29681-78-5Relevant academic research and scientific papers
HETEROARYL COMPOUNDS
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Paragraph 00266, (2021/05/29)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
ACC INHIBITORS AND USES THEREOF
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Paragraph 0743, (2017/05/17)
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores
Trstenjak, Uro?,Ila?, Janez,Kikelj, Danijel
supporting information, p. 302 - 313 (2013/07/27)
Dual antithrombotic agents acting as anticoagulants and aggregation inhibitors could have substantial advantages over currently prescribed combinations of antithrombotic drugs. Herein, we report compounds with moderate inhibitory activity for factor Xa an
Skeletal diversity via a folding pathway: Synthesis of indole alkaloid-like skeletons
Oguri, Hiroki,Schreiber, Stuart L.
, p. 47 - 50 (2007/10/03)
(Chemical Equation Presented) Inspired by the skeletal diversity of naturally occurring indole alkaloids and the rich potential of chemistry developed by Padwa and coworkers, we conceived a pathway entailing six modes of intramolecular reactions leading t
Theoretical Insights Regarding the Cycloaddition Behavior of Push-Pull Stabilized Carbonyl Ylides
Weingarten, M. David,Prein, Michael,Price, Alan T.,Snyder, James P.,Padwa, Albert
, p. 2001 - 2010 (2007/10/03)
A series of diazoamido keto esters were prepared by the reaction of N-substituted 3-carbethoxy-2-piperidone with n-butylmagnesium chloride followed by the addition of ethyl 2-diazomalonyl chloride. Treatment of these diazo amides with rhodium(II) acetate afforded transient push-pull carbonyl ylide dipoles which could be readily trapped with electron deficient dipolarophiles. All attempts to induce the dipolar cycloaddition to occur across tethered alkenyl π-bonds failed to give internal cycloadducts. However, placing a sp2 center on the tethered side chain was found to result in the formation of a tricyclic adduct in 95% yield. The stereochemistry of the cycloadduct was firmly established by an X-ray crystallographic study and occurred endo with respect to the amido carbonyl ylide dipole. A detailed computational study was undertaken to provide better insight into the factors that influence the intramolecular cycloaddition process. The calculations indicate that a severe cross-ring 1,3-diaxial interaction caused by the bridgehead methyl group promotes a boat or twist-boat conformation in the piperidine ring fused to the newly forming one. The presence of a carbonyl group in the dipolarophile tether helps to relieve the steric congestion by virtue of favoring a second boat in the latter ring. Without the C=O group, both nascent and piperidine rings are in the chair conformation at lowest energy, and the reaction barrier is disadvantaged by 5.6 kcal/mol, allowing other competing processes to intervene.
Synthesis of new deazatetrahydropterins as potential NO synthase modulators
Nallet, Jean-Pierre,Megard, Anne-Lise,Dreux, Jacques
, p. 491 - 500 (2007/10/03)
As part of our research on NO synthase modulators, a series of deazatetrahydropterins were synthesized and their effects were assessed. In this paper, we describe the synthesis of new substituted (especially at the 4a position) 2-amino-4-hydroxy-3,4,4a,5,6,7-hexahydropyrido[2,3-d]pyrimidines. These compounds showed no interesting pharmacological activity. Elsevier.
THE USE OF ω-IODOAZIDES AS PRIMARY PROTECTED ELECTROPHILIC REAGENTS. ALKYLATION OF SOME CARBANIONS DERIVED FROM ACTIVE METHYLENE COMPOUNDS AND N,N-DIMETHYLHYDRAZONES.
Khoukhi, Mostafa,Vaultier, Michel,Carrie, Robert
, p. 1031 - 1034 (2007/10/02)
Some carbanions derived from active methylene compounds and N,N-dimethylhydrazones were alkylated in good yields with the ω-iodoazides 3, 4 and 13 used as primary amino protected electrophilic reagents.
