# US 10,369,121 B2 · Pharmaceutical composition for preventing or treating immune diseases or inflammatory diseases, containing biguanide derivative compound as active ingredient

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- Number: US 10,369,121 B2
- Document ID: US10369121B2
- Status: Granted
- Kind: B2
- Application number: 15/502,981
- Filed: 2014-08-25
- Published: 2017-11-23
- Granted: 2019-08-06
- Earliest claimed: 2013-08-23
- Assignees: The Catholic University of Korea Industry-Academic Cooperation Foundation
- Applicants: The Catholic University of Korea Industry—Academic Cooperation Foundation
- Inventors: Mi-La Cho; Chul-Woo Yang; Dong-Yun Shin; Min-Jung Park; Seon-Yeong Lee; Sung-Hee Lee; Eun-Ji Yang; Hye-Jin Son; Eun-Kyung Kim; Jae-Kyung Kim
- Web page: https://patentgrep.com/patent/US10369121B2

## CPC

- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07C 279/18: having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
- C07C 279/26: X and Y being nitrogen atoms, i.e. biguanides
- A61K 2121/00: Preparations for use in therapy
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-α, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.

## Claims

### Claim 1

A method for treating an inflammatory bowel disease or a graft versus host disease in a subject, comprising administering a pharmaceutical composition comprising a biguanide derivative or a pharmaceutically acceptable salt thereof as an active ingredient,
wherein the biguanide derivative is 1-isopropylbiguanide or 1-(3-fluorophenyl)biguanide.

### Claim 2 (depends on 1)

The method of claim 1, wherein the biguanide derivative is characterized by reducing or suppressing the generation of an inflammatory cytokine.

### Claim 3 (depends on 2)

The method of claim 2, wherein the inflammatory cytokine is IL-17 or TNF-α.

### Claim 4 (depends on 1)

The method of claim 1, wherein the biguanide derivative is characterized by promoting or increasing the activity of a regulatory T cell.

### Claim 5 (depends on 1)

The method of claim 1, wherein the biguanide derivative is included in the composition at the concentration of 1 μM to 1,000 μM.

### Claim 6 (depends on 1)

The method of claim 1, wherein the composition is administered to the subject in an amount of 1 to 100 mg per 1 kg body weight of the subject.