DR. PHILLIP DENNIS, M.D., PH.D.
Osteopathic Medicine in Baltimore, MD

7378403, May 27, 2008

Sep 3, 2003

10/526851

Alan P. Kozikowski - Chicago IL, US
Phillip Dennis - Ellicott City MD, US
Haiying Sun - Ann Arbor MI, US
John Brognard - Carlsbad CA, US

The United States of America as represented by the Department of Health and Human Services - Washington DC
Georgetown University - Washington DC

A61K 31/662, A61K 31/683, C07F 9/09, C07F 9/30

514129, 558186

Disclosed are inhibitors of the serine/threonine kinase Akt, pharmaceutical compositions comprising such inhibitors, and a method of preventing or treating a disease or condition in an animal by the use of such inhibitors. The Akt inhibitors have the formula (I) wherein X and Y are independently selected from the group consisting of O, CF, CH, and CHF; wherein A is independently selected from the group consisting of P(O)OH, CH000H, and CH(COOH); Ris selected from the group consisting of H, OH, isosteres of OH, C-Calkyloxy, C-Caryloxy, C-Ccycloalkyloxy, C-Ccycloalkyl C-Calkoxy, C-Calkenyloxy, C-Ccycloalkenyloxy, C-Caralkyloxy, C-Calkylaryloxy, C-Caralkenyloxy, and C-Calkenylaryloxy; R-Rare independently selected from the group consisting of H, OH, isosteres of OH; and Rand Rare independently selected from the group consisting of C-Calkyl, C-Caryl, C-Ccycloalkyl, C-Calkenyl, C-Ccycloalkenyl, C-Caralkyl, C-Calkylaryl, C-Caralkenyl, and C-Calkenylaryl; with the provisos that (i) when X is O, Y is O or CH, and Ris H, at least one of Rand R-Ris not OH; (ii) when A is CHCOOH or CH(COOH), X and Y cannot be simultaneously O; and (iii) all of R-Rare not simultaneously H. The inhibitors can be in the form of a salt also.