A method of verifying a program code of a synthesis computer program is disclosed. The synthesis computer program is configured for computer-controlling an automatic synthesizer (114) to automatically synthesize at least one oligonucleotide, the synthesis computer program having a plurality of program cycles for computer-controlling the automatic synthesizer (114) to sequentially synthesize the oligonucleotide by using at least one sequence of synthesis cycles. The method comprises:
i. applying an automatic parsing procedure to the program code of the synthesis computer program, the automatic parsing procedure comprising automatically searching for parameter values of parameters of at least one predetermined list of parameters of interest in the program cycles of the synthesis computer program; and
ii. automatically assembling a matrix of parameters comprising, for the program cycles of the synthesis computer program, the parameters of interest and the corresponding parameter values of the parameters of interest.
A method of verifying a program code of a synthesis computer program is disclosed. The synthesis computer program is configured for computer-controlling an automatic synthesizer (114) to automatically synthesize at least one oligonucleotide, the synthesis computer program having a plurality of program cycles for computer-controlling the automatic synthesizer (114) to sequentially synthesize the oligonucleotide by using at least one sequence of synthesis cycles. The method comprises:
i. applying an automatic parsing procedure to the program code of the synthesis computer program, the automatic parsing procedure comprising automatically searching for parameter values of parameters of at least one predetermined list of parameters of interest in the program cycles of the synthesis computer program; and
ii. automatically assembling a matrix of parameters comprising, for the program cycles of the synthesis computer program, the parameters of interest and the corresponding parameter values of the parameters of interest.
Further disclosed is a computer program and a computer-readable storage medium for performing the method of verifying a program code of a synthesis computer program, a system (110) for verifying a program code of a synthesis computer program and a method of synthesizing at least one oligonucleotide.
The present invention relates to the combination therapy of a bispecific antibody which binds human TYRP1 and CD3 and a second TYRP1-specific antibody.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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.
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.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
5.
QUANTIFICATION OF LOW AMOUNTS OF ANTIBODY SIDE-PRODUCTS
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. an increased SPR signal, can be determined in the dissolution phase of the SPR analysis.
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.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
7.
FOLR1 PROTEASE-ACTIVATABLE T CELL BISPECIFIC ANTIBODIES
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.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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.
Methods for selecting cell pools for production of recombinant proteins are disclosed. In particular, disclosed is the use of one or more genes whose expression level can be used as a biomarker to predict which cell pool, among a plurality of cell pools, produces a recombinant protein with higher titre and/or higher quality.
C12Q 1/6881 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for tissue or cell typing, e.g. human leukocyte antigen [HLA] probes
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
C12N 15/00 - Mutation or genetic engineeringDNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purificationUse of hosts therefor
11.
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
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.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
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.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to systems and methods to detect liver cirrhosis in digital images. Various embodiments of the present invention relate to systems and methods to detect liver cirrhosis in computed tomography (CT) scans and, more specifically but not limited, to systems and methods to detect liver cirrhosis via a model trained on highly-interpretable features.
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.
The present invention generally relates to chimeric receptors comprising an extracellular domain comprising a mutated Fc domain. The invention also relates to transduced immune cells expressing the chimeric receptors of the invention and/or nucleic acid molecules encoding the chimeric receptors of the present invention. Further provided are kits comprising such cells and/or nucleic acid molecules encoding the chimeric receptors, and antibodies capable of binding to the chimeric receptors.
C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07D 205/02 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 295/10 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
The invention provides new heteroaromatic compounds having the general formula (I′), or a solvate or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, and n are as defined herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
The invention provides new heteroaromatic compounds having the general formula (I′), or a solvate or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, and n are as defined herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention generally relates to immunoconjugates, particularly immunoconjugates comprising a mutant interleukin-2 polypeptide and an antibody that binds to PD-1. In addition, the invention relates to polynucleotide molecules encoding the immunoconjugates, and vectors and host cells comprising such polynucleotide molecules. The invention further relates to methods for producing the mutant immunoconjugates, pharmaceutical compositions comprising the same, and uses thereof.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention provides novel compounds having the general formula:
The present invention provides novel compounds having the general formula:
The present invention provides novel compounds having the general formula:
wherein ring A, ring B, ring C, bond a, and R1 to R7 are as described herein, or a pharmaceutically acceptable salt thereof, compositions including the compounds and methods of using the compounds.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
The present invention relates to a method for the generation of single stranded DNA (ssDNA) molecules from circular double stranded DNA (dsDNA) molecules.
C12N 15/66 - General methods for inserting a gene into a vector to form a recombinant vector using cleavage and ligationUse of non-functional linkers or adaptors, e.g. linkers containing the sequence for a restriction endonuclease
22.
