393860-82-7Relevant academic research and scientific papers
NOVEL 4-(ARYL)-N-(3-ALKOXYFURO[2,3-B]PYRAZIN-2-YL)-PIPERAZINE-1-CARBOXAMIDE DERIVATIVE AND ANTIPROLIFERATIVE EFFECT THEREOF
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Paragraph 0052, (2019/04/29)
The present invention relates to a novel 4-(aryl)-N-(3-alkoxyfuro[3,2-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative compound useful in the prevention or treatment of cancer; a preparation method thereof; and a pharmaceutical composition comprising t
NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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Page/Page column 77, (2014/09/29)
The present invention relates to compounds of the formula (I), the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
AKT / PKB INHIBITORS
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Page/Page column 197, (2011/06/11)
The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
Intramolecular Diels-Alder synthesis of 7-aza-α-carboline compounds
Wallace, Michael B.,Scorah, Nicholas,Vu, Phong H.,Brown, Jason W.,Stafford, Jeffrey A.,Dong, Qing
supporting information; experimental part, p. 1739 - 1741 (2010/05/18)
An efficient, versatile, and scalable route for the synthesis of 7-aza-α-carboline compounds is described. The tricyclic system has been prepared from modified pyrazinones using a key intramolecular [4+2] Diels-Alder transformation.
Diversity-oriented synthesis of substituted furo[2,3-b]pyrazines
Mehta, Vaibhav P.,Modha, Sachin G.,Ermolat'Ev, Denis,Van Hecke, Kristof,Van Meervelt, Luc,Van Der Eycken, Erik V.
experimental part, p. 27 - 41 (2009/07/25)
A highly efficient method for the synthesis of diversely substituted furo[2,3-b]pyrazines has been elaborated. The Ag+- or iodine-mediated electrophilic cyclization of readily generated 5-chloro-3-substituted ethynyl-1-(4-methoxybenzyl)-pyrazin-2(1H)-ones affords substituted furo[2,3-b]pyrazines, which undergo various palladium catalyzed reactions to generate a library of difficult to attain diversely substituted furo[2,3-b]pyrazines. CSIRO 2009.
KINASE INHIBITORS
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Page/Page column 270-271, (2009/12/02)
Compounds are provided for use with kinases that comprise a compound selected from the rou consistin of:wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods an intermediates useful for making the compounds; and methods of using said compounds.
Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives
Francois, Isabelle E.J.A.,Cammue, Bruno P.A.,Bresseleers, Sara,Fleuren, Hein,Hoornaert, Georges,Mehta, Vaibhav P.,Modha, Sachin G.,Van der Eycken, Erik V.,Thevissen, Karin
supporting information; experimental part, p. 4064 - 4066 (2010/03/25)
We synthesized a family of 3,5-dichloropyrazin-2(1H)-one derivatives and assessed their in vitro fungicidal activity against Candida albicans. Compounds 11 and 20 were most active against C. albicans and induced accumulation of reactive oxygen species in
KINASE INHIBITORS
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Page/Page column 147, (2010/11/27)
Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein.
Synthesis of sidechain adapted β-turn mimics for modifying the C-terminus of substance P
Pawar, Vijaykumar G.,De Borggraeve, Wim M.,Maes, Veronique,Tourwé, Dirk A.,Compernolle, Frans,Hoornaert, Georges J.
, p. 1707 - 1710 (2007/10/03)
Sidechain adapted β-turn mimics of type 1 characterised by a fixed cis-conformation of the peptide chain in the aminopiperidinonecarboxylate scaffold have been synthesised from pyrazinones in order to perform a β-turn scan of the messenger region of substance P. The synthesis of a substance P peptide analogue is also described.
Structure based design of simplified analogues of insect kinins
Kamoune, Laila,De Borggraeve, Wim M.,Verbist, Bie M. P.,Broeck, Jozef Vanden,Coast, Geoffrey M.,Compernolle, Frans,Hoornaert, Georges
, p. 9555 - 9562 (2007/10/03)
Based on a receptor interaction model, simplified analogues of insect kinins were prepared. The compounds were templated on a conformationally restricted amino piperidinone carboxylate scaffold. The conformation of the analogues was studied by NMR and the
