NMDA RECEPTOR MODULATORS AND USES THEREOF
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
1 . A compound represented by:
wherein:
R 1 , R 2 , R 3 , and R 4 are each independently selected from the group consisting of hydrogen; halogen, C 1 -C 6 alkyl, or —OH;
R 5 is selected from the group consisting of —CH 2 -phenyl and hydrogen, provided that R 5 is —CH 2 -phenyl when R 1 and R 3 are —OH and R 2 and R 4 are methyl;
X is selected from the group consisting of OR x and NR x R x , wherein R x is independently selected, for each occurrence, from the group consisting of hydrogen, and C 1 -C 6 alkyl; pharmaceutically acceptable salts, stereoisomers, and hydrates thereof.
2 . The compound of claim 1 represented by:
3 . The compound of claim 1 represented by:
4 . The compound of claim 1 represented by:
5 . The compound of claim 1 represented by:
6 . The compound of claim 1 represented by:
7 . The compound of claim 1 represented by:
8 . The compound of claim 1 represented by:
wherein X is OH or NH 2 .
9 . A pharmaceutical composition, comprising:
a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
10 . The pharmaceutical composition of claim 9 , suitable for oral administration.
11 . The pharmaceutical composition of claim 9 , suitable for injection.
12 . A method of treating depression, Alzheimer's disease, attention deficit disorder, ADHD, schizophrenia, or anxiety, in a patient in need thereof, comprising administering to said patient:
a pharmaceutically effective amount of a compound of claim 1 .