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Nuevo compuestos heterocíclicos que contienen el grupo nitro para el tratamiento de la tuberculosis susceptible a medicamentos y resistente a múltiples medicamentos

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOCZ20151203002
Publicado:
15/01/2016
Caducidad:
15/01/2017
Resumen:
Una universidad checa ha desarrollado un grupo nitro que contiene tetrazoles, oxadiazoles y triazoles con importante actividad antitubercular in vitro, incluyendo especies resistentes a múltiples medicamentos, sin resistencia cruzada con medicamentos antituberculosos de primera y segunda línea y con baja toxicidad in vitro e in vivo. Se buscan socios interesados en continuar con el desarrollo (acuerdos de cooperación técnica) y licenciar la tecnología.

Details

Tittle:
Nitro group-containing heterocyclic compounds useful in the treatment of drug-susceptible and multidrug-resistant tuberculosis.
Summary:
A Czech university has developed a series of nitro-group containing tetrazoles, oxadiazoles and triazoles with outstanding in vitro antitubercular activity, including multidrug-resistant species, with no cross-resistance with first and second line antituberculosis drugs, with low in vitro and in vivo toxicity. The institution is seeking partners interested in further development (technical cooperation agreement) and also in licensing the invention (licensing agreement).
Description:
As reaction to the fact that more and more drugs are becoming less efficient because of growing resistance of bacteria to them, there is incessant effort to develop new types of pharmaceuticals with novel active compounds.

A Czech university has developed three large series of substituted nitro group-containing tetrazoles, oxadiazoles and triazoles. Majority of the prepared compounds possess high antimycobacterial effect (minimal inhibitory concentration - MIC = 0.03 - 0.5 µM) against drug-susceptible, multidrug-resistant and extensively drug-resistant mycobacteria.

Structure-activity relationship has been studied and showed, that one part of the molecule can be functionalized with no negative effect on antimycobacterial effect. Hence, this part of the molecule can be used to improve properties like pharmacokinetics or toxicity - e.g. water soluble derivatives can be prepared.

Selected compounds with the most promising antitubercular effect were studied on five human cell lines (including isolated human hepatocytes), on eight bacterial and eight fungal strains and showed no toxic effect up to 30 µM.

Majority of the compounds acts as decaprenylphosphoryl-d-ribose oxidase DprE1 inhibitors. Lead compounds (T6303 and T6478) were studied in vivo in liposomal formulations - repeated dose (14 days) toxicity (Oral) study fulfils Principles of Good Laboratory Practice - GLP as stated by OECD (1997 revision, C (97), 186 (Final) showed that NOAEL (No Observed Adverse Effect Level) were 50 and 200 mg/kg/day, respectively. Inventor offers these novel highly active compounds for further development of drugs directed on antituberculosis chemotherapy.

The institution is seeking partners interested in further development (technical cooperation agreement) and also licensing the invention (licensing agreement).
Advantages and Innovations:
Series of tetrazoles, oxadiazoles and triazoles:
· are easily and cheaply accessible in large-scales via simple synthetic procedures from commercially available substrates
· have high antimycobacterial effect (minimal inhibitory concentration - MIC = 0.03 - 0.5 µM) against drug-susceptible, multidrug-resistant and extensively drug-resistant mycobacteria, with no-cross resistance with common antituberculosis drugs
· have highly selective action - no in vitro effect against bacterial and fungal strains, low toxicity against human cell lines (including isolated human hepatocytes) and low in vitro genotoxicity (bacterial reverse mutation test - OECD Test guideline No. 471)
Repeated Dose (14 days) Toxicity (Oral) of T6303 and T6478 (GLP principles [OECD Principles of Good Laboratory Practice (as revised in 1997), C (97) 186 (Final)]) - NOAEL (No Observed Adverse Effect Level) was established as 50 mg/kg/day and 200mg/kg/day, respectively.
Stage of Development:
Available for demonstration
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
PCT patent application has been filed in the USA, Europe and 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 (licensing agreement).

Client

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

Keywords

Technology Keywords:
06002007 Ensayos in vitro, experimentos
06002008 Microbiología
06001015 Productos farmacéuticos / medicamentos