Pharmaceutical composition comprising chito-oligomers

Inventors

Gislason, JohannesPeter, MartinEinarsson, Jon M.Bahrke, Sven

Assignees

Genis ehf

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Publication Number

US-7985741-B2

Patent

Publication Date

2011-07-26

Expiration Date


Abstract

Compositions are provided comprising chito-oligomers obtainable from chitin, comprising oligomers of N-acetyl glucosamine (NAG) and glucosamine, wherein at least 50% of the oligomers have a chain length of about 2-50, and the degree of deacetylation of the oligomers is in the range of about 0-70%, preferably about 30-50%. The compositions are highly useful as pharmaceutical compositions for treatment of joint disorders such as rheumatoid arthritis and osteoarthritis. Also provided are methods for treatment of joint disorders and treatment against inflammatory activity.

Core Innovation

The disclosed invention relates to chito-oligomers of N-acetyl glucosamine (NAG) and glucosamine for pharmaceutical composition use. The oligomers are obtained by a process including a first step of partially deacetylating chitin and a second step of enzymatically hydrolyzing the partially deacetylated chitin. The disclosed oligomers have a chain length in the range of about 2-50 and a degree of deacetylation in the range of about 0-70%.

The chito-oligomers comprise a size larger than a dimer and have an inhibitory effect on chitinase-like proteins. At least about 10 wt % of the chito-oligomers have a chain length of 2 to 12, and the disclosed compositions are described with preference ranges for degree of deacetylation and size distribution.

The invention addresses inflammatory activity in joint-related conditions, including joint disorders selected from osteoarthritis and rheumatoid arthritis. The therapeutic approach is described as administering a therapeutically effective amount of the disclosed chito-oligomers to treat a disorder selected from joint disorders, inflammatory disorders, and other rheumatoid conditions.

Claims Coverage

The document includes one independent claim directed to a treatment method, with six inventive features centered on the chito-oligomer composition, manufacturing process, and treatment use.

Treatment by administering therapeutically effective chito-oligomers

A method comprising administering a therapeutically effective amount of chito-oligomers of N-acetyl glucosamine (NAG) and glucosamine.

Oligomers produced by partially deacetylating chitin and enzymatically hydrolyzing

The chito-oligomers are obtained by a process comprising a first step of partially deacetylating chitin and a second step of enzymatically hydrolyzing the partially deacetylated chitin.

Chain length and degree of deacetylation ranges

The oligomers have a chain length in the range of about 2-50 and the degree of deacetylation of the oligomers is in the range of about 0-70%.

Inhibitory effect on chitinase-like proteins with size larger than a dimer

The oligomers comprise a size larger than a dimer and have an inhibitory effect on chitinase-like proteins.

Weight-percent fraction of chain length 2 to 12

At least about 10 wt % of the chito-oligomers have a chain length of 2 to 12.

Disorder selected from joint disorders, inflammatory disorders, and other rheumatoid conditions

The method is for treatment of a disorder selected from the group containing joint disorders, inflammatory disorders, and other rheumatoid conditions.

Overall claim coverage centers on a treatment method that administers NAG/glucosamine chito-oligomers produced from partially deacetylated chitin via enzymatic hydrolysis, where the oligomers are defined by chain length, degree of deacetylation, size larger than a dimer, inhibitory effect on chitinase-like proteins, and a required wt% fraction of chain length 2 to 12.

Stated Advantages

Inhibitory effect on chitinase-like proteins.

Therapeutic symptom relief in preliminary human subject administration outcomes after 3-4+ weeks.

Documented Applications

Treatment of joint disorders, including osteoarthritis and rheumatoid arthritis.

Treatment of inflammatory disorders and other rheumatoid conditions via administration of the disclosed chito-oligomers.

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