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Chemical synthesis of imidazo[1,2-a]pyridine derivatives with anti-inflammatory properties

New compound with anti-inflammatory properties
Type: Patent. Reference code: 202210R-Marcilla, A
Holding entities
  • Universitat de València
  • Consejo Superior de Investigaciones Científicas (Spanish Research Council) 
  • Universidad Complutense de Madrid
  • Centro Nacional de Investigaciones Cardiovasculares Carlos III (National Centre of Cardiovascular Research Carolos II)

 

UV inventor staff
  • Marcilla Diaz, Antonio
  • PDI-Catedratic/a d'Universitat
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  • Del Pozo Losada, Carlos
  • PDI-Catedratic/a d'Universitat
  • Director/a Titulacio Master Oficial
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  • Sanchez Lopez, Christian Miquel
  • PI-Invest Formacio Predoc Ministeri
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Non-UV inventor staff
  • Francisco A. Sánchez Sancho
  • José María Cumella Montánchez
  • María Gracia Baquero Gálvez
  • Aurelio García Csáky
  • Silvia Roscales García
  • Eduardo Oliver Pérez
  • Borja Ibáñez Cabeza
  • Jesús del Pozo Losada

 

Background

Presently, there are a large variety of safe and effective anti-inflammatory agents, such as aspirins and other non-steroidal anti-inflammatory drugs (NSAID). An efficient anti-inflammatory drug should be able to stop inflammation without interfering in normal homeostasis. Even though conventional NSAIDS do present gastric and renal side effects, the majority of selective inhibitors lack these side effects. However, they are associated with cardiac side effects in long-term use. Thus, the search for anti-inflammatory drugs without side effects has become critical, and pharmaceutical companies and research groups have been working tirelessly to achieve this goal.

Invention

Researchers at the UV, together with research staff from CSIC, the UCM and the CNIC, as well as researcher Jesús del Pozo, have produced several compounds through the chemical synthesis process and the production of imidazo[1,2-a]pyridine derivatives with powerful anti-inflammatory properties in vitro and in vivo in diseases involving inflammatory and pro-fibrotic processes. The imidazo[1,2-a]pyridine backbone is present in many commercial drugs, showing many therapeutic applications. The compounds in this invention are based on structures with Alk5 tyrosine kinase inhibitor activity, which is the receptor I of transforming growth factor TGFβ. These compounds demonstrate powerful anti-inflammatory properties both in vitro (on cultured human macrophages) and in vivo on an animal model, as well as anti-fibrotic effect in a murine model.

Applications

The present invention has applications in:

  • Biomedicine
  • Pharmaceuticals
  • Cosmetics
  • Nutraceuticals

Effective formulations can be obtained for topical, oral and parenteral application.

Competitive advantages

The invention presents the following advantages:

  • Product optimisation, maintaining product batches with identical properties.
  • Economic in nature, with synthesis being cheaper than obtaining from natural products.
  • Rapid production of the compounds.
  • Use of small amounts of product in in vitro tests.
Intellectual property status
  • Patent applied
Contact
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Geolocation

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