24176-70-3Relevant academic research and scientific papers
Heterocyclic compound and preparation and application thereof
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Paragraph 0110-0111; 0114-0115, (2020/07/24)
The invention relates to bromodomain inhibitors, and provides a compound represented by a general formula I, a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method thereof, a pharmaceutical composition containing the same, and applicationthereof in pharmacy.
Bromine structural domain inhibitor compound and application thereof
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Paragraph 0342-0343; 0346-0347, (2019/08/02)
The invention relates to a bromine structural domain inhibitor and provides a compound shown in a general formula I, pharmaceutical salt, an enantiomer, a diastereoisomer, an atropisomer, racemate, apolymorphic substance and solvate of the compound or an isotope labelled compound (including a deuterium substituted compound), a preparation method of the compound, pharmaceutical composition containing the compound and an application of the above components in pharmaceuticals.
Aniline pyrimidines, its preparation method and medical use (by machine translation)
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Paragraph 0190; 0269; 0270; 0271, (2018/03/01)
The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
Fidanze, Steven D.,Liu, Dachun,Mantei, Robert A.,Hasvold, Lisa A.,Pratt, John K.,Sheppard, George S.,Wang, Le,Holms, James H.,Dai, Yujia,Aguirre, Ana,Bogdan, Andrew,Dietrich, Justin D.,Marjanovic, Jasmina,Park, Chang H.,Hutchins, Charles W.,Lin, Xiaoyu,Bui, Mai H.,Huang, Xiaoli,Wilcox, Denise,Li, Leiming,Wang, Rongqi,Kovar, Peter,Magoc, Terrance J.,Rajaraman, Ganesh,Albert, Daniel H.,Shen, Yu,Kati, Warren M.,McDaniel, Keith F.
supporting information, p. 1804 - 1810 (2018/04/23)
Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin
BROMODOMAIN INHIBITORS
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Paragraph 0662, (2014/09/29)
The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specificati
DIHYDRO-PYRROLOPYRIDINONE INHIBITORS
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Paragraph 1104, (2014/09/29)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
TETRACYCLIC BROMODOMAIN INHIBITORS
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Page/Page column 101, (2014/09/29)
The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Υ2, Υ3, A1, A2, A3 and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
INHIBITORS OF PROTEIN KINASES
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Page/Page column 146, (2009/12/05)
The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
Treatment Method
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Page/Page column 10, (2009/01/20)
The present invention is directed to methods of treating an ocular neovascular disorder in a mammal by administration of pyrimidine derivatives, benzodiazepinyl derivatives and pharmaceutical compositions containing the same. The invention encompasses methods of treating an ocular neovascular disorder by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, (S)-3-oxo-8-[3-(pyridin-2-ylamino)-1-propyloxy]-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or salts or solvates thereof. Combination therapies for the treatment of ocular neovascular disorders are also encompassed.
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase
Sammond, Douglas M.,Nailor, Kristen E.,Veal, James M.,Nolte, Robert T.,Wang, Liping,Knick, Victoria B.,Rudolph, Sharon K.,Truesdale, Anne T.,Nartey, Eldridge N.,Stafford, Jeffrey A.,Kumar, Rakesh,Cheung, Mui
, p. 3519 - 3523 (2007/10/03)
A series of dianilinopyrimidineureas demonstrate potency as VEGFR2 kinase inhibitors.
