Akt inhibitors, pharmaceutical compositions, and uses thereof

Details Akt inhibitors, pharmaceutical compositions, and uses thereof Akt inhibitors, pharmaceutical compositions, and uses thereof

2003-09-03

2008-05-27

Saeed, Kamal A. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

C558S186000

Reexamination Certificate

active

07378403

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, CF2, CH2, and CHF; wherein A is independently selected from the group consisting of P(O)OH, CH2000H, and CH(COOH)2; R2is selected from the group consisting of H, OH, isosteres of OH, C1-C25alkyloxy, C6-C10aryloxy, C3-C8cycloalkyloxy, C3-C8cycloalkyl C1-C6alkoxy, C2-C22alkenyloxy, C3-C8cycloalkenyloxy, C7-C32aralkyloxy, C7-C32alkylaryloxy, C9-C32aralkenyloxy, and C9-C32alkenylaryloxy; R3-R6are independently selected from the group consisting of H, OH, isosteres of OH; and R1and R7are independently selected from the group consisting of C1-C25alkyl, C6-C10aryl, C3-C8cycloalkyl, C2-C22alkenyl, C3-C8cycloalkenyl, C7-C32aralkyl, C7-C32alkylaryl, C9-C32aralkenyl, and C9-C32alkenylaryl; with the provisos that (i) when X is O, Y is O or CH2, and R3is H, at least one of R2and R4-R6is not OH; (ii) when A is CH2COOH or CH(COOH)2, X and Y cannot be simultaneously O; and (iii) all of R2-R6are not simultaneously H. The inhibitors can be in the form of a salt also

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