67868-84-2Relevant academic research and scientific papers
HIF-2α INHIBITORS FOR TREATING IRON OVERLOAD DISORDERS
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Paragraph 0197, (2016/05/02)
The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating iron overload disorders. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and reduced liver iron accumulation and serum iron parameters in both prophylactic and treatment mouse models.
HIF-2-ALPHA INHIBITOR POLYMORPHS
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Paragraph 0243-0244, (2016/09/26)
Chemical compounds that modulate HIF-2α activity, their polymorphs, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with HIF-2α, are described herein.
Facile one-pot transformation of phenols into o-cyanophenols
Nakai, Yuhta,Moriyama, Katsuhiko,Togo, Hideo
, p. 6077 - 6083 (2015/03/30)
The treatment of phenols with paraformaldehyde in the presence of MgCl2 and Et3N in THF at 80 C, followed by reaction with molecular iodine and aq. ammonia at room temperature provided the corresponding o-cyanophenols in moderate to good yields. The present reaction is a one-pot transformation of phenols into o-cyanophenols using much less expensive reagents than are typically used; the reaction is free of both transition-metals and cyanide. The utility of this reaction was highlighted during our preparation of Febuxostat from p-bromophenol.
Highly asymmetric NHC-catalyzed hydroacylation of unactivated alkenes
Piel, Isabel,Steinmetz, Marc,Hirano, Keiichi,Froehlich, Roland,Grimme, Stefan,Glorius, Frank
supporting information; experimental part, p. 4983 - 4987 (2011/06/21)
NHC-catalysis proto(n)type: The title reaction produces 21 different chroman-4-one-type products in good yields and excellent enantioselectivities, in each case building up a new all-carbon quaternary stereocenter (see scheme). Based on DFT calculations a
N-heterocyclic carbene-catalyzed hydroacylation of unactivated double bonds
Hirano, Keiichi,Biju, Akkattu T.,Piel, Isabel,Glorius, Frank
supporting information; experimental part, p. 14190 - 14191 (2010/02/15)
(Chemical Equation Presented) An intramolecular N-heterocyclic carbene (NHC)-catalyzed hydroacylation of unactivated double bonds is reported. Systematic variation of the catalyst structure revealed an N- mesitylthiazolylidene annulated with a seven-membered ring to be especially reactive. This NHC enables a unique C-C bond-forming reaction to afford substituted chroman-4-ones in moderate to excellent yields, even ones containing all-carbon quaternary centers.
Sulphur containing amino pyrimidine compounds for the treatment of inflammatory disorders
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Page/Page column 11-13, (2009/04/23)
The present invention relates to novel sulphur containing amino pyrimidine compounds of formula (I) for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also rel
2-THIO-SUBSTITUTED IMIDAZOLE DERIVATIVES AND THEIR USE IN PHARMACEUTICS
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Page/Page column 37-38, (2008/06/13)
The invention relates to 2-thio-substituted imidazole derivatives of formula (I), wherein the radicals R1, R2, R3 and m have the meanings as cited in the description. The inventive compounds comprise an immunomodulatory action and/or an action that inhibits the release of cytokines and are thus suited for treating diseases associated with a disorder of the immune system.
Antiangiogenic combination therapy for the treatment of cancer
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, (2008/06/13)
The present invention provides combinations of a DNA topoisomerase I inhibiting agent and a selective COX-2 inhibiting agent for preventing, treating, and/or reducing the risk of developing a neoplasia disorder in a mammal.
Substituted benzopyran derivatives for the treatment of inflammation
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, (2008/06/13)
A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
Substituted benzopyran analogs for the treatment of inflammation
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, (2008/06/13)
A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
