- Synthesis of Triptycene-Based Molecular Rotors for Langmuir-Blodgett Monolayers
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We describe syntheses of six triptycene-containing molecular rotors with several single-crystal X-ray diffraction analyses. These rod-shaped molecules carrying an axial rotator are designed to interleave on an aqueous surface into Langmuir-Blodgett (LB) monolayers containing a two-dimensional trigonal array of dipoles rotatable about an axis normal to the surface. Monolayer formation was verified with the simplest of the rotor structures. On an aqueous subphase containing divalent cations (Mg2+, Ca2+, Zn2+, Sr2+, or Cd2+), the LB isotherm yielded an area of 53 ± 3 ?2/molecule (monolayer of type A), compatible with the anticipated triangular packing of axes normal to the surface. On pure water, the area is 30 ± 3 ?2/molecule, and it is proposed that in this monolayer (type B), the molecular axes are tilted by 40-45° to a structure similar to those observed in single crystals of related triptycenes. After transfer to a gold surface, ellipsometry and PM IRRAS yield tilt angles of 29 ± 4° (monolayers of type A) and 38 ± 4° (type B). A full-scale examination of monolayers from all the rotors on a subphase and after transfer is underway and will be reported separately.
- Kaleta, Ji?í,Kaletová, Eva,Císa?ová, Ivana,Teat, Simon J.,Michl, Josef
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- Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors
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High levels of Pim expression have been implicated in several hematopoietic and solid tumor cancers, suggesting that inhibition of Pim signaling could provide patients with therapeutic benefit. Herein, we describe our progress towards this goal using a screening hit (rac-1) as a starting point. Modification of the indazole ring resulted in the discovery of a series of imidazopyridazine-based Pim inhibitors exemplified by compound 22m, which was found to be a subnanomolar inhibitor of the Pim-1 and Pim-2 isoforms (IC50values of 0.024?nM and 0.095?nM, respectively) and to potently inhibit the phosphorylation of BAD in a cell line that expresses high levels of all Pim isoforms, KMS-12-BM (IC50?=?28?nM). Profiling of Pim-1 and Pim-2 expression levels in a panel of multiple myeloma cell lines and correlation of these data with the potency of compound 22m in a proliferation assay suggests that Pim-2 inhibition would be advantageous for this indication.
- Wurz, Ryan P.,Sastri, Christine,D'Amico, Derin C.,Herberich, Brad,Jackson, Claire L.M.,Pettus, Liping H.,Tasker, Andrew S.,Wu, Bin,Guerrero, Nadia,Lipford, J. Russell,Winston, Jeffrey T.,Yang, Yajing,Wang, Paul,Nguyen, Yen,Andrews, Kristin L.,Huang, Xin,Lee, Matthew R.,Mohr, Christopher,Zhang,Reid, Darren L.,Xu, Yang,Zhou, Yihong,Wang, Hui-Ling
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p. 5580 - 5590
(2016/11/09)
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- CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is i
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Page/Page column 65
(2015/09/22)
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- BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS
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The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
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Page/Page column 50
(2012/11/13)
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- Compounds
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Compounds of Formula (I), compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
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Page/Page column 34
(2009/08/14)
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- SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS
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The present invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
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Page/Page column 45
(2009/03/07)
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- COMPOUNDS
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Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.
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Page/Page column 25
(2009/12/24)
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- Aryl-4-ethynyl-isoxazole derivatives
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The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula I wherein R1 to R5 are as described in the specification and pharmaceutically acceptable salt thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites, being useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
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Page/Page column 9
(2008/06/13)
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