Title:
BLOOD-BRAIN BARRIER DISRUPTION INHIBITORS
Document Type and Number:
WIPO Patent Application WO/2004/063167
Kind Code:
A1
Abstract:
The invention aims at providing blood-brain barrier disruption inhibitors. The invention provides blood-brain barrier disruption inhibitors containing as the active ingredient pyrazolone derivatives represented by the general formula (I), physiologically acceptable salts thereof, or hydrates or solvates of the same: (I) wherein R1 is hydrogen, aryl, alkyl, or alkoxycarbonylalkyl, and R2 is hydrogen, aryloxy, arylmercapto, alkyl, or hydroxyalkyl, or R1 and R2 may be united to form alkylene; and R3 is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, benzyl, naphthyl, phenyl, or phenyl which is mono- to tri-substituted with one or more members selected from the group consisting of alkyl, alkoxy, hydroxyalkyl, alkoxycarbonyl, alkylmercapto, alkylamino, dialkylamino, halogeno, trifluoromethyl, carboxyl, cyano, hydroxyl, nitro, amino, and acetamido.
Inventors:
KAWAKAMI JUNICHI (JP)
Application Number:
PCT/JP2004/000105
Publication Date:
July 29, 2004
Filing Date:
January 09, 2004
Export Citation:
Assignee:
MITSUBISHI PHARMA CORP (JP)
KAWAKAMI JUNICHI (JP)
KAWAKAMI JUNICHI (JP)
International Classes:
A61K31/4152; A61P7/00; A61P9/00; A61P25/00; A61P29/00; A61P35/00; A61P43/00; C07D231/26; (IPC1-7): C07D231/26; A61K31/4152; A61P7/00; A61P9/00; A61P25/00; A61P29/00; A61P35/00; A61P43/00
Foreign References:
| EP0208874A1 | 1987-01-21 |
Other References:
WATANABE T. ET AL.: "Protective effects of MCI-186 on cerebral ischemia: Possible involvement of free radical scavenging and antioxidant actions", THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 268, no. 3, 1994, pages 1597 - 1604, XP002979375
HAUSER S.L. ET AL.: "Cytokine accumulations in CSF of multiple sclerosis patients: Frequent detection of interleukin-1 and tumor necrosis factor but not interleukin-6", NEUROLOGY, no. 40, 1990, pages 1735 - 1739, XP002979376
HAUSER S.L. ET AL.: "Cytokine accumulations in CSF of multiple sclerosis patients: Frequent detection of interleukin-1 and tumor necrosis factor but not interleukin-6", NEUROLOGY, no. 40, 1990, pages 1735 - 1739, XP002979376
Attorney, Agent or Firm:
SIKs & Co. (Kyobashi-Nisshoku Bldg. 8-7, Kyobashi 1-chom, Chuo-ku Tokyo, JP)
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