- The first ready-to-use benzene-based heterotrifunctional cross-linker for multiple bioconjugation
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The synthesis and applications of the first water-soluble benzene derivative bearing a set of three different and orthogonal bioconjugatable groups (aminooxy, azido and thiol) are described. The combined use of a 5-amino isophthalic acid scaffold and unusual acid-labile protecting groups for temporarily masking aminooxy and thiol moieties has enabled the development of a highly convergent approach towards the synthesis of such a trivalent bioconjugation platform in good yields. The potential utility of this ready-to-use cross-linking reagent for creating complex and fragile tri-component (bio)molecular systems was illustrated through (1) the rapid preparation of a three-colour FRET cascade with valuable spectral properties and (2) the luminescent/fluorescent labelling of peptides and peptide- oligonucleotide conjugates. Thus, such (bio)molecular assemblies were readily obtained via a three-step process or in a one-pot manner, both involving oxime ligation, thiol-alkylation (SN2 or Michael addition) and copper-catalysed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) reactions.
- Viault, Guillaume,Dautrey, Sebastien,Maindron, Nicolas,Hardouin, Julie,Renard, Pierre-Yves,Romieu, Anthony
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p. 2693 - 2705
(2013/06/05)
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- Molecular chirality and chiral capsule-type dimer formation of cyclic triamides via hydrogen-bonding interactions
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Chiral properties of bowl-shaped cyclic triamides bearing functional groups with hydrogen-bonding ability were examined. Chiral induction of cyclic triamide 3a was observed by addition of chiral amine in solution, and chiral separation was achieved by sim
- Fujimoto, Noriko,Matsumura, Mio,Azumaya, Isao,Nishiyama, Shizuka,Masu, Hyuma,Kagechika, Hiroyuki,Tanatani, Aya
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supporting information; experimental part
p. 4809 - 4811
(2012/06/30)
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- PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
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Page/Page column 87
(2009/03/07)
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- Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE
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A series of N-((2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification
- Wu, Yong-Jin,Zhang, Yunhui,Good, Andrew C.,Burton, Catherine R.,Toyn, Jeremy H.,Albright, Charles F.,Macor, John E.,Thompson, Lorin A.
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scheme or table
p. 2654 - 2660
(2010/01/16)
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- MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS
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The invention relates to novel macrocyclic compounds of the Formula (I) in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 35-36
(2008/06/13)
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- Novel phenylcarboxyamides as beta-secretase inhibitors
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There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y as defined herein, their pharmaceutical compositions and
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Page/Page column 8-9
(2008/06/13)
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- MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS
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The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 60
(2008/06/13)
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- Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof
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The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
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Page/Page column 193
(2010/11/24)
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- NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
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There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
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Page/Page column 40-41
(2010/11/23)
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- Rigid macrocyclic triamides as anion receptors: Anion-dependent binding stoichiometries and 1H chemical shift changes
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The cyclic triamide of 3′-amino-3-biphenylcarboxlic acid is readily synthesized in a stepwise manner and represents a novel class of anion receptors with a large central cavity. This macrocycle binds more strongly to tetrahedral anions than spherical or p
- Choi, Kihang,Hamilton, Andrew D.
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p. 10241 - 10249
(2007/10/03)
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- Naphthylsulfonic acids and related compounds as glucose uptake agonists
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Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
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