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Kubas H.,Merz Pharmaceuticals GmbH | Meyer U.,Merz Pharmaceuticals GmbH | Hechenberger M.,Merz Pharmaceuticals GmbH | Klein K.-U.,Merz Pharmaceuticals GmbH | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

The metabotropic glutamate receptor subtype 5 has evolved into a promising target for the treatment of various diseases of the central nervous system, such as Fragile X and l-DOPA induced dyskinesia. One of the most advanced clinical compound is Novartis' AFQ-056 (Mavoglurant), which served us as a template for a scaffold hopping approach, generating a structurally diverse set of potent analogs. Both the limited aqueous solubility and the relatively poor metabolic stability of AFQ-056 were improved with hexahydrocyclopenta[c]pyrrole derivative 54a, which proved to be a valuable candidate for further development. © 2013 Elsevier Ltd. All rights reserved.

Kulakov I.V.,Institute of Organic Synthesis | Turdybekov D.M.,Scientific Production Holding Phytochemistry
Chemistry of Heterocyclic Compounds | Year: 2010

Bicyclic pyrimido[2,1-b][1,3]thiazines were produced by the acylation of 4-aryl-substituted 3,4-di-hydropyrimidine(1H)-2-thiones with 3-bromopropionyl chloride, and their structures were proved by the data from X-ray crystallographic analysis. ©2010 Springer Science+Business Media, Inc.

Il'in A.I.,Anti infective Drugs Research Center | Kulakov I.V.,Institute of Organic Synthesis | Leonova N.V.,Anti infective Drugs Research Center | Kasymbekova S.S.,Anti infective Drugs Research Center | And 2 more authors.
Russian Journal of General Chemistry | Year: 2011

Reactions of (N-1-methylglucosaminocarbonothioyl)-4-bromobenzamide with copper(II) sulfate in the ratios 1:1 and 2:1 affords the corresponding chelate complexes of the metal. Their structure was proved by high resolution mass spectrometry. The complex of (N-1-methylglucosaminocarbonothioyl)-4- bromobenzamide with copper(II) sulfate (ratio 1:1) exhibits pronounced antibacterial activity. © Pleiades Publishing, Ltd., 2011.

Kubas H.,Merz Pharmaceuticals GmbH | Meyer U.,Merz Pharmaceuticals GmbH | Krueger B.,Merz Pharmaceuticals GmbH | Hechenberger M.,Merz Pharmaceuticals GmbH | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

A virtual screening approach using various in silico methodologies led to the discovery of 2-(m-tolylamino)-7,8-dihydroquinazolin-5(6H)-one (1) as a moderately active negative allosteric modulator (NAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) showing high selectivity against the subtype mGluR1. Modifications of the parent compound by rational design yielded a series of highly potent derivatives which will serve as valuable starting points for further hit-to-lead optimization efforts toward a suitable drug candidate for the treatment of l-DOPA induced dyskinesia. © 2013 Elsevier Ltd. All rights reserved.

You G.,Institute of Organic Synthesis | Cheng Z.,Institute of Organic Synthesis | Peng H.,Institute of Organic Synthesis | He H.,Institute of Organic Synthesis
Journal of Applied Polymer Science | Year: 2014

A novel, halogen-free, phosphorus-nitrogen containing flame retardant 2[4-(2,4,6-Tris{4-[(5,5-dimethyl-2-oxo-2λ5-[1,3,2]dioxaphosphinan-2-yl)hydroxymethyl]phenoxy}-(1,3,5)-triazine (TNTP) was successfully synthesized in a three-step process, and characterized by FTIR, NMR spectroscopy, mass spectra, and elemental analysis. A series of modified DGEBA epoxy resin with different loadings of TNTP were prepared and cured by 4,4-diaminodiphenylsulfone (DDS). Thermal gravimetric analysis and vertical burning test (UL-94) were used to evaluate the flame retardancy of TNTP on DGEBA epoxy resin. The results showed that TNTP had a great impact on flame retardancy. All modified thermosets by using TNTP exhibited higher Tg than pure DGEBA/DDS. The loading of TNTP at only 5.0 wt % could result in satisfied flame retardancy (UL-94, V-0) together with high char residue (27.3%) at 700°C. The addition of TNTP could dramatically enhance the flame retardancy of DGEBA epoxy resins, which was further confirmed by the analysis of the char residues by scanning electron microscopy and FTIR. Furthermore, no obviously negative effect was found on the Izod impact strength and flexural property of DGEBA epoxy resins when TNTP loading limited in 5.0 wt %. DGEBA/DDS containing 2.5 wt % TNTP could enhance Izod impact strength from 10.47 to 10.94 kJ m-2, and showed no appreciable effect on the flexural property (85.20 MPa) comparing with pure DGEBA/DDS (87.03 MPa). Results indicated that TNTP as a phosphorus-nitrogen synergistic intumescent flame retardant could be used for DGEBA epoxy resin. © 2014 Wiley Periodicals, Inc.

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