Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2002-09-20
2004-12-14
Berch, Mark L. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S341000, C546S275400, C546S168000, C544S238000, C544S357000, C544S405000
Reexamination Certificate
active
06831083
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a novel 3-phenyl-2-pyrazoline derivative or 3-phenyl-tetrahydropyridazine derivative, as well as to a pharmaceutically acceptable salt thereof. More particularly, the present invention relates to an agent containing the above compound, which can activate glutamic acid transporter and is useful for treatment and/or prevention of cerebral ischemia (cerebral infarct and brain edema), cephalotrauma, glaucoma, retinopathy, epilepsy and amyotrophic lateral sclerosis (ALS), all caused by glutamic acid toxicity.
BACKGROUND ART
Glutamic acid is an important excitatory neurotransmitter in the central nervous system and has a close connection with neuropathy caused during cerebral ischemia. There are reports on the excessive effusion of glutamic acid caused by ischemia in test animals, and also on persistent effusion of large amount of glutamic acid in the brain tissue of cerebral ischemia patient [B. Meldrum: Trends. Pharmacol. Sci. 1990, 11, 379-387]. Therefore, it is expected that brain tissue can be protected from cell death by controlling the excessive effusion of glutamic acid caused during ischemia.
Glutamic acid which effuses excessively into synapse gaps, is taken into cells by the action of glutamic acid transporter present in neurocytes or astrocytes, whereby an equilibrium is maintained. Up to now, five kinds of sodium-dependent glutamic acid transporters (GLT-1, GLAST, EAACI, EAAT4 and EAAT5) have been cloned, and an active study has been made in recent years in order to make clear the functions thereof. It is considered that glutamic acid transporter is activated with an increase in the ectocytic concentration of glutamic acid, caused during ischemia and has an important role in protecting neurocytes from glutamic acid toxicity. Also, there is a report that the degeneration of glutamic acid transporter has a connection with neurodegeneration such as amyotrophic lateral sclerosis (ALS). Therefore, by activating glutamic acid transporter and removing the glutamic acid excessively effusing into synapse gaps, protective effects can be expected for various diseases considered to be caused by glutamic acid toxicity, such as cerebral ischemia (cerebral infarct and brain edema), sequela of cerebral ischemia, cephalotrauma, glaucoma, retinopathy, epilepsy, amyotrophic lateral sclerosis (ALS) and the like. However, there has heretofore been no report on any drug capable of activating glutamic acid transporter.
REFERENCES:
patent: 1-226815 (1989-09-01), None
patent: 11-292764 (1999-10-01), None
Fujiwara Junya
Kibayashi Kenji
Sakai Kazuya
Shiga Yoshio
Shimada Fumiki
Berch Mark L.
Burns Doane , Swecker, Mathis LLP
Habte Kahsay
Mitsui Chemicals Inc.
LandOfFree
Pyrazoline derivative or tetrahydropyridazine derivative and... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pyrazoline derivative or tetrahydropyridazine derivative and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrazoline derivative or tetrahydropyridazine derivative and... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3285490