Abstract: The present invention relates to drug formulations for the stabilization of amorphous forms of drugs. In particular the present invention relates to pharmaceutical compositions comprising sponge-like carrier matrices, particularly polyelectrolyte complexes or porous particles. The invention also relates to methods for the production of such pharmaceutical compositions.

Abstract: A method for making an article comprising a core material and a coating thereon, the method comprising the steps of: (a) providing the core material; (b) applying one or more layers of a crosslinkable polycationic material, wherein the polycationic material is a reaction product of: (i) an epoxide of formula (I) wherein X equals bromo, chloro, iodo, or cyano, and R1, R2, R3, R4, independently of one another, are selected from the group consisting of hydrogen, linear or branched C1-C6-alkyl, and linear or branched C1-C6-alkyl which is substituted with halogen, and (ii) a polymer having repeating units comprising one or more secondary or tertiary amine group(s); (c) applying one or more layers of a polyanionic material; and (d) cross-linking the layers of polyelectrolytes formed by steps (b) and (c).

Abstract: The present invention relates to amino acid sequences that are directed against proteins from the group of the Angiopoietin/Tie family such as Tie1, Tie2, Ang1, Ang2, Ang3, Ang4, Angptl1, Angptl12, Angptl13, Angptl14, Angptl15, Angptl16, as well as to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consist of one or more of such amino acid sequences.

Abstract: The present invention relates to a method for the production of a nanoparticulate pharmaceutical composition. The method comprises the steps of a) suspending in water a poorly soluble active ingredient without the presence of a detergent, b) mechanically treating said suspension to obtain particles comprising the active ingredient with an effective average size of less than about 5000 nm, c) contacting said active ingredient or suspension with a first polyelectrolyte during and/or before mechanically treating, d) optionally contacting said suspension with a one or more second or further polyelectrolytes during, before and/or after mechanically treating, e) optionally drying said suspension. The invention also pertains to the pharmaceutical compositions obtained by the method of the invention.

Abstract: The present invention relates to amino acid sequences that are directed against receptors for growth factors, compounds comprising such sequences, as well as nucleic acid sequences encoding the same. In one embodiment the invention relates to amino acid sequences that bind to a receptor tyrosine kinase. The receptor tyrosine kinase and/or growth factor receptor may be of human origin. In one embodiment the amino acid sequences are Nanobodies™.

Abstract: The present invention relates to particular polypeptides, nucleic acids encoding such polypeptides; to methods for preparing such polypeptides; to host cells expressing or capable of expressing such polypeptides; to compositions and in particular to pharmaceutical compositions that comprise such polypeptides, for prophylactic, therapeutic or diagnostic purposes.

Abstract: The invention relates to immunoglobulin single variable domains directed against specific human CXCR4 epitopes (herein also referred to interchangeably as “compounds of the invention”, “amino acid sequences of the invention”, or “building blocks of the invention”) and polypeptides comprising them (herein also referred to as “polypeptides of the invention”, “compounds of the invention”, or “constructs of the invention”).

Abstract: Polypeptides that bind to IL-23R including polypeptides having a multimerizing, e.g. trimerizing, domain and a polypeptide sequence that binds IL-23R. The multimerizing domain may be derived from human tetranectin. IL-23R binding polypeptides inhibit activation of IL-23R by native IL-23 and can be used as therapeutics agents for a variety of immune related disorders and cancers. Methods for selecting polypeptides and preparing multimeric complexes are described.

Abstract: The invention relates to phytotoxic halogenated derivatives of benzoxazinones. The aim of the invention relates to the production of novel phytosanitary products that are suitable for agricultural weed control, based on natural chemical substances. The invention comprises novel chemical compounds having high levels of phytotoxic activity and the preparation methods thereof. Said substances are derived from natural products with the 1,4-benzoxazin-3-one skeleton involved in different chemical defense interactions in plants. The inventive compounds have suitable phytotoxic activity levels for use in weed control and for use as stable models for the development of novel phytosanitary products based on the 1,4-benzoxazin-3-one skeleton.

Abstract: The invention relates to salts of the active ingredient clopidogrel with polyanions. The salts are predominantly in amorphous form, and the polyanions have at least 4 negative charges.

Abstract: Method for the chemical synthesis of capsinoids, natural compounds with proven biological activity, from vanillin, comprising the protection of the alcohol group thereof, reduction of the aldehyde to alcohol, esterification of same and deprotection of the first protected alcohol group. In this way, the desired compounds are generated with high purity and said compounds can be easily separated with no mixing owing to the competitive esterification on the aromatic ring.

Abstract: The present invention relates to a method for generating immunoglobulin sequences against cell-associated antigens, more particularly, antigens that are membrane-anchored. The invention also provides immunoglobulin sequences obtainable by the method of the invention. Specifically, the present invention relates to the generation of immunoglobulin sequences by use of DNA vaccination. More specifically, the present invention relates to generation of immunoglobulin sequences in camelids, preferably directed against cell-associated antigens, in particular antigens with multiple transmembrane spanning domains, including GPCRs and ion channels, by DNA vaccination. Furthermore, the present invention relates to said immunoglobulin sequences against cell-associated antigens, more particularly, antigens that are membrane-anchored, such as e.g. GPCRs and ion channels, more preferably ion channels.

