- CHEMICAL COMPOUNDS
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The invention is directed to 6-(4-pyι?midinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 137
(2010/07/10)
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- FUSED BENZENE DERIVATIVE AND USE
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The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3' (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5' (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.
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Page/Page column 79
(2010/02/12)
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- A simple stereoselective synthesis of enantiopure 2-substituted pyrrolidines and piperidines from chiral (R)-phenylglycinol-derived bicyclic 1,3-oxazolidines
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Chiral, nonracemic 2-substituted pyrrolidines and piperidines were prepared in high ee and moderate to good chemical yields in three steps from (R)-phenylglycinol and γ- or δ-chloroketones. The key step of the synthesis was the stereo- selective reductive ring-opening of chiral bicyclic 1,3- oxazolidines prepared by condensation of (R)-phenylglycinol and the corresponding ketones.
- Andres, Jose M.,Herraiz-Sierra, Ignacio,Pedrosa, Rafael,Perez-Encabo, Alfonso
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p. 1719 - 1726
(2007/10/03)
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- Synthesis of pyrrolizidine bases by highly diastereoselective and regioselective catalytic carbon-hydrogen insertion reactions of chiral pyrrolidinediazoacetamides
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Pyrrolizidines, (1S,8S)-1-hydroxypyrrolizidin-3-one and (-)-heliotridane, have been prepared in high yield from diazoacetamides of 2-substituted-pyrrolidines by carbon-hydrogen insertion catalyzed by dirhodium(II) tetrakis[methyl 1-acylimidazolidin-2-one-4(S)-carboxylates].
- Doyle, Michael P.,Kalinin, Alexey V.
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p. 1371 - 1374
(2007/10/03)
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- Direct Asymmetric Synthesis of Quaternary Carbon Centers via Addition-Elimination Process: Nitroolefination of α-Substituted δ-Lactones
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The reactions of chiral nitro enamines 2a-c with zinc enolates 4-6 of α-substituted δ-lactones afforded α,α-disubstituted δ-lactones with a high ee through an addition-elimination process.The best results were obtained with the reaction of 2c with 5.Michael-type addition of the enolate onto the nitro enamine is kinetically controlled and decides the absolute stereochemistry of the product.A cyclic transition model is proposed to rationalize the S-selectivity.
- Fuji, Kaoru,Node, Manabu,Nagasawa, Hideko,Naniwa, Yoshimitsu,Taga, Tooru,et al.
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p. 7921 - 7925
(2007/10/02)
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