摘要:
Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety with certain acyl groups; conversion of the amide group in amino acid-3 to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要:
Embodiments described herein discuss an approach to implementing load-balancing across multiple monitoring servers. One such embodiment describes a network monitoring device. The network monitoring device includes an ingress port, for receiving mirrored network packets, and a number of egress ports. The egress ports are associated with a number of monitoring servers, and used to forward the mirrored network packets to the monitoring servers. A packet classifier, coupled to the ingress port, examines the mirrored network packets, and determines which of the monitoring servers should receive the packets.
摘要:
A charge pump comprises at least one charge pump cell and control logic. The at least one charge pump cell is configured to receive a power supply voltage and provide a pump output voltage higher than the power supply voltage. The control logic is configured to receive an oscillator signal and a level detector enable signal, provide at least one cell clock signal, based on the oscillator signal, to the at least one charge pump cell, control the at least one pump cell to charge while the level detector enable signal is asserted, and control the at least one pump cell to continue to charge after the level detector enable signal is deasserted and until a full pulse cycle of the oscillator signal is completed.
摘要:
Disclosed is a moisture curable sealant composition that includes silane functional poly-α-olefin polymer, thermoplastic elastomer, and tackifying agent.
摘要:
Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
摘要:
A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
摘要:
Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
摘要:
7,8-Bicyclic-chroman derivatives of Formula I: wherein the substituents are defined as in the specification or the pharmaceutically acceptable salts thereof, are disclosed. They are useful for the treatment of inflammatory disorders, neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
摘要:
Using NMRScore to generate an RMSD and evaluating whether the RMSD is below 1 ppm, in order to indicate that a docking software generated pose is a good match with the experimental assessment of a paradigm protein target and paradigm ligand, and therefore that the pose will be useful and accurate for the same target and similar ligands, or similar targets and the same ligands.
摘要:
A method of reducing the appearance of skin conditions associated with loss of skin tightness, skin firmness, or dark circles under the eyes with topical compositions comprising compounds of any of the Formulae I or Ia as described herein, is disclosed.