Abstract: The invention relates to a compound of formula (I) wherein A1, R1, R2, R3, R4 and R5 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention relates to oligonucleotides that are capable of inducing expression of ubiquitin-protein ligase E3A (UBE3A) from the paternal allele in animal or human neurons. The oligonucleotides target the suppressor of the UBE3A paternal allele by hybridization to SNHG14 long non-coding RNA downstream of SNORD109B. The present invention further relates to pharmaceutical compositions and methods for treatment of Angelman syndrome.

Abstract: The invention comprises a process for the preparation of a [Ru(OAc)2(Ligand)] catalysts of the formula I wherein R1 is C1-6 alkyl and R3 is hydrogen or C1-6 alkyl and R4 is hydrogen or C1-6-alkoxy. [Ru(OAc)2(Ligand)] catalysts are versatile hydrogenation catalysts.

Abstract: Herein is reported a method for the enzymatic preparation/production of an antibody with a modified glycosylation in the Fc-region comprises the steps of incubating an antibody that has a glycosylation in the Fc-region with one or more enzymes for a time sufficient and under conditions suitable to modify the glycosylation of the Fc-region to a defined form, separating in one or more chromatography steps the antibody with a modified glycosylation in the Fc-region from the one or more enzymes and thereby producing the antibody with a modified glycosylation in the Fc-region and one or more recycled enzymes, and repeating the incubating step with the one or more recycled enzymes at least once.

Abstract: The invention provides a novel process for manufacturing a compound of formula (I), or a salt thereof, wherein PG1, PG2 and PG3 are amino protective groups. The process according to the invention is particularly suitable for large-scale manufacturing under GMP conditions.

Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one useful as pharmaceutically active compounds.

Abstract: The present invention relates to antibodies and Fc-region fusion polypeptides which are asymmetrically modified with respect to their Fc-receptor, especially their FcRn, and methods of using the same.

Abstract: The invention relates to novel TNF family ligand trimer-containing antigen binding molecules comprising (a) at least one moiety capable of specific binding to a target cell antigen and (b) a first and a second polypeptide that are linked to each other by a disulfide bond, characterized in that the first polypeptide comprises two ectodomains of a TNF ligand family member or fragments thereof that are connected to each other by a peptide linker and in that the second polypeptide comprises only one ectodomain of said TNF ligand family member or a fragment thereof.

Abstract: The invention provides new heterocyclic compounds having the general formula (I) wherein A and R1 to R4 are as described heroin, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Abstract: The present invention relates to the combination therapy of a bispecific antibody which binds human TYRP1 and CD3 and a second TYRP1-specific antibody.

Abstract: The application relates to devices and methods for determining an administration regimen of a drug to a subject. Determining an administration regimen for a subject comprises computing the amount of drug to be administered to the subject per elemental period of time, and determining and evaluating combinations of at least two dosage forms that can be used to administered the amount of drug, against at least two different criteria. The methods of the invention find applications in the selection of administration regimen for drugs that are available in multiple dosage forms, and especially drugs that are administered routinely over prolonged periods, such as e.g. in the routine prophylaxis of haemophilia.

Abstract: The present invention relates to oligonucleotides that are capable of inducing expression of ubiquitin-protein ligase E3A (UBE3A) from the paternal allele in animal or human neurons. The oligonucleotides target the suppressor of the UBE3A paternal allele by hybridization to SNHG14 long non-coding RNA downstream of SNORD1091B. The present invention further relates to pharmaceutical compositions and methods for treatment of Angelman syndrome.

Abstract: The present invention generally relates to improved Protease-activatable antigen-binding molecules that comprise an anti-idiotype-binding moiety which reversibly masks a CD3 antigen binding moiety of the molecule. Furthermore, the invention relates to novel Protease-cleavable peptide linkers and their used in such Protease-activatable antigen-binding molecules. In addition, the present invention relates to polynucleotides encoding such Protease-activated T cell binding molecules, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the Protease-activated T cell binding molecules of the invention, and to methods of using the same, e.g., in the treatment of disease.

Abstract: The present invention generally relates to antibodies that bind to CD3, including multispecific antibodies e.g. for activating T cells. In addition, the present invention relates to polynucleotides encoding such antibodies, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the antibodies, and to methods of using them in the treatment of disease.

Abstract: The current invention is directed to a method for determining homodimeric avid-binding side-products of a bispecific antibody in a sample comprising the correctly assemble heterodimeric affine-binding bispecific antibody and the mis-assembled homodimeric avid-binding side-product of the bispecific antibody using surface plasmon resonance, wherein the correctly assembled heterodimeric affine-binding bispecific antibody comprises one or more binding site for a first antigen and one or more binding sites for a second antigen, wherein the mis-assembled homodimeric avid-binding side-product of the bispecific antibody comprises two or more binding sites to the first antigen but at least more than the correctly assembled bispecific antibody, wherein the correctly assembled bispecific antibody is a heterodimer and the mis-assembled bispecific antibody is a homodimer, wherein the presence of the homodimeric avid-binding side-product is determined if residual binding, i.e.

Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3 and R4 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: Herein is reported an anti-transferrin receptor antibody that specifically binds to human transferrin receptor and cynomolgus transferrin receptor, which comprises i) a humanized heavy chain variable domain derived from the heavy chain variable domain of SEQ ID NO: 01, and ii) a humanized light chain variable domain derived from the light chain variable domain of SEQ ID NO: 26, wherein the antibody has an off-rate for the human transferrin receptor that is equal to or less than (i.e. at most) the off-rate of the anti-transferrin receptor antibody 128.1 for the cynomolgus transferrin receptor, whereby the off-rates are determined by surface plasmon resonance, and whereby the anti-transferrin receptor antibody 128.1 has a heavy chain variable domain of SEQ ID NO: 64 and a light chain variable domain of SEQ ID NO: 65.

Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided.

Abstract: Methods for facilitating selection of cell lines for production of recombinant proteins are disclosed. In particular, disclosed is the use of machine learning models trained on multiomics data to predict one or more values indicative of the titre and/or quality of a recombinant protein expressed by different cell lines, enabling ranking the cell lines based on the predicted values and selecting those predicted to produce the recombinant protein with higher titre and/or higher quality.

Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.