gebhart/patrepeval huggingface dataset:
Synthesis of cephalosporins with substituted thiadiazoles directly attached to the C3-position. I. Synthesis of 3-(5-substituted-1,3,4-thiadiazol-2-yl)ceph-3-em derivatives. (1980)

3-(5-Substituted-1, 3, 4-thiadiazol-2-yl) ceph-3-em derivatives were prepared by oxidative ring closure with 2, 3-dichloro-5, 6-dicyanobenzoquinone directly or after acetylation of 3-thiocarbonylhydrazones, which were obtained from the reaction of 3-formylceph-3-ems and thiocarbonylhydrazines. The antibacterial activity of 7-thienylacetamido-3-(5-substituted-1, 3, 4-thiadiazol-2-yl) ceph-3-em derivatives (4) against gram-positive organisms was similar to that of cephalothin (CET), while the activity against gram-negative organisms was superior to that of CET. A similar oxidative ring closure reaction with other thiocarbonylhydrazones is also discussed.
Amorphous magnetic alloys of cobalt-titanium (1981)

Amorphous cobalt-titanium films were deposited by r.f. sputtering for titanium content in excess of 14 atom percent. The properties of amorphous CoTi films are similar to those of transition metal-metalloid glasses: they have soft magnetic properties and their resistivity is in the 100–200μΩcm range. Contrary to most metal-metalloid glasses, these films have very small magnetostriction, are most thermally stable, and more corrosion resistant.
MIMO Wireless Power Transfer for Mobile Devices (2016)

Since the time of Nikola Tesla, the dream of ubiquitous wireless power transfer (WPT) has tantalized generations of inventors and engineers. A practical, ubiquitous WPT infrastructure could offer tremendous benefits for mobile devices, such as extending battery lifetime, on-the-fly recharging, or, in some cases, eliminating batteries and pesky charging cords altogether. But these benefits can be achieved only if the spatial and temporal distribution of wireless power can be controlled. The authors consider approaches to achieving control over the distribution of long-range (electromagnetic far-field) wireless power, using multi-input, multi-output (MIMO) concepts adapted from the communication domain. They survey recent results in MIMO WPT theory and experiment, and conclude with their own experimental evidence that MIMO WPT can leverage the physics of multipath propagation to selectively enhance or block wireless power delivery, with a typical control range of 20 dB (100 times) in practical indoor environments. This article is part of a special issue on energy harvesting.
Recognition of 16 Base Pairs in the Minor Groove of DNA by a Pyrrole−Imidazole Polyamide Dimer (1998)

Cell-permeable small molecules that bind predetermined DNA\nsequences with affinities and specificities comparable to those\nof natural DNA-binding proteins have the potential to regulate\nthe expression of specific genes. Recently, an eight-ring hairpin\npyrrole-imidazole (Py-Im) polyamide which binds six base pairs\nof DNA was shown to inhibit transcription of a specific gene in\ncell culture. Polyamides recognizing longer DNA sequences\nshould provide more specific biological activity. To specify a\nsingle site within the 3 billion base pair human genome, ligands\nwhich specifically recognize 15-16 base pairs are necessary.\nFor this reason, recognition of 16 base pairs represents a milestone\nin the development of chemical approaches to DNA recognition.\nWe examine here the affinity and specificity of a Py-Im\npolyamide dimer which targets 16 contiguous base pairs in the\nminor groove of DNA.
Translational pharmacology of TD139, an inhaled small molecule galectin‐3 (Gal‐3) inhibitor for the treatment of idiopathic pulmonary fibrosis (IPF) (2020)

