.beta.-hydroxyaspartic acid derivatives
AssigneeSuntory Limited
InventorsKeiko Shimamoto, Yoshimi Yasuda, Masahiro Sakaitani, Bruno Lebrun
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AssigneeSuntory Limited
InventorsKeiko Shimamoto, Yoshimi Yasuda, Masahiro Sakaitani, Bruno Lebrun
Estimating the term…
The present invention provides blockers for glutamate transporters. During a series of syntheses searching for glutamate uptake inhibition in Xenopus oocytes injected with bovine glutamate transporter genes (BGLAST), we obtained .beta.-hydroxyaspartic acid derivatives of the following chemical formula (1): ##STR1## wherein R represents an aromatic acyl group which may be substituted on the ring, a straight or branched lower aliphatic acyl group, an aryl group which may be substituted on the ring, an aralkyl group which may be substituted on the ring, or a straight or branched lower alkyl group; and salts thereof. These compounds are blockers of glutamate transporters, which are useful for the understanding of the function of glutamate transporters and show promise for the treatment of various neurodegenerative diseases.
A .beta.-hydroxyaspartic acid derivative of the following chemical formula (1):
A method of inhibiting the uptake of glutamate by cells expressing a L-glutamate transporter, comprising administering a .beta.-hydroxyaspartic acid derivative to cells expressing a L-glutamate transporter, in an amount sufficient to inhibit the uptake of glutamate, said .beta.-hydroxyaspartic acid derivative having the following chemical formula (1):
A method of treating a patient having neuropathy or a neurodegenerative disease wherein a L-glutamate transporter is involved in the onset or development of the disease, comprising administering a .beta.-hydroxyaspartic acid derivative in a pharmaceutically effective amount, to a patient in need of treatment for a neuropathy or a neurodegenerative disease, said .beta.-hydroxyaspartic acid derivative having the following chemical formula (1):
A composition for inhibiting the uptake of glutamate into cells expressing a L-glutamate transporters thereon comprising a .beta.-hydroxyaspartic acid derivative of the following chemical formula (1):
A pharmaceutical composition comprising as an active ingredient a .beta.-hydroxyaspartic acid derivative of the following chemical formula (1):
A food composition comprising a .beta.-hydroxyaspartic acid derivative of the following chemical formula (1):
Dependencies are inferred from the claim text.