heterocyclic compounds useful as inhibitors of PDK1
2010
A compound of formulas II, III, IV, or V: ** ** Formula or a pharmaceutically acceptable salt thereof, wherein: 5 is a single or double bond; R1 is hydrogen or C1-6 aliphatic optionally substituted: -L2-A1-L1- is -OCH2CH2-, -CH> = CHCH 2, or -C≡C-CH2-; or -L2-A1-L1 is -O-C2, C3 alkenylene, or alkynylene C3, optionally substituted; or -L2-A1-L1 is one of the following: ** ** Formula wherein ring B is a 5-membered heteroaryl ring having 1-3 heteroatoms selected from nitrogen, oxygen, and sulfur, and ring C is a 6-membered heteroaryl ring having 1-3 nitrogens that; or -L2-A1-L1 is one of the following: ** ** Formula wherein ring B is a 5-membered heteroaryl ring having 1-3 heteroatoms selected from nitrogen, oxygen, and sulfur, and ring C is a 6-membered heteroaryl ring having 1-3 nitrogens that; or -L2-A1-L1 is one of the following: ** ** Formula ring A 2 is a monocyclic carbocyclic ring of 3-7 membered, saturated or unsaturated PAR15 tially, a carbocyclic ring bicyclic 7-10 membered saturated or partially unsaturated, monocyclic heterocyclic ring of 4- 7 members saturated or partially unsaturated, having 1-2 independently nitrogen, oxygen or sulfur, a bicyclic heterocyclic ring 7-10 membered saturated or partially unsaturated heteroatoms selected having 1 -3 heteroatoms independently selected from nitrogen, oxygen or sulfur, a phenyl ring, a bicyclic ring 8-10 membered aryl, a heteroaryl ring 5-6 membered monocyclic having 1-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, a bicyclic heteroaryl ring having 1-4 8-10 membered heteroatoms independently selected from nitrogen, oxygen or sulfur, or a tricyclic ring 10-16 membered saturated, partially unsaturated or aromatic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen or sulfur, wherein the ring A2 is optionally substituted with 1-4 groups Rx; each Rx is independently -R, alkylidenyl optionally substituted oxo, halo, -NO2, -CN, -OR, -SR, - N (R ') 2, -C (O) R, -CO2R, -C (O ) C (O) R, -C (O) CH2C (O) R, -S (O) R, -S (O) 2R, -C (O) N (R ') 2, -S (O) 2N (R ') 2, -OC (O) R, - N (R') C (O) R, -N (R ') N (R') 2, -N (R ') OR, -N (R ') C (> = NR') N (R ') 2, -C (> = NR') N (R ') 2, -C> = NOR, -N (R') C (O) N (R ') 2, - N (R') S (O) 2N (R ') 2, -N (R') S (O) 2R, or -OC (O) N (R ') 2; each R is independently hydrogen or an optionally substituted group selected from C1-6 aliphatic a, a monocyclic carbocyclic 3-7 membered ring, saturated or partially unsaturated carbocyclic ring bicyclic 7-10 membered saturated or partially unsaturated, ring monocyclic heterocyclic 4-7 membered saturated or partially unsaturated ring having 1-2 heteroatoms independently selected from nitrogen, oxygen or sulfur, a bicyclic heterocyclic ring 7-10 membered saturated or partially unsaturated selected having 1- 3 heteroatoms selected independently nitrogen, oxygen or sulfur, a phenyl ring, a bicyclic ring 8-10 membered aryl, a heteroaryl 5-6 membered ring having 1-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, or a bicyclic heteroaryl ring 8-10 membered having 1-4 heteroatoms independently selected from nitrogen, oxygen or sulfur; each R 'is independently -R, or two R' groups on the same nitrogen are taken together with their intervening atoms to form a 5-8 membered saturated, partially unsaturated or aromatic, optionally substituted, having 1 to 4 heteroatoms independently selected from nitrogen, oxygen or sulfur; L3 is a covalent bond or optionally substituted methylene; the ring A3 is an optionally substituted pyridinyl optionally substituted or phenyl ring; each of R3, R4, and R5 is independently -R, -halo, -NO2, -CN, -OR, -SR, -N (R ') 2, -C (O) R, -CO2R, - C ( O) C (O) R, -C (O) CH2C (O) R, -S (O) R, -S (O) 2R, -C (O) N (R ') 2, -S (O) 2N (R ') 2, -OC (O) R, -N (R') C (O) R, -N (R ') N (R') 2, - N (R ') OR, -N ( R ') C (> = NR') N (R ') 2, -C (> = NR') N (R ') 2, -C> = NOR, -N (R') C (O) N ( R ') 2, -N (R') S (O) 2N (R ') 2, -N (R') S (O) 2R, or - OC (O) N (R ') 2; or R3 and R4 or R4 and R5 taken together with their intervening atoms to form a fused, optionally substituted, selected from a carbocyclic ring of 4-7 membered partially unsaturated, phenyl, a 5-6 membered heterocyclic ring, partially unsaturated heterocycle having 1-3 heteroatoms independently selected from nitrogen, oxygen or sulfur, or 5-6 membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen or sulfur. each R6 is independently -R, -C (O) R, -CO2R, -C (O) C (O) R, -C (O) CH2C (O) R, -S (O) R, -S (O ) 2R, - C (O) N (R ') 2, or -S (O) 2N (R') 2; or: R3 and R6 are taken together with their intervening atoms to form an optionally substituted fused ring selected from a 5-6 membered heterocyclic ring, saturated or partially unsaturated, having 1-3 40 heteroatoms independently selected from nitrogen, oxygen or sulfur, or 5-6 membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen or sulfur;
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