TREATMENT OF NON SMALL CELL LUNG CANCER WITH ALECTINIB
The present invention relates to a method of treating anaplastic lymphoma kinase (ALK)- positive non-small cell lung cancer (NSCLC), comprising administering to a subject in need of such treatment a therapeutically effective amount of alectinib, or a pharmaceutically acceptable salt thereof, wherein the subject has resected stage Ib ALK-positive NSCLC with a tumour greater or equal to 4cm to stage IIIa ALK-positive NSCLC.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A CCI testing system (1) to test closure integrity of a container (2) with a hollow interior (223), an outlet (221), an open end (222) and a stopper (21) arranged to close the hollow interior (223), comprises a container holder (13), a test gas supply (171), a test gas detector (11) and a chamber (14). The container holder (13) is configured to tightly receive a first aperture being one of the open end (222) of the container (2) or the outlet (221) of the container (2). The test gas supply (171) comprises a test gas. The test gas detector (11) is tightly coupled to the container holder (13) and configured to detect test gas exiting the first aperture when being received by the container holder (13). The chamber (14) is coupled to the container holder (13) to form an encasing of a second aperture being the other one of the open end (222) of the container (2) or the outlet (221) of the container (2) when the first aperture is received by the container holder (13). The test gas supply (171) is coupled to the chamber (14). The test gas detector (11) is configured to apply a subatmospheric pressure to the container holder (13) and the container holder (13) is configured to effect the subatmospheric pressure to the first aperture. The test gas supply (171) is configured to supply test gas into the chamber (14). The chamber (14) has an exhaust outlet (141). The chamber (14) is configured to expose the second aperture to a gas flow generated by the test gas supply (171) supplying test gas into the chamber (14) and out of the chamber (14) via the exhaust outlet (141), when the first aperture is received by the container holder (13).
G01M 3/20 - Investigating fluid tightness of structures by using fluid or vacuum by detecting the presence of fluid at the leakage point using special tracer materials, e.g. dye, fluorescent material, radioactive material
G01M 3/22 - Investigating fluid tightness of structures by using fluid or vacuum by detecting the presence of fluid at the leakage point using special tracer materials, e.g. dye, fluorescent material, radioactive material for pipes, cables, or tubesInvestigating fluid tightness of structures by using fluid or vacuum by detecting the presence of fluid at the leakage point using special tracer materials, e.g. dye, fluorescent material, radioactive material for pipe joints or sealsInvestigating fluid tightness of structures by using fluid or vacuum by detecting the presence of fluid at the leakage point using special tracer materials, e.g. dye, fluorescent material, radioactive material for valves
G01M 3/28 - Investigating fluid tightness of structures by using fluid or vacuum by measuring rate of loss or gain of fluid, e.g. by pressure-responsive devices, by flow detectors for pipes, cables, or tubesInvestigating fluid tightness of structures by using fluid or vacuum by measuring rate of loss or gain of fluid, e.g. by pressure-responsive devices, by flow detectors for pipe joints or sealsInvestigating fluid tightness of structures by using fluid or vacuum by measuring rate of loss or gain of fluid, e.g. by pressure-responsive devices, by flow detectors for valves
25.
PYRAZOLE DERIVATIVES AS SARM1 INHIBITORS USEFUL FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS
The invention provides compounds having the general formula (I) wherein X, Y, Z, and R1to R8a are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds in the treatment or prevention of diseases that are associated with SARM1.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 25/00 - Drugs for disorders of the nervous system
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A CCI testing method to test physical container closure integrity of a container (2), comprises the steps of: (120) obtaining a container having a hollow interior, an outlet, an open end and a stopper arranged to close the hollow interior; (121) tightly connecting a first aperture being one of the outlet of the container and the open end of the container to a test gas detector; (122) connecting a second aperture being the other one of the outlet of the container and the open end of the container to a test gas supply; (123) arranging the test gas detector to apply a detector pressure at the first aperture; (124) arranging the test gas supply to provide test gas at a first test gas pressure to the second aperture; (125) measuring test gas at the first aperture by means of the test gas detector while the test gas is provided at the first test gas pressure; (126) determining a first leakage rate based on the test gas measured at the first test gas pressure; and (127, 128, 129) determining a second leakage rate at a second pressure. A first pressure difference being a difference between the first test gas pressure and the detector pressure differs from a second pressure difference being a difference between the second pressure and the detector pressure.
G01M 3/20 - Investigating fluid tightness of structures by using fluid or vacuum by detecting the presence of fluid at the leakage point using special tracer materials, e.g. dye, fluorescent material, radioactive material
27.
