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Nuevo compuesto para el tratamiento exitoso de enfermedades degenerativas de la retina

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20190830001
Publicado:
03/09/2019
Caducidad:
03/09/2020
Resumen:
Una universidad española ha descubierto el uso del compuesto 3-(2-isotiocianatetil)-5-metoxi-1H-indol para el tratamiento preventivo o terapéutico de enfermedades degenerativas de la retina: retinitis pigmentosa, glaucoma, degeneración macular asociada a la edad y retinopatía diabética. En el tratamiento preventivo y terapéutico de las enfermedades degenerativas de la retina pueden utilizarse tanto el compuesto descubierto como sus sales farmacéuticamente aceptables. Las sales pueden prepararse a partir de ácidos orgánicos, ácidos inorgánicos, sales metálicas, sales de amonio, sales formadas a partir de bases orgánicas y sales con aminoácidos. Este compuesto ha demostrado in vitro e in vivo su capacidad neuroprotectora en varios modelos bajo condiciones de laboratorio. La universidad busca compañías farmacéuticas interesadas en la explotación comercial de esta tecnología mediante acuerdos de licencia de patente o colaboración técnica.

Details

Tittle:
New compound to successfully treat degenerative diseases of the retina
Summary:
A Spanish University has found the use of the compound 3-(2-isothiocyanatethyl)-5-methoxy-1H-indol, for the preventive or therapeutic treatment of degenerative diseases of the retina. This compound has demonstrated, in vitro and in vivo, its neuroprotective capacity in various models under laboratory conditions. Pharmaceutical companies interested in the commercial exploitation of this technology via patent licensing or technical collaboration agreements are sought.
Description:
Currently, pharmacological treatment of degenerative diseases of the retina focuses on two main action lines:

1. In the use of preventive strategies attempting to counteract the underlying mechanisms of the disease, such as gene therapy.

2. In attempting to prevent cell death by administering anti-inflammatory and antiapoptotic compounds (e.g. a cocktail of antioxidants), as well as neurotrophic factors delaying cell death of the retina, slowing thus the progression of the disease.

Degenerative processes of the retina have a great impact on the quality of life of patients. In this sense, it is particularly interesting to find suitable pharmacological treatments.

A Spanish research group has found a chemical compound, 3-(2-isothiocyanatethyl)-5-methoxy-1H-indol (Figure 1), with a potent antioxidant and cytoprotective effect which can be used as a therapeutic strategy to avoid, prevent or mitigate retinal degeneration in diseases such as: retinitis pigmentosa, glaucoma, age-related macular degeneration and diabetic retinopathy.

In the preventive or therapeutic treatment of the degenerative diseases of the retina described above, both the discovered compound and its pharmaceutically acceptable salts can be used. These salts can be prepared from: organic acids, inorganic acids, metallic salts, ammonium salts, salts formed from organic bases, and salts with amino acids.

This compound can be easily prepared through different methods described in the scientific literature. Soluble complexes can be prepared with different excipients. The pharmaceutical composition can be administered in daily doses orally, rectally, subcutaneously, intramuscularly, intravascularly, injectablely or intravenously. It may be administered locally as a solution (e.g., eye drops, intraocular injection, or intravitreal injection), or as an implant.

Different animal models of retinal degeneration have been studied, among them:

1. Cytoprotection against sodium nitroprusside induced toxicity in the cell line derived from 661W photoreceptors: The use of the compound significantly increased neuronal survival. In fact, the viability of the 661W cell line increased up 20% respect to the control. (see Figure 2)

2. Visual responses rescue in the animal model of retinosis pigmentaria rd10: The murine strain rd10 is the most suitable model for testing therapies related to retinitis pigmentosa. Different doses of the compound administered intraperitoneally have been studied, from the beginning to an advanced stage of the degenerative process, and it has already proved that the compound exerts a protective effect, and therefore, it is an effective agent to treat retinitis pigmentosa.

3. Measurement of the amplitude of the electroretinogram (ERG): There is a certain dose of the compound (10 mg/Kg) that achieves a statistically significant improvement in the functional response of the retina respect to control (see Figure 3).

4. Measurement of visual acuity and contrast sensitivity in the murine model rd10:

Visual acuity gives a measure of the functional activity of the retina. This test showed that in rd10 mice treated with the compound (a dose of 10 mg/Kg), visual acuity increased 35.6% respect to control (see Figure 4).

Contrast sensitivity: in animals treated with the compound (a dose of 10 mg/Kg), contrast sensitivity increased between 11% and 15% with respect to the control, depending on the spatial frequency of the stimulus (see Figure 5).

Pharmaceutical companies interested in acquiring this compound for commercial exploitation through patent licensing agreement or technical collaboration agreements for development of new applications are sought.

Advantages and Innovations:
The most innovative aspects of the present invention differ from the current drugs because:
· It shows a reducing effect on retinal degeneration associated with different degeneration models.
· It is a powerful inducer of the signalling pathway Nrf2, unlike melatonin.
· It is an effective antioxidant, unlike sulforaphane.

The discovered compound has demonstrated the following advantages over the medicines currently used to treat degenerative diseases of the retina (including melatonin and sulforaphane):

1) It possesses a combination of biological activities with great therapeutic effect.
2) It is a powerful inducer of the signaling pathway Nrf2, effect that does not possess melatonin.
3) It rescued visual responses regarding rd10 mice treated with the vehicle (control).
4) It increased visual acuity up to 35.6%.
5) It increased contrast sensitivity from 11% to 15%.
Stage of Development:
Under development/lab tested
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
Spanish patent. PCT also applied for.

Partner sought

Type and Role of Partner Sought:
- Type of partner sought: Industry

- Specific area of activity of the partner: Pharmeutical company interested in prevention or treatment of degenerative diseases of the retina, among them:
· Retinitis pigmentosa.
· Glaucoma.
· Diabetic retinopathy.
· Age-related macular degeneration.

- Task to be performed: Commercial exploitation through patent licensing agreement or technical collaboration agreement to develop new applications.

Client

Type and Size of Client:
University
Already Engaged in Trans-National Cooperation:
No
Languages Spoken:
English
Spanish

Keywords

Technology Keywords:
06001015 Productos farmacéuticos / medicamentos
03004010 Special chemicals, intermediates