- INDOLINONE DERIVATIVES AS INHIBITORS OF MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE
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The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).
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Page/Page column 86-87
(2018/09/20)
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- Design of α7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies
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We report here the synthesis of a large library of 1,2,3-triazole derivatives which were in vitro tested as α7 nAchR ligands. The SAR study revealed that several crucial factors are involved in the affinity of these compounds for α7 nAchR such as a (R) quinuclidine configuration and a mono C-3 quinuclidine substitution. The triazole ring was substituted by a phenyl ring bearing small OMe/CH2F groups or fluorine atom and by several heterocycles such as thiophenes, furanes, benzothiophenes or benzofuranes. Among the 30 derivatives tested, the two derivatives 10 and 39 with Ki in the nanomolar range were identified (2.3 and 3 nM respectively). They exhibited a strict selectivity toward the α4β2 nicotinic receptor (up to 1 μM) but interacted with the 5HT3 receptors with Ki around 3 nM. Synthesis, SAR studies and a full description of the derivatives are reported.
- Ouach, Aziz,Pin, Frederic,Bertrand, Emilie,Vercouillie, Johnny,Gulhan, Zuhal,Mothes, Céline,Deloye, Jean-Bernard,Guilloteau, Denis,Suzenet, Franck,Chalon, Sylvie,Routier, Sylvain
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p. 153 - 164
(2015/11/18)
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- INHIBITORS OF HSP90
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The invention provides a compound which is (a) a pyrrolopyrimidine derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: Formula (I) wherein R1, R2, R3/
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Page/Page column 65
(2010/04/30)
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- OPHTHALMIC LENS MATERIALS CONTAINING CHROMOPHORES THAT ABSORB BOTH UV AND SHORT WAVELENGTH VISIBLE LIGHT
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Chromophores that absorb both UV and short wavelength visible light are disclosed. The chromophores are particularly suitable for use in intraocular lens materials.
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Page/Page column 2-4
(2009/03/07)
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- Oligonucleotide-directed assembly of materials: Defined oligomers
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A nano-architectural system that has high variability while maintaining component specificity is described. Tetraphenylcyclobutadiene(cyclopentadienyl)cobalt complexes and phenyleneethynylene trimers were synthesized and subsequently modified with oligonu
- Waybright,Singleton,Wachter,Murphy,Bunz
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p. 1828 - 1833
(2007/10/03)
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