GEORGETOWN UNIVERSITY;THE GOVERNMENT OF THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRET ARY DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人:
KOZIKOWSKI, ALAN P.,DENNIS, PHILLIP,SUN, HAIYING,BROGNARD, JOHN
申请号：
CA2497572
公开号：
CA2497572C
申请日:
2003.09.03
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
Disclosed are inhibitors of the serine/threonine kinase Akt, pharmaceuticalcompositions comprising such inhibitors, and a method of preventing ortreating 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 independentlyselected from the group consisting of O, CF2, CH2, and CHF； wherein A isindependently selected from the group consisting of P(O)OH, CH2000H, andCH(COOH)2； R2 is selected from the group consisting of H, OH, isosteres of OH,C1-C25 alkyloxy, C6-Cl0 aryloxy, C3-C8 cycloalkyloxy, C3-C8 cycloalkyl C1-C6alkoxy, C2-C22 alkenyloxy, C3-C8 cycloalkenyloxy, C7-C32 aralkyloxy, C7-C32alkylaryloxy, C9-C32 aralkenyloxy, and C9-C32 alkenylaryloxy； R3-R6 areindependently selected from the group consisting of H, OH, isosteres of OH；and Rl and R7 are independently selected from the group consisting of C1-C25alkyl, C6-C10 aryl, C3-C8 cycloalkyl, C2-C22 alkenyl, C3-C8 cycloalkenyl, C7-C32 aralkyl, C7-C32 alkylaryl, C9-C32 aralkenyl, and C9-C32 alkenylaryl； withthe provisos that (i) when X is O, Y is O or CH2, and R3 is H, at least one ofR2 and R4-~R6 is not OH； (ii) when A is CH2C00H or CH(COOH)2, X and Y cannotbe simultaneously O； and (iii) all of R2-R6 are not simultaneously H. Theinhibitors can be in the form of a salt also.
