Abstract: An objective of the present invention is to provide low-molecular-weight compounds that can inhibit Src family kinases. The present invention relates to compounds represented by general formula (I) or pharmacologically acceptable salts thereof. In the formula, Ar1 is optionally substituted C6-10 arylene or 5- to 10-membered heteroarylene, and Ar2 is optionally substituted C6-10 aryl or 5- to 10-membered heteroaryl. R1 and R2 are defined as described in the specification.

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

Abstract: Methods of treating joint damage in a subject eligible for treatment are provided involving administering an antagonist that binds to a B-cell surface marker, such as CD20 antibody, to the subject in an amount effective to slow progression of the joint damage as measured by radiography. Further provided are articles of manufacture useful for such methods.

Abstract: The training device for medicine injection devices comprises a plunger slidably arranged in the cavity of a body. The plunger comprises a compressible element arranged at a distal end of the plunger and adapted to provide a resistance between compressible element and inner wall if the cavity of the body when the plunger is moved in the cavity towards the distal end of the body. The resistance corresponds to an injection resistance of a medicine injected into a patient. The invention also comprises a reset device for resetting the training device from a used status to a condition for reuse.

Abstract: An objective of the present invention is to provide an effective pharmaceutical composition or a dosage regimen for preventing and/or treating bleeding, a disease accompanying bleeding, or a disease caused by bleeding. The inventors discovered that by administering a pharmaceutical composition comprising a bispecific antigen-binding molecule that recognizes (a) blood coagulation factor IX and/or activated blood coagulation factor IX and (b) blood coagulation factor X and/or activated blood coagulation factor X according to a given dosage regimen, bleeding, a disease accompanying bleeding, or a disease caused by bleeding can be prevented and/or treated more effectively.

Abstract: The present invention relates to a process for producing crystalline and amorphous forms of a diazabicyclooctane derivative represented by Compound (I) and methods for producing the same.

Abstract: An objective of the present invention is to provide low-molecular-weight compounds that can inhibit Src family kinases. The present invention relates to compounds represented by general formula (I) or pharmacologically acceptable salts thereof. In the formula, Ar1 is optionally substituted C6-10 arylene or 5- to 10-membered heteroarylene, and Ar2 is optionally substituted C6-10 aryl or 5- to 10-membered heteroaryl. R1 and R2 are defined as described in the specification.

Abstract: Fixed dose HER2 antibody formulations for subcutaneous administration are provided along with their use in the treatment of cancer. The formulations include fixed dose subcutaneous formulations of pertuzumab and subcutaneous co-formulations of pertuzumab and trastuzumab, and their use in the treatment of cancer.

Abstract: The present invention relates to variable domains of a camelid heavy-chain antibodies directed against a phosphorylated tau protein and conjugates thereof. The present invention also relates to the use of these domains or conjugates for treating or diagnosing disorders mediated by neurofibrillary tangles, neuropil threads or dystrophic neurites, such as tauopathies.

Abstract: Herein is reported a method for producing an antibody preparation comprising the steps of a) applying a buffered solution comprising different isoforms of an antibody to a cation exchange chromatography material, b) applying a first solution with a first conductivity to the cation exchange chromatography material, whereby the antibody isoforms remain bound to the cation exchange chromatography material, and c) applying a second solution with a second conductivity to the cation exchange chromatography material and thereby obtaining the antibody preparation, whereby the conductivity of the second solution exceeds the conductivity of the first solution by not more than 10%.

Abstract: Methods are provided for the adjuvant treatment of operable HER2-positive primary breast cancer in human patients by administration of pertuzumab in addition to chemotherapy and trastuzumab. The methods reduce the risk of recurrence of invasive breast cancer or death for a patient diagnosed with HER2-positive early breast cancer (eBC) compared to administration of trastuzumab and chemotherapy, without pertuzumab.

Abstract: Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Provided herein are compounds of Formula (I): and forms thereof, including compositions thereof and uses therewith for treating spinal muscular atrophy.

Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Abstract: A method for determining a biological response of a target (41, 42) to a soluble candidate substance includes the steps: introducing a soluble candidate substance into a laminar flow of a buffer liquid (2) to form a candidate substance solute (3) having an initial concentration profile (31); dispersing the initial concentration profile (31) to form a dispersed concentration profile (32); directing the dispersed concentration profile (32) into a detection channel (12) to form a final symmetrical concentration profile (33) therein; introducing a target into the detection channel (12) to obtain a combined concentration profile including a constant target concentration profile overlying the final symmetrical concentration profile (33); holding in the detection channel (12) at least one half of the combined concentration profile; and optically scanning the combined concentration profile to detect an optical signal representative of the biological response of the target to the soluble candidate substance.

Abstract: An apparatus (2) for the automatic testing of substances for carcinogenicity comprises: a plate support (3) on which at least one micro-well plate (1) can be placed; a movable pipetting unit (4) comprising a predetermined number of pipettes (40); a number of containers (5) containing a liquid culture medium (50), the number of containers (5) corresponding to the number of pipettes (40) of the pipetting unit (4); a dish support (6) on which a corresponding number of dishes (60) can be placed, each having a bottom and an upstanding side wall (601); a plurality of spinners (63) for spinning the dishes (60); a plurality of suction cups (62) for placing a lid (600) on each of the dishes; and a plurality of laterally arranged belts (64,65) for transporting the closed dishes (60) to an intermediate storage (8).

Abstract: A method for training staff for quality control when filling amorphous products into primary packaging. The method includes a provision step during which a test set having a plurality of primary packages filled with an amorphous product is provided, wherein at least one of the filled primary packages is afflicted by a contaminant comprising a fluorescent marker. A training step includes presenting the test set to a person to be trained, who carries out a visual quality control for detecting contaminants. The result of the training step is documented. A verification step is conducted during which the test set is irradiated by excitation light, wherein fluorescing contaminants are detected and the result of the verification step is documented. A comparison step is done during which the result of the training step and the result of the verification step are compared. Also disclosed is an inventive test kit and test set.

Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.

Abstract: A method is provided for determining the efficacy of GPC3-targeting drug therapy for cancer in a patient before the start of GPC3-targeting drug therapy or for determining the continuation of GPC3-targeting drug therapy for a patient treated with GPC3-targeting therapy. The method includes determining the number of an immunocyte or an expression level of a molecule expressed on the immunocyte in a biological sample isolated from the patient before the start of GPC3-targeting drug therapy and/or the patient treated with the GPC3-targeting drug therapy, wherein when the number of the immunocyte or the expression level of the molecule expressed on the immunocyte is a predetermined value, the efficacy of the GPC3-targeting drug therapy is determined or the continuation of the GPC3-targeting drug therapy is determined. GPC3-targeting drugs and drug preparations for use according to the disclosed methods are also provided.