A novel series of pyrazolylpiperidine N-type calcium channel blockers
摘要:
Selective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered synthetic x-conotoxin MVIIA from Conus magnus (ziconotide [Prialt (R)]) has been approved for the treatment of chronic pain in humans, its mode of delivery and narrow therapeutic window have limited its usefulness. Therefore, the identification of orally active, small-molecule N-type calcium channel blockers would represent a significant advancement in the treatment of chronic pain. A novel series of pyrazole-based N-type calcium channel blockers was identified by structural modification of a high-throughput screening hit and further optimized to improve potency and metabolic stability. In vivo efficacy in rat models of inflammatory and neuropathic pain was demonstrated by a representative compound from this series. (C) 2012 Elsevier Ltd. All rights reserved.
Magnetically nano core–shell Fe3O4@Cu(OH)x: a highly efficient and reusable catalyst for rapid and green reduction of nitro compounds
作者:Zahra Shokri、Behzad Zeynizadeh、Seyed Ali Hosseini、Behrooz Azizi
DOI:10.1007/s13738-016-0962-3
日期:2017.1
Magnetically separable nano core–shell Fe3O4@Cu(OH)x with 22 % Cu content was prepared by the addition of sodium hydroxide to a mixture of CuCl2·2H2O and nano Fe3O4 in water. Characterization of the impregnated copper hydroxide was carried out by X-ray fluorescence (XRF), X-ray diffraction (XRD) atomic absorption spectroscopy (AAS), scanning electron microscopy (SEM), value stream mapping (VSM) and Brunauer–Emmett–Teller (BET) analysis. The core–shell nanocatalyst exhibited the excellent catalytic activity toward reduction of various nitro compounds to the corresponding amines with NaBH4. All reactions were carried out in H2O (55–60 °C) within 3–15 min to afford amines in high to excellent yields. Reusability of core–shell Cu(OH)x catalyst was examined 9 times without significant loss of its catalytic activity.
Encapsulation of Pd(II) into superparamagnetic nanoparticles grafted with EDTA and their catalytic activity towards reduction of nitroarenes and Suzuki-Miyaura coupling
Fe3O4@EDTA–Pd(II) was screened for the Suzuki reaction and reduction of nitrocompounds in water. The Pd content of the catalyst was measured to be 0.28 mmol Pd g−1. In addition, the Fe3O4@EDTA–Pd catalyst can be easily separated and recovered with an external permanent magnet. The anchored solid catalyst can be recycled efficiently and reused five times with only a very slight loss of catalytic activity
Green and convenient protocols for the efficient reduction of nitriles and nitro compounds to corresponding amines with NaBH4 in water catalyzed by magnetically retrievable CuFe2O4 nanoparticles
作者:Behzad Zeynizadeh、Farkhondeh Mohammad Aminzadeh、Hossein Mousavi
DOI:10.1007/s11164-019-03794-4
日期:2019.6
er and Barrett–Joyner–Halenda analyses. The prepared magnetically copper ferrite nanocomposite was successfully applied as a simple, cost-effective, practicable, and recoverable catalyst on the green, highly efficient, fast, base-free, and ligand-free reduction of nitriles and also on the affordable and eco-friendly reduction of nitrocompounds with the broad substrate scope to the corresponding amines
[EN] TRAF 6 INHIBITORS<br/>[FR] INHIBITEURS DE TRAF 6
申请人:HELMHOLTZ ZENTRUM MUENCHEN DEUTSCHES FORSCHUNGSZENTRUM GESUNDHEIT & UMWELT GMBH
公开号:WO2019180207A1
公开(公告)日:2019-09-26
The invention relates to compounds which are suitable for the treatment of cancer, an immune disease, Parkinson's disease, Cardiac Hypertrophy or Type-2 diabetes and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds.
[EN] FIBRE REACTIVE FORMAZAN DYES, THEIR PREPARATION AND THEIR USE<br/>[FR] COLORANTS FORMAZAN RÉACTIFS AUX FIBRES, LEUR PRÉPARATION ET LEUR UTILISATION
申请人:HUNTSMAN ADVANCED MAT (SWITZERLAND) GMBH
公开号:WO2017129297A1
公开(公告)日:2017-08-03
A reactive dye of formula (1), wherein Z1 and Z2 are each independently of the other vinyl or a radical -CH2-CH2-Y and Y is a group removable under alkaline conditions, n is the number 1, 2, 3 or 4, m is the number 2, 3 or 4, q is the number 0 or 1, and the substituents -(SO3H)n, -SO2-Z1 and -NH-CO-(CH2)m-SO2-Z2 are bound to the benzene rings A, B and/or C, said benzene rings A, B and/or C are optionally further substituted by at least one substituent selected from the group C1-C4alkyl, C1-C4alkoxy and halogen, is suitable for dyeing and printing cellulosic or amide-group-containing fibre materials.