Abstract:
N-(2-oxaadamantan-1-yl)ureas of formula I, where R3 is H, C 1 -C 3 alkyl, cyclohexyl or phenyl; R is -[CH 2 ] n -Y; n is 0-15; in -[CH 2 ] n - 0-n/3 of the methylene groups are optionally replaced by non adjacent oxygen atoms; and Y is a 3- or 4-substituted phenyl, a 3- or 4-substituted cyclohexyl, a N-substituted piperidin-4-yl, a N-substituted piperidin-3-yl, a di- or tri-fluorosubstituted phenyl, 4-chloro-3-trifluoromethylphenyl, 3-chloro-4-trifluoromethylphenyl, 4-fluoro-3-trifluoromethylphenyl, or 3-fluoro-4-trifluoromethylphenyl; have epoxide hydrolase (sEH) inhibitory activities similar to those of their N-(adamantan-1-yl)urea analogs. Thus, compounds I are useful as API for the treatment of sEH mediated diseases. Besides, in general, compounds (I) have higher water solubilities and lower melting points, what make them more promising from the point of view of pharmacokinetics and formulation.
Abstract:
The invention relates to compounds, particularly fluorogenic amino acid derivatives, which can be used as optical probes. The invention further relates to processes for the preparation of such compounds, the use of such compounds as probes and methods of detecting a target using such compounds as probes.
Abstract:
La presente invención se refiere aun método in vitrode pronóstico o predicción de la respuesta al tratamiento con fármacos antipsicóticos, por parte de sujetos que han sufrido un primer episodio psicótico (FEP), y en concreto, al empleo del valor de expresión, en una muestra biológica aislada de dichos sujetos, del ratio formado por dos de las isoformas -isoforma activa e isoforma truncada-, del receptor (TrKB) del factor de crecimiento neuronal BDNF, denominadas TrKB-FL y TrkB-T, respectivamente. La presente invención describe además kits y usos de los mismos para llevar a cabo el método de la invención.
Abstract:
La presente invención se refiere a un método in vitro para diagnosticar o para determinar el riesgo de desarrollar una enfermedad neurodegenerativa en un sujeto basado en la determinación del patrón de metilación en ciertas regiones del ADN mitocondrial de dicho sujeto o en la determinación del nucleótido en la posición polimórfica 16519 del ADN mitocondrial de dicho sujeto. Finalmente, la presente invención se refiere a ácidos nucleicos adecuados para poner en práctica la invención.
Abstract:
A bioreactor (1) for cell co-culture comprising at least first and second cell culture chambers (2, 4). The first and second chambers (2, 4) are separated by a porous membrane (6) for cell culture. The membrane (6) comprises at least one sealing gasket (12) integrated in the membrane (6) being integral therewith. The sealing gasket (12) defines a closed perimeter delimiting a first cell culture area (16).
Abstract:
Pseudomonas sp. CECT8437 is a cold-adapted bacterium isolated from a marine sediment sample collected from Deception Island (South Shetland Islands, Antarctica) that is noted for the highly mucous appearance of its colonies. An exopolysaccharide (EPS) is produced by this strain, which comprises glucose, galactose, fucose and uronic acid in a molar ratio of 2:1:1:0.3 approximately. The EPS shows the following weight percentages, approximately: 37.29% C, 6.17% H, 2.25% N, and 0.41 % S. Its molecular weight (MW) is higher than 2 x 10 6 Da. The EPS is useful for the following purposes: (i) cryoprotectant agent; (ii) emulsifier agent; (iii) thickening, stabilizing or structural agent; (iv) dermoprotective agent; and (v) agent for increasing skin elasticity. The EPS can be used in cosmetic compositions.
Abstract:
The invention provides a method, and corresponding system and apparatus, for assessing the acceptability of an individual forced spirometry manoeuvre as well as an indication of the quality of a full spirometry test, comprising more than one manoeuvre. An automatic validation of the spirometry measurements are provided by identifying wrong/flawed tests, or acceptable/valid tests. Hence an indication is provided regarding the quality of the measurements performed, and feedback or indication is provided regarding the reliability, or confidence level, of the manoeuvre or set of manoeuvres. Preferably no expert intervention is necessary, however a minimum intervention might be considered useful in order to rule out any doubtful manoeuvres and dissipate ambiguities.
Abstract:
In a first aspect, the present invention provides a method of measuring attention of a person comprising presenting one or more stimulus aimed at attracting attention of the person; and obtaining positions of the eyes of the person. The method further comprises detecting one or more eye fixations from the obtained positions of the eyes; and measuring the angle of convergence of the eyes over time from the obtained positions of the eyes during one or more of the detected eye fixations.
Abstract:
It is described a method of binding site and binding energy determination by mixed explicit solvent all-atoms molecular dynamics simulations. The macromolecular target for which high affinity binders are sought is simulated in several mixed solvent environments comprising water and at least one amphiphilic organic co-solvent. The simulations are run so that the mixture of solvents are free to react to the presence of the target without the addition of any forces other than those found in the original potential. A correction is applied that helps dissociating the distribution of the different chemical groups found in the amphiphilic organic solvents when calculating their free energies of binding. Additionally, a second correction can be applied accounting for the aggregation of said solvents. The correction helps determining more meaningful absolute, and more accurate relative free energies of binding that can be applied in the rational design of new binders to macromolecular targets.
Abstract:
Los compuestos de fórmula (I) o sus sales farmacéuticamente aceptables, o sus estereoisómeros o mezcla de estereoisómeros, donde:R 1 , R 2 , R 4, R 5 , y R 7 , son independientemente seleccionados del grupo que consiste en H, Cl,C(=O)O(C 1 -C 4 )alquilo, O(C 1 -C 4 )alquilo; y (C 1 -C 4 )alquilo; R 3 se selecciona del grupo que consiste en H 1 , Cl, C(=O)O(C 1 -C 4 )alquilo, O(C 1 -C 4 )alquilo, (C 1 -C 4 )alquilo, pirrolidinil-1-carbonil, and morfolin-1-carbonil; R 6 es seleccionado del grupo que consiste en H and (C 1 -C 4 )alquilo; y R 8 es seleccionado del grupo que consiste en H, F, Br, (C 1 -C 4 )alquilo, y fenilo; inhiben la proliferación celular de células tumorales independientemente de la proteína p53 y también pueden inducir apoptosis en varias células tumorales independientemente de la proteína p53, siendo útiles para el tratamiento de varios tipos de cáncer.