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July 12 2010 - expires (July 07 2011)

Spiropiperidyl rifamycins for the treatment of mycobacterial infections

Reference: 10 ES 24D4 3HY3

Profile Country of Origin: Spain les.gif

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A research group from a Spanish university has developed new rifamycin derivatives from the spiropiperidylrifamycins family and a procedure for their preparation. These new compounds exhibit a high antibiotic activity and therefore can be used for the treatment of mycobacterial infections such as multi-resistant tuberculosis. Collaboration is sought for commercial exploitation of this technology via license agreement.

Multi-resistant tuberculosis is defined as that tuberculosis which is caused by starins of Mycobacterium tuberculosis resistant simultaneously to at least isoniazid and rifampicin. Its incidence has increased in the last years in an alarming rate in numerous regions worldwide. The importance of this problem is illustrated in the decision taken by the WHO (World Health Organization) in 1994 to put into action a plan for the control and surveillance of multiresistant tuberculosis at a worldwide level. Among the strategies that have been developed against this serious problem which threatens worldwide health, is the development of new drugs to fight the types of strains involved. The Spanish university has developed and patented new rifamycin derivatives from the spiropiperidylrifamycins family, which exhibit a high antibiotic activity, and also a procedure for their preparation. The formula of the compound is shown in the attached image, wherein R1 is a radical selected between hydrogen and alkyl; R2 is selected from hydroxyalkyl, phenyl, phenyl mono-substituted and phenyl di-substituted in position 3 and 4; R3 is selected from phenyl, phenyl mono-substituted and phenyl di-substituted in position 3 and 4; the substituents of the of the phenyl of R2 and R3 selected from halogen, (C1-C4)-alkyl and (C1-C4)-alkoxyl and R4 is selected from hydrogen, alkyl, allyl and homoallyl. The above described compound, with their pharmaceutically acceptable salts and their solvates, have proved to be useful for the treatment of mycobacterial infections, in particular for the treatment of infections produced by Mycobacterium tuberculosis, Mycobacterium avium-intracellulare complex or Mycobacterium kansasi. Innovative Aspects: The antimycobacterial activity of these new spiropiperidylrifamycins are comparable and, in many cases better, than the one shown by the existing drugs at present time.

Domain of Application

Pharmaceutical and Medicinal application

Stage of Development

Development phase - Laboratory tested

Exploitation of RTD Results

National Programmes

IPR

Patent(s) applied for but not yet granted
European Patent Applied: EP 1 783 129 A1

Company Details

Type: Research institute/University

Size: > 500

Collaboration Type

  • License Agreement

- Type of partner sought: industry. - Specific area of activity of the partner: Pharmaceutical industry. - Task to be performed by the partner sought: commercial exploitation of the patent.

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