- HISTONE DEACETYLASE 6 SELECTIVE INHIBITORS FOR THE TREATMENT OF BONE DISEASE
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This invention relates to methods for treating bone disease associated with osteoclast activation using HDAC6 selective inhibitors, e.g., small molecule inhibitors such as reverse amide compounds.
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Page/Page column 78
(2013/03/26)
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- REVERSE AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF
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The present invention relates to novel "reverse amide" compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
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Page/Page column 83
(2011/08/08)
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- Discovery of new C3aR ligands. Part 1: Arginine derivatives
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The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflamma
- Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Dipesa, Alan,Ganguly, Tanmoy,Giannaras, Alexander,Kumar, Seema,Lewis, Timothy,Maounis, Florence,Nicolas, Jean-Marie,Mansley, Tamsin,Pasau, Patrick,Preda, Dorin,Stebbins, Karin,Volosov, Alexander,Zou, Dong
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p. 3258 - 3261
(2008/02/08)
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- PROCESS FOR PEPTIDE SYNTHESIS OF PEPTIDES CONTAINING A 4-HYDROXY-PROLINE SUBSTRUCTURE
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The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula (VIII) wherein R12 and R13 are as defined herein.
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- Mechanism of the catalytic oxidation of tertiary alcohols by the water- soluble Mn-TMPyP/KHSO5 system: β-Fragmentation versus O-neophyl rearrangement
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Oxidation of 4-(1-hydroxy-1-phenylethyl)benzoic acid HPEBA with a water- soluble metalloporphyrin as catalyst and KHSO5 as oxygen atom donor gives the major products, acetophenone AC and acetylbenzoic acid ABA, by a C(aliph)-C(Ar) bond cleavage, but a minor product, benzoyloxybenzoic acid BOBA, requires the insertion of an oxygen atom to form the ester. This compound becomes the main oxidation product on increasing the amount of acetonitrile in the reaction medium, and its formation is oxygen-dependent. The conversion is drastically lowered by using D2O instead of H2O, suggesting that an alkoxyl radical is formed in the rate-determining step. Labeling experiments using 18O2 or H218O under different reaction conditions show that the carbonyl oxygen atoms of AC and ABA originate either from substrate, water or dioxygen. However, the carbonyl oxygen atom in the ester group of BOBA originates from dioxygen while the other oxygen atom of the ester remains unlabeled. These results can be explained by an O-neophyl rearrangement of the initial alkoxyl radical to afford a carbon-based radical which then reacts with dioxygen or Mn(IV)-OH/water. In a competitive reaction pathway, direct β-scission of the alkoxyl radical leads to unlabeled products. The oxidation of other tertiary diaryl alcohols is also discussed.
- Wietzerbin, Karine,Bernadou, Jean,Meunier, Bernard
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p. 1467 - 1477
(2007/10/03)
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- Acid labile immunoconjugate intermediates
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Trityl derivatives useful as "linkers" for preparation of imunoconjugates comprising drugs end antibodies are provided. Immunoconjugates and processes for their preparation and use are also provided. This invention also provides for prodrugs comprising a
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- Phenylvinylogously Extended Triphenylmethylium Systems
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As isoconjugated models for (phenylazo)tritylium ions of type A the tritylium systems containing one to three styryl or phenylethynyl substituents have been investigated.In accordance with simple theoretical model considerations these ions have VIS absorptions at considerably longer wavelengths than tritylium ion itself.They also show the expected bathochromic band shifts in going from the singly branched (1, 4) to the doubly and triply branched systems 2, 3 and 5, 6 as well as the predicted bathochromic shifts for 4-methoxystyryl (1b-3b) and hypsochromic shifts for 4-( dimethylammoniostyryl)- and 4-(nitrostyryl)tritylium ions 1c-3c and 1d, respectively.For most of the newly prepared tritylium systems fully resolved NMR spectra were obtained, whose signal positions correlate very well with the charge distributions derived from the elementary conjugation model.For the 4,4'-(1,2-ethenediyl)bistritylium system 12, whose color resembles that of 4-styryltritylium ion 1a, only the resonance lines of the inner protons 3,β-H and carbons C-4,β show significant deviations from the corresponding signal positions of the reference systems 1a and tritylium (13). - Key Words: Chromophores, combined / Ethene, diphenyl- / Ethyne, diphenyl- / Phenylmethylium
- Hellwinkel, Dieter,Fritsch, Helmut
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p. 2351 - 2360
(2007/10/02)
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