NOVEL METHODS FOR PREPARING SEMI-SOLID COMPOSITIONS AND USES THEREOF
The present application discloses methods and uses for preparation of a dry solid composition as a precursor for a stable gel body formation upon addition of water. The invention also discloses the compositions obtained from said methods and uses. Said gel bodies can, for example, be used in pharmaceutical compositions to administer drug substances to patients with difficulties to swallow.
Provided herein are methods of treating B-cell proliferative disorders (such as diffuse large B-cell lymphoma (DLBCL)) using immunoconjugates comprising anti-CD79b antibodies in combination with an anti-CD20 antibody (such as rituximab) and one or more chemotherapeutic agents (such as gemcitabine and oxaliplatin).
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The invention relates to Her2 targeting 4-1BB agonists, in particular 4-1BBL trimer-containing antigen binding molecules comprising at least one antigen binding domain capable of specific binding to Her2 and their use in the treatment of cancer as well as their use in combination with T-cell activating anti-CD3 bispecific antibodies.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
C07D 491/12 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains three hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The present invention generally relates to novel protease activatable Fc domain binding molecules, polynucleotides encoding such molecules, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the molecules of the invention, and to methods of using these molecules in the treatment of disease.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 9/64 - Proteinases derived from animal tissue, e.g. rennin
Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to Her2-targeted bispecific agonistic CD28 antigen binding molecules characterized by monovalent binding to CD28, methods for their production, pharmaceutical compositions containing these antibodies, and methods of using the same.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
34.
PHARMACEUTICAL FORMULATION COMPRISING A COATED TABLET
The invention relates to pharmaceutical formulation in form of a pharmaceutical formulation comprising GDC-0077 (INAVOLISIB) or a salt thereof, the formulation having a colored coating.
The invention provides new MAGL inhibitors having the general formula (II)AB(II) wherein the variables are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
The invention provides new MAGL inhibitors having the general formula (II)AB(II) wherein the variables are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The invention provides viral protease inhibitors having the general formula (I)
The invention provides viral protease inhibitors having the general formula (I)
The invention provides viral protease inhibitors having the general formula (I)
wherein the variables are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 207/267 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
38.
PROCESSES FOR THE PREPARATION OF PHENYLTETRAHYDROFURAN COMPOUNDS
Provided are phenyltetrahydrofuran compounds that are useful as intermediates in the preparation of pharmaceutical compounds and further provided are processes for the preparation of phenyltetrahydrofuran compounds.
C07D 307/12 - Radicals substituted by oxygen atoms
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
39.
PROCESS FOR THE PREPARATION OF PREPARING 1-ETHYL-N-((1,2,3,5,6,7-HEXAHYDRO-S-INDACEN-4-YL)CARBAMOYL)PIPERIDINE-4-SULFONAMIDE
The present invention relates to a process for the preparation of compound (6), (6). Compound (6) is a key precursor for the formation of 1-ethyl-N-((1,2,3,5,6,7- hexahydro-s-indacen-4-yl)carbamoyl)piperidine-4-sulfonamide (compound (I), Formula (I)) or a pharmaceutically acceptable salt thereof, which is useful as an NLRP3 inhibitor.
C07D 211/64 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
C07D 211/72 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to multispecific antibodies that bind to HLA-G ant to a T cell activating antigen, their preparation, formulations and methods of using the same.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 39/00 - Medicinal preparations containing antigens or antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
43.
MUTANT TRANSAMINASE WITH INCREASED ASYMMETRIC REDUCTIVE AMINATION ACTIVITY AS WELL AS METHODS AND USES INVOLVING THE SAME
The present invention relates to a mutant transaminase, a nucleic acid encoding the mutant transaminase, a vector comprising the nucleic acid, a cell comprising the mutant transaminase or nucleic acid and a method for the enzymatic reductive transamination of a ketone and the formation of a primary amine in the presence of mutant transaminase.
Herein is reported an antibody that binds to human A-beta protein, wherein the antibody comprises a heavy chain variable domain (VH) and a light chain variable domain comprising CDRs selected from (1) CDRs of SEQ ID NO: 85, 86, 87, 81, 82 and 83; or (2) CDRs of SEQ ID NO: 85, 89, 87, 81, 82 and 83; or (3) CDRs of SEQ 5 ID NO: 85, 86, 87, 81, 82 and 91; or (4) CDRs of SEQ ID NO: 85, 89, 87, 81, 82 and 91.
