Akt Inhibitors, Pharmaceutical Compositions, And Uses Thereof

Abstract

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>-C<SUB>32 </SUB>alkylaryl, C<SUB>9</SUB>-C<SUB>32 </SUB>aralkenyl, and C<SUB>9</SUB>-C<SUB>32 </SUB>alkenylaryl; with the provisos that (i) when X is O, Y is O or CH<SUB>2</SUB>, and R<SUB>3 </SUB>is H, at least one of R<SUB>2 </SUB>and R<SUB>4</SUB>-R<SUB>6 </SUB>is not OH; (ii) when A is CH<SUB>2</SUB>COOH or CH(COOH)<SUB>2</SUB>, X and Y cannot be simultaneously O; and (iii) all of R<SUB>2</SUB>-R<SUB>6 </SUB>are not simultaneously H. The inhibitors can be in the form of a salt also


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Document History
  • Publication: May 27, 2008
  • Application: May 19, 2005
    US US 52685105 A
  • Priority: May 19, 2005
    US US 52685105 A
  • Priority: Sep 3, 2003
    US US 0327607 W
  • Priority: Sep 3, 2002
    US US 40723902 P

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