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SULPHATED DISACCHARIDES FOR THE TREATMENT OF NEURODEGENERATIVE AND/OR NEUROVASCULAR DISEASESCM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.2519242.A1
Fecha publicacion
07/11/2012
Numero solicitud
EP20100798098

En detalle

Resumen

[0000] The present invention relates to the use of a series of sulphated disaccharides for the preparation of a medicament for the treatment or prevention of a neurodegenerative and/or neurovascular disease, of a traumatic brain injury or of a traumatic spinal cord injury. The present invention also relates to the use of said sulphated disaccharides for the preparation of a neuroprotective medicament or of an antioxidant medicament. The neurodegenerative and/or neurovascular diseases are preferably: Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis and stroke.

Reivindicaciones

C L A I M S 1 .- Use of a compound of formula (I), <img class="EMIRef" id="73201845-imgf000028-0001" /> (I) wherein: R<1> is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyi of less than ten carbon atoms and -COCH<3>; R<2> is selected from hydrogen, -COCH<3> and -S0<3>Y; R<3> is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyi of less than ten carbon atoms, -COCH<3> and -COPh, wherein Ph is phenyl; G is selected from -COOR<4> and -COOY; A and B are independently selected from hydrogen, -S0<3>H, -S0<3>Y and -COCH<3>, wherein either A or B is necessarily either -S0<3>H or -S0<3>Y; R<4> is selected from hydrogen, C1-C2 alkyl and arylalkyl of less than sixteen carbon atoms, Y is an organic or inorganic cation; or a pharmaceutically acceptable salt, prodrug or solvate thereof, for the preparation of a medicament for the treatment or prevention of a neurodegenerative and/or neurovascular disease, of a traumatic brain injury or of a traumatic spinal cord injury in a mammal. 2. - Use according to claim 1 , wherein R<1> is selected from hydrogen and linear C1-C4 alkyl and G is selected from -COOR<4> and -COOY, wherein R<4> is hydrogen or C-|-C<2> alkyl and Y is an inorganic cation. 3. - Use according to claim 2, wherein R<1> is hydrogen, R<2> is -COCH<3> and R<3> is hydrogen. 4. - Use according to claim 2, wherein R<1> is methyl, R<2> is -COCH<3> and R<3> is hydrogen. 5.- Use according to claim 3 or 4, wherein A is hydrogen, B is -SO<3>Y and G is -COOY, wherein Y is an inorganic cation. 6.- Use according to claim 3 or 4, wherein A is -SO<3>Y, B is hydrogen and G is -COOY, wherein Y is an inorganic cation. 7. - Use according to claim 3 or 4, wherein A and B are -SO<3>Y and G is -COOY, wherein Y is an inorganic cation. 8. - Use according to claim 5, wherein the compound of formula (I) is: <img class="EMIRef" id="73201845-imgf000029-0001" /> 9.- Use according to claim 6, wherein the compound of formula (I) is: <img class="EMIRef" id="73201845-imgf000029-0002" /> 10.- Use according to claim 7, wherein the compound of formula (I) is: <img class="EMIRef" id="73201845-imgf000029-0003" /> 1 1.- Use according to any one of claims 1 to 10, wherein the neurodegenerative and/or neurovascular disease is associated with oxidative stress. 12.- Use according to any one of claims 1 to 1 1 , wherein the medicament is a neuroprotective and/or neuroreparative medicament. 13.- Use according to any one of claims 1 to 12, wherein the treatment or prevention results in the treatment or prevention of a neurodegenerative and/or neurovascular disease selected from among the group consisting of Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, stroke, transient ischemic brain attack, Huntington's disease, Friedreich's ataxia, spongiform encephalopathies, dementia with Lewy bodies, Pik's disease, mild cognitive impairment, epilepsy, migraine, schizophrenia, bipolar disorder, vascular dementia and arteriosclerosis. 14.- Use according to any one of claims 1 to 13, wherein the disease is Alzheimer's disease. 15. - Use according to any one of claims 1 to 13, wherein the disease is Parkinson's disease. 16. - Use according to any one of claims 1 to 13, wherein the disease is amyotrophic lateral sclerosis. 17. - Use according to any one of claims 1 to 13, wherein the disease is stroke. 18. - Use of a compound of formula (I) as defined in any one of claims 1 to 10, or a pharmaceutically acceptable salt, prodrug or solvate thereof, for the preparation of a neuroprotective and/or neuroreparative medicament. 19. - Use of a compound of formula (I) as defined in any one of claims 1 to 10, or a pharmaceutically acceptable salt, prodrug or solvate thereof, for the preparation of an antioxidant medicament. 20.- A compound of formula (I) as defined in any one of claims 1 to 10, or a pharmaceutically acceptable salt, prodrug or solvate thereof, for use in the treatment or prevention of a neurodegenerative and/or neurovascular disease, of a traumatic brain injury or of a traumatic spinal cord injury in a mammal. 21. - The compound according to claim 20, wherein the neurodegenerative and/or neurovascular disease is selected from the group consisting of Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, stroke, transient ischemic brain attack, Huntington's disease, Friedreich's ataxia, spongiform encephalopathies, dementia with Lewy bodies, Pik's disease, mild cognitive impairment, epilepsy, migraine, schizophrenia, bipolar disorder, vascular dementia and arteriosclerosis. 22. - A compound of formula (I) as defined in any one of claims 1 to 10, or a pharmaceutically acceptable salt, prodrug or solvate thereof, for use as a chondroprotector and/or antioxidant. A process for the preparation of the compound of formula <img class="EMIRef" id="73201845-imgf000031-0001" /> (lc) characterized in that it comprises the following stages: (a) reacting the compound of formula (Va) <img class="EMIRef" id="73201845-imgf000031-0002" /> (Va) with the S0<3>. pyridine complex; (b) treating the intermediate compound obtained in stage (a) with sodium hydroxide; (c) purifying by precipitation in water/isopropyl alcohol; and (d) in the event that after stage (c) the compound of formula (lc) still contains salts, optionally purifying it by column chromatography.

Etiquetas

Inventores
Verges Milano JosepGarcia Garcia AntonioRuhi Roura RamonMontell Bonaventura EulaliaGarcia Lopez ManuelaAlaez Verson Carlos RaulEscaich Ferrer JosepEgea Maiquez JavierLorrio Gonzalez SilviaNegredo Madrigal Pilar
Solicitantes
BioibericaUniversidad Autónoma de MadridVerges Milano JosepGarcia Garcia AntonioRuhi Roura RamonMontell Bonaventura EulaliaGarcia Lopez ManuelaAlaez Verson Carlos RaulEscaich Ferrer JosepEgea Maiquez JavierNegredo Madrigal PilarLorrio Gonzalez Silvia
Clasificacion ipc
A61K 31/ 7016 A IA61P 25/ 00 A IA61P 25/ 28 A IA61P 25/ 16 A IA61K 31/ 715 A IC07H 3/ 04 A IC07H 5/ 04 A IC07H 5/ 06 A I
Clasificacion cpc
514/53536/54
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