Herein is reported an anti-TREM2 antibody specifically binding to human TREM2 comprising in the heavy chain variable domain a HVR-H1 of SEQ ID NO: 305, a HVR-H2 of SEQ ID NO: 306 and a HVR-H3 of SEQ ID NO: 307, and in the light chain variable domain a HVR-L1 of SEQ ID NO: 309, a HVR-L2 of SEQ ID NO: 310 and a HVR-L3 of SEQ ID NO: 311 (TREM2 3295), or in the heavy chain variable domain a HVR-H1 of SEQ ID NO: 329, a HVR-H2 of SEQ ID NO: 330 and a HVR-H3 of SEQ ID NO: 331, and in the light chain variable domain a HVR-L1 of SEQ ID NO: 333, a HVR-L2 of SEQ ID NO: 334 and a HVR-L3 of SEQ ID NO: 335 (TREM2 3306), wherein the does not induce pSyk in the absence or presence of human Abeta protein.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
46.
SYNTHESIS OF A BIS-MESYLATE SALT OF 4-AMINO-N-(1-((3-CHLORO-2-FLUOROPHENYL)AMINO)-6-METHYLISOQUINOLIN-5-YL)THIENO[3,2-D]PYRIMIDINE-7-CARBOXAMIDE AND INTERMEDIATES THERETO
A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl) thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
Herein is reported an antibody that binds to human A-beta protein, wherein the antibody comprises a heavy chain variable domain (VH) and a light chain variable domain comprising CDRs selected from (1) CDRs of SEQ ID NO: 85, 86, 87, 81, 82 and 83; or (2) CDRs of SEQ ID NO: 85, 89, 87, 81, 82 and 83; or (3) CDRs of SEQ ID NO: 85, 86, 87, 81, 82 and 91; or (4) CDRs of SEQ ID NO: 85, 89, 87, 81, 82 and 91.
The present invention relates to oligonucleotides which alter the splicing pattern of progranulin in cells, and their use in the treatment of neurological disorders.
The present invention relates to antisense oligonucleotides that are capable of modulating expression of Tau in a target cell. The oligonucleotides hybridize to MAPT mRNA. The present invention further relates to conjugates of the oligonucleotide and pharmaceutical compositions and methods for treatment of Tauopathies, Alzheimzer's disease, fronto-temporal dementia (FTD), FTDP-17, progressive supranuclear palsy (PSP), chronic traumatic encephalopathy (CTE), corticobasal ganglionic degeneration (CBD), epilepsy, Dravet syndrome, depression, seizure disorders and movement disorders.
Herein is reported an anti-TREM2/Abeta protein antibody comprising a first binding site binding to human TREM2 comprising a heavy chain variable domain comprising a HVR-H1 of SEQ ID NO: 305, a HVR-H2 of SEQ ID NO: 306 and a HVR-H3 of SEQ ID NO: 307, and a light chain variable domain comprising a HVR-L1 of SEQ ID NO: 309, a HVR-L2 of SEQ ID NO: 310 and a HVR-L3 of SEQ ID NO: 311 (TREM2 3295), or a heavy chain variable domain comprising a HVR-H1 of SEQ ID NO: 329, a HVR-H2 of SEQ ID NO: 330 and a HVR-H3 of SEQ ID NO: 331, and a light chain variable domain comprising a HVR-L1 of SEQ ID NO: 333, a HVR-L2 of SEQ ID NO: 334 and a HVR-L3 of SEQ ID NO: 335 (TREM2 3306), and a second binding site binding to human Abeta protein comprising a heavy chain variable domain comprising a HVR-H1 of SEQ ID NO: 09, a HVR-H2 of SEQ ID NO: 10 and a HVR-H3 of SEQ ID NO: 11, and in the light chain variable domain a HVR- L1 of SEQ ID NO: 13, a HVR-L2 of SEQ ID NO: 14 and a HVR-L3 of SEQ ID NO: 15 (Abeta 8675).
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
51.
PROCESS FOR THE PREPARATION OF 3-SUBSTITUTED 5-AMINO-6H-THIAZOLO[4,5-D]PYRIMIDINE-2,7-DIONE COMPOUNDS
The present invention relates to a splice variant of a CERT1 protein that acts as a biomarker for a TDP-43 pathology, in particular motor neuron diseases such as amyotrophic lateral sclerosis (ALS) and frontotemporal lobar degeneration (FTLD), but also other neurological diseases, such as Alzheimer's disease. In particular, the present invention relates to methods for identifying a splice variant of CERT1 comprising a cryptic peptide sequence, and to related methods of identifying a TDP-43 pathology and/or reduced TDP-43 function in a subject and to methods for predicting whether a therapy is likely to be successful. Also claimed are antibodies binding to the CERT1 splice variant and kits comprising the antibody.
