Abstract: A polymeric prodrug is described which comprises at least one polymer attached via at least one permanent bond to a bicine linker. The bicine linker is attached via a temporary linkage to an amine containing biologically active moiety. The amine containing biologically active moiety—such as a drug—can be released by cleaving the temporary linkage.

Abstract: Methods for discriminating between fully complementary hybrids and those that differ by one or more base pairs and libraries of unimolecular, double-stranded oligonucleotides on a solid support. In one embodiment, the present invention provides methods of using nuclease treatment to improve the quality of hybridization signals on high density oligonucleotide arrays. In another embodiment, the present invention provides methods of using ligation reactions to improve the quality of hybridization signals on high density oligonucleotide arrays. In yet another embodiment, the present invention provides libraries of unimolecular or intermolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA.

Abstract: A cascade carrier linked prodrug is described which comprises a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.

Abstract: The present invention relates to binding surfaces for the immobilization of ligands, ligand surfaces and structured surface arrays which present a plurality of identical or different ligands. The invention further relates to a process for the production and the use of such surfaces and to specific binder molecules which can be used for the preparation thereof.

Abstract: The application relates to a composition comprising a hyperbranched polymer attached to a core and a biologically active moiety. The biologically active moiety is attached to the core by means of a substantially non-enzymatically cleavable linker L. The composition can be used to deliver the biologically active moiety to its target.

Abstract: Methods for discriminating between fully complementary hybrids and those that differ by one or more base pairs and libraries of unimolecular, double-stranded oligonucleotides on a solid support. In one embodiment, the present invention provides methods of using nuclease treatment to improve the quality of hybridization signals on high density oligonucleotide arrays. In another embodiment, the present invention provides methods of using ligation reactions to improve the quality of hybridization signals on high density oligonucleotide arrays. In yet another embodiment, the present invention provides libraries of unimolecular or intermolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA.

Abstract: A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.

Abstract: Methods for discriminating between fully complementary hybrids and those that differ by one or more base pairs and libraries of unimolecular, double-stranded oligonucleotides on a solid support. In one embodiment, the present invention provides methods of using nuclease treatment to improve the quality of hybridization signals on high density oligonucleotide arrays. In another embodiment, the present invention provides methods of using ligation reactions to improve the quality of hybridization signals on high density oligonucleotide arrays. In yet another embodiment, the present invention provides libraries of unimolecular or intermolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA.

Abstract: The invention relates to a device for carrying out an almost simultaneous synthesis of a plurality of samples. The device is especially suitable for use in automated laboratory processes in the area of combinatorial chemistry. The aim of the invention is to provide a device of this type which enables the synthesis of a plurality of samples bonded to microbeads, said microbeads being provided in the cavities of a support plate. To this end, a plane support plate (1) is provided with a plurality of cavities (11) arranged regularly in an iterative grid. The cavities accommodate microbeads (12). A removable covering (2) is provided, said covering being provided with webs (21) which each cover at least one of a row of associated cavities (11) in such a way that a capillary gap (3) is formed between the microbeads (12) and the webs (21) and larger recesses (22) are left respectively between the adjacent webs (21). A dosed liquid dispenser (4) is allocated to each capillary gap (3).

Abstract: Libraries of unimolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA. In a related aspect, the present invention provides libraries of conformationally restricted probes on a solid support. The probes are restricted in their movement and flexibility using double-stranded oligonucleotides as scaffolding. The probes are also useful in various screening procedures associated with drug discovery and diagnosis. The present invention further provides methods for the preparation and screening of the above libraries.

Abstract: The present invention relates to sensors for the detection of molecular interactions between immobilized ligands and non-immobilized interaction partners (receptors). These surfaces use novel ligand-anchor conjugates which allow highly specific interaction with suitable interaction partners. Furthermore the invention relates to methods of providing the sensing surface and in particular methods of synthesising the ligand-anchor conjugates (LAC).

Abstract: Libraries of unimolecular, double-stranded oligonucleotides on a solid support. These libraries are useful in pharmaceutical discovery for the screening of numerous biological samples for specific interactions between the double-stranded oligonucleotides, and peptides, proteins, drugs and RNA. In a related aspect, the present invention provides libraries of conformationally restricted probes on a solid support. The probes are restricted in their movement and flexibility using double-stranded oligonucleotides as scaffolding. The probes are also useful in various screening procedures associated with drug discovery and diagnosis. The present invention further provides methods for the preparation and screening of the above libraries.

