Abstract: Ultrashort acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein: X is a halogen; h is from 1 to 2; Y is hydrogen or methoxy; Z1 and Z2 are methyl; W1 and W2 are carbon; and A is a pharmaceutically acceptable anion.

Abstract: A device for dispensing a unit dose of substance comprises a nozzle assembly (2) including a container (24) housing a unit dose of the substance, and an outer body (4) to which the nozzle assembly (2) is releasably attached. The body (4) includes a system actuable to effect discharge of the substance from the nozzle assembly (2) and actuating means operably by a user to effect discharge. Preferably the discharge system comprises a spring-loaded air piston (68) actuable to inject air into the container (24) to cause discharge of the substance. In one embodiment a driving spring for the air piston is loaded with spring energy by the action of installing the nozzle assembly on the body, the driving spring thereafter being held in a cocked state until operating of the actuating means by the user to effect release of the spring energy to cause discharge.

Abstract: A method and package for storing a pressurized container which is filled with a drug formulation at a predetermined pressure. The drug formulation includes a mixture of a drug and a propellant. The package which encloses the pressurized container substantially prevents ingression of water vapor and particulate matter into the package while permitting egression of the propellant which may leak from the pressurized container.

Abstract: The use of a HIV-RT inhibitor to enhance the sensitivity to zidovudine of zidovudine-resistant HIV populations, the inhibitor being one which induces a mutation at the 181 or 184 position of the RT coding sequence.

Abstract: This invention relates to pharmaceutical compositions of 5-alkynuracil.

Abstract: According to the invention there are provided Hexahydro-Pyrrolo[3,4-b]pyrrol-2-one compounds of formula (1), (relative stereochemistry indicated), wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (1) are useful inter alia in the treatment or chronic bronchitis.

Abstract: Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X1 and X2 are independently halogen; ha and hb are independenity from 0 to 2; Z1 and Z2 are indepentdently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl with the proviso that Z1 and Z2 are not both hydrogen; Y1, Y2, and Y3 and Y4 are independently hydrogen, halogen or C1-3 alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if ha and hb are both 0, then r is 0 and n is 0 to 2; R1 to R14 are independently hydrogen, halogen, C1-3 alkoxy, or R2 and R3 together with the carbon atoms to which they are bonded, R5 and R6 together with the carbon atoms to which they are bonded, R9 and R10 together with the carbon atoms to which they are bonded, R12 and R13 together with the carbon atoms to which they are bonded, may

Abstract: Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms.

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: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof. Also described are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine.

Abstract: The invention provides a system and method for synthesizing chemicals onto supports in a parallel manner to produce a combinatorial collection of compounds. The system includes a plurality of middle plates, with each middle plate defining a plurality of reaction zones arranged in a two dimensional array. The reaction zones are adapted to receive a solid support, such as a sheet of membrane, and the middle plates are stackable on each other to form a three dimensional array of reaction zones. The system also includes a pair of end plates, where the middle plates are located between the end plates, and where the end plates include an array of fluid guides corresponding to the array of reaction zones, to allow for selective routing of reagents through the reaction zones.

Abstract: Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R3 is a group ZR4 wherein Z is joined to R4 through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR′), V(CHR) or V where R and R′ are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NRb where Rb is hydrogen or Rb is C1-4 alkyl; and R4 is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R3 is a group ZR4 in which Z is NRb, and NRb and R4 together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors.

Abstract: The invention relates to combinations of atovaquone and proguanil, their use in the treatment and prophylaxis of parasitic infections such as protozoal parasitic infections, e.g., malaria and toxoplasmosis, and infections caused by P. carinii and their use in the manufacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.

Abstract: The invention provides exemplary systems and methods for processing solid supports. According to one system, a probe is provided having a distal end and a lumen terminating at the distal end. The transport mechanism is adapted to place the distal end of the probe into a well having a plurality of solid supports that are held within a fluid. A detection mechanism is provided to detect the presence or absence of one of the solid supports at the distal end while the distal end is within the fluid. A measuring system is provided to measure the general size of the attached solid support.

Abstract: The invention provides improved chemical synthesizers and methods for their use. In one exemplary embodiment, a chemical synthesizer system has a reaction vessel block having a plurality of reaction vessels which are adapted to hold solid supports. A wash plate is removably attachable to a top end of the reaction vessel block. The wash plate has a plurality of fluid delivery orifices which are aligned with the reaction vessels when the wash plate is attached to the top end of the reaction vessel block. In this way, fluids may be supplied to each of the reaction vessels through the orifices. The system can include a vortex mixer that is held stationary by evacuation a cavity formed between the mixer base and a gasket.

Abstract: A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilizing fractional crystallization of salts formed with a chiral base; a reducing agent; a protecting group removing agent or a protecting group providing agent.

Abstract: The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the .beta.-diastereomer, and intermediates useful in the process.

Abstract: A metered dose inhaler having part or all of its internal metallic surfaces coated with one or more fluorocarbon polymers, in combination with one or more non-fluorocarbon polymers, for dispensing an inhalation drug formulation comprising salmeterol, or a salt thereof, and a fluorocarbon propellant, optionally in combination with one or more other pharmacologically active agents and one or more excipients.

Abstract: The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation, ##STR1## wherein R.sub.1 to R.sub.6 represent various substituents.