SMALL-MOLECULAR INHIBITOR OF ROTAMASE ENZYME ACTIVITY
Document Type and Number:
Japanese Patent JP2000169444
To obtain a new compound having affinity to an FK 506 binding protein (FKBP)-type immunophilin, capable of inhibiting rotamase activity of the immunophilin, and useful for treating neurological disorders, such as Alzheimer's disease and Parkinson's disease.
A compound of the formula [R1 is a 1-9C alkyl, a 1-9C alkenyl, a 3-5C cycloaklyl or the like; X is O or S; Y is O or a NR2 group (R2 is H or a 1-6 alkyl); Z is H], for example, (2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2- pyridinecaboxylic acid. The compound is obtained, for example, by reacting a corresponding L-proline methyl ester with a corresponding methyloxalyl chloride. The compound of the formula is useful for treatment when used in a dose level of 0.1-10,000 mg as an active compound.
Hamilton, Gregory S.
Steiner, Joseph P.
June 20, 2000
June 05, 1996
GUILFORD PHARMACEUT INC
C12N9/99; A61K31/00; A61K31/40; A61K31/401; A61K31/4025; A61K31/405; A61K31/427; A61K31/44; A61K31/4427; A61K31/443; A61K31/4433; A61K31/4439; A61K31/444; A61K31/454; A61K38/00; A61K45/00; A61P21/00; A61P21/02; A61P25/00; A61P25/02; A61P25/14; A61P25/16; A61P25/24; A61P25/28; A61P37/00; A61P43/00; C07B53/00; C07D207/16; C07D401/04; C07D401/06; C07D405/06; C07D405/10; C07D405/12; C07D407/04; C07D409/04; C07D409/06; C07D409/12; C07D409/14; C07D417/02; C07D417/04; C07D417/12; C07K5/078; (IPC1-7): C07D207/16; A61K31/401; A61K31/4025; A61K31/427; A61K31/454; A61K38/00; A61P25/00; A61P25/14; A61P25/28; C07D401/06; C07D405/12; C07D409/12; C07D409/14; C07D417/12; C12N9/99