Abstract: Disclosed is a method for the identification of active compounds interacting with a target molecule, comprising the steps of: (a) forming a binding matrix comprising at least two different ligands on a solid support by immobilising said ligands via a common intermediate molecule on the support; (b) contacting a target of interest with said binding matrix; (c) parallely determining a binding value of the ligand/target interaction for each type of ligand comprised in the binding matrix; (d) selecting those ligands the binding value of which in an immobilised state with the target exceeds a predetermined threshold; (e) replacing the common intermediate molecule by a replacing fragment in order to form new ligands of increased molecular weight, with the replacing fragment being coupled to the ligand(s) of step (d) at the common binding position between the ligand and the intermediate molecule; (f) determining the affinity of the ligands formed in step (e) towards the target.

Abstract: The present invention relates to binding surfaces for the immobilization of ligands, ligand surfaces and structured surface arrays which present a plurality of identical or different ligands. The invention further relates to a process for the production and the use of such surfaces and to specific binder molecules which can be used for the preparation thereof.

Abstract: The invention relates to an an SPR surface plasmon resonance spectroscopy sensor for parallel measurement of a plurality of samples, comprising a body (1a) having several SPR sensor areas (2) for guiding radiation in order to carry out SPR measurements and which are coated with a material which is suitable for SPR in such a way that each SPR sensor area (2) can be exclusively associated with a single sample. The radiation conducting body (1a) forms a unit with the SPR sensor areas (2), whereby the path of the rays guided by the SPR sensor areas (2) can also extend through the radiation conducting body (1a).

Abstract: The invention relates to an SPR sensor array comprising a plurality of SPR sensor surface areas (120) arranged on a substrate (10, 20) in a two-dimensional matrix located in a plane to which the SPR sensor surface areas (120) are parallel and whereby radiation capable of exciting surface plasmons in the SPR sensor surface areas (120) under specific physical conditions can be guided through the substrate (10, 20) to be reflected from the SPR sensor surface areas, as well as separating means (110) for separating each SPR sensor surface area (120) from its neighboring SPR sensor surface area (120), wherein the separating means (110) and SPR sensor surface areas (120) are provided such that at least outside of surface plasmon resonance occurring in the SPR sensor surface areas (120) the radiation (40) guided through the substrate (10, 20) is reflected in the region of the separating means to a different degree than in the region of the SPR sensor surface areas (120) to create a contrast between the separating mea

Abstract: A parallel high throughput screening method on a solid support is disclosed that allows the detection of low affinity binding partners, comprising the steps of:(a) providing a library of different ligands;(b) forming a binding matrix comprising the ligands on a solid support by immobilising said ligands on the support; (c) contacting a target of interest with said binding matrix; (d) parallely determining a binding value of the ligand/target interaction for each type of ligand comprised in the binding matrix; (e) selecting those ligands the binding value of which in an immobilised state towards the target exceeds a predetermined threshold; (f) evaluating the affinity of each of the ligands selected in step (e) in a non-immobilised state towards the target; (g) identifying at least one ligand of step (f) as low affinity binding ligand.

Abstract: The invention relates to a device and a method for picking up individual objects or particles and placing them in containers or cavities filled with liquid. The invention allows in particular a simple handling of the objects and thus considerably reduces the operation costs of such a plant (FIG. 2). In this method and device, an adhesive is applied to an end portion of a transport structure. An object to be transported is held by the adhesive until it is delivered to the desired location.

Abstract: The present invention relates to binding surfaces for the immobilization of ligands, ligand surfaces and structured surface arrays which present a plurality of identical or different ligands. The invention further relates to a process for the production and the use of such surfaces and to specific binder molecules which can be used for the preparation thereof.

Abstract: The invention relates to an an SPR surface plasmon resonance spectroscopy sensor for parallel measurement of a plurality of samples, comprising a body (1a) having several SPR sensor areas (2) for guiding radiation in order to carry out SPR measurements and which are coated with a material which is suitable for SPR in such a way that each SPR sensor area (2) can be exclusively associated with a single sample. The radiation conducting body (1a) forms a unit with the SPR sensor areas (2), whereby the path of the rays guided by the SPR sensor areas (2) can also extend through the radiation conducting body (1a).