Abstract:
Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made 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 on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
Abstract:
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.
Abstract:
A negative switch may enable switching of two different negative voltages. The switch may include a negative cascode bias generator which biases the gate of a cascade protection device. When the negative switch is passing a large negative voltage, the bias generator generates a lowered voltage to provide a cascade voltage for snapback protection of a passing transistor. When a relatively low negative voltage is to be switched, the bias generator may produce a positive voltage greater than the threshold voltage of the cascode protection device so that both high and low negative voltages may be switched by the same circuit without exposing the passing device to a voltage in excess of its snapback limit.
Abstract:
Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
Abstract:
Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
Abstract:
Translational motion of a scanning head relative to a planar target, or vice versa, is achieved by a belt and pulley system with a counterweight that is also driven by a belt and pulley system at the same speed but in the opposite direction as the scanning head. The components and belt and pulley system are oriented such that all moving components remain on one side of the target and remain so during their entire range of movement.
Abstract:
A moving coil actuator that moves in a rapid back-and-forth motion is constructed with a magnet assembly that concentrates the magnetic flux in a region of limited length and with a coiled electric conductor that includes two separated regions of densely wound coil, the assembly and conductor arranged such that only one of the coil regions resides in a concentrated flux region at either end of the actuator stroke. This is achieved with either a single region of concentrated flux or two spatially separated regions of concentrated flux. In either case, the force constant, i.e., the motor force generated in each coil per unit of current through the coil, is non-linear, with a maximal force at each end of the stroke and a minimal force at the stroke mid-point. The result is an efficient use of the electric current and relatively small amounts of materials of construction, and accordingly less weight for the actuator to carry during its travel and its changes of direction.
Abstract:
Methods and apparatuses associated with stepping down a high voltage in a high voltage switch. An additional transistor may be coupled to a switching transistor, and the additional transistor biased to a voltage level in between the high voltage to be switched and a switch reference voltage. When the switch is off, the high voltage may thus be spread across multiple devices to prevent a voltage from the gate to the drain to exceed a threshold associated with gate-aided breakdown of the drain-to-substrate channel-side pn-junction.
Abstract:
A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.