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
The present invention relates to a cell retention device for use within a culture vessel of a microbioreactor, to a microreactor comprising said cell retention device, and to a system comprising a plurality of microreactors each comprising said cell retention device. The present invention also relates to the use of the cell retention device of the invention for filtering culture medium out of a microbioreactor and to the use of the microbioreactor comprising the cell retention device of the invention for seed train culture, inoculum train culture or a main fermentation (production phase). The present invention further relates to a method of exchanging culture medium in a microbioreactor comprising the cell retention device of the invention.
Techniques described herein include, for example, generating a feature map for an input image, generating a plurality of concentric crops of the feature map, and generating an output vector that represents a characteristic of a structure depicted in a center region of the input image using the plurality of concentric crops. Generating the output vector may include, for example, aggregating sets of output features generated from the plurality of concentric crops, and several methods of aggregating are described. Applications to classification of a structure depicted in the center region of the input image are also described.
G06V 10/77 - Processing image or video features in feature spacesArrangements for image or video recognition or understanding using pattern recognition or machine learning using data integration or data reduction, e.g. principal component analysis [PCA] or independent component analysis [ICA] or self-organising maps [SOM]Blind source separation
G06V 10/80 - Fusion, i.e. combining data from various sources at the sensor level, preprocessing level, feature extraction level or classification level
G06V 10/82 - Arrangements for image or video recognition or understanding using pattern recognition or machine learning using neural networks
G06V 20/69 - Microscopic objects, e.g. biological cells or cellular parts
55.
SEGMENTATION OF OPTICAL COHERENCE TOMOGRAPHY (OCT) IMAGES
Systems and methods for performing automated retinal segmentation. Performing the automated retinal segmentation includes receiving an image input for a retina of a subject. Layer element data is generated using the image input and a first neural network. The layer element data identifying a set of retinal layer elements. Initial pathological element data is generated using the image input and a second neural network. The initial pathological element data identifies a set of retinal pathological elements. The initial pathological element data is refined using the layer element data to generate refined pathological element data. The refined pathological element data more accurately identifies the set of retinal pathological elements as compared to the initial pathological element data.
The invention relates to novel compounds having the general formula (I), wherein X, R1, R2, R3 and n are as described herein, composition including the compounds and methods of using the compounds.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
57.
Double Stranded Oligonucleotide For Modulating JAK1 Expression
The present invention relates to double stranded oligonucleotides that are complementary to JAK1, leading to modulation of the expression of JAK1. Modulation of JAK1 expression is beneficial for a range of medical disorders including inflammatory bowel disease, organ transplant rejection, graft-versus-host disease, multiple sclerosis, rheumatoid arthritis (RA), juvenile idiopathic arthritis, psoriasis, dermatitis, diabetic nephropathy, systemic lupus erythematosus (SLE), dry eye disease, cancer, myelofibrosis, and asthma. Also included are compositions comprising the double stranded oligonucleotide and methods of treatment using the double stranded oligonucleotide.
The invention relates to novel antibodies that bind to lymphotoxin beta receptor (LTBR) and to bispecific antigen binding molecules comprising these novel LTBR antibodies and an antigen binding domain that binds a tumor associated antigen, in particular to Fibroblast Activation Protein (FAP), to methods of producing these molecules and to methods of using the same.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention relates to fusion proteins targeted to the central nervous system (CNS) and its use for the treatment of lysosomal storage disorders (LSD).
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
60.
MACROCYCLES FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I), wherein Q1to Q4, and M1to M3 are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61P 37/00 - Drugs for immunological or allergic disorders
A component (1) configured to be used as part of a sterile product manufacturing equipment (2) in an aseptic process comprises a contact part and a heating structure. The contact part (12) is configured to directly or indirectly contact a sterile product. It is made of a thermally conductive material. The heating structure (13) is thermally coupled to the contact part (12). The component (1) according to the invention allows for heat sterilization while the component (1) is assembled in the manufacturing equipment (2) without requiring removal of the component (1).
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.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
Herein is reported a method for the determination of viral genome DNA copy number in a sample, wherein the method comprises the steps of incubating the sample with proteinase K and determining the viral genome DNA copy number by digital droplet polymerase chain reaction, wherein the sample is free of DNA, which is not encapsidated within a viral particle, wherein the incubation with proteinase K is in the presence of 0.05 (w/v) % to 1.5 (w/v) % sodium dodecyl sulfate.
C12Q 1/70 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving virus or bacteriophage
64.
