# US 2022/0031797 A1 · Pharmaceutical compositions containing hyaluronic acid and carnosine and relative use

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- Number: US 2022/0031797 A1
- Document ID: US20220031797A1
- Status: Published application
- Kind: A1
- Application number: 17/482,696
- Filed: 2021-09-23
- Published: 2022-02-03
- Earliest claimed: 2017-10-03
- Assignees: Fidia Farmaceutici S.P.A.
- Applicants: Fidia Farmaceutici S.P.A.
- Inventors: Antonella Schiavinato; Valentina Greco; Luciano Messina; Susanna Vaccaro; Enrico Rizzarelli; Sebastiano Sciuto
- Web page: https://patentgrep.com/patent/US20220031797A1

## CPC

- A61K 38/05: Dipeptides
- A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof
- A61K 31/728: Hyaluronic acid
- A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid}
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0029: {Parenteral nutrition; Parenteral nutrition compositions as drug carriers}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- 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

Pharmaceutical compositions are described containing Hyaluronic Acid and Carnosine for use in the treatment and prevention of osteoarthritis (OA) and for the treatment of rheumatoid arthritis (RA).

## Claims

### Claim 1

A method for the treatment of osteoarthritis and/or for the treatment of rheumatoid arthritis (RA), which comprises administering to a patient in need thereof a pharmaceutical composition comprising a hyaluronic acid (HA)/carnosine conjugate with a direct amide bond between the carboxyl group of hyaluronic acid and the amine group of carnosine, wherein the hyaluronic acid (HA)/carnosine conjugate is obtained by covalently conjugating the dipeptide of carnosine with hyaluronic acid by amidation with the formation of a direct amide bond between the carboxyl of HA and the amine group of carnosine, with a derivatization degree of the carboxyl group of HA higher than 25% or ranging from 30 to 100%, or ranging from 30 to 60%, or varying within the range of 35±3% or 45±5%.

### Claim 2 (depends on 1)

The method according to claim 1, which further comprises treating
pathologies caused directly by RA selected from pulmonary fibrosis, pleurisy and pleuropericarditis, xerophthalmia, uveitis and scleritis, and/or
pathologies indirectly related to or depending on RA selected from premature pathological aging, heart attack, stroke, arterosclerosis and coronary atherosclerosis, arterial hypertension, dementia, diabetes, osteoporosis and amyloidosis, cancer, proteinuria and nephritis, gastric lesions, cataracts, psoriatic arthritis, gastritis, vasculitis, type I diabetes and autoimmune thyroiditis.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the HA has an average molecular weight ranging from 400 to 3×106 Da or ranging from 1×105 Da to 1×106 Da or within the range of 130-220 k Da or within the range of 500-750 k Da and mixtures thereof.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the derivatization degree of HA ranges from 30 to 60% and the average molecular weight of HA ranges from 1×105 Da to 1×106, or is within the range of 130-220 k Da or 500-750 k Da and mixtures thereof.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the hyaluronic acid used for the amide derivative of HA with carnosine is the sodium salt of HA or the tetrabutylammonium salt of HA.

### Claim 6 (depends on 1)

The method according to claim 1, wherein said pharmaceutical composition is administer topically, orally, intra-articularly, parenterally or surgically.

### Claim 7 (depends on 1)

The method according to claim 1, wherein said pharmaceutical composition is administered in the form of a biomaterial comprising derivatives of HA conjugated with carnosine, wherein said derivatives are selected from esters of HA, amides of HA, internal esters of HA, percarboxylates of HA and sulfates of HA.

### Claim 8 (depends on 7)

The method according to claim 7, which further comprises treating
pathologies caused directly by RA selected from pulmonary fibrosis, pleurisy and pleuropericarditis, xerophthalmia, uveitis and scleritis, and/or
pathologies indirectly related to or depending on RA selected from premature pathological aging, heart attack, stroke, arterosclerosis and coronary atherosclerosis, arterial hypertension, dementia, diabetes, osteoporosis and amyloidosis, cancer, proteinuria and nephritis, gastric lesions, cataracts, psoriatic arthritis, gastritis, vasculitis, type I diabetes and autoimmune thyroiditis.

### Claim 9 (depends on 8)

The method according to claim 8, wherein the biomaterials are in the form of fibers, gels, hydrogels, microspheres, sponges, woven or nonwoven fabrics, or films, and are administered topically, orally, intra-articularly, parenterally or surgically.

### Claim 10 (depends on 1)

The method according to claim 1, wherein said pharmaceutical composition further comprises pharmacologically and/or biologically active substances and/or with controlled release systems of drugs and/or natural polymers or polymers of a synthetic nature.