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On the basis of structural information for the cyclic hexapeptide endothelin (ET) receptor antagonist, TAK-044, a series of thieno[2,3-d]pyrimidine-2,4-dione derivatives bearing a carboxyl group and aromatic rings that were important for receptor binding were designed, synthesized, and evaluated for ET receptor binding affinities and inhibitory activities against ET-induced vasoconstriction. Optimization of each substituent in the thieno[2,3-d]pyrimidine ring led to the discovery of a novel and potent nonpeptide ET receptor antagonist, 6-(4-methoxymethoxyphenyl)-5-methylsulfonylaminomethyl-1-(2- methylthiobenzyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]p yrimidine-3- acetic acid (32 g), which binded to human ETA and ETB receptor subtypes with affinities (IC50) of 7.6 and 100 nM, respectively. Compound 32 g effectively antagonized ET-induced vasoconstriction and the inhibitory effect mediated by the ETB receptor was more potent than that of bosentan, while the inhibitory effect mediated by the ETA receptor was slightly less potent than that of bosentan.  相似文献   
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Applied Intelligence - A multi-agent system (MAS) is expected to be applied to various real-world problems where a single agent cannot accomplish given tasks. Due to the inherent complexity in the...  相似文献   
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Stationary projectors mainly used in system applications have recently gained a wider application range, including general presentations in halls and large conference rooms and being used, for example, in digital signage and for monitoring purposes. Consequently, they are required to meet new market demands for durability, reliability, and flexibility in installation in addition to their conventional basic performance such as especially high brightness. To achieve especially high brightness, a new optical system with two lamps is proposed; the profile of the cover glass that prevents the glass from scattering is made aspherical, the profile of the beam‐combining mirror is improved with its position optimized, and the size of the incident plane of the integrator rod is made larger (1.1 times). These measures resulted in an optical system of an even higher efficiency with 7000 lm, which is the highest in its class (according to a June 2010 investigation). Also, the arrangement of two parallel lamps completely eliminated the effect of heat passing from one lamp to the other, which helped secure durability, reliability, and flexibility in installation. Furthermore, the combined use of the unique non‐telecentric optical system, adopted from the conventional single‐lamp model, helps maintain the class‐highest contrast ratio.1,2  相似文献   
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This is an extensive overview of the core and special space?Ctime and Arbitrary Lagrangian?CEulerian (ALE) techniques developed by the authors?? research teams for patient-specific cardiovascular fluid?Cstructure interaction (FSI) modeling. The core techniques are the ALE-based variational multiscale (ALE-VMS) method, the Deforming-Spatial-Domain/Stabilized Space?CTime formulation, and the stabilized space?Ctime FSI technique. The special techniques include methods for calculating an estimated zero-pressure arterial geometry, prestressing of the blood vessel wall, a special mapping technique for specifying the velocity profile at an inflow boundary with non-circular shape, techniques for using variable arterial wall thickness, mesh generation techniques for building layers of refined fluid mechanics mesh near the arterial walls, a recipe for pre-FSI computations that improve the convergence of the FSI computations, the Sequentially-Coupled Arterial FSI technique and its multiscale versions, techniques for the projection of fluid?Cstructure interface stresses, calculation of the wall shear stress and oscillatory shear index, arterial-surface extraction and boundary condition techniques, and a scaling technique for specifying a more realistic volumetric flow rate. With results from earlier computations, we show how these core and special FSI techniques work in patient-specific cardiovascular simulations.  相似文献   