FORECASTING OF SUBJECT-RELATED ATTRIBUTES USING GENERATIVE MACHINE-LEARNING MODELS
A computer-implemented method of predicting, simulating, or forecasting values of one or more specified subject-related attributes during a clinical trial comprises: receiving input data comprising: a medical history of a subject, the medical history comprising values of a plurality of subject-related attributes of a subject; and data specifying a requested output, the data comprising: the one or more specified subject-related attributes of the subject and a time frame; and applying a trained generative machine-learning model to the received input data, the trained generative machine-learning model configured to generate output data based on the input data, the output data comprising: respective values of the one or more specified subject-related attributes of the subject in the specified time frame.
G06N 3/008 - Artificial life, i.e. computing arrangements simulating life based on physical entities controlled by simulated intelligence so as to replicate intelligent life forms, e.g. based on robots replicating pets or humans in their appearance or behaviour
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
G16H 70/40 - ICT specially adapted for the handling or processing of medical references relating to drugs, e.g. their side effects or intended usage
G06F 16/81 - Indexing, e.g. XML tagsData structures thereforStorage structures
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
G16H 50/50 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for simulation or modelling of medical disorders
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
The present invention relates to a multispecific antibody for use in transporting a com- pound across the Blood Brain Barrier (BBB), wherein the antibody binds to at least two target proteins selected from the group consisting of transferrin receptor (TFRC), CD98 (SLC3A2) and PODXL.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
Provided herein are diagnostic and therapeutic methods for the treatment of cancer using polygenic risk scores (PRSs) for liver damage. In particular, the invention provides methods for patient selection and methods of treatment.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
The invention relates to a compound of formula (Ia) wherein R1and R2 are as defined in the description and in the claims. The compound of formula (Ia) can be used as a medicament.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
The application relates to a compound of formula (I) or (II) wherein L, R1, R2, R3and R4 are as defined in the claims. The compound of formula (I) or (II) can be used as a medicament that modulates SIK activity in autoimmune, inflammatory and other conditions.
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
69.
PROCESS FOR THE REDUCTION OF AROMATIC IMINES WITH NOVEL IMINE REDUCTASES (IREDS)
The present invention relates to a process for producing a chiral aromatic amine comprising the steps of a) providing an aromatic imine, and b) contacting the aromatic imine from step a) with an imine reductase, thereby stereoselectively reducing the aromatic imine with the imine reductase to a chiral aromatic amine and to novel imine reductases which are capable to catalyse the reaction.
The invention relates to a process for the coupling of an aryl halogenide with an N- nucleophile compound which is characterized in that the coupling takes place in the presence of a dinuclear copper(II) complex bearing substituted salben-type ligands having the formula (I). Also described are novel dinuclear copper(II) complex bearing substituted salben-type ligands within the scope of formula (I).
C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
B01J 31/28 - Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups of the platinum group metals, iron group metals or copper
C07C 209/10 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of halogen atoms with formation of amino groups bound to carbon atoms of six-membered aromatic rings or from amines having nitrogen atoms bound to carbon atoms of six-membered aromatic rings
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07D 207/323 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atoms
C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07B 43/04 - Formation or introduction of functional groups containing nitrogen of amino groups
C07B 43/06 - Formation or introduction of functional groups containing nitrogen of amide groups
C07C 227/18 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
C07C 231/08 - Preparation of carboxylic acid amides from amides by reaction at nitrogen atoms of carboxamide groups
C07C 303/36 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
C07F 1/00 - Compounds containing elements of Groups 1 or 11 of the Periodic Table
C07B 45/04 - Formation or introduction of functional groups containing sulfur of sulfonyl or sulfinyl groups
The application relates to a compound of formula (I) wherein L, R1, R2R3, R4, R5and R6 are as defined in the claims. The compounds of formula (I) are SIK-activity modulators and can be used as a medicament.
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
72.
MACROCYCLES FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present application relates to compounds of formula (I), wherein R1to R6, Q1and A1to AS are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds. The compounds of formula (I) are antagonists of STING and thus useful for the treatment of various diseases and disorders.
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
The present disclosure relates to systems and methods for processing signals from wearable motion sensors associated with gait activity of a subject. In some cases, a signal representative of the gait activity of the subject may be received from the wearable motion sensors. One or more directional components of the signal, which are independent of an orientation of the wearable motion sensors on the subject, may be identified. One or more gait features may be extracted from the signal based on the one or more directional components of the signal. At least one of a diagnosis, a progression, a treatment, and a treatment response for a neurological dysfunction may be determined based on the one or more gait features.