Introduction Gal‐3 is a pro‐fibrotic β‐galactoside‐binding lectin highly expressed in the lungs of IPF patients . TD139 is an inhaled, small molecule Gal‐3 inhibitor in development for IPF[2]. In this study the translational pharmacology of TD139 from pre‐clinical to clinical studies are presented. Methods TD139 was evaluated in pre‐clinical studies investigating Gal‐3 in vitro and in vivo in naïve and bleomycin‐treated mice (male C57/Bl6 mice) , . A randomized, double‐blind, multi‐centre, placebo‐controlled, phase IIa study was completed to assess safety, tolerability, and PK/PD of TD139 in 24 patients with IPF. Inhaled TD139 was delivered at 0.3 mg, 3 mg or 10 mg QD to IPF patients (8 patients/cohort, 5:3 ratio (active:placebo)) for 14 days. Patients underwent bronchoalveolar lavage (BAL) prior to dosing and after 14 days. TD139 drug concentration was measured in the BAL fluid, BAL macrophages and plasma. Gal‐3 expression on BAL macrophages was measured by flow cytometry and systemic biomarkers of Gal‐3 inhibition and fibrosis measured in plasma. Results TD139 demonstrated high affinity (K D = 2.1 ± 0.1 nM (mean ± SD, n=4)) in vitro and reduced Gal‐3 expression ex vivo on IPF macrophages (IC 50 = 361 ± 108 nM (mean ± SD, n=3 patients)). TD139 in vivo attenuated mechanistic PD (BAL Gal‐3) and fibrotic endpoints (total lung collagen/histology) in bleomycin‐treated mice with duration driven by lung retention. Clinically, inhaled TD139 was well tolerated at all doses with concentrations in BAL macrophages >567‐fold higher than systemic exposure. Gal‐3 expression on BAL macrophages was significantly lower in the 3 mg (% change −52.52%, 95% CI −85.43% to −4.74%, P=0.023) and 10 mg (% change −78.60%, 95% CI −110.48% to −29.78%, P<0.0001) dose groups compared to placebo, with a concentration‐dependent inhibition. Reduced Gal‐3 expression on BAL macrophages was associated with lower plasma biomarkers relevant to IPF pathobiology (PAI‐1, YKL‐40 and PDGF‐BB). Conclusion TD139 is safe and well tolerated in man and demonstrates low systemic exposure coupled with high lung concentrations resulting in suppression of Gal‐3 on BAL macrophages and decreased plasma biomarkers associated with IPF progression. Pre‐clinical in vitro and in vivo studies have shown to be clinically translatable. This study supported the progression of TD139 into a phase IIb IPF study . Support or Funding Information All studies were funded by Galecto Biotech AB.
Sideband locking of a single-section semiconductor distributed-feedback laser in an optical phase-lock loop (2009)

The bandwidth and performance of optical phase-lock loops (OPLLs) using single-section semiconductor lasers (SCLs) are severely limited by the nonuniform frequency modulation response of the lasers. It is demonstrated that this restriction is eliminated by the sideband locking of a single-section distributed-feedback SCL to a master laser in a heterodyne OPLL, thus enabling a delay-limited loop bandwidth. The lineshape of the phase-locked SCL output is characterized using a delayed self-heterodyne measurement.
<title>GaN blue-light-emitting diode using room-temperature ohmic contacts</title> (2001)

Room temperature ohmic contacts to p- and n-type GaN using surface treatments were applied to the fabrication of GaN blue light emitting diode (LED). The state-of-the-art LED operation of the forward voltage of 3.1 V at the injection current of 20 mA was demonstrated without annealing processes. The surface treatment on p-type GaN using aqua regia solution caused the contact resistivity to decrease by three orders of magnitude. The inductively coupled plasma treatment on n-type GaN resulted in the contact resistivity of ~ 10E-6 ohm-cm2 at as-deposited state. Both treatments allowed the room temperature ohmic contacts to be realized on both substrates. Angle resolved synchrotron x-ray photoelectron spectroscopy was employed to examine the atomic composition at the treated surface. From this, the formation of ohmic contacts was deduced as due to the production of vacancies below the contact, that is, Ga vacancies for p-type contact and N vacancies for n-type one.
ChemInform Abstract: SYNTHESIS AND ANTIHYPERTENSIVE ACTIVITY OF 4′‐SUBSTITUTED SPIRO(4H‐3,1‐BENZOXAZINE‐4,4′‐PIPERIDIN)‐2(1H)‐ONES (1983)

Abstract Die aus dem Carbamat (II) zugängliche Dilithi?m‐ Verbind ung reagiert mit dem Urethan (I) zum Benzo xazin (III), das nach Spaltung zu (IV) mit dem Epoxid (V) zum Aminoalkohol (VI) reagiert.
Potent Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease. Use of Cyclopentane and Cyclopentene Derived P2-Scaffolds (2007)

This thesis describes the design, synthesis and structure-activity relationships analysis of potential inhibitors targeting the hepatitis C virus (HCV) NS3 protease. Also discussed is the disease caused by HCV infection and the class of enzymes known as proteases. Furthermore are explained why such enzymes can be considered to be suitable targets for developing drugs to combat diseases in general and in particular HCV, focusing on the NS3 protease. Moreover, some strategies used to design protease inhibitors and the desired properties of potential drug candidates are briefly examined. Synthesis of linear and macrocyclic NS3 protease inhibitors comprising a designed trisubstituted cyclopentane moiety as an N-acyl-(4R)-hydroxyproline bioisostere is also addressed, and several very potent and promising compounds are evaluated.
The Mutagenesis Protein UmuC Is a DNA Polymerase Activated by UmuD′, RecA, and SSB and Is Specialized for Translesion Replication (1999)

