- Direct synthesis of 4-arylpiperidines via palladium/copper(I)-cocatalyzed negishi coupling of a 4-piperidylzinc iodide with aromatic halides and triflates
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A general procedure for the synthesis of 4-arylpiperidines via the coupling of 4-(N-BOC-piperidyl)zinc iodide with aryl halides and triflates is presented. The reaction requires cocatalysis with both Cl2Pd(dppf) and a copper(I) species. An impr
- Corley, Edward G.,Conrad, Karen,Murry, Jerry A.,Savarin, Cecile,Holko, Justin,Boice, Genevieve
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- Imidazole derivatives, its pharmaceutical composition and use thereof
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Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
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- THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
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To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].
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- BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES
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The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.
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- QUINOLINE- AND ISOQUINOLINE-BASED COMPOUNDS EXHIBITING ATP-UTILIZING ENZYME INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF
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Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.
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- Oxazolidinone derivatives
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The present invention relates to compounds of the formula: STR1 wherein R is H or alkyl; Y1 is --CH= or --N=; and Y2 --CH=, --C(OH)=, --C(NO2)=, --C(NH2)=, --C(Hal)=, --N=; X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, optionally substituted by phenyl-2-oxo-5 -methoxymethyl-oxazolidinyl; bicyclo[2.2.1]-hept-5 -en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally substituted by amino, alkyl, --CN, oxo hydroxyimino, ethylenedioxy or by --OR1, R1 is --CH(C6 H5)2, --(CH2)n C6 H5, alkyl, H, --(CH2)n NHCOCH3, --(CH2)n NH2, --(CH2)n CN, --(CH2)n SCH3 --(CH2)n SO2 CH3, --CO-lower-alkyl, --COC6 H5, optionally substituted by oxazolidine; or by =CR2 R3, R2 is alkyl R3 is H, --CN, alkyl, phenyl or COO-alkyl; or by --(CH2)n R4 R4 is --CN, amino, --NHCOCH3, --COC6 H5 Hal, phenyl or hydroxy; or by --COR5, R5 is alkyl, --CH=CH--C6 H5, --C6 H5, --C6 H5 CF3 or --O-alkyl; or by --NR6 R7, R6 is or --COCH3 ; R7 is --COCH3, benzyl or --(CH2)n NHCOC6 H4 Hal; and n is 1-3; These can be used for the prevention or control of depressive, panic and anxiety states, and treatment of certain cognitive disorders and neurodegenerative diseases.
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