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Modulación selectiva de receptor GPR55. Nuevo y prometedor enfoque para el tratamiento de enfermedades y del dolor

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20150706003
Publicado:
31/08/2015
Caducidad:
30/08/2016
Resumen:
Un centro de investigación español y una universidad canadiense han descubierto una familia de derivados de cromenopirazol que actúan como moduladores del receptor 55 acoplado a proteína G (GPR55). Por lo tanto, estos compuestos son útiles en el tratamiento de patologías en las que GPR55 es relevante, como diabetes, cáncer, dolor inflamatorio y neuropático, enfermedades óseas, Parkinson y esclerosis múltiple. Los cromenopirazoles modulan GPR55 de forma selectiva y no afectan a las células HEK 293 normales, incluso en concentraciones elevadas. Se buscan compañías farmacéuticas interesadas en desarrollar los compuestos bajo licencia de patente.

Details

Tittle:
Selective modulation of GPR55 receptor, a new and promising approach for the treatment of diseases and pain.
Summary:
A Spanish public research organization and a Canadian university have found a family of chromenopyrazole derivatives which act as modulators of G-protein-coupled receptor 55 (GPR55). Therefore, these compounds are useful for the treatment of pathologies where GPR55 is relevant, such as diabetes, cancer, inflammatory and neuropathic pain, bone diseases, Parkinson and multiple sclerosis. Pharmaceutical companies interested in the development of these compounds under a patent licence are sought.
Description:
G-protein-coupled receptor 55 (GPR55) has been proposed as an atypical cannabinoid receptor and could be a serious alternative for one of the non-CB1/CB2 receptors. It has been shown that this receptor is involved in processes of inflammatory and neuropathic pain, metabolic disorders, bone development and proliferation processes of tumor cells (breast, ovarian, prostate, glioblastoma and subcutaneous carcinoma). Therefore, GPR55 is considered a promising biological target in the search of new compounds for the treatment of such diseases.

It has been found that some chromenopyrazoles of the present invention act as partial agonist of GPR55 with half maximal effective concentrations (EC50) within the nanomolar range (8.7 to 0.4 nM), as measured by cellular impedance measurements. They can be useful in the treatment of type 2 diabetes and osteoporosis.

In addition, some of these compounds behave as GPR55 antagonists when assays are performed in the presence of the endogenous ligand lysophosphatidylinositol (LPI). In this case, the compounds may be interesting as anti-proliferative and anti-migratory for treating breast, ovarian, skin and prostate cancer. Furthermore, they may also be useful for the treatment of arthritis and metabolic bone diseases.

Pharmaceutical companies, spin-offs or start-ups interested in a patent license and capable of developing these compounds through the completion of the relevant clinical trials are sought.

These two research institutions carry out their research in chemistry and chemical technology, particularly medicinal chemistry, with more than 40 years of experience on the design and synthesis of potential new drugs, dealing with multidisciplinary basic research and its aims are to provide new drug leads and to contribute to the identification of novel therapeutic targets. Key issues are the training of postgraduate students and cooperation with pharmaceutical companies.
Advantages and Innovations:
* GPR55 is a relatively unexplored therapeutic target. Currently, there are very few specific agonists and antagonists for this receptor. Patent analysis regarding GPR55 outlines the fair interest of big pharmaceutical companies.

* These chromenopyrazoles selectively modulate GPR55 and do not affect normal Human Embryonic Kidney 293 cells, even at high concentrations.

* In silico ADMET (Absorption, Distribution, Metabolism, Excretion, Toxicity) predictions: the pharmacokinetic profile of compounds is improved compared to lysophosphatidylinositol profile. Therefore, compounds are useful for the preparation of pharmacologic tools to study the GPR55 receptor and also be potential drugs for new therapeutic strategies.

* None of the compounds of this invention binds to CB1 cannabinoid receptor.

* Chromenopyrazoles as innovative chemical structures.

* It is anticipated that novel lead candidates targeting GPR55 could represent a new tool to better understand GPR55-mediated diseases and generate an innovative class of an effective next-generation of therapeutics.
Stage of Development:
Under development/lab tested
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:
We are seeking a pharmaceutical or biopharmaceutical company, spin-off or start-up that is interested on the development of new drugs for the treatment of type 2 diabetes, cancer, inflammatory and neuropathic pain, bone diseases, Parkinson disease or multiple sclerosis, from preclinical phase.

Client

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

Keywords

Technology Keywords:
06001003 Citología, cancerología, oncología
06001014 Neurología, investigación cerebral
06001015 Productos farmacéuticos / medicamentos