173253-42-4Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
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Paragraph 0195, (2020/10/31)
Aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in onco
IMIDAZO[1,2-A]PYRAZINE MODULATORS OF THE ADENOSINE A2A RECEPTOR
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Page/Page column 78; 79, (2019/01/17)
The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers, isotopologues,or N-oxides thereof. The present invention is further concerned with the use of such a compound or salt, stereoisomer, tautomer, isotopologues,or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.
NOVEL 4-(ARYL)-N-(2-ALKOXYTHIENO[3,2-B]PYRAZIN-3-YL)-PIPERAZINE-1-CARBOXAMIDE DERIVATIVE, AND ANTIPROLIFERATIVE EFFECT THEREOF
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Paragraph 0050, (2017/11/04)
The present invention relates to a novel 4-(aryl)-N-(2-alkoxythieno[3,2-b]pyrazin-3-yl)-piperazin-1-carboxamide derivative compound useful in the prevention or treatment of cancer; a preparation method thereof; and a pharmaceutical composition comprising the same. The novel 4-(aryl)-N-(2-alkoxythieno[3,2-b]pyrazin-3-yl)-piperazin-1-carboxamide derivative compound of the present invention can effectively inhibit the growth of proliferating cells, and thus can be useful in the prevention or treatment of cancer.
5-(PYRIDIN-2-YL-AMINO)-PYRAZINE-2-CARBONITRILE COMPOUNDS AND THEIR THERAPEUTIC USE
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Page/Page column 67, 68, (2013/05/23)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) aDNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionisin g radiation.
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing
Reader, John C.,Matthews, Thomas P.,Klair, Suki,Cheung, Kwai-Ming J.,Scanlon, Jane,Proisy, Nicolas,Addison, Glynn,Ellard, John,Piton, Nelly,Taylor, Suzanne,Cherry, Michael,Fisher, Martin,Boxall, Kathy,Burns, Samantha,Walton, Michael I.,Westwood, Isaac M.,Hayes, Angela,Eve, Paul,Valenti, Melanie,De Haven Brandon, Alexis,Box, Gary,Van Montfort, Rob L. M.,Williams, David H.,Aherne, G. Wynne,Raynaud, Florence I.,Eccles, Suzanne A.,Garrett, Michelle D.,Collins, Ian
experimental part, p. 8328 - 8342 (2012/02/06)
Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The optimization of the pyrazolopyridines to a series of potent and CHK1-selective isoquinolines demonstrates how fragment-growing and scaffold morphing strategies arising from a structure-based understanding of CHK1 inhibitor binding can be combined to successfully progress fragment-derived hit matter to compounds with activity in vivo. The challenges of improving CHK1 potency and selectivity, addressing synthetic tractability, and achieving novelty in the crowded kinase inhibitor chemical space were tackled by multiple scaffold morphing steps, which progressed through tricyclic pyrimido[2,3-b] azaindoles to N-(pyrazin-2-yl)pyrimidin-4-amines and ultimately to imidazo[4,5-c]pyridines and isoquinolines. A potent and highly selective isoquinoline CHK1 inhibitor (SAR-020106) was identified, which potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice. (Figure presented)
PYRAZOLE COMPOUNDS
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Page/Page column 79, (2009/03/07)
The present invention is directed to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE
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Page/Page column 88, (2009/10/18)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation: (I).
Pyrazine compounds
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, (2008/06/13)
A compound of formula (I) wherein R1is selected from the group consisting of phenyl substituted by one or more halogen atoms, naphthyl and naphthyl substituted by one or more halogen atoms; R2is selected from the group consisting of —NH2and —NHC(═O)Ra; R3is selected from the group consisting of —NRbRc, —NHC(═O)Raand hydrogen, R4is selected from the group consisting of hydrogen, -C1-4alkyl, -C1-4alkyl substituted by one or more halogen atoms, —CN, —CH2OH, —CH2ORdand —CH2S(O)xRd; wherein Rarepresents C1-4alkyl or C3-7cycloalkyl, and Rband Rc, which may be the same or different, are selected from hydrogen and C1-4alkyl, or together with the nitrogen atom to which they are attached, form a6-membered nitrogen containing heterocycle, which heterocycle can be further susbtituted with one or more C1-4alkyl; Rdis selected from C1-4alkyl or C1-4alkyl substituted by one or more halogen atoms; x is an integer zero, one or two; and pharmaceutically acceptable derivatives thereof; with the proviso that R1does not represent (a); when R2is —NH2, and both R3and R4are hydrogen.
N-heterocyclyl sulphonamide derivatives and their use as endothelin antagonists
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, (2008/06/13)
The invention concerns pharmaceutically useful N-heterocyclyl sulphonamide derivatives, their pharmaceutically acceptable salts, processes for their manufacture, their use for antagonising one or more actions of endothelin in a human or other warm-blooded animal, their use in methods of treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role.
