INSULIN-REGULATED AMINOPEPTIDASE (IRAP) INHIBITORS AND USES THEREOF

摘要

Disclosed is a 4H-chromene also known as 4H-naphtho[1 ,2-bjpyran compound of formaul (I) where the substituents are as disclosed in the description. In particular A is quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,8-naphthyridyl, phthalazinyl or pteridinyl and/or R1 is an amide. Examples of compounds of formula (I) are: Ethyl 2-amino-7 -hydroxy-4-quinolin-4-yl-4H-chromene-3-carboxylate; Ethyl 2-(acetylamino )-7 -hydroxy-4-pyridin-3-yl-4H-chromene-3-carboxylate; Ethyl 2-amino-7 -hydroxy-4-quinolin-3-yl-4H-chromene-3-carboxylate and Ethyl 2-(acetylamino )-7-hydroxy-4-quinolin-3-yl-4H-chromene-3-carboxylate. Also disclosed is a composition comprising a compound of formula (I0 and the use of a compound of formula (I) in the manufacture of a medicament for treating a diseases or condition in which IRAP activity is implicated, for enhancing memory and/or learning in a subject. Further disclosed is a method for determining the IRAP (insulin regulated aminopeptidase) inhibitory activity of a compound.