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Compuestos moduladores de DREAM. Nuevo enfoque para el tratamiento de enfermedades neurodegenerativas y autoinflamatorias

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20150706004
Publicado:
20/10/2015
Caducidad:
10/09/2016
Resumen:
Tres instituciones españolas de investigación han descubierto una nueva familia de moléculas orgánicas útiles en el tratamiento de enfermedades neurodegenerativas y autoinflamatorias y en trastornos de percepción sensorial. DREAM controla los niveles de expresión y/o actividad de diferentes proteínas implicadas en la regulación del calcio, excitabilidad neuronal y supervivencia neuronal. También es la primera proteína conocida de unión a Ca2+ que actúa como regulador transcripcional de unión a ADN. Se buscan compañías farmacéuticas interesadas en desarrollar y comercializar estos compuestos bajo licencia de patente.


Details

Tittle:
DREAM modulator compounds. A new approach for the treatment of neurodegenerative and auto-inflammatory diseases.
Summary:
Three Spanish public institutions have found a new family of organic molecules useful for the treatment of neurodegenerative and auto-inflammatory diseases along with sensory perception disorders. The mechanism of action of these compounds is by modulation of an interesting and promising enzyme. Pharmaceutical companies interested in the development and commercialization of these compounds under a patent licence are sought.
Description:
To date, there are many diseases lacking of an appropriate treatment, so it is mandatory to search for new drugs with novel mechanism of action in order to increase the current therapeutic arsenal. In this sense, a new approach would be the modulation of DREAM enzyme.

DREAM (Downstream Regulator Element Antagonist Modulator) enzyme controls expression levels and/or activity of different proteins involved in calcium regulation, neuronal excitability and neuronal survival. Also, DREAM represents the first known Ca+2 (ion calcium) binding protein that acts as a DNA (deoxyribonucleic acid)-binding transcriptional regulator.

Furthermore, it was found that the activation of DREAM enzyme reduces the development of dyskinesia which is an adverse side effect in Parkinson´s patients treated with L-Dihydroxyphenylalanine (L-DOPA) without interfering the therapeutic motor effects of this drug.

Moreover, this enzyme is involved in the regulation of apoptosis process (cancer), the accumulation of -Y-beta;-amyloid peptide (Alzheimer) and the removal of certain inflammatory signals (inflammatory diseases), among others.

In in vitro tests, these compounds show a selective modulation of Kv4.3 cannel (potassium voltage-gated channel subfamily D member 3) by DREAM activation.

In addition, the compounds of this invention exhibit a neuroprotective effect in cells by inhibiting the release of lactate dehydrogenase enzyme (LHD), which is a reflection of their inhibitory effect of cell death by oxidative stress.

All these facts indicate that these compounds are able to activate DREAM enzyme which may be useful for treating diseases such as neurodegenerative diseases (Alzheimer, Huntington, etc.) dyskinesia, schizophrenia and depression, chronic and neuropathic pain, and processes involving inflammation.

Pharmaceutical companies interested in a patent license and capable of developing these compounds through the completion of the relevant clinical trials are sought.

These three Spanish research institutions carries 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:
* In vitro tests have shown that the phenylacetamide derivatives described in this patent, inhibit cell apoptosis and show a neuroprotective effect.

* The above mentioned phenylacetamide derivatives modulate selectively the DREAM activity on Kv4.3 channel (potassium voltage-gated channel subfamily D member 3).

* The DREAM modulators here reported are readily synthesized in only two-steps.
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 filed

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 neurodegenerative diseases (Alzheimer, Huntington), dyskinesia, schizophrenia and depression, chronic and neuropathic pain, and processes involving inflammation, by performing the corresponding clinical trials or preclinical stage, at least.

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