The present invention relates to methods for treating multiple sclerosis (MS) in a patient which in some cases involves subcutaneously administering an anti-CD20 antibody into the patient at a dose of about 920 mg. Compositions, formulations and articles of manufacture with instructions for such use are also included.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 38/47 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
A61K 47/42 - ProteinsPolypeptidesDegradation products thereofDerivatives thereof, e.g. albumin, gelatin or zein
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
76.
MACROCYCLES FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I-2), wherein R1to R3, Q1, Q2, A1to A7and M1 are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
The present invention relates to compounds of formula (Ia), wherein R2, T1to T4, and M1to M3 are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61P 37/00 - Drugs for immunological or allergic disorders
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
The invention provides compounds having the general formula (I) wherein X, Y, Z, U, V, and R1to R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the5 compounds in the treatment or prevention of diseases that are associated with SARM1.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61P 25/00 - Drugs for disorders of the nervous system
79.
MGLU2/3 ANTAGONISTS FOR THE TREATMENT OF INTELLECTUAL DISABILITIES
This invention relates to a new medical use for certain chemical compounds and pharmaceutical compositions containing them. The invention relates to compounds which are mGlu2/3 negative allosteric modulators for use in the treatment of intellectual disabilities. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of intellectual disabilities comprising a compound according to the invention and a pharmaceutically acceptable carrier.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A method implemented by one or more computer device includes accessing a set of medical data associated with a patient, in which the set of medical data includes a plurality of modalities of medical data. The method includes inputting one or more one of the plurality of modalities of medical data into a first machine-learning model trained to generate a first vector representation and inputting another one of the plurality of modalities of medical data into a second machine-learning model trained to generate a second vector representation. The method includes generating a combined vector representation based on the first vector representation and the second vector representation, and storing the combined vector representation to a database associated with the one or more computing devices.
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
A61B 5/00 - Measuring for diagnostic purposes Identification of persons
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
81.
NEW SOLID FORMS OF (3R)-N-[2-CYANO-4-FLUORO-3-(3-METHYL-4-OXO-QUINAZOLIN-6-YL)OXY-PHENYL]- 3-FLUORO-PYRROLIDINE-1-SULFONAMIDE
The present invention provides solid forms of (3R)-N-[2-cyano-4- fluoro-3-(3-methyl-4-oxo-quinazolin -6-yl )oxy - phenyl]-3-fluoro- pyrrolidine-1-sulfonamide of formula (I) and solvates thereof, as well as therapeutic uses thereof and pharmaceutical composition comprising them.
C07D 487/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains three hetero rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
82.
PIPERAZINYLSULFONYLARYL COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
The present invention relates to compounds of formula (I), wherein R1, R2, R3, Y, Q1, Q2, Q3, Q4 and Q5 are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Provided are methods for the treatment of a Tau associated disease, comprising administering to a subject an effective amount of a compound modulating a protein-protein interaction between a protein comprising a NTF2-like domain having the amino acid sequence set forth as SEQ ID NO: 3 and Tau protein.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The invention relates to novel compounds having the general formula (I) wherein A, R1, R2 and n are as described herein, composition including the compounds and methods of using the compounds.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
Provided are mutant interleukin-7 polypeptides, immunoconjugates, particularly immunoconjugates comprising a mutant interleukin-7 polypeptide and an antibody that binds to PD-1. In addition, provided are polynucleotide molecules encoding the mutant interleukin-7 polypeptides or the immunoconjugates, and vectors and host cells comprising such polynucleotide molecules. Also provided are methods for producing the mutant interleukin-7 polypeptides, immunoconjugates, pharmaceutical compositions comprising the same, and uses thereof.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention is directed to pharmaceutical combinations for treating hepatitis B virus (HBV) infection comprising administering at least two, preferably two or three, different HBV therapeutics. In particular, the present invention relates to pharmaceutical combinations comprising an RNAi oligonucleotide targeting HBV and an anti-PDL1 antisense oligonucleotide.
Herein is reported a composition comprising a pair of a first nucleic acid and a second nucleic acid, wherein the first nucleic acid comprises in the order a first part of a stem nucleic acid sequence, a cleavage site, a first stem loop nucleic acid sequences which 5′- and 3′-parts form a duplex, a first part of a catalytic core sequence, a second stem loop nucleic acid sequences which 5′- and 3′-parts form a duplex, a second part of the catalytic core sequence, and a second part of the stem nucleic acid sequence, which is complementary to the first part of the stem nucleic acid sequence and, thus, form a duplex therewith, wherein the second nucleic acid is complementary to at least a part of the first or the second part of the stem nucleic acid sequence, wherein binding of the second nucleic acid to the first nucleic acid results in a conformational change of the first nucleic acid, which is at least one of the dissociation of the first part of the first stem sequence from the second part of the stem sequence and the hybridization of one of the parts with the second nucleic acid, or the dissociation of loop I and loop II resulting in an inactivation of the catalytic activity, or the association of loop I and loop II resulting in an activation of the catalytic activity.
