Abstract

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.

IPC Classes  ?

• A61K 31/12 - Ketones
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon

Abstract

Described herein are compositions comprising activators of TRP and ASIC channels that may be useful to improve or preserve exercise performance and exercise recovery.

IPC Classes  ?

• A61K 36/54 - Lauraceae (Laurel family), e.g. cinnamon or sassafras
• A61K 36/67 - Piperaceae (Pepper family), e.g. Jamaican pepper or kava
• A61K 36/906 - Zingiberaceae (Ginger family)
• A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps

Abstract

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.

IPC Classes  ?

• A61K 31/05 - Phenols
• A61K 31/085 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
• A61K 31/12 - Ketones
• A61K 31/121 - Ketones acyclic
• A61K 36/906 - Zingiberaceae (Ginger family)
• A61K 36/9068 - Zingiber, e.g. garden ginger
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The invention relates to methods and compositions for treating muscle cramps, muscle spasms, muscle spasticity, dystonias, and fasciculations.

IPC Classes  ?

• A61K 36/906 - Zingiberaceae (Ginger family)
• A61K 36/26 - Aristolochiaceae (Birthwort family), e.g. heartleaf
• A61K 36/268 - Asarum (wild ginger)

Abstract

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.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide

Abstract

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).

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide