Ligands for metabotropic glutamate receptors and inhibitors of NAALADase

• US 7,381,745 B2
• Filed: 02/25/2003
• Issued: 06/03/2008
• Est. Priority Date: 04/28/1999
• Status: Expired due to Term

• Current Assignee: Georgetown University
• Original Assignee: Georgetown University
• Inventors: Nan, Fajun, Wroblewski, Jarda T., Kozikowski, Alan P.
• Primary Examiner(s): Wilson; James O.
• Assistant Examiner(s): TRUONG, TAMTHOM NGO
• Application Number:
  US10/374,765
• Publication Number:
  US 20040002478A1
• Time in Patent Office: 1,925 Days
• Field of Search: 514/79, 514/114, 514/381, 514/553, 514/563, 514/574, 514/75, 514/533, 514/616, 544/243, 548/257, 562/11, 562/41, 562/443, 562/8, 562/10, 562/24, 560/38, 560/85, 564/15
• US Class Current: 514/533
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: C07C 271/22 to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
• CPC Class Codes: C07C 275/16 being further substituted by carboxyl groups
• CPC Class Codes: C07C 275/26 having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
• CPC Class Codes: C07C 323/59 with acylated amino groups bound to the carbon skeleton
• CPC Class Codes: C07C 335/08 of a saturated carbon skeleton
• CPC Class Codes: C07C 59/347 containing keto groups
• CPC Class Codes: C07C 69/716 Esters of keto-carboxylic acids or aldehydo-carboxylic acids
• CPC Class Codes: C07D 257/04 Five-membered rings
• CPC Class Codes: C07F 9/301 Acyclic saturated acids which can have further substituents on alkyl
• CPC Class Codes: C07F 9/303 Cycloaliphatic acids

Abstract

The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Claims

1. A compound of the formula:

2. The compound of claim 1, wherein R₂ is hydrogen.

3. The compound of claim 1, wherein the compound is a single stereoisomer.

4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient.