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Derivados heterocíclicos bloqueadores de canales TRPM8

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20151209002
Publicado:
12/01/2016
Caducidad:
12/01/2017
Resumen:
Un centro de investigación y una universidad españoles han sintetizado y estudiado compuestos heterocíclicos que bloquean la activación de termorreceptores, en particular canales termosensoriales TRPM8. Por lo tanto, estos compuestos podrían ser útiles en el tratamiento de enfermedades del sistema respiratorio, de la piel, del ojo, derivadas de la quimioterapia, así como el cáncer. Se buscan compañías farmacéuticas o biotecnológicas interesadas en desarrollar estos compuestos bajo una licencia de patente.


Details

Tittle:
Heterocyclic derivatives TRPM8 channels blockers and their uses
Summary:
A Spanish public research organization and a University have synthesised and studied heterocycle compounds which block thermoreceptors activation, particularly thermosensitive channels TRPM8. Therefore, these compounds could be useful for the treatment of respiratory system disease, skin disease, eye disease, derived from chemotherapy, as well as cancer.

Pharmaceutical or Biotechnological companies interested in the development of theses compounds under a patent licence are sought.
Description:
TRPM8 channels, a subset of the Transient Receptor Potential (TRP) family of cation channels have been implicated in sensing temperature, are activated by voltage, low temperatures and cooling compounds. These channels respond to covers the entire perceived temperature spectrum, from warm to painfully hot (>42ºC), from pleasingly cool to excruciatingly cold (< 15ºC).
In assays carried out, these compounds have shown blocking activity through TRPM8 receptor higher than 80% at a concentration of 50 µM. Furthermore, they are able to maintain a good inhibitory activity above 70%, at 5 µM concentration.

Most representative compounds of the invention show IC50 values (half maximal inhibitory concentration) of 50-100 nM.
Biological evaluation of a collection of theses heterocyclic compounds in some human cellular lines has revealed that some of them have a significant activity like antitumor agents.
The blocked activity of theses heterocycle compounds has allow us to propose their used as potential therapeutic agents to treat some respiratory system diseases (cough, asthma, etc.), skin problems (pruritus, atopic dermatitis, psoriasis, etc.), chemotherapy (cold allodynia), as well as cancer (melanoma, prostate, kidney, breast, pancreas, osteosarcoma, etc.).
Advantages and Innovations:
-Potent antagonists TRPM8
-They keep a good inhibit activity TRPM8 with IC50 50-100 nM.
-Some of these heterocycles has antitumor activity in micromolar order in four cell lines.
- Antitumor capacity of some compounds in 60 cancer cell lines is been evaluating currently.
-Analgesic activity compounds.
Stage of Development:
Field tested/evaluated
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
Spanish priority patent application

Partner sought

Type and Role of Partner Sought:
Pharmaceutical or Biotechnological companies interested on the development of new drugs for the treatment of respiratory system diseases, skin diseases, eyes diseases, derived from chemotherapy, as well as cancer, from preclinical phase or a SME that carries out at least preclinical phase with the ultimate aim of seeking sublicensees.

Client

Type and Size of Client:
R&D Institution
Already Engaged in Trans-National Cooperation:
No
Languages Spoken:
English
Spanish

Keywords

Technology Keywords:
06001014 Neurología, investigación cerebral
06001015 Productos farmacéuticos / medicamentos