Abstract: The present invention is related to the field of immunology and more specifically to cancer immunotherapy, particularly with immunotherapeutic combinations and treatment methods to prevent tumor cell growth and/or to eliminate those cells. The methods described in the present invention are based on the blockade of receptors with protein kinase activity in tyrosine residues (Receptor Tyrosine Kinases, RTK) and of ligands for those receptors. Immunotherapeutic combinations are described that cause the blockade of RTK receptors and/or their ligands, by means of a combination of passive and active immunotherapy. The referenced procedures can be applied to patients in different clinical stages with tumors of epithelial origin that over-express those receptors. The combination of active and passive immunotherapy can be simultaneous or sequential independent of whether the therapeutic procedure will be used in patients with advanced disease or as adjuvant therapy.

Abstract: A method for the manufacture of refractive optical elements includes (a) placing a substrate close to a starting material, both arranged inside a chamber; (b) vaporizing or subliming the starting material by means of light irradiation; and (c) depositing this vapour phase on the substrate. The coating deposited has a refractive optical functionality on account of its composition and profile and also presents an increase in the threshold of damage at high light intensities.

Abstract: A method and related apparatus for registering diffractive optical structures, in which: (a) a transparent substrate is positioned next to a starting material inside a chamber, (b) the starting material is vapourised or sublimated, (c) the vapour phase is deposited on the substrate, and (d) the area of the substrate on which the vapour phase was deposited is irradiated concurrently with a random distribution of the light intensity. The deposit has a diffractive optical functionality owing to the local changes produced in its structure, which are controlled by the distribution of the light intensity used in the production process.

Abstract: A chemically anchorable fastening element (6), includes a holding section (16; 56) for contacting a wall of a borehole (6) and provided with a thread-tapping outer thread (19) and with a load application element (18; 58), a connection section (26; 66) adjoining the holding section (16; 56) and having a smaller radial dimensions than the holding section (16; 56), and an anchoring section (36; 76) adjoining the connection section (26; 66) and likewise having smaller radial dimensions than the holding section (16; 56).

Abstract: A method for making an article comprising a core material and a coating thereon, the method comprising the steps of: (a) providing the core material; (b) applying one or more layers of a crosslinkable polycationic material, wherein the polycationic material is a reaction product of: (i) an epoxide of formula (I) wherein X equals bromo, chloro, iodo, or cyano, and R1, R2, R3, R4, independently of one another, are selected from the group consisting of hydrogen, linear or branched C1-C6-alkyl, and linear or branched C1-C6-alkyl which is substituted with halogen, and (ii) a polymer having repeating units comprising one or more secondary or tertiary amine group(s); (c) applying one or more layers of a polyanionic material; and (d) cross-linking the layers of polyelectrolytes formed by steps (b) and (c).

Abstract: Devices useful in the delivery of DNA encoding neurotrophic agents, anti-fibrotic agents, and related compositions are disclosed herein for use in the treatment of central and/or peripheral nervous system injury. Methods of making and using the disclosed devices and DNA are also described. In various embodiments, the invention also discloses compositions and devices that may further include a targeting agent, such as a polypeptide that is reactive with an FGF receptor (e.g., bFGF), or another ligand that binds to cell surface receptors on neuronal cells, or a support cell. The invention also discloses methods of promoting neuronal survival and regeneration via transfection of an axon as it grows through a device or composition of the present invention, or via transfection of a repair cell.

Abstract: An expansion anchor has an anchor member (21; 51) that has a longitudinal bore (24), a load application element (25, 55) and an expansion section (22; 52) located between first and second sections (26, 27; 56, 57) of the anchor member (21) and a cross-section of which widens from the first section (26; 56) toward the second section (27; 57; and an expansion sleeve (13; 43) having an axial longitudinal bore (14) with which it is guided over the first section (26; 56) of the anchor member (21; 41) and an expansion region (15) located adjacent to the expansion section (22; 52) of the anchor member (21; 41), with at least one of the anchor member (21; 41) and the expansion sleeve (13; 43) having at least one through-opening (18; 58) for a hardenable mass (31) and which opens into one of the axial bore (54) of the anchor member or the axial bore (14) of the expansion sleeve.

Abstract: A pharmaceutical composition for malignant tumour embolisation comprises a polymer and, associated with the polymer in a releasable form, a COX inhibitor, e.g. a non-steroidal anti inflammatory drug, such as ibuprofen. The polymer is preferably-in particulate form, such as in the form of microspheres. A suitable polymer is a crosslinked polyvinyl alcohol polymer formed by the copolymerisation of PVA macromer with other ethylenically unsaturated monomers. The composition provides a synergistic treatment for the symptoms of malignant tumours, leading to tumour necrosis or ischaemia, with anti-angiogenic effects, promotion of apoptosis, decrease in invasiveness of tumour cells and resultant tumour regression.