Patent Number: 6,310,203

Title: Precursor compounds to substituted 1,2,4-triazolo[3,4,-a]phathalazine GABA alpha 5 ligands

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: ##STR1## in which R.sup.1 is hydrogen, halogen, CF.sub.3, OCF.sub.3, CN or an optionally substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy or C.sub.2-4 alkynyloxy group; R.sup.2 is hydrogen, halogen, CF.sub.3, OCF.sub.3, CN or an optionally substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy or C.sub.2-4 alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.

Inventors: Carling; William Robert (Bishops Stortford, GB), Ladduwahetty; Tamara (London, GB), MacLeod; Angus Murray (Bishops Stortford, GB), Merchant; Kevin John (Stevennge, GB), Moore; Kevin William (Bundngford, GB), Sternfeld; Francine (London, GB), Street; Leslie Joseph (Harlow, GB)

Assignee: Merck Sharpe & Dohme Limited

International Classification: C07D 487/00 (20060101); C07D 487/04 (20060101); C07D 487/04 ()

Expiration Date: 10/30/2018