Universidad de Alcalá-OTRI

New inhibitor compounds of the tyrosine phosphatase 1B protein

Posted by from Universidad de Alcalá-OTRIResponsive · Patents for licensing · Spain

Summary of the technology

The research group in "Biological Chemistry" of the University of Alcalá has developed new compounds inhibitors of the Tyrosine Phosphatase 1B Protein, which are related to new Formulas I, II and III, with methods to prepare them, with the use of them as inhibitors of protein tyrosine phosphatase 1B (PTP1B) and with the use of the intermediates that lead to that compounds to prepare an inhibitor of PTP1B comprised by that formulas.

These compounds have application in the treatment or prevention of diseases in which it is known that PTP1B is involved in the pathogenesis, so they can be used for the treatment of insulin resistance, glucose intolerance, obesity, diabetes mellitus, hypertension and ischemic diseases of large and small blood vessels, conditions that accompany type 2 diabetes and other disorders where insulin resistance is indicated.

The group looks for companies in the health and pharmaceutical sector with the aim of reaching technical collaboration agreements, commercial agreements or patent licenses agreements.

Universidad de Alcalá-OTRI

Description of the technology

The invention describes the presentation of three families of compounds with inhibitory activity on PTP1B. The new compounds of this invention have a structure of pyrroloquinoxaline and pyrroloquinoxalinium, never before used in the inhibition of PTP1B.

More specifically, the present invention is related to the field of chemical synthesis of new compounds and their use as inhibitors of PTP1B, which are useful in the treatment or prevention of diseases in which PTP1B is known to be involved in the pathogenesis

As inhibitors of phosphatase activity and, in particular, as inhibitors of PTP1B, the novel compounds of the present invention can be used for the treatment of insulin resistance, glucose intolerance, obesity, diabetes mellitus, hypertension and ischemic diseases of large and small blood vessels, conditions that accompany type 2 diabetes including dyslipidemia, for example, hyperlipidemia and hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell cancer and carcinomas such as liposarcoma, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention can be used for the treatment of cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involved with inflammation and the immune system.

The present invention also concerns the use of the compounds of the invention for its use in the treatment of renal insufficiency (diabetic and non-diabetic), diabetic nephropathy, glomerulonephritis, glomerular sclerosis, proteinuria of primary renal disease, diabetic retinopathy, all types of cardiac failure including acute and chronic congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, ventricular and supraventricular arrhythmias, atrial fibrillation and atrial flutter, angina pectoris (both unstable and stable), myocardial infarction and its sequelae, ischemia / reperfusion injury, damaging vascular restoration including vascular restenosis, treatment of other vascular disorders such as migraines, peripheral vascular disease and Raynaud, multiple sclerosis, cerebral infarction, spinal cord injury, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and polyglutamine diseases such as Huntington's and spinocerebellar ataxia, infectious diseases including leishmaniosis, diseases implicated in inflammation and the immune system and diseases involved in muscle degeneration.

Current development status

Experimental technologies

Desired business relationship

Technology selling

Patent licensing

Technology development

New technology applications

INNOVATIVE ASPECTS

This invention presents new Formulas I, II and III, with methods for preparing them, with the use of them as inhibitors of protein tyrosine phosphatase 1B (PTP1B). These new formulas allow the treatment of insulin resistance, glucose intolerance, obesity, diabetes mellitus, hypertension and ischemic diseases of large and small blood vessels, conditions that accompany type 2 diabetes and other disorders where insulin resistance It is indicated.

They can also be used for the treatment of cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involved with inflammation and the immune system.

Nothing similar has been found in patent databases or in the scientific literature consulted.

COMPETITIVE ADVANTAGES

The formulas described in the invention represent a novelty in terms of the inhibition of PTP1B, since they are sufficiently lipophilic allosteric inhibitors, that represents an advantage over the active center inhibitors discovered before, which show a very low bioavailability and which failed in clinical trials.

It presents commercial potential at an international level, focused mainly on the markets of the US, Europe, Australia, Japan and India with reasonable difficulty and cost of implementation.

Applications

The group looks for companies in the health and pharmaceutical sector with the aim of reaching technical collaboration agreements, commercial agreements or patent licenses.

Intellectual property status

Granted Patent
Patent granted on June 17, 2015, with publication number ES2522717
OEPM Spain

Technology Owner

Universidad de Alcalá-OTRI

Research & Technology Organization

Related keywords

  • Biological Sciences
  • Medicine, Human Health
  • Medical Research
  • Biology / Biotechnology
  • Biochemistry / Biophysics Technology
  • Cellular and Molecular Biology Technology
  • Protein Engineering
  • Pharmaceutical Products / Drugs
  • diabetes
  • metabolic syndrome
  • insulin
  • obesity
  • tyrosine phosphatase protein
  • ptp1b
  • pyrroloquinoxaline
  • pyrroloquinoxalinium
  • dihydropyrroloquinoxaline
  • compounds

About Universidad de Alcalá-OTRI

Research & Technology Organization from Spain

The Technology Transfer Office at Alcalá University serves as a liaison between the University and its socioeconomic environment in terms of research and innovation. It encorages collaboration between research groups from universities and companies/institutions, with the objective to promote and commercialize research results and scientific capabilities.

Some of the services offered by this office are specified in the following list:

- Promotion of R & D and improvement of the relationships with companies.
- Promote the participation in R & D projects applicants to public calls (regional, national and European).
- Advising, processing and monitoring of patents and other forms of industrial protection.
- Support in the negotiation of contracts and agreements for R&D&i

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