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The computational challenges posed by fluid–structure interaction (FSI) modeling of parachutes include the lightness of the parachute canopy compared to the air masses involved in the parachute dynamics, in the case of “ringsail” parachutes the geometric complexities created by the construction of the canopy from “rings” and “sails” with hundreds of ring “gaps” and sail “slits”, and in the case of parachute clusters the contact between the parachutes. The Team for Advanced Flow Simulation and Modeling () has successfully addressed these computational challenges with the Stabilized Space–Time FSI (SSTFSI) technique, which was developed and improved over the years by the and serves as the core numerical technology, and a number of special techniques developed in conjunction with the SSTFSI technique. The quasi-direct and direct coupling techniques developed by the , which are applicable to cases with incompatible fluid and structure meshes at the interface, yield more robust algorithms for FSI computations where the structure is light and therefore more sensitive to the variations in the fluid dynamics forces. The special technique used in dealing with the geometric complexities of the rings and sails is the Homogenized Modeling of Geometric Porosity, which was developed and improved in recent years by the . The Surface-Edge-Node Contact Tracking (SENCT) technique was introduced by the as a contact algorithm where the objective is to prevent the structural surfaces from coming closer than a minimum distance in an FSI computation. The recently-introduced conservative version of the SENCT technique is more robust and is now an essential technology in the parachute cluster computations carried out by the . We provide an overview of the core and special techniques developed by the , present single-parachute FSI computations carried out for design-parameter studies, and report FSI computation and dynamical analysis of two-parachute clusters.  相似文献   
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The nuclear spin dynamics in nuclear spin ordered solid3He in low magnetic fields on the melting curve has been studied by pulsed NMR down to 0.6 mK. The free induction decay signals (FID) were measured in single crystals of solid3He at three operating frequencies of 920, 1380, and 1840 kHz. The FIDs were nonexponential and dependent on the rf pulse strength p H 1 t w , where is the gyromagnetic ratio,H 1 is the rf field strength, andt w is the pulse width. At small p they decayed almost linearly in time with a small exponential tail at the end. When p was further increased they became shorter and neither exponential nor linear in time. At large p they decayed very rapidly and sometimes could not be observed at all because of the dead time of the NMR detection system. Such behavior of the FID was observed in many different single crystals in the given temperature range at 920 kHz. Tsubota and Tsuneto have shown by solving the nonlinear equations of motion numerically that the motion of the nuclear spin becomes chaotic when the tipping angle exceeds a critical value. Comparing their result with our experimental results, we concluded that some of the results of the rapid decay of the FID at large p might be attributed to the onset of the chaotic motion. At 1840 kHz it is expected that the nonlinear effects in the equations of motion become less effective than that at 920 kHz. In fact, at this operating frequency the FIDs even at large p and the tipping angle-dependent frequency shift could be observed. These frequency shifts were in rather good agreement with Namaizawa's theory provided an effective tipping angle was taken into account.  相似文献   
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本文对微机图象法在脉冲MAG焊接中的应用作了探讨,设计和采用了带有CCD摄象机的微机控制系统,对脉冲MAG焊接熔池进行了观察、监控和图象处理。其结果证明了采用微机图象法来实现实时控制是可行的。  相似文献   
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A series of symmetrical dialkyl methanesulfonate amphiphiles [DiC n CHSO 3 ] m M (n = 6, 7, 8) with different counter cations (Mm+ = H+, Li+, Na+, K+, Cu2+, Zn2+, Mg2+, Ca2+, Sc3+) were synthesized in five steps. Their solubility and critical micelle concentration (CMC) in water were determined highlighting a huge effect of the chain length and the nature of the cation. The hydrophilic–lipophilic balance of the surfactants were assessed with the phase inversion temperature (PIT)-slope method based on the deviation from the PIT of the reference C10E4/n-octane/0.01 M NaCl(aq) emulsion through addition of increasing amounts of the dialkyl methanesulfonates. The hydrophilicity of the surfactants was thus ranked in terms of dPIT/dxsulfonate. A “cation” scan with the [DiC 6 CHSO 3 ] m M /benzene/water systems at fw = 0.5 was finally performed confirming the hydrophilicity ranking obtained with the PIT-slope method. It revealed that the [DiC 6 CHSO 3 ] 2 Mg behaves as a “Balanced Surfactant” able to form spontaneously a three-phase microemulsion system (Winsor III) just in the presence of water and oil, in the same way as the catalytic surfactant dimethyldioctylammonium molybdate, which has the same PIT-slope.  相似文献   
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