Enantiomerically pure R-etifoxine, pharmaceutical compositions thereof and methods of their use
Enantiomerically pure R-etifoxine and pharmaceutically acceptable salts, solvates, hydrates or prodrugs thereof are provided. Also provided are pharmaceutical compositions comprising the compounds and methods of treating disorders associated with central nervous system using the compounds and pharmaceutical compositions.
1 . Enantiomerically pure R-etifoxine, or a pharmaceutically acceptable salt or hydrate thereof.
2 . The compound of claim 1 , wherein the compound is a salt.
3 . The compound of claim 2 , wherein the salt is a hydrochloride salt.
4 . A pharmaceutical composition comprising the compound of claim 1 - 3 and a pharmaceutical carrier, excipient or diluent.
5 . The pharmaceutical composition of claim 4 that is formulated for oral administration.
6 . The pharmaceutical composition of claim 5 that is formulated as an oral capsule or a tablet.
7 . The pharmaceutical composition of claim 4 that is formulated for topical administration.
8 . The pharmaceutical composition of claim 7 that is formulated as a gel.
9 . A pharmaceutical unit dosage comprising the pharmaceutical composition of claim 5 .
10 . A method for modulating activity of GABA A receptor comprising contacting the receptor with an effective amount of a compound of claim 1 .
11 . A method of treating, preventing, ameliorating or managing symptoms associated with a mental disease or a disease of central nervous system comprising administering to a subject in need thereof an effective amount of a compound of claim 1 .
12 . The method of claim 11 , wherein the disease is multiple sclerosis, muscle relaxation in spinal spasticity, cerebral palsy, trigeminal neuralgia, pain and drug withdrawal symptoms or other nervous disorder.
13 . The method of claim 11 , wherein the disease is a cardiovascular disorder or a gut motility disorder.
14 . The method of claim 11 , wherein the disease is anxiety.
15 . The method of claim 10 , wherein the compound is administered as an oral or topical formulation.
16 . The method of claim 15 , wherein the oral formulation is a capsule.
17 . The method of claim 15 , wherein the topical formulation is a gel.
18 . The method of claim 11 , wherein the amount of the compound administered is about 1 mg up to about 2000 mg/day.
19 . The method of claim 11 , wherein the amount of the compound administered is about 10 mg up to about 1000 mg/day.
20 . The method of claim 11 , wherein the amount of the compound administered is about 13 mg up to about 800 mg/day.
21 . The method of claim 11 , wherein the amount of the compound administered is about 15 mg up to about 300 mg/day.
22 . The method of claim 11 , wherein the amount of the compound administered is about 25 mg up to about 200 mg/day.
23 . The method of claim 11 , wherein the amount of the compound administered is about 50 mg up to about 150 mg/day.
24 . The method of claim 11 , wherein the amount of the compound administered is about 50 mg/day.
25 . The method of claim 11 , wherein the amount of the compound administered is about 100 mg/day.
26 . The method of claim 11 , wherein the amount of the compound administered is about 150 mg/day.
27 . The method of claim 11 further comprising administering an additional anxiolytic drug to the patient.
28 . The method of claim 27 , wherein the additional anxiolytic drug is selected from Buspirone, Gepirone, Ipsapirone, Tondospirone, Alprazolam, Bromazepam, Camazepam, Chlordiazepoxide, Clobazam, Clorazepate, Chotiazepam, Cloxazolam, Diazepam, Ethyl Loflazepate, Etizolam, Fluidazepam, Flutazolam, Flutoprazepam, Halazepam, Ketazolam, Lorazepam, Loxapine, Medazepam, Metaclazepam, Mexazolam, Nordazepam, Oxazepam, Oxazolam, Pinazepam, Prazepam, Tofisopam, Cyclarbamate, Emylcamate, Hydroxyphenamate, Meprobamate, Phenprobamate, Tybamate, Alpidem, Benzoctamine, Captodiamine, Chlormezanone, Flesinoxan, Fluoresone, Glutamic Acid, Hydroxyzine, Lesopitron, Mecloralurea, Mephenoxalone, Mirtazepine, Oxanamide, Phenaglycodol, Suriclone and Zatosetron.