Abstract: Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.

Abstract: Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract: 14-membered macrolide compounds such as erythromycins are provided with functional groups at the 14- and/or 15-position by providing a 14-membered aglycone template and feeding it to a strain capable of hydroxylating it at the 14 and/or 15 position. The strain may be found by screening, selected from known strains (e.g. Streptomyces eurythermus DSM 40014) or produced by genetically engineering a strain to express a cytochrome P450 enzyme.

Abstract: The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: —X1—(CH2)m-Q-(CH2)n—X2—??III D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to process and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

Abstract: An actuation indicator that includes a drum sub-assembly, which includes a rotatable actuation indicator wheel, a rocking, ratchet pawl for rotating the indicator wheel in a set direction and a rocking mechanism for the pawl driven by a slipping clutch arrangement, is described. The slipping clutch arrangement includes a slipping clutch spring engaged at one end to a pinion of a rack and pinion assembly and at a second end to the ratchet pawl.

Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.

Abstract: There is provided a propellant-operable self-activating and self-returning metering valve for an aerosol container for dispensing a formulation comprising a substance in a fluid propellant contained therein. There is also provided a canister for use in a metered dose inhaler having the valve thereon.

Abstract: The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.

Abstract: According to the present invention there is provided an inhalation device for dispensing medicament comprising a body (150), the body being shaped for receipt of a medicament carrier (286); and an actuator (10) having a mouthpiece (20), the actuator being reversibly movable between a dispensing position and a storage position; wherein the body includes an air channel (253), and the actuator includes an air hole (225) such that the air channel communicates with the air hole when the actuator is in the dispensing position and the air channel and air hole do not communicate when the actuator is in the storage position.

Abstract: A valve that includes a valve body, a valve stem having a dispensing passage, and a sealing ring that contacts the valve stem is described. The sealing ring includes a flexible component and a rigid component.

Abstract: Valve for an aerosol container for dispensing a suspension of a substance in a liquid propellant contained therein. The valve comprises a valve body (1) having at least one orifice (16) to allow a quantity of the suspension to pass from the container into the valve. The valve further comprises a ring (18) disposed around the valve body (1), the ring being positioned below the at least one orifice to reduce the volume of suspension that can be accommodated within the container below the at least one orifice when the container is orientated with the valve at the bottom, the ring having at least one portion of reduced axial thickness to provide a trough (19) around the valve body below the at least one orifice.

Abstract: There is provided a medicament dispenser comprising a body, a medicament container and reset means for resetting a mechanical mechanism after actuation thereof, wherein the reset means comprises a reset coupling. The coupling is reversibly deformable in response to the application of non-mechanical energy thereto. The non-mechanical energy may comprise heat energy, electrical current energy, electrical field energy or magnetic field energy.

Abstract: A dispensing apparatus for dispensing a unit dose of a pharmaceutical substance, in particular one for intranasal administration, is disclosed. The unit dose is contained in a cylinder which is moved relative to a piston to expel the contents thereof through a passage in the piston and out of a nozzle opening. The dispensing apparatus includes a case with a base part and a cover.

Abstract: The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.

Abstract: A metering valve that includes a valve body defining a metering chamber having an inlet valve adapted to be reversibly actuable from an open position to a closed position located at the inlet, and an outlet valve adapted to be reversibly actuable from a dispensing to a non-dispensing position located at the outlet, where the outlet valve includes an outlet valve seat adapted to be in biasable contact with an outlet valve poppet is described. Aerosol containers and inhalation devices that include such metering valves are also described, as are methods of using such inhalation devices.

Abstract: There is provided a dispenser suitable for dispensing medicament, particularly medicament for use in the treatment of respiratory disorders. The dispenser comprises a housing having a support; a container, locatable within said housing, having an outlet, wherein said container dispenses through said outlet in response to movement of the container relative to the housing; and an actuation indicator having an indexing mechanism actuatable by movement of the container relative to the housing. A couple mechanism is provided which couples the indexing mechanism to the container to compensate for any variation in pre-actuation positionings of the indexing mechanism and container.

Abstract: The present invention relates to novel pharmaceutical aerosol formulations comprising: (A) salmeterol xinafoate in the form of particles coated by spray-drying with at least one surfactant in the absence of any other coating excipient, in suspension in (B) a liquefied propellant gas which is 1,1,1,2,3,3,3-heptafluoro-n-propane or 1,1,1,2-tetrafluoroethane and mixtures thereof for administration particularly by the pulmonary route and to a process for preparing these formulations. It also relates to novel particles suitable for use in such formulations.

Abstract: There is provided a dispenser comprising a body for receipt of a carrier for a composition; an exit channel definable by the body for passage of the composition to a user; a cover for the exit channel reversibly movable between a storage position in which the cover fully protects the exit channel, to an in-use position wherein the exit channel is exposed. Biasing means act on the cover when the cover is not in the in-use or storage positions, to bias the cover towards either the in-use position or the storage position.

Abstract: A filtration assembly operable in connection with a crystal form screening workstation that provides for automated crystal form screening is disclosed. The assembly includes first and second valves, with each valve having an internal passage and first, second and third ports. A filter line is interposed between the first and second valves in fluid communication with the second port of the first valve and the second port of the second valve. A filter medium is in disposed in or at the end of the filter line and adapted to filter a drug-containing suspension flowing through the filter line. The filter medium is operable to filter fluids under both positive and negative pressure conditions.