Cyclic dipeptides and azetidinone compounds and their use in treating CNS injury and neurodegenerative disorders
AssigneeGeorgetown University
InventorsAlan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
Life of this patent
Estimating the term…
Abstract
The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.
Claims21
A method of treating a neurodegenerative disorder in a subject comprising administering to said subject in need of such treatment an effective amount of a compound having the formula:
- or a pharmaceutically acceptable salt or hydrate thereof, wherein:
- n is an integer from 0 to 3;
- X is selected from the group consisting of —S—, —O—, —NR— and CH2—;
- R1 and R2 are each independently selected from the group consisting of —H, —OR, —SR, —NRR, —NO2, CN, —C(O)OR, —C(O)NRR, —C(NR)NRR, trihalomethyl, halogen, (C1-C6) alkyl, substituted (C1-C6) alkyl, (C2-C6) alkenyl, substituted (C2-C6) alkenyl, (C2-C6) alkynyl, substituted (C2-C6) alkynyl, (C5-C20) aryl, substituted (C5-C20) aryl, 5-20 membered heteroaryl, substituted 5-20 membered heteroaryl, (C6-C26) alkaryl, substituted (C6-C26) alkaryl, 6-26 membered alk-heteroaryl and substituted 6-26 membered alk-heteroaryl,
- or R1 and R2 taken together are —CH2—(CH2)m—CH2—, where m is an integer from 0 to 6;
- each alkyl, alkenyl, alkynyl, aryl, alkaryl, heteroaryl or alk-heteroaryl substitutent is independently selected from the group consisting of —OR, —SR, —NRR, —CN, —NO2, —C(O)OR, —C(O)NRR, —C(S)NRR, —C(NR)NRR, halogen and trihalomethyl;
- and
- each R is independently selected from the group consisting of —H, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C5-C20) aryl, 5-20 membered heteroaryl, (C6-C26) alkaryl and 6-26 membered alk-heteroaryl.
A compound of the formula
- or a pharmaceutically acceptable salt or hydrate thereof.
Dependencies are inferred from the claim text.