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Title:
PYRAZOLONE DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2009/001949
Kind Code:
A1
Abstract:
Disclosed is a novel pyrazolone derivative represented by the general formula (I), an optical isomer of the derivative, a pharmaceutically acceptable salt of the derivative or the optical isomer, or a hydrate or solvate of the derivative, the optical isomer or the pharmaceutically acceptable salt. The novel pyrazolone derivative has an inhibitory activity on the production of PAI-1, an inhibitory activity on the fibrosis of a tissue and a fibrinolytic activity, and is therefore useful for the prevention and/or treatment of a disease induced by a morbid thrombosis, such as a tissue fibrosis disease (e.g., pulmonary fibrosis, renal fibrosis), an ischemic heart disease (e.g., myocardial infarction, angina pectoris), intra-atrial thrombosis, pulmonary embolism, deep vein thrombosis, disseminated intravascular coagulation, an ischemic brain disease (e.g., cerebral infarction, cerebral hemorrhage) and arteriosclerosis. Also disclosed is a pharmaceutical agent useful for the prevention and/or treatment of a disease or condition mediated by a plasminogen activator inhibitor-1, which comprises the novel pyrazolone derivative. (I) wherein R1 to R3 are as defined in the claims.

Inventors:
GOMI, Noriaki (KOWA COMPANY LTD., 17-43, Noguchi-cho 2-chome, Higashimurayama-sh, Tokyo 22, 1890022, JP)
五味宣明 (〒22 東京都東村山市野口町2丁目17番地43号 興和株式会社 東京創薬研究所内 Tokyo, 1890022, JP)
INA, Shinji (KOWA COMPANY LTD., 17-43, Noguchi-cho 2-chome, Higashimurayama-sh, Tokyo 22, 1890022, JP)
稲真嗣 (〒22 東京都東村山市野口町2丁目17番地43号 興和株式会社 東京創薬研究所内 Tokyo, 1890022, JP)
Application Number:
JP2008/061787
Publication Date:
December 31, 2008
Filing Date:
June 23, 2008
Export Citation:
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Assignee:
KOWA COMPANY, LTD. (6-29, Nishiki 3-chome Naka-ku, Nagoya-sh, Aichi 25, 4608625, JP)
興和株式会社 (〒25 愛知県名古屋市中区錦3丁目6番29号 Aichi, 4608625, JP)
GOMI, Noriaki (KOWA COMPANY LTD., 17-43, Noguchi-cho 2-chome, Higashimurayama-sh, Tokyo 22, 1890022, JP)
五味宣明 (〒22 東京都東村山市野口町2丁目17番地43号 興和株式会社 東京創薬研究所内 Tokyo, 1890022, JP)
INA, Shinji (KOWA COMPANY LTD., 17-43, Noguchi-cho 2-chome, Higashimurayama-sh, Tokyo 22, 1890022, JP)
International Classes:
C07D231/20; A61K31/4152; A61K31/4155; A61K31/454; A61P7/02; A61P9/10; A61P11/00; A61P13/12; C07D231/22; C07D401/06; C07D405/12
Domestic Patent References:
2006-12-07
2003-02-13
2005-03-24
1995-11-30
2003-01-03
2006-06-15
1998-11-19
1994-05-11
Foreign References:
JPH07149642A1995-06-13
JPH07149643A1995-06-13
JPH07165573A1995-06-27
JPH07165574A1995-06-27
JPH10287622A1998-10-27
JP2003089687A2003-03-28
JP2004203793A2004-07-22
EP0563798A11993-10-06
US6280919B12001-08-28
DE3941240A11991-06-20
Other References:
J. CLIN. INVEST. vol. 97, 1996, page 232
CLIN. INVEST. MED. vol. 17, 1994, pages 69 - 76
JOURNAL OF MEDICINAL CHEMISTRY vol. 19, no. 2, 1976, pages 239 - 43
JOURNAL OF MEDICINAL CHEMISTRY vol. 30, no. 10, 1987, pages 1724 - 8
BIOCHEM. BIOPHYS. RES. COMM. vol. 288, no. 747, 2001,
See also references of EP 2172458A1
Attorney, Agent or Firm:
AOKI, Atsushi et al. (SEIWA PATENT & LAW, Toranomon 37 Mori Bldg. 5-1,Toranomon 3-chome, Minato-k, Tokyo 23, 1058423, JP)
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