In the latter case, partial inhibition of voltage-gated sodium channels reduces neuronal excitability and reduces seizure propagation. Other sodium channel blockers, such as lamotrigine and carbamazepine are used to treat epilepsy. Drugs, such as lidocaine, that block voltage-gated sodium channels are used as local anaesthetics. At the terminals, the action potential triggers the influx of calcium and the release of neurotransmitter. Voltage-gated sodium channels are responsible for the initial phase of the action potential, which is a wave of electrical depolarisation usually initiated at the soma of the neuron and propagated along the nerve axon to the terminals.
In addition, the invention relates to compositions containing these derivatives, salts and prodrugs thereof, and processes for their preparation. The present invention relates to α-aminocarboxyamide derivatives, salts and prodrugs thereof, and to the use of these derivatives, salts and prodrugs thereof in treating diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels. A method of treating a substance related disorder in a mammal comprising administering an effective amount of a compound according to claim 1. A method of treating a bipolar disorder in a mammal comprising administering an effective amount of a compound according to claim 1.Ģ3. A method of treating depression or a mood disorder in a mammal comprising administering an effective amount of a compound according to claim 1.Ģ2. A pharmaceutical composition comprising a compound as claimed in claim 1 and a pharmaceutically acceptable carrier therefor.Ģ1. A compound according to claim 8 substantially in crystalline form.ġ0. A compound selected from: (2S,6R)-6-(4-phenyl)-L-prolinamide hydrochloride.ĩ. A compound according to claim 1 wherein R 3 and R 1, together with the interconnecting atoms form a saturated or unsaturated 5-membered ring.ħ. A compound according to claim 1, wherein R 3 and R 4 are hydrogen.Ħ. A compound according to claim 1 wherein R 6 is -O-R 8 or -OCH R 9R 8, and R 7 is hydrogen or R 5 and wherein R 8 is a phenyl ring optionally substituted by one or more groups independently selected from C 1-3alkyl, halogen, cyano, haloC 1-3alkyl, hydroxy, C 1-3alkoxy and C 1-3haloalkoxy.ĥ. A compound according to claim 1 wherein q is 1.Ĥ. A compound according to claim 1 wherein X is C.ģ.
A compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof wherein R 1 and R 2 are independently hydrogen, C 1-6alkyl or C 3-6cycloalkylC 1-6alkyl or such R 1 and R 2, together with the nitrogen to which they are attached, form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring q is 1 or 2 R 3 and R 4 are hydrogen or when q is 1, R 3 and R 4, together with the interconnecting atoms, form a cyclopropane ring or such R 3 and R 1, together with the interconnecting atoms form a saturated or unsaturated 5- to 6-membered ring X is carbon or nitrogen n is 0, 1 or 2, wherein when present each R 5 is independently selected from C 1-3alkyl, halogen, cyano, haloC 1-3alkyl, hydroxy, C 1-3alkoxy and C 1-3haloalkoxy either R 6 or R 7 is -O-R 8, -OCHR 9R 8, -NCH 2R 8 or -(CH 2) 2R 8 and the other R 6 or R 7 is hydrogen or R 5 wherein R 8 is a phenyl ring optionally substituted by one or more groups independently selected from C 1-3alkyl, halogen, cyano, haloC 1-3alkyl, hydroxy, C 1-3alkoxy and C 1-3haloalkoxy and R 9 is hydrogen or C 1-3alkyl.Ģ. METHODS FOR THE DETECTION AND QUANTITATION OF THE P95 COMPONENT OF HER2/NEU (ERBB2)Ĭomposition exhibiting synergistic antioxidant activityġ. Wound dressings with elastase-sequestering Novel substituted succinic acid metallo-beta-lactamase inhibitors and their use in treating bacterial infections METHOD FOR THE PREVENTION AND TREATMENT OF ALZHEIMER'S DISEASE HETEROARYL SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE OMEGA-3 PENTAENOIC ACID COMPOSITIONS AND METHODS OF USE METHODS AND COMPOSITIONS FOR TREATING NON-ERK MAPK PATHWAY INHIBITOR-RESISTANT CANCERS Pharmaceutical composition promoting defecationĪCETAMINOPHEN COMPOSITIONS HAVING MINIMIZED SIDE EFFECTS INCLUDING REDUCED HEPATOTOXICITY
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