Replication of DNA lesions leads to the formation of mutations. In Escherichia coli this process is regulated by the SOS stress response, and requires the mutagenesis proteins UmuC and UmuD'. Analysis of translesion replication using a recently reconstituted in vitro system (Reuven, N. B., Tomer, G., and Livneh, Z. (1998) Mol. Cell 2, 191-199) revealed that lesion bypass occurred with a UmuC fusion protein, UmuD', RecA, and SSB in the absence of added DNA polymerase. Further analysis revealed that UmuC was a DNA polymerase (E. coli DNA polymerase V), with a weak polymerizing activity. Upon addition of UmuD', RecA, and SSB, the UmuC DNA polymerase was greatly activated, and replicated a synthetic abasic site with great efficiency (45% bypass in 6 min), 10-100-fold higher than E. coli DNA polymerases I, II, or III holoenzyme. Analysis of bypass products revealed insertion of primarily dAMP (69%), and to a lesser degree dGMP (31%) opposite the abasic site. The UmuC104 mutant protein was defective both in lesion bypass and in DNA synthesis. These results indicate that UmuC is a UmuD'-, RecA-, and SSB-activated DNA polymerase, which is specialized for lesion bypass. UmuC is a member of a new family of DNA polymerases which are specialized for lesion bypass, and include the yeast RAD30 and the human XP-V genes, encoding DNA polymerase eta.
Bend-it (2018)

Elastically deforming wire structures are lightweight, durable, and can be bent within minutes using CNC bending machines. We present a computational technique for the design of kinetic wire characters, tailored for fabrication on consumer-grade hardware. Our technique takes as input a network of curves or a skeletal animation, then estimates a cable-driven, compliant wire structure which matches user-selected targets or keyframes as closely as possible. To enable large localized deformations, we shape wire into functional spring-like entities at a discrete set of locations. We first detect regions where changes to local stiffness properties are needed, then insert bendable entities of varying shape and size. To avoid a discrete optimization, we first optimize stiffness properties of generic, non-fabricable entities which capture well the behavior of our bendable designs. To co-optimize stiffness properties and cable forces, we formulate an equilibrium-constrained minimization problem, safeguarding against inelastic deformations. We demonstrate our method on six fabricated examples, showcasing rich behavior including large deformations and complex, spatial motion.
Mark detection for alignment and registration in a high-throughput projection electron lithography tool (1992)

The design considerations and performance requirements of an alignment and registration method for high-throughput projection electron lithography are discussed. We have devised a mark detection system for a lithography tool employing the SCALPEL principle. The process involves scanning the image of a mark from a mask, over a mark that is fabricated on a wafer and measuring the integrated backscattered-electron intensity. Using a mark that consists of equally spaced lines of tungsten on silicon, we have investigated the effects of spatial and rotational misalignment, and focus in a small field of view SCALPEL machine. We have modeled these and other effects and found agreement between experimental and theoretical results. The measured precision of estimating position from the experimental data is ∼10 nm. By extrapolation we believe that in a practical lithography machine this value can be improved significantly.
A new approach to subsurface gravity (2006)

The borehole gravity method can be applied to making Gravity Measurements While Drilling (GMWD) if an appropriate gravity sensor can be developed for use in a drilling environment. We performed a study to determine at a high level the potential value of developing GMWD for solving a wide range of important petroleum exploration and production (E&P) problems. The study investigated the potential applications of using GMWD to steer a drill bit.
Hyperspectral bright greenish-yellow fluorescence (BGYF) imaging of aflatoxin contaminated corn kernels (2006)

Aflatoxin contaminated corn poses a serious threat to both domestic animals and humans, because of its carcinogenic properties. Traditionally, corn kernels have been examined for evidence of bright greenish-yellow fluorescence (BGYF), which is an indication of possible presence of <i>Aspergillus flavus</i>, one of the aflatoxin producing strains of fungi, when illuminated with a high-intensity ultra-violet light. The BGYF test is typically the first step that leads to an in-depth chemical analysis for possible aflatoxin contamination. The objective of the present study was to analyze hyperspectral BGYF response of corn kernels under UVA excitation. The target corn samples were collected from a commercial corn field in 2005 and showed abundant BGYF response. The BGYF positive kernels were manually picked out and imaged under a visible near-infrared hyperspectral imaging system under UV radiation with excitation wavelength centered at 365 nm. Initial results exhibited strong emission spectra with peaks centered from 500 nm to 515 nm wavelength range for BGYF positive kernels. Aflatoxin levels on the BGYF positive and negative corn kernels (used as control) were measured subsequently with high performance liquid chromatography. The mean aflatoxin concentration level was 5114 ppb for the BGYF positive and undetectable for the normal kernels.
c-kit ligand stimulates tyrosine phosphorylation of a similar pattern of phosphotyrosyl proteins in primary primitive normal hematopoietic progenitors that are constitutively phosphorylated in comparable primitive progenitors in chronic phase chronic myelogenous leukemia. (1996)

