- Synthesis of Functionalized Aliphatic Acid Esters via the Generation of Alkyl Radicals from Silylperoxyacetals
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We describe a catalytic method for the synthesis of a variety of functionalized aliphatic acid esters using silylperoxyacetals, which are versatile alkyl radical precursors with a terminal ester moiety. In the presence of an appropriate transition-metal catalyst, the in situ generation of alkyl radicals and the subsequent bond-forming process proceeds smoothly to afford synthetically valuable aliphatic acid derivatives. The present method can be applied to the efficient synthesis of a pharmaceutically important 1,1-diarylalkane motif. In addition, a novel strategy for the synthesis of structurally diverse hydroxy acid derivatives via a C?O bond formation process that utilizes TEMPO has been developed.
- Matsumoto, Akira,Shiozaki, Yoko,Sakurai, Shunya,Maruoka, Keiji
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supporting information
p. 2431 - 2434
(2021/08/07)
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- SUBSTITUTED AMINOPURINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
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Paragraph 0385
(2016/05/02)
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- CHEMOKING RECEPTOR ANTAGONISTS
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Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 153
(2013/03/26)
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- PHENYL-HETEROARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds
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Page/Page column 84
(2012/06/01)
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- 3-(AMINOARYL)-PYRIDINE COMPOUNDS
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
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Page/Page column 91-92
(2012/06/01)
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- N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 129
(2012/08/08)
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- PYRIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 98
(2012/08/08)
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- N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
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Page/Page column 170
(2012/08/08)
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- PYRIMIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a pyrimidine compound of formula (I): wherein one of X and Y but not both is N, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tantomers, diastereomers, deuterated versions, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds
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Page/Page column 87-88
(2012/08/08)
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- HETEROARYL COMPOUNDS AS KINASE INHIBITORS
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The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor
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Page/Page column 66
(2011/04/14)
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- PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
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Page/Page column 65
(2011/04/14)
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- Mild acetalisation of mono and dicarbonyl compounds catalysed by titanium tetrachloride. Facile synthesis of β-keto enol ethers
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The use of TiCl4, as a catalyst for the acetalisation, at room temperature, of carbonyl compounds is reported. Cyclic ketones and cyclic 1,4-diketones easily afford dimethyl acetals, but cyclic 1,3-diketones give β-keto enol ethers. Additionally, aryl ketones and acyclic ketones failed to react. β-keto aldehydes can be monoprotected either as β-keto enol ethers or β-keto dimethyl acetals depending on the reaction time and catalyst amount. Some mechanistic features are accounted for.
- Clerici, Angelo,Pastori, Nadia,Porta, Ombretta
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p. 217 - 225
(2007/10/03)
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- Inhibitors of leukotriene B4. Synthesis and SAR of new β-enaminoester open-chain analogues of Zeneca ZD2138
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A series of methoxy tetrahydropyranyl β-enaminoester has been discovered as inhibitors of LTB4 production. These are unusual open chain analogues of Zeneca ZD2138, the highly potent orally active 5-LO inhibitor under development for the treatment of asthma and rheumatoid arthritis. In vitro, compound 1a inhibited LTB4 formation in human whole blood with an IC50 of 0.04 μM. In inflamed exudate in the rat 1a inhibited formation of LTB4 with an oral ED50 3h after dosing of 3.0 mg/kg.
- Bird,Olivier
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p. 515 - 520
(2007/10/03)
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- Ester derivatives and pharmaceutical compositions containing them
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The invention concerns ester derivatives of the formula I wherein Ar is phenyl, naphthyl, indenyl, indanyl, a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from
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