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Nuevos derivados aromáticos de oxiácidos basados en fósforo activos contra micobacterias, incluyendo cepas multirresistentes

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOCZ20151022002
Publicado:
20/11/2015
Caducidad:
19/11/2016
Resumen:
Una universidad checa ha desarrollado una serie de fosfinatos, fosfonatos, fosfatos de salicilanilida aromáticos y difenilbenzo[e][1,3,2]oxazafosfinina-4-uno 2-óxidos cíclico con actividad antituberculosa in vitro, incluyendo cepas resistentes a múltiples medicamentos y cepas no tuberculosas. La patente ha sido solicitada aunque todavía no ha sido concedida. Se buscan socios con el fin de establecer acuerdos de licencia y cooperación técnica para continuar con el desarrollo de las moléculas antituberculosas altamente activas.

Details

Tittle:
New aromatic derivatives of phosphorus-based oxyacids active against mycobacteria including multiresistant strains.
Summary:
A Czech university has developed a series of aromatic salicylanilide phosphates, phosphinates, phosphonates and cyclic diphenylbenzo[e][1,3,2]oxazaphosphinin-4-one 2-oxides with in vitro anti-tubercular activity, including multidrug-resistant and non-tuberculous strains. Patent has been applied but not yet granted. Partners are sought for licensing (licence agreement) and for further development (technical cooperation agreement) of the highly active anti-tubercular molecules.
Description:
Currently old diseases that were supposed to be eliminated are coming back again. For example numbers of tuberculosis patents rises in the world and the current drugs are not satisfactory in terms of efficiency so the novel ways of combating the tuberculosis are sought.
A Czech University is trying to address growing need of the novel approaches to curing the disease and therefore it has developed a large series of substituted aromatic salicylanilide phosphates, phosphinates, phosphonates and their cyclic form diphenylbenzo[e][1,3,2]oxazaphosphinin-4-one 2-oxides with potent in vitro antitubercular activity (minimal inhibitory concentration (MIC = 0.5 - 4 µM), including multidrug-resistant strains where is activity retained (MIC = 1 µM) or non-tuberculous mycobacteria (M. avium, M. kansasii).
Structure-activity relationship has been studied and showed, that one part of the molecule can be functionalized to improve bioavailability and properties like pharmacokinetics or toxicity. There is no cross-resistance to established clinically used drugs indicating different and unique mechanism of action.

Partners are sought for licensing (licence agreement) and for further development (technical cooperation agreement) of the highly active anti-tubercular molecules.


Advantages and Innovations:
Series of aromatic salicylanilide phosphates, phosphinates, phosphonates and their cyclic forms diphenylbenzo[e][1,3,2]oxazaphosphinin-4-one 2-oxides:
- are easily accessible in large-scales via simple synthetic procedures
- share high anti-mycobacterial effect (minimal inhibitory concentration MIC = 4-0.5 µM) against drug-susceptible and multidrug-resistant mycobacteria, with no-cross resistance with established anti-tuberculosis drugs
- have different mechanism than both old and novel (e.g. delamanid, PA-824) antimycobacterial agents
- are active also against non-tuberculous mycobacteria
Stage of Development:
Available for demonstration
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
USA, Europe, Japan

Partner sought

Type and Role of Partner Sought:
University is seeking a leading pharmaceutical company in the field interested in further collaboration on development of the novel highly active compounds suitable for anti-tuberculosis and anti-mycobacterial therapy on the basis of technical cooperation agreement and also purchase of a licence is expected.

Client

Type and Size of Client:
University
Already Engaged in Trans-National Cooperation:
Si
Languages Spoken:
Czech
English
Greek
Slovak

Keywords

Technology Keywords:
06001015 Productos farmacéuticos / medicamentos