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US 2010/0144730 A1Published application
Pyridinonyl pdk1 inhibitors
AssigneesSunesis Phamaceuticals, Biogen Idec Inc.
InventorsKenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
Life of this patent
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Abstract
The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
Claims32
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- X is absent, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene,
- wherein if X is substituted or unsubstituted phenylene and L1 is absent, then R1 is not substituted or unsubstituted pyridinyl, substituted or unsubstituted benzo-oxazolyl, substituted or unsubstituted phenyl, or substituted or unsubstituted quinazolinyl, and
- wherein if X is substituted or unsubstituted phenylene, then R1 is not substituted or unsubstituted cyclohexyl;
- R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
- wherein if R1 is substituted or unsubstituted phenyl and X absent, then L1 is not absent, and
- wherein if R1 is substituted or unsubstituted phenyl, then X is not substituted or unsubstituted pyridinonyl, or substituted or unsubstituted imidazolyl;
- R2, R4, R5, R6, R7, and R8 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- and
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
15 more elements
2-3. (canceled)
(canceled)
7-8. (canceled)
10-14. (canceled)
16-17. (canceled)
The compound of claim 17, wherein L2 is unsubstituted C1-C5 alkylene.
19-22. (canceled)
The compound of claim 22, wherein L1 is unsubstituted C1-C5 alkylene.
(canceled)
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
- R2, R4, R5, and R6 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- and
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
- Z1, Z2, and Z3 are independently —N═, —NH—, —O—, —S—, or —CH═;
- and
- R23 is hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
13 more elements
(canceled)
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- t is an integer from 1 to 4;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- X is absent, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene;
- R2, R4, R5, and R6 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- and
- R22 is hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
12 more elements
(canceled)
32-33. (canceled)
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- v is an integer from 1 to 3;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- X is absent, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene;
- R2, R4, R5, and R6 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- Z4 is —N(R28)—, —C(R29)(R30)—, or
- and
- R26, R27, R28, R29, R30, R31, and R32 are independently selected from hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
13 more elements
35-37. (canceled)
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- X is absent, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene;
- R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
- R2, R4, R5, and R6 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- and
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- Z5 and Z6 are independently ═N— and ═C(R23)—;
- and
- R23 and R33 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
14 more elements
A compound having the formula:
- wherein
- n is an integer from 1 to 5;
- w is 0 or 1;
- L1 and L2 are independently absent, —O—, —NH—, —S—, —S(O)—, S(O)2—, substituted or unsubstituted alkylene, or substituted or unsubstituted heteroalkylene;
- X is absent, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene,
- R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
- R2 is halogen;
- R4, R5, and R6 are independently hydrogen, halogen, —OH, —CF3, —NO2, —OR10, —S(O)nR11, —C(O)R12, —NR13R14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 is hydrogen, —OH, —CF3, —OR10, —S(O)nR11, —C(O)R12, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R3 is optionally attached to X thereby forming a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R10 is independently —C(O)R15, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R11 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if n is 2, then R11 is optionally —NR17R18, and wherein if n is 1 or 2, then R11 is not hydrogen;
- R12 and R15 are independently hydrogen, —NR19R20, —OR21, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R13 is independently hydrogen, —C(O)R15, —S(O)2R16, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R14, R17, R18, R19, R20 and R21 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- and
- R16 is independently hydrogen, —NR19R20, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
13 more elements
A method of decreasing PDK1 catalytic activity, said method comprising contacting a PDK1 with an effective amount of a pyridinonyl PDK1 inhibitor, a benzyl-pyridinonyl PDK1 inhibitor, or a benzyl-pyridinonylamide PDK1 inhibitor.
(canceled)
A method of treating cancer in a subject in need thereof, said method comprising administering to said subject a therapeutically effective amount of a pyridinonyl PDK1 inhibitor, a benzyl-pyridinonyl PDK1 inhibitor, or a benzyl-pyridinonylamide PDK1 inhibitor.
(canceled)
A method of selectively reducing PDK1 mediated phosphorylation of Akt relative to PDK1 mediated phosphorylation of PKC in a cell, the method comprising the step of contacting said cell with an effective amount of a pyridinonyl PDK1 inhibitor, a benzyl-pyridinonyl PDK1 inhibitor, or a benzyl-pyridinonylamide PDK1 inhibitor.
45-46. (canceled)
Dependencies are inferred from the claim text.