Pierre Fabre Medicament

Neurolixis

University of California

Universite Jagellone

Uniwersytet Jagiellonski Collegium Medicum

Mark Andrew Varney

Bruno Paillard

Adrian Newman-Tancredi

Laurence Del Frari

Valérie Brunner

Adrian Newman Tancredi

Adam Bucki

Joanna Sniecikowska

Magdalena Jastrzebska-Wiesek

Khaleelurrahman Abdulrazak

Xin Tao

Anna Wesolowska

Valerie Brunner

The present invention relates to a method of treatment of movement disorders, comprising administering to a patient in need thereof an effective amount of befiradol, wherein the administering step provides an average patient's maximum plasma concentration of befiradol below 15 ng/mL which occurs more than 4 hours post administration, said method minimizing side effects of dizziness and nausea. Sustained release pharmaceutical compositions that can be used according to this method are also described.

Method for treating movement disorders with befiradol

The present application concerns the treatment and prevention of diseases associated with an increased risk of sudden unexpected death in epilepsy, such as Fragile X syndrome, by administering a selective 5-HT1A receptor agonist.

Use of serotonin 5-HT1A receptor agonists to treat diseases associated with sudden unexpected death in epilepsy

The present invention relates to the reduction of the side-effects induced by tetrabenazine or other inhibitors of vesicular monoamine transporter (VMAT), in the treatment of central nervous system disorders such as Huntington's disease, L-DOPA-induced dyskinesias in Parkinson's disease, Tourette's syndrome or tardive dyskinesia. The invention comprises administering to a patient in need thereof an effective amount of activates selective serotonin 5-HTreceptors agonist, whereby the side-effects of depression or Parkinsonism induced by tetrabenazine or other VMAT inhibitors are minimized.

Use of selective serotonin 5-HTreceptor agonists for treating side-effects of VMAT inhibitors

The invention concerns compounds that possess a high affinity at 5-HTreceptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.

Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors

The present invention relates to a method of treatment of movement disorders, comprising administering to a patient in need thereof an effective amount of befiradol, where in the administering step provides an average patient's maximum plasma concentration of befiradol below 15 ng/mL which occurs more than 4 hours post administration, said method minimizing side effects of dizziness and nausea. Sustained release pharmaceutical compositions that can be used according to this method are also described.

Growing community of inventors

Dana Point, CA, United States of America

Mark Andrew Varney