US 7,589,068 B2
Inhibitors of Akt activity
Nicholas D. P. Cosford, San Diego, Calif. (US); Mark E. Layton, Harleysville, Pa. (US); Jun Liang, Palo Alto, N.J. (US); Craig W. Lindsley, Schwenksville, Pa. (US); Philip E. Sanderson, Valley Forge, Pa. (US); and Zhijian Zhao, Wilmington, Del. (US)
Assigned to Merck & Co., Inc., Rahway, N.J. (US)
Appl. No. 11/795,156
PCT Filed Feb. 10, 2006, PCT No. PCT/US2006/004715
§ 371(c)(1), (2), (4) Date Jul. 12, 2007,
PCT Pub. No. WO2006/091395, PCT Pub. Date Aug. 31, 2006.
Claims priority of provisional application 60/652737, filed on Feb. 14, 2005.
Prior Publication US 2008/0009507 A1, Jan. 10, 2008
Int. Cl. A01N 43/04 (2006.01); A01N 43/58 (2006.01); A01N 43/42 (2006.01); A61K 31/70 (2006.01); A61K 31/50 (2006.01); A61K 31/495 (2006.01); A61K 31/52 (2006.01); A61K 31/47 (2006.01); C07D 487/00 (2006.01); C07D 491/00 (2006.01); C07H 15/00 (2006.01); C07H 17/00 (2006.01); C07H 17/02 (2006.01); C09B 25/00 (2006.01)
U.S. Cl. 514—43  [514/249; 514/263.22; 514/314; 536/17.4; 536/29.2; 544/277; 544/350; 546/173] 5 Claims
 
1. A compound of the Formula E:

OG Complex Work Unit Drawing
wherein:
a is 0 or 1; b is 0 or 1; n is 0, 1 or 2: p is 0, 1 or 2;
Ring K is selected from:

OG Complex Work Unit Drawing
Q is selected from: 2-azepinone, benzimidazolyl, benzimidazolonyl, 2-diazapinone, imidazolyl, 2-imidazolidinone, indolyl, isoquinolinyl, morpholinyl, piperidyl, piperazinyl, pyridyl, pyrrolidinyl, 2-piperidinone, 2-pyrimidinone, 2-pyrollidinone, quinolinyl, tetrazolyl, tetrahydrofuryl, tetrahydroisoquinolinyl, and thienyl, optionally substituted with one to three substituents selected from R6b;
R1 is selected from: oxo, (C═O)aOb(C1-C10)alkyl, CO2H, halo, OH, CN, (C1-C6)alkoxy, O(C═O)(C1-C6)alkyl and N(Rb)2;
R2 is selected from: oxo, (C═O)aOb(C1-C10)alkyl, CO2H, halo, OH, CN, (C1-C6)alkoxy, O(C═O)(C1-C6)alkyl,(C2-C10)alkenyl and N(Rb)2, said alkenyl optionally substituted with oxo;
R6b is selected from:

OG Complex Work Unit Drawing
optionally substituted with 1 to 3 substituents selected from oxo, OH, N(Rb)2, halogen and Oa(C1-C6)alkyl; and
Rb is independently selected from H and (C1-C6)alkyl;
or a pharmaceutically acceptable salt or a stereoisomer thereof.