Characteristic of Philadelphia (Ph)+ chronic myelogenous leukemia (CML) is the presence of the chimeric BCR/ABL (p210) protein possessing elevated protein tyrosine kinase activity relative to the normal c-abl tyrosine kinase. Our previous studies demonstrated subtle differences in the growth, phenotypic and morphologic characteristics of the most primitive subpopulations of primary lin-Ph+ chronic phase CML blasts and comparable primary lin- normal blasts. Recently, in comparing proteins phosphorylated on tyrosine in these cell populations, we reported a prominent 62 kDa phosphotyrosyl (P-tyr) protein constitutively present in primary primitive lin- CML chronic phase blasts which was virtually undetectable in primary primitive lin- normal blasts. In the present studies, we demonstrate that this P-tyr p62 from primary primitive lin- chronic phase CML blasts co-immunoprecipitates with ras-GAP. Furthermore, in addition to the p210 protein, we show in whole cell lysates the presence of other clearly consistent but less prominent P-tyr proteins with molecular weights of approximately 155, 140, 110, 55 and 45 kDa as well as more minor P-tyr proteins of approximately 190, 85, 52, 42 and 39 kDa constitutively present in primary primitive lin- chronic phase CML blasts. In analyzing proteins tyrosine phosphorylated in primary primitive lin- normal blasts in response to various hematopoietic growth factors, we found a striking similarity in the phosphorylation of four major (approximately 140, 110, 62 and 56 kDa) and three minor (approximately 51, 45 and 42 kDa) P-tyr proteins after stimulation with c-kit ligand and the P-tyr proteins constitutively phosphorylated in primary primitive lin- chronic phase CML blasts. Other growth factors tested (ie GM-CSF, G-CSF, IL-3, FLT3 ligand and EPO) were much less active or stimulated phosphorylation of other proteins. It is provocative that at least seven proteins rapidly and transiently phosphorylated on tyrosine in the c-kit ligand signal transduction pathway in lin- normal blasts may be constitutive substrates for the p210 activated tyrosine kinase in comparable lin- chronic phase CML blasts. In addition, it is intriguing that some of the biological effects on hematopoietic progenitors attributed to the c-kit ligand may be similar to some of the observed biological consequences of the p210 protein, including survival and expansion of a more mature stem cell population, probably at the time of lineage commitment rather than at the level of the earliest self-renewing stem cell.
Tetrakis(selenodiazole)porphyrazines 1: Tetrakis(selenodiazole)porphyrazine and its <font>Mg</font>(<font>II</font>) and <font>Cu</font>(<font>II</font>) Derivatives. Evidence for their Conversion to Tetrakis(pyrazino)porphyrazines through Octaaminoporphyrazines (1999)

The new phthalocyanine-like macrocycle tetrakis(selenodiazole)porphyrazine, TSeDPzH 2 , and its Mg ( II ) and Cu ( II ) complexes have been prepared and their general, spectroscopic (IR, UV-vis), and magnetic properties investigated. It has been observed that the peripheral selenodiazole rings of the TSeDPz skeleton can be opened by the action of H 2 S , with release of the Se atoms and formation of a new macrocycle, i.e. octaaminoporphyrazine, which is easily converted into tetrakis(pyrazino)porphyrazine derivatives.
ChemInform Abstract: 2‐ACETYLPYRIDINE THIOSEMICARBAZONES. 3. SELENIUM ANALOGS AS POTENTIAL ANTIMALARIAL AGENTS (1981)

Abstract S‐Methylierung der Acetylpyridinthiosemicarbazone (I) führt zu den Derivaten (II), die mit NaSeH unter Argon zu den Selenosemicarbazonen (III) reagieren; (IIIc) wird alternativ durch Umsetzen von Acetylpyridinhydrazon (IV) mit Phenylisoselenocyanat synthetisiert.
Extracting repeats from media streams (2004)

