Abstract: The invention describes the use of a PDE4 inhibitor in combination with BH4 or a BH4 derivative for the prevention and/or treatment of respiratory diseases.

Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R31, R4, R5, R51, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.

Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4-inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions for use, e.g., in treatment of airway disorders.

Abstract: The invention relates to compounds of formula 1 and formula 10 and to compositions comprising these compounds and methods of treating gastrointestinal disorders by administering these compounds.

Abstract: Novel administration forms and preparation for acid-labile active compounds are described. The novel administration forms contain individual active compound units, the active compound being present in the active compound units in a matrix made of a mixture comprising at least one fatty alcohol and at least one solid paraffin, in a matrix made of a mixture of a triglyceride and at least one solid paraffin or in a matrix made of a mixture comprising at least one fatty acid ester and at least one solid paraffin. In particular, the active compound units are microspheres which can be produced by prilling.

Abstract: The invention relates to novel pyrrolodihydroisoquinoline derivatives which are efficacious inhibitors of cellular (hyper)proliferation and/or inducers of apoptosis in cancer cells.

Abstract: Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, having reporters comprising gas-filled microbubbles stabilised by monolayers of film-forming surfactants, the reporter being coupled or linked to at least one vector.

Abstract: Separation of target material from a liquid sample is achieved by coupling the target to targetable encapsulated gas microbubbles, allowing the microbubbles and coupled target to float to the surface of the sample to form a floating microbubble/target layer, and separating this layer from the sample. In a positive separation process the microbubbles are then removed from the target, e.g. by bursting. In a negative separation process target-free sample material is recovered following separation of the floating layer. The method may also be used diagnostically to detect the presence of a disease marker in a sample. Novel separation apparatus is also described.

Abstract: Nucleoside analogues or base analogues having structure (1), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.

Abstract: Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, having reporters comprising gas-filled microbubbles stabilized by monolayers of film-forming surfactants, the reporter being coupled or linked to at least one vector.

Abstract: This invention relates to a set of aqueous marker compositions, each composition having a selected 1/Ti value which is substantially invariant over an at least 10° C. temperature range between 15 and 40° C. and preferably over an at least ±2% magnetic field strength range about a selected field strength value between 0.01 and 5T and comprising an aqueous matrix material having a non-zero 1/Ti temperature dependence within said temperature range with distributed therein a first paramagnetic material having a Ti relaxivity which is substantially invariant within said range(s) and/or a second paramagnetic material having within said ranges(s) and T1 relaxivity which has a non-zero temperature dependence of opposite polarity to the temperature dependence of 1/Ti of said matrix material, said set containing a plurality of said compositions with different selected 1/Ti values preferably encompassing at least the range 1.0 to 2.

Abstract: The invention provides a method of detecting myocardial ischemia in a human or a non-human body, said method comprising administering to said body a physiologically acceptable manganese complex or salt thereof, subjecting said body to a magnetic resonance imaging procedure capable of generating images with time intervals of less than 0.5 seconds and thereafter providing a series of images of the myocardium of said body whereby to identify regions of abnormal blood flow. The method in accordance with the invention is of use not only in detecting myocardial ischemia, but also in discriminating between reversibly and irreversibly injured myocardial tissues, thereby providing important information about myocardial viability, e.g. during or following a severe heart attack or coronary occlusion. The method of the invention also provides an effective means of monitoring reperfusion of the myocardium.

Abstract: The invention provides compounds comprising a linear, branched or dendrimeric polymer backbone with linked thereto at least one reporter moiety, said polymer backbone comprising a plurality of amine-containing acids. Such compounds may be linked to one or more targeting agents and are useful as therapeutic and diagnostic agents, in particular in medical imaging techniques.

Abstract: A process for the crystallisation of a sterically hindered organic compound from a saturated or supersaturated solution of said compound in a solvent therefor, characterised in that crystallisation is effected under elevated pressure at a temperature above the boiling point of said solution at atmospheric pressure and up to the boiling point of said solution at said elevated pressure.

Abstract: Oil-in-water emulsions in which the oil phase comprises condensed or dissolved oil-soluble gas/fluid or gas precursor are useful as ultrasound contrast agents. Such products contain insignificant amounts of free gas bubbles or microbubbles in their stored form and exhibit good stability, but may be designed to promote rapid microbubble generation immediately before or upon administration.

Abstract: The invention provides a composition of matter of the formula (I): V—L—R where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V—L—R is other than a non-metal radionuclide substituted peptide (e.g. 125I substituted angiotensin II) and L—V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.

Abstract: Tripodal chelating agents incorporating imine C.dbd.N bonds are disclosed for the formation of lanthanide and other metal complexes which are relatively stable in the presence of water at neutral pH.

Abstract: A method for the qualitative or quantitative determination of an analyte in a test sample wherein a labelled reagent is caused to be immobilized in bound form on a solid phase to provide an indication of the presence or quantity of the analyte in the same is disclosed and is characterized in that the labelled reagent comprises a gold sol bound to a substance capable of specifically binding to said analyte or to a specific binding partner therefor, at least 75% by weight of the gold particles of the gold sol having a mean diameter of less than 5 nanometers.