analgesic agent in the treatment of pain. 
     
     
         6 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1  in the form of (R)-pirlindole (S)-mandelate salt. 
     
     
         7 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1 , in the form of (R)-pirlindole mesylate salt. 
     
     
         8 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1 , in the form of (R)-pirlindole citrate salt. 
     
     
         9 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 3 , characterized in that the at least one additional analgesic agent is a compound that decrease neuronal hyperexcitability selected from the group consisting of: inhibitors of the sodium channels (carbamazepine, oxcarbazepine, eslicarbazepine, phenytoin, valproic acid), calcium channel antagonists (pregabalin), ionotropic and metabotropic glutamate receptor antagonists, y-aminobutyric acid activity enhancers (gabapentin) or μ, η, and δ opioid receptor agonists, partial agonists/antagonists or antagonists. 
     
     
         10 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 3 , characterized in that the at least one additional analgesic agent is a compound selected from the group consisting of: paracetamol, nonsteroidal anti-inflammatory drugs acetylsalicylic acid, diclofenac, nabumetone, nimesulide, nabumetone, etodolac, piroxicam, lysine clonixinate, diflunisal, acemetacin, glucametacin, indometacin, proglumetacin, oxametacin, sulindac, aceclofenac, fentiazac, ketorolac, zomepirac, meloxicam, tenoxicam, lornoxican, fenoprofen, fenbufeno, flurbiprofen, benoxaprofen, ibuprofen, ketoprofen, dexketoprofen, pirprofen, indoprofen, naproxen, oxaprozin, tiaprofen, dexibuprofen, meclofenamic acid, mefenamic acid, flufenamic acid, tolfenamic acid, niflumic acid, etofenamate, azapropazone, orgotein, feprazone, morniflumate, tenidap, glycosaminoglycan, polysulfate, celecoxib, rofecoxib, parecoxib, valdecoxib, and etoricoxib, glucosamine or diacerein. 
     
     
         11 . (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof for use according to  claim 1  wherein pain is neuropathic pain. 
     
     
         12 . Pharmaceutical composition for the treatment of pain comprising (R)-pirlindole enantiomer or a pharmaceutically acceptable salt thereof according to  claim 1  together with pharmaceutically acceptable carriers, vehicles or excipients.

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