Patent Number: 7,612,091

Title: Caspase inhibitors and uses thereof

Abstract: The present invention provides a compound of formula I: ##STR00001## wherein: X is --OR.sup.1 or --N(R.sup.5).sub.2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R.sup.1 is: C.sub.1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF.sub.3, Cl, F, OMe, OEt, OCF.sub.3, CN, or NMe.sub.2; C.sub.1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with --O-- or --NR.sup.5--; R.sup.2 is C.sub.1-6 straight chained or branched alkyl; R.sup.3 is hydrogen, halo, OCF.sub.3, CN, or CF.sub.3; R.sup.4 is hydrogen, halo, OCF.sub.3, CN, or CF.sub.3; and each R.sup.5 is independently H, C.sub.1-6 straight chained or branched alkyl, aryl, --O--C.sub.1-6 straight chained or branched alkyl, or --O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.

Inventors: Charrier; Jean-Damien (Grove, Wantage, GB), Mortimore; Michael (Burford, Oxfordshire, GB), Studley; John R. (Abingdon, Oxfordshire, GB)

Assignee: Vertex Pharmaceuticals Incorporated

International Classification: C07D 215/22 (20060101); A61K 31/47 (20060101)

Expiration Date: 1/03/02017