Abstract: Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides.

Abstract: N-(3-Methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide ethanolamine salt and its uses are described.

Abstract: Disclosed is a total synthesis of a biologically active ?-Lactam—Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. Also disclosed are proteasome inhibiting compounds having the formula: wherein: R1 is a cyclolower alkyl group; or R1 is a lower alkyl group; and R2 is either hydrogen or a lower alkyl group; R3 is either hydrogen or a lower alkyl group; R4 a halo-lower alkyl group; and R5 is either hydrogen or a lower alkyl group.

Abstract: A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4? is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4? to a group R4, or where R4? is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.

Abstract: A gravity-powered toy vehicle, such as a model roller coaster, with an energy-storing flywheel coupled to the wheels to reduce the vehicle velocity s it approaches that which is proportionately realistic for the model scale. The initial potential energy of the vehicle is mostly conserved over the course of the track just as with a real roller coaster. At all points on the track the velocity of the model vehicle is reduced by a constant proportion compared to an unrestrained free-fall vehicle. Thus the dynamic velocity profile of the toy vehicle is the same as for a full size vehicle throughout its descending and ascending journey, but at a proportionately reduced speed.

Abstract: A gravity-powered toy vehicle, such as a model roller coaster, with an energy-storing flywheel coupled to the wheels to reduce the vehicle velocity so it approaches that which is proportionately realistic for the model scale. The initial potential energy of the vehicle is mostly conserved over the course of the track just as with a real roller coaster. At all points on the track the velocity of the model vehicle is reduced by a constant proportion compared to an unrestrained free-fall vehicle. Thus the dynamic velocity profile of the toy vehicle is the same as for a full size vehicle throughout its descending and ascending journey, but at a proportionately reduced speed.

Abstract: A gravity-powered toy vehicle, such as a model roller coaster, with an energy-storing flywheel coupled to the wheels to reduce the vehicle velocity so it approaches that which is proportionately realistic for the model scale. The initial potential energy of the vehicle is mostly conserved over the course of the track just as with a real roller coaster. At all points on the track the velocity of the model vehicle is reduced by a constant proportion compared to an unrestrained free-fall vehicle. Thus the dynamic velocity profile of the toy vehicle is the same as for a full size vehicle throughout its descending and ascending journey, but at a proportionately reduced speed.