234108-73-7Relevant articles and documents
Selective palladium-catalysed amination of 4-chloropyridines with benzylamines using the Josiphos ligand
Hawkins, Janet L.,Gregson, Clare L.,Hassall, Lorraine A.,Holmes, Jane L.
, p. 6734 - 6737 (2014)
A synthetic strategy for the synthesis of a library of 4-N-benzylamino-2-N-phenyl-pyridines is herein described. The approach involves a Pd-assisted cross-coupling of a 4-chloro-N-phenylpyridin-2-amine intermediate with a range of benzylamines. A variety of ligands were screened, the most successful being the Josiphos ligand, which gave the desired products in good to moderate yields. The reactions occur quickly, within 30 min, with full conversion of the intermediate into the desired product.
HETEROCYCLIC COMPOUNDS AS CBP/EP300 BROMODOMAIN INHIBITORS
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Page/Page column 61-62, (2022/04/03)
The present invention provides heterocyclic compounds of formula (I), which are therapeutically useful as CBP/EP300 inhibitors. These compounds are useful in the treatment and/or prevention of diseases or disorders mediated by CBP and/or EP300 in an individual. The present invention also provides preparation of the compounds and pharmaceutical compositions comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer or a tautomer, an N-oxide or an ester thereof.
Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt
Uhlenbrock, Niklas,Smith, Steven,Weisner, J?rn,Landel, Ina,Lindemann, Marius,Le, Thien Anh,Hardick, Julia,Gontla, Rajesh,Scheinpflug, Rebekka,Czodrowski, Paul,Janning, Petra,Depta, Laura,Quambusch, Lena,Müller, Matthias P.,Engels, Bernd,Rauh, Daniel
, p. 3573 - 3585 (2019/03/28)
The Ser/Thr kinase Akt (Protein Kinase B/PKB) is a master switch in cellular signal transduction pathways. Its downstream signaling influences cell proliferation, cell growth, and apoptosis, rendering Akt a prominent drug target. The unique activation mechanism of Akt involves a change of the relative orientation of its N-terminal pleckstrin homology (PH) and the kinase domain and makes this kinase suitable for highly specific allosteric modulation. Here we present a unique set of crystal structures of covalent-allosteric interdomain inhibitors in complex with full-length Akt and report the structure-based design, synthesis, biological and pharmacological evaluation of a focused library of these innovative inhibitors.
Pd-catalyzed amidation of aryl(Het) halides with tert-butyl carbamate
Qin, Lijin,Cui, Hongmeng,Zou, Dapeng,Li, Jingya,Wu, Yangjie,Zhu, Zhiwu,Wu, Yusheng
experimental part, p. 4445 - 4448 (2010/09/12)
Pd-catalyzed cross-coupling reaction of tert-butyl carbamate with various aryl(Het) halides with Cs2CO3 as base in 1,4-dioxane as solvent was investigated, which resulted in the formation of the desired compounds in moderate to excellent yields.
Rearrangement of N,N-di-tert-butoxycarbonylpyridin-4-amines and formation of polyfunctional pyridines
Liu, Yahua,Ding, Qiang,Wu, Xu
, p. 6025 - 6028 (2008/12/21)
(Chemical Equation Presented) N,N-Di-tert-butoxycarbonylpyridin-4-amines were found to be rearranged to tert-butyl 4-(tert-butoxycarbonylamino) nicotinates by treatment with LDA in THF.
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors
Siu, Tony,Liang, Jun,Arruda, Jeannie,Li, Yiwei,Jones, Raymond E.,Defeo-Jones, Deborah,Barnett, Stanley F.,Robinson, Ronald G.
scheme or table, p. 4186 - 4190 (2009/04/07)
This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the molecule and appending basic amines to enhance the physiochemical properties of the
NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
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Page/Page column 49-50, (2010/11/08)
The invention relates to novel compounds corresponding to the general formula (I) below: and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also
INHIBITORS OF AKT ACTIVITY
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Page/Page column 40, (2008/06/13)
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and method
INHIBITORS OF AKT ACTIVITY
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Page/Page column 42-43, (2010/11/08)
The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 37-38, (2008/06/13)
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and method