Many media streams consist of distinct objects that repeat. For example, broadcast television and radio signals contain advertisements, call sign jingles, songs and even whole programs that repeat. The problem we address is to identify explicitly the underlying structure in repetitive streams and deconstruct them into their component objects. Our architecture assumes no a priori knowledge of the streams, and does not require a pre-trained database. Everything the system needs is learned on the fly. We demonstrate that using a modestly capable computer it is perfectly feasible to identify, in realtime, repeating objects that occur days or even weeks apart in audio or video streams. We outline the algorithms, enumerate several applications and present results from real streams.
ChemInform Abstract: Synthesis of Perfluoro Ethers by Liquid Phase Fluorination. (1989)

Abstract Liquid phase fluorination of the ethers (I), (III), and (V) with F2 diluted with N 2 yields the corresponding perfluorinated products (II), (IV), and (VI) as outlined in the reaction scheme.
Target cell killing effects of CD20 targeting chimeric antigen receptor T cells derived from the type II anti-CD20 antibody. (2017)

e14548 Background: Chimeric Antigen Receptor T cells (CAR-Ts) targeting CD19 have shown very promising clinical outcomes in treatment of B-cell linage hematological malignancies. However, many patients with relapsed diseases were found to have down-regulated/loss of CD19 surface expression after CD19 CAR-T therapy. To solve this issue of CD19 single-targeting escape, we explored the application of another B-cell antigen, CD20, for targeted CAR-T therapy. Methods: We constructed four CD20 targeting CARs (all with 4-1BB co-stimulatory signaling) base on single-chain variable fragments (scFV) derived from four well-studied CD20 specific antibodies: Leu16, Rituximab, Obinutuzumab, and Ofatumumab. Leu16, Rituximab, and Obinutuzumab belong to the type I anti-CD20 antibody family and appear to bind to different epitopes located on the large loop of CD20, whereas Ofatumumab is the type II anti-CD20 antibody which has been shown to interact with the hydrophobic residues on the small loop surrounding a deep binding cleft. Results: All four CAR-T cells can specifically recognized CD20 positive target cells in our pre-clinical studies. They all showed up-regulated antigen-specific cell activation and high level of IFN-g release upon CD20 stimulation, and CAR-T20-Ofatumumab cells appeared to have significantly higher cell activation and more than 2-fold increase in IFN-g release compared to the other three CAR-T20 cells with their scFVs deriving from type I anti-CD20 antibodies. CAR-T20-Ofatumumab cells also showed higher degranulation upon stimulation, and it displayed ~50% of increase in ability to kill CD20 positive cells in cytotoxicity assays. Conclusions: Our data suggested that CAR-T20-Ofatumumab has better in vitro function and appears to be a CAR superior to those derived from other three antibodies. A possible explanation for this observation is that Ofatumumab interacts with the hydrophobic residues on the small loop, which is very close to cell membrane and confers more extensive binding to the small loop with striking slow off-rate. Our results suggest that CAR-Ts targeting CD20 with the scFVs from the type II anti-CD20 antibody may have superior cell killing effects.
Enhanced Potency of a Broadly Neutralizing HIV-1 Antibody <i>In Vitro</i> Improves Protection against Lentiviral Infection <i>In Vivo</i> (2014)

In the absence of an effective HIV-1 vaccine, alternative strategies are needed to block HIV-1 transmission. Direct administration of HIV-1-neutralizing antibodies may be able to prevent HIV-1 infections in humans. This approach could be especially useful in individuals at high risk for contracting HIV-1 and could be used together with antiretroviral drugs to prevent infection. To optimize the chance of success, such antibodies can be modified to improve their potency, breadth, and in vivo half-life. Here, knowledge of the structure of a potent neutralizing antibody, VRC01, that targets the CD4-binding site of the HIV-1 envelope protein was used to engineer a next-generation antibody with 5- to 8-fold increased potency in vitro. When administered to nonhuman primates, this antibody conferred protection at a 5-fold lower concentration than the original antibody. Our studies demonstrate an important correlation between in vitro assays used to evaluate the therapeutic potential of antibodies and their in vivo effectiveness.
Progressive Transmission of Uncompressed Video over mmW Wireless (2010)

In this paper we propose a new progressive rate adaptation scheme for uncompressed video over millimeter wave wireless (mmW) in which the video data rate can be adapted to any rate smoothly and with minimal video quality degradation. Two major steps: 1. Progressive pixel differential transformation (PPDT) in which difference values of pixels are compressed and transmitted in a new systematic way for progressive rate adaptation. 2. Progressive pixel dropping (PPDP) in which pixels at different positions are evenly dropped in a new systematic way for progressive rate adaptation if the data rate is still too high to fit into the available channel bandwidth after the first step. Simulation results show that our proposed rate adaptation scheme can achieve at least 20 dB quality improvement in PSNR (peak signal to noise ratio) than the conventional rate adaptation schemes.