Compound having immune disease treatment effect and use thereof

Patent metadata

Field	Value
Publication number	US-10100006-B2
Application number	US-201715819758-A
Country	US
Kind code	B2
Filing date	Nov 21, 2017
Priority date	Apr 29, 2014
Publication date	Oct 16, 2018
Grant date	Oct 16, 2018

Abstract

Provided is a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present subject matter has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune response.

First claim

The invention claimed is:

1. A method of treating immune diseases in a mammalian in need thereof, comprising administering a therapeutically effective amount of N-ethyl-N-(4-fluorophenyl)-biguanide or a pharmaceutically acceptable salt thereof to the mammalian.

2. The method of claim 1 , wherein the N-ethyl-N-(4-fluorophenyl)-biguanide or a pharmaceutically acceptable salt thereof decreases or inhibits production of inflammatory cytokines, inhibits production of auto-antibodies, and inhibits differentiation of osteoclasts.

3. The method of claim 2 , wherein the inflammatory cytokine is IL-17, IL-6, TNF-α, IFN-γ, MMP-9, or STAT-3.

4. The method of claim 2 , wherein the autoantibody is IgG, IgG1, or IgG2a.

5. The method of claim 1 , wherein the N-ethyl-N-(4-fluorophenyl)-biguanide or a pharmaceutically acceptable salt thereof promotes or increases activity of regulatory T cells and decreases or inhibits activity of Th17 cells as pathological cells.

6. The method of claim 1 , wherein the immune disease is selected from the group consisting of autoimmune diseases; inflammatory diseases; and transplantation rejection diseases.

7. The method of claim 6 , wherein the autoimmune disease is selected from rheumatoid arthritis, Behcet's disease, multiple myositis or skin myositis, autoimmune hematocytopenia, autoimmune myocarditis, atopic dermatitis, asthma, primary cirrhosis, dermatomyositis, Goodpasture syndrome, autoimmune meningitis, sjogren's syndrome, lupus, Addison's disease, alopecia areata, ankylosing myelitis, autoimmune hepatitis, autoimmune mumps, Crohn's disease, insulin-dependent diabetes, dystrophic epidermolysis bullosa, epididymitis, glomerulonephritis, Graves' disease, Guillain-Barre syndrome, Hashimoto's disease, hemolytic anemia, multiple sclerosis, myasthenia gravis, pemphigus vulgaris, psoriasis, rheumatic fever, sarcoidosis, scleroderma, vasculitis, vitiligo, myxedema, pernicious anemia, and ulcerative colitis.

8. The method of claim 6 , wherein the transplantation rejection disease is a graft versus host disease.

Assignees

• The Catholic Univ Of Korea Industry—Academic Cooperation Foundation
• Catholic Univ Korea Ind Academic Cooperation Foundation

Inventors

• Cho Mi-La
• Shin Dong-Yun
• Park Sung-Hwan
• Yang Chul-Woo
• Choi Jong-Young
• Park Min-Jung
• Son Hye-Jin
• Lee Sung-Hee
• Lee Seon-Yeong
• Kim Eun-Kyung
• Kim Jae-Kyung
• Lee Seung-Hun
• Park Seong-Hyeok

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P7/06

  Antianaemics · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P5/14

  of the thyroid hormones, e.g. T3, T4 · CPC title