Abstract: This invention relates to a novel continuous process for making alkyl 7-amino-5-methyl-[1,2,5]-oxadiazolo¬[3,4-b]pyridine-carboxylate, wherein R is C1-3-alkyl. The process of the invention present invention overcomes disadvantages of processes of the prior art by avoiding the highly energetic intermediates, using readily available and inexpensive starting materials and reagents, and avoiding the isolation of intermediates. The process according to the invention is suitable for use on industrial scale.

Abstract: Provided herein are antibodies that selectively bind to complex comprising a non-classical HLA-I (e.g. HLA-E) and a neoantigen having variable heavy chain domains (VH), variable light chain domains (VL), and complementarity determining regions (CDRs) as disclosed herein, as well as methods and uses thereof.

Abstract: The present invention relates to compound of formula (I), wherein R1 is chloro, bromo iodo or a brosylate group. The present invention also relates to methods of making this compound and its use in carrying out organic transformations.

Abstract: The invention provides novel biparatopic LRP5/LRP6 cross-reactive binding polypeptides, and more specifically novel biparatopic LRP5/LRP6 cross-reactive immunoglobulin single variable domain constructs which can inhibit Wnt signaling pathways. The invention also relates to specific sequences of such polypeptides, methods of their production, and methods of using them, including methods of treatment of diseases such as cancer.

Abstract: The present invention relates to bicyclic heterocycle compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are inhibitors of CD38 and are useful in the treatment of cancer.

Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: The invention relates to a method for closed sampling from filling plants comprising the following steps in: filling a sample quantity into a container (1) with a wall (3); applying a reinforcing element (20) to the container (1) with the wall; introducing a fracture point (22) into the wall of the container (1) in the area of the reinforcing element (20); introducing a sampling attachment (30) with hollow tube (40) into the wall of the container (1) in the area of the fracture point (22); filling a sample container (50) connected to the hollow tube (40) once or several times; removing the sample container (50) from the hollow tube (40) and closing the sample container (50); removing the sampling attachment (30) with hollow tube (40) from the container; and sealing the fracture point (22) of the container in the area of the reinforcing element (20). The subject matter of the invention is also a sampling device, in particular for carrying out the method.

Abstract: The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing oxidative stress, for example in patients with type 1 or type 2 diabetes, as well as to the use of such SGLT-2 inhibitors in treatment and/or prevention of cardiovascular diseases in patients, for example type 1 or type 2 diabetes patients. The present invention further relates to certain SGLT-2 inhibitors for treating and/or preventing a metabolic disorder and preventing, reducing the risk of or delaying the occurrence of a cardiovascular event in patients, for example patients with type 1 or type 2 diabetes.

Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients with insufficient glycemic control despite a therapy with an oral and/or a non-oral antidiabetic drug.

Abstract: The present invention relates to certain DPP-4 inhibitors for treating and/or preventing oxidative stress, vascular stress and/or endothelial dysfunction as well as to the use of such DPP-4 inhibitors in treatment and/or prevention of diabetic or non-diabetic patients, including patient groups at risk of cardiovascular and/or renal disease.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The disclosure relates to compounds specific for IL23A and BAFF, compositions comprising the compounds, and methods of use thereof. Nucleic acids, cells, and methods of production related to the compounds and compositions are also disclosed.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: A nebulizer for nebulizing a fluid from a cartridge and a cartridge for such a nebulizer is proposed. The cartridge comprises a container containing the fluid to be nebulized and is fluidically connected to the nebulizer by inserting a connecting element of the nebulizer for conveying the fluid out of the container. The cartridge is preferably adapted to sealingly receive the connecting element and can optionally comprise a membrane or sealing wall which seals the cartridge initially and is piercable or breakable by the connecting element upon insertion. The cartridge can further comprise an at least partially flexible and/or bendable tube for conveying the fluid out of the container. The tube is preferably wettable with the fluid and/or comprises an at least partially hydrophilic and/or polar surface. Further, the tube can at least partially be shaped as a helix.

Abstract: The present disclosure provides certain 3H,4H,5H,6H,7H-pyrimido[4,5-b][1,4]oxazine-4,6-dione derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The present disclosure provides certain substituted 1,2,4-oxadiazole derivatives of the below formula (I) that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The present invention relates to novel agonistic anti-TrkB antibodies and therapeutic and diagnostic methods and compositions for using the same.

Abstract: The present disclosure provides certain uracil derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: Disclosed are heteroaromatic carboxamides of formula (I), wherein R, R1, A1, A2, L1, and L2 are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the compounds of formula (I) for treatment of diseases, which can be influenced by inhibition of plasma kallikrein.