Dong Wha Pharmaceutical Co. Ltd.

Dongwha Pharm. Ind. Co., Ltd.

Yong-Ho Chung

Eun-Joo Kim

Yun-Ha Hwang

Yong-Youp Park

Do-Hui Kim

Pan-Soo Kim

Hong-Suk Suh

Jin Soo Lee

Jei Man Ryu

Jin-soo Lee

Jin-Soo Lee

Sae-Kwang Ku

Jei-Man Ryu

Seok-Hoon Ahn

Young-Goo Jin

Sang-Mi Jin

Jei-Man Rye

Sun-Ki Cho

This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis.

Use of 4-[(4-thiazolyl)phenoxy]alkoxy-benzamidine derivatives for the prophylaxis and treatment of osteoporosis

A method of treating osteoporosis comprising administering to a subject a composition comprising a compound, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or a salt thereof, is described. A method of inhibiting osteoclast activity and stimulating osteoblast activity in a subject also is described.

Use of 4-[(4-thiazolyl)phenoxy]alkoxy-benzamidine derivatives for treatment of osteoporosis

This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prevention and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-iso-propyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1, which is known as an antagonist of leukotriene-Breceptor, as a pharmaceutical composition for the prevention and treatment of osteoporosis. [Formula 1], wherein, R is a hydrogen atom or a hydroxy group.

The present invention relates to 3-amido-1,2-benzoisoxazole derivatives and their salts represented by formula 1, processes for preparation and usees thereof. More particularly, it relates to a method for improving its bioavailability introducing amino acid residue to the amine group of a 3-amido-1,2-benzoisoxazole. The compounds according to the present invention are used as an antagonist against Leukotriene-B-4 receptor, an inhibitor or therapeutics of osteoroposis, thus inhibiting osteolysis and stimulating osteogensis.

3-amido-1,2-benzoisoxazole derivatives, process for preparation, and use thereof

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Anyang-si, South Korea

Yong-Ho Chung