Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula:
in which R1 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; R2 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.
Type:
Grant
Filed:
April 11, 2000
Date of Patent:
October 30, 2001
Assignee:
Merck Sharpe & Dohme Limited
Inventors:
William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein A, B, R2, R3 and q are as defined in the disclosure, pharmaceutical compositions containing them; methods for their production; their use in therapy and methods of treatment of disease states where cognition enhancement is required, such as Alzheimer's disease.
Type:
Grant
Filed:
April 22, 1999
Date of Patent:
December 5, 2000
Assignee:
Merck Sharpe & Dohme Limited
Inventors:
Helen Jane Bryant, Mark Stuart Chambers, Sarah Christine Hobbs