# US 8,785,416 B2 · Sulphated disaccharides for the treatment of neurodegenerative and/or neurovascular diseases

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- Number: US 8,785,416 B2
- Document ID: US8785416B2
- Status: Granted
- Kind: B2
- Application number: 13/520,069
- Filed: 2010-12-22
- Published: 2012-12-06
- Granted: 2014-07-22
- Earliest claimed: 2009-12-29
- Assignees: Bioiberica, S.A.; Universidad Autonoma De Madrid
- Applicants: Josep Verges Milano; Antonio Garcia Garcia; Ramon Ruhi Roura; Eulalia Montell Bonaventura; Manuela Garcia Lopez; Carlos Raul Alaez Verson; Josep Escaich Ferrer; Javier Egea Maiquez; Pilar Negredo Madrigal; Silvia Lorrio Gonzalez
- Inventors: Josep Verges Milano; Antonio Garcia Garcia; Ramon Ruhi Roura; Eulalia Montell Bonaventura; Manuela Garcia Lopez; Carlos Raul Alaez Verson; Josep Escaich Ferrer; Javier Egea Maiquez; Pilar Negredo Madrigal; Silvia Lorrio Gonzalez
- Web page: https://patentgrep.com/patent/US8785416B2

## CPC

- A61K 31/7016: Disaccharides, e.g. lactose, lactulose (lactobionic acid A61K31/7032)
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

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.

## Claims

### Claim 1

A method for the treatment of a neurodegenerative and/or neurovascular disease, in a mammal, comprising administering to a mammal in need thereof an effective amount of a compound of formula (I),
wherein:
R1 is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyl of less than ten carbon atoms and —COCH3;
R2 is selected from hydrogen, —COCH3 and —SO3Y;
R3 is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyl of less than ten carbon atoms, —COCH3 and —COPh, wherein Ph is phenyl;
G is selected from —COOR4 and —COOY;
one of A or B is selected from hydrogen, —SO3H, —SO3Y and —COCH3, and the other
A or B is —SO3H or —SO3Y;
R4 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 thereof; 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, Pick's disease, mild cognitive impairment, epilepsy, migraine, schizophrenia, bipolar disorder, vascular dementia and cerebrovascular arteriosclerosis.

### Claim 2 (depends on 1)

The method according to claim 1, wherein R1 is selected from hydrogen and linear C1-C4 alkyl and G is selected from —COOR4 and —COOY, wherein R4 is hydrogen or C1-C2 alkyl and Y is an inorganic cation.

### Claim 3 (depends on 2)

The method according to claim 2, wherein R1 is hydrogen, R2 is —COCH3 and R3 is hydrogen.

### Claim 4 (depends on 2)

The method according to claim 2, wherein R1 is methyl, R2 is —COCH3 and R3 is hydrogen.

### Claim 5 (depends on 3, 4)

The method according to claim 3 or claim 4, wherein A is hydrogen, B is
—SO3Y and G is —COOY, wherein Y is an inorganic cation.

### Claim 6 (depends on 3, 4)

The method according to claim 3 or claim 4, wherein A is —SO3Y, B is hydrogen and G is —COOY, wherein Y is an inorganic cation.

### Claim 7 (depends on 3, 4)

The method according to claim 3 or claim 4, wherein A and B are —SO3Y and G is —COOY, wherein Y is an inorganic cation.

### Claim 8 (depends on 4)

The method according to claim 4, wherein the compound of formula (I) is selected from the group consisting of:

### Claim 9 (depends on 7)

The method according to claim 7, wherein the compound of formula (I) is:

### Claim 10 (depends on 1, 8)

The method according to claim 1 or claim 8, wherein the neurodegenerative and/or neurovascular disease is associated with oxidative stress.

### Claim 11 (depends on 1, 8)

The method according to claim 1 or claim 8, wherein the disease is Alzheimer's disease.

### Claim 12 (depends on 1, 8)

The method-according to claim 1 or claim 8, wherein the disease is Parkinson's disease.

### Claim 13 (depends on 1, 8)

The method according to claim 1 or claim 8, wherein the disease is amyotrophic lateral sclerosis.

### Claim 14 (depends on 1, 8)

The method-according to claim 1 or claim 8, wherein the disease is stroke.

### Claim 15

A method for the treatment of an oxidation-associated neurodegenerative and/or neurovascular disease, comprising administering to a mammal in need thereof an effective amount of a compound of formula (I)
wherein:
R1 is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyl of less than ten carbon atoms and —COCH3;
R2 is selected from hydrogen, —COCH3 and —SO3Y;
R3 is selected from hydrogen, linear or branched C1-C4 alkyl, phenylalkyl of less than ten carbon atoms, —COCH3 and —COPh, wherein Ph is phenyl;
G is selected from —COOR4 and —COOY;
one of A or B is selected from hydrogen, —SO3H, —SO3Y and —COCH3, and the other
A or B is —SO3H or —SO3Y;
R4 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 thereof;
wherein the oxidation-associated 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, Pick's disease, mild cognitive impairment, epilepsy, migraine, schizophrenia, bipolar disorder, vascular dementia and cerebrovascular arteriosclerosis.

### Claim 16 (depends on 15)

The method according to claim 15, wherein the compound of formula (I) is selected from a group consisting of:

### Claim 17 (depends on 16)

The method according to claim 16, wherein the compound of formula (I) is: