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Nuevos compuestos para el tratamiento de la diabetes tipo 2 y otras enfermedades mediante modulación de complejo enzimático AMPK

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20150727005
Publicado:
31/08/2015
Caducidad:
30/08/2016
Resumen:
Dos centros de investigación españoles han descubierto una familia de compuestos derivados heterocíclicos de indol que actúan como activadores de la proteína quinasa AMPK (serina/treonina quinasa activada por monofosfato de adenosina). Esta enzima regula el estado energético de la célula, por lo que estos compuestos son útiles en el tratamiento del cáncer y enfermedades metabólicas y cardiovasculares, entre otras. Se buscan compañías farmacéuticas interesadas en desarrollar estos compuestos bajo una licencia de patente.



Details

Tittle:
New compounds for the treatment of Type 2 Diabetes and other diseases by modulation of the enzymatic complex AMPK
Summary:
Two Spanish research organizations have found a family of indol heterocyclic compounds which act as activators of protein kinase AMPK (serine/threonine protein kinase activated by adenosine monophosphate ). This enzyme regulates the energy status of the cell. Therefore, these compounds are useful for the treatment of cancer, metabolic and cardiovascular diseases, among others.
Pharmaceutical companies interested in the development of these compounds under a patent licence are sought.
Description:
Serine/Threonine protein kinase activated by adenosine monophosphate (AMPK) is an enzyme involved in energy production processes such as glycolysis, lipid oxidation and gluconeogenesis. Therefore, AMPK is currently considered as a promising therapeutic target for the treatment of metabolic diseases such as type 2 diabetes and obesity.

Since AMPK is also present in the heart, its activation leads to a decrease in cardiac hypertrophy and heart failure risk.

In addition, activation of AMPK reduces the expression of lipogenic enzymes such as fatty acid synthase (FAS) and acetyl CoA carboxylase (ACC) suppressing in this way the proliferation of prostate cancer cells.

Furthermore, the indol derivatives of this invention have been successfully tested and are able to activate AMPK through assays on mammalian Hek293 cells with values similar to those obtained from Phenformin, a well-known activator of AMPK, but at lower doses.

Therefore, these compounds are especially useful for the treatment of diseases where the function of AMPK is relevant as for example, cancer, metabolic and cardiovascular 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 Spanish research institution 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:
* The compounds are able to induce in vivo activation of AMPK enzymatic complex. It has already been demonstrated the anti-diabetogenic effect of AMPK activation.
* Simple synthesis procedure of new indole derivatives.
* Indol heterocyclic compounds that regulate cellular energy metabolism.
* Direct activation of AMPK inhibits prostate cancer growth in vitro and in vivo. Persistent activation of AMPK results in mitotic arrest and apoptosis of prostate cancer cells.
* Inhibition of de novo lipogenesis is the key mechanism of AMPK-mediated anti-tumor effect.
* The research group is currently working on more evaluation tests.
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:
Seeking a pharmaceutical company, spin-off or start-up that, working on the search of AMPK modulators, is interested on the development of a new drug for the treatment of type 2 diabetes, cancer, cardiovascular or metabolic diseases by performing clinical trials, 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:
06001003 Citología, cancerología, oncología
06002009 Diseño molecular
06001011 Enfermedades circulatorias y del corazón
06001015 Productos farmacéuticos / medicamentos