The present invention is, in part, directed to tolperisone analogs (e.g., compounds of formula (I), (I-a), (I-b), (II), (Il-a), (III), (Ill-a), (ΙΙΙ-b), (III-c), (IV), (IV-a), (V), or (V-a)) and methods of use thereof for the treatment of various conditions including elevated muscle tone and tension (e.g., spasticity, muscle spasm). In one aspect, the tolperisone analogs disclosed herein have an additional substituent at the α-position, which blocks the generation of a β- elimination product.
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 31/4453 - Pipéridines non condensées, p. ex. pipérocaïne substituées uniquement en position 1, p. ex. propipocaïne, dipérodone
2.
COMPOSITIONS AND METHODS AFFECTING EXERCISE PERFORMANCE
Described herein are compositions comprising activators of TRP and ASIC channels that may be useful to improve or preserve exercise performance and exercise recovery.
The invention relates to methods and compositions comprising a TRP channel or ASIC channel activator for preventing or treating a disease, disorder, or condition described herein.
The present invention relates to compositions of capsaicinoids, capsinoids, or related analogs or combinations thereof, and methods of preparation, formulation, and the medical use of these compositions. In one aspect, the present invention features a composition formulated for oral administration, said composition comprising an effective amount of a capsaicinoid, capsinoid, or related analog or combination thereof.
The present invention relates to compositions of ion channel activators and methods of preparation, formulation, and the medical use of these compositions. In one aspect, the present invention features a composition formulated for oral administration, said composition comprising an effective amount of an ion channel activator (e.g., a TRPV1 channel activator, a TRPA1 channel activator, an ASIC channel activator, or combination thereof).