- HEAT SHOCK PROTEIN 90 INHIBITORS
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Substituted aromatic compounds of formula (I) shown below: (formula I) The definition of each variable in formula (I) appears in the Specification. Also disclosed is a pharmaceutical composition containing one of the substituted aromatic compounds. Further disclosed is a method of using one of these compounds for treating a medical condition associated with HSP90.
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Page/Page column 26; 33; 35; 87
(2018/10/19)
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- Selective anti-markovnikov cyclization and hydrofluorination reaction in superacid HF/SbF5: A tool in the design of nitrogen-containing (fluorinated) polycyclic systems
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The selective synthesis of tetrahydroquinolines and fluorinated arylamines was performed in superacid HF/SbF5 through a superelectrophilic ammonium-carbenium activation process. This anti-Markovnikov oriented reaction was applied to the straightforward synthesis of highly valued (fluorinated) nitrogen-containing heterocyclic compounds.
- Compain, Guillaume,Bonneau, Celine,Martin-Mingot, Agnes,Thibaudeau, Sebastien
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p. 4463 - 4472
(2013/06/05)
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- 5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrroloindole: A Novel 5-HT2C/5-HT2B Receptor Antagonist with Improved Affinity, Selectivity, and Oral Activity
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The preparation of a series of conformationally restricted analogues of indolylurea 1, namely tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described.The binding affinities of these compounds at 5-HT2A, 5-HT2B, and 5-HT2C receptors were determined.Of these compounds, the 1,2,3,5-tetrahydropyrroloindole derivative, compound 11, was found to have high affinity for the 5-HT2C (pK1 8.0) and 5-HT2B receptors (pA2 8.5), with excellent selectivity over the 5-HT2A and various other receptors (pK1B 8.8), and an in vivo functional model, mCPP-induced hypolocomotion (ID50 5.5 mg/kg po). 11 should therefore be of significant utility as a pharmacological tool to delineate the functional significance of blockade of 5-HT2B and 5-HT2C receptors.
- Forbes, Ian T.,Ham, Peter,Booth, Deborah H.,Martin, Roger T.,Thompson, Mervyn,et al.
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p. 2524 - 2530
(2007/10/02)
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