Abstract: Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is S02; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g.

Abstract: Particles of a substantially water insoluble biologically active substance, such as Cyclosporin, are loaded with a charged glyceryl ester as an electrostatic stabilizer which imparts to the particles a zeta potential and having an active substance:stabilizer weight ratio of 1:1 to 400:1 and an average particle diameter of 1 nanometer to 10 micrometers. Compositions having such particles are found to be useful delivery systems.

Abstract: The invention relates to an apparatus for the photo-initiated chemical cross-linking of material (28). To form one or more mouldings the material is enclosed in an optically transparent mould (26). The apparatus has at least one light source (12), for example a pulsed UV light source by which the material (28) can be acted upon by a light that triggers the cross-linking. The region to be cross-linked in the mould (26) is determined at least partially by beam-delimiting elements (20, 22) between the light source (12) and the mould (26). That can be achieved by arranging between the light source (12) and the mould (26) a mask (20) having transparent and non-transparent surface portions. The mask (20) is then projected onto the material (28) that is enclosed in the mould (26) by projection optics (24). The projection of the mask (20) onto the material is effected in a telecentric beam path.

Abstract: The invention relates to novel composite materials comprising (a) an inorganic or organic bulk material having covalently bound to its surface initiator moieties for radical polymerization; and (b) a hydrophilic surface coating obtainable by applying one or more different ethylenically unsaturated hydrophilic macromonomers of formula (1) as outlined in the claims to the bulk material surface provided with the initiator radicals and polymerizing said macromonomers. The composite materials of the invention have desirable characteristics regarding adherence to the substrate, durability, hydrophilicity, wettability, biocompatibility and permeability and are thus useful for the manufacture of biomedical articles such as ophthalmic devices.

Abstract: The present invention relates to novel crosslinkable amphiphilic block copolymers of formula wherein the variables are as defined in the claims, a process for their preparation and their use for the manufacture of mouldings. The block copolymers of the invention are especially useful for the manufacture of ophthalmic mouldings such as in particular contact lenses.

Abstract: The invention provides an isolated inflammation-related gene, the protein molecule encoded by the gene, and the use of the gene in diagnosis and treatment of inflammatory conditions.

Abstract: Novel derivatives of rapamycin, particularly 9-deoxo-rapamycins, 26-dihydro-rapamycins, and 40-O-substituted and 28,40-O,O-disubstituted rapamycins. are found to have pharmaceutical utility, particularly as immunosuppressants.

Abstract: The present invention is directed to an ophthalmic product comprising, as a colouring agent, the extract of an alga. A preferred class of alga the extract of which is useful in the present invention is blue alga (Spirulina type), more preferred it is Japanese blue alga (Spirulina platensis). The ophthalmic product is preferably a contact lens care product.

Abstract: TADDOL dendrimers are described. Their use as crosslinkers in polymerisation reactions and the use of Ti salts of polymer-bound TADDOL dendrimers as catalysts in enantioselective addition reactions is disclosed.

Abstract: The present invention describes coated articles and methods for preparing such articles, wherein the primary coating comprises a plasma-induced polymer carrying reactive groups. The invention further relates to the reaction of said primary coatings carrying reactive groups with monomeric, oligomeric or macromolecular compounds of synthetic, semisynthetic or biological origin to provide hybrid-type coated articles (secondary coatings).

Abstract: Compounds of the formula I as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, particularly inflammatory airways diseases. They are particularly useful in reducing post-surgical inflammation, especially that resulting from transplant surgery.

Abstract: The present invention relates to certain N-(substituted glycyl)-2-cyanopyrrolidines of formula I wherein Y is as defined herein, in free form or in acid addition salt form. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

Abstract: An oral dosage form comprising fluvastatin and HPMC, which oral dosage form is color-stable upon prolonged periods of storage.

Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.

Abstract: Methods for the prevention and treatment of colorectal cancer are provided. Specifically, the method relates to the administration of an effective adenoma or microadenoma preventing amount of 6-fluoroursodeoxycholic acid (6-FUDCA) or a pharmaceutically acceptable salt or pharmaceutically acceptable conjugate thereof to a mammal in need of such treatment. The methods find general use in the prevention of the formation of secondary bile acids, the reduction of deoxycholic acid, and the protection against cytotoxic effects of other bioacids and carcinogens.

Abstract: Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.

Abstract: Fusion polypeptides and salts thereof comprising at least one IgE-binding domain fused to at least one human serum albumin component, optionally via a peptide linker, and in particular, dimeric fusion polypeptides comprising HSA protein fused, at each of its amino and carboxy termini, to an extracellular domain of the &agr;-chain of the human high affinity receptor for IgE (Fc&egr;RI&agr;); process for the preparation thereof, functionally equivalent polypeptides which are intermediates in their preparation, and polynucleotide and oligonucleotide intermediates and vectors therefor. They are indicated for use in the prevention and/or treatment of IgE-mediated allergic diseases and related disorders such as atopic dermatitis, atopic asthma and chronic urticaria.

Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.

Abstract: 33-Epichloro-33-desoxyascomycin of formula I and various tautomeric or forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula I, or compound of formula I in other than Form A, or compound of formula I in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.

Abstract: A pharmaceutical composition in the form of an emulsion preconcentrate for oral administration and containing a cyclosporin. The pharmaceutical composition has a carrier medium for the cyclosporin that contains a hydrophilic organic solvent; a mixed mono-, di-, and tri-glyceride or a transesterified and polyethoxylated vegetable oil; and a polyoxyethylene-sorbitan-fatty acid ester surfactant. The pharmaceutical composition provides high bioavailability and low inter- and intra-subject variability.