GEORGETOWN UNIVERSITY;THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, THE DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人:
申请号：
EP03751981.6
公开号：
EP1537129B1
申请日:
2003.09.03
申请国别(地区):
EP
年份:
2013
代理人:
摘要：
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<；SUB>；2<；/SUB>；, CH<；SUB>；2<；/SUB>；, and CHF； wherein A is independently selected from the group consisting of P(O)OH, CH<；SUB>；2<；/SUB>；000H, and CH(COOH)<；SUB>；2<；/SUB>；； R<；SUB>；2 <；/SUB>；is selected from the group consisting of H, OH, isosteres of OH, C<；SUB>；1<；/SUB>；-C<；SUB>；25 <；/SUB>；alkyloxy, C<；SUB>；6<；/SUB>；-C<；SUB>；10 <；/SUB>；aryloxy, C<；SUB>；3<；/SUB>；-C<；SUB>；8 <；/SUB>；cycloalkyloxy, C<；SUB>；3<；/SUB>；-C<；SUB>；8 <；/SUB>；cycloalkyl C<；SUB>；1<；/SUB>；-C<；SUB>；6 <；/SUB>；alkoxy, C<；SUB>；2<；/SUB>；-C<；SUB>；22 <；/SUB>；alkenyloxy, C<；SUB>；3<；/SUB>；-C<；SUB>；8 <；/SUB>；cycloalkenyloxy, C<；SUB>；7<；/SUB>；-C<；SUB>；32 <；/SUB>；aralkyloxy, C<；SUB>；7<；/SUB>；-C<；SUB>；32 <；/SUB>；alkylaryloxy, C<；SUB>；9<；/SUB>；-C<；SUB>；32 <；/SUB>；aralkenyloxy, and C<；SUB>；9<；/SUB>；-C<；SUB>；32 <；/SUB>；alkenylaryloxy； R<；SUB>；3<；/SUB>；-R<；SUB>；6 <；/SUB>；are independently selected from the group consisting of H, OH, isosteres of OH； and R<；SUB>；1 <；/SUB>；and R<；SUB>；7 <；/SUB>；are independently selected from the group consisting of C<；SUB>；1<；/SUB>；-C<；SUB>；25 <；/SUB>；alkyl, C<；SUB>；6<；/SUB>；-C<；SUB>；10 <；/SUB>；aryl, C<；SUB>；3<；/SUB>；-C<；SUB>；8 <；/SUB>；cycloalkyl, C<；SUB>；2<；/SUB>；-C<；SUB>；22 <；/SUB>；alkenyl, C<；SUB>；3<；/SUB>；-C<；SUB>；8 <；/SUB>；cycloalkenyl, C<；SUB>；7<；/SUB>；-C<；SUB>；32 <；/SUB>；aralkyl, C<；SUB>；7<；/SUB
