1618-47-9Relevant academic research and scientific papers
Synthesis of Triptycene-Based Molecular Rotors for Langmuir-Blodgett Monolayers
Kaleta, Ji?í,Kaletová, Eva,Císa?ová, Ivana,Teat, Simon J.,Michl, Josef
, p. 10134 - 10150 (2015)
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.
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors
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
, p. 5580 - 5590 (2016/11/09)
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.
CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page/Page column 65, (2015/09/22)
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
BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS
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Page/Page column 50, (2012/11/13)
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.
SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS
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Page/Page column 45, (2009/03/07)
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.
Aryl-4-ethynyl-isoxazole derivatives
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Page/Page column 9, (2008/06/13)
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.