The present invention relates to combination therapies employing tumor targeted anti- CD3 bispecific antibodies (T cell engager) and FAP-targeted LTBR antibodies, the use of these combination therapies for the treatment of cancer and methods of using the combination therapies.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The present invention generally relates to humanized antigen binding receptors capable of specific binding to an Fc domain comprising the amino acid mutation P329G according to EU numbering. The present invention also relates to T cells, transduced with an antigen binding receptor which is recruited by specifically binding to/interacting with the mutated Fc domain of therapeutic antibodies.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
90.
METHODS FOR TREATMENT OF CANCER WITH AN ANTI-TIGIT ANTAGONIST ANTIBODY
The present invention relates to methods, uses, and compositions for the treatment of cancer (e.g., a lung cancer; a cervical cancer; a breast cancer; a head and neck cancer; a liver cancer; a bladder cancer; a gastric cancer; an esophageal cancer; a pancreatic cancer; a kidney or renal cancer; a melanoma; an ovarian cancer; or a colorectal cancer). More specifically, the invention concerns the treatment of patients having cancer with an anti-TIGIT antagonist antibody, including treatment with an anti-TIGIT antagonist antibody in a combination therapy.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 35/04 - Antineoplastic agents specific for metastasis
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention relates to systems and methods for analyzing data from motion activity monitoring technology. It is particularly, but not exclusively, concerned with a method for determining motion activity patterns during sleep.
The invention provides compounds having the general formula (I) wherein A1, A2, X1, X2, R1, R2, R3, R4, and R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds in the treatment or prevention of diseases that are associated with TREM2.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
93.
PROCESS FOR THE PREPARATION OF A CHIRAL PYRROLO TRIAZOLE ALCOHOL
The invention relates to a novel process for the preparation of chiral pyrrolo triazole alcohols of the formula (I) wherein X is a halogen atom, n is an integer of 1, 2 or 3 and wherein the spiral bond (II) stands for (III) or for (IV) or mixtures of the enantiomers. The chiral pyrrolo triazole alcohols of the formula (I) are versatile intermediates for the preparation of compounds that have the potential to serve as active pharmaceutical ingredients in drugs.
Herein is reported a bispecific antibody specifically binding to human Abeta protein and human transferrin receptor (bispecific anti-Abeta/TfR antibody) as well as the use of such bispecific antibodies as a medicament in the treatment of Alzheimer's Disease, including where the bispecific antibody is administered intravenously at a dose of 0.2 mg/kg to 7.2 mg/kg once every four weeks.
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
95.
SULFONYLPIPERAZINYL COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
The present invention relates to compounds of formula (I), wherein R1 to R3, A, Q1, Q2, W and X are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
The present invention relates to compounds of formula (I), wherein R1 to R3, A, Q1, Q2, W and X are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Provided herein are methods for assessing splice-switching ASOs using a reporter to detect splicing of a cryptic sequence located in the reporter pre-mRNA.
The present invention relates to double stranded oligonucleotides that are complementary to JAK1, leading to modulation of the expression of JAK1. Modulation of JAK1 expression is beneficial for a range of medical disorders including inflammatory bowel disease, organ transplant rejection, graft-versus-host disease, multiple sclerosis, rheumatoid arthritis (RA), juvenile idiopathic arthritis, psoriasis, dermatitis, diabetic nephropathy, systemic lupus erythematosus (SLE), dry eye disease, cancer, myelofibrosis, and asthma. Also included are compositions comprising the double stranded oligonucleotide and methods of treatment using the double stranded oligonucleotide.
It is disclosed crystalline forms of (R)-N-(4-([1, 2, 4]triazolo [1, 5-c]pyrimidin-7-yloxy)-3-methylphenyl)-5-((3, 3-difluoro-1-methylpiperidin-4-yl)oxy)-6-methoxyquinazolin-4-amine, methods for the preparation thereof, pharmaceutical compositions comprising one or more of the crystalline forms as an active ingredient, and use of the crystalline forms in the treatment of hyperproliferative diseases.
The present invention relates to compounds of formula (Ib),
3, M and L are as described herein, and their pharmaceutically acceptable salt, enantiomers and diastereomers thereof, and compositions including the compounds and methods of using the compounds.
C07D 513/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
22R) having the general formula (I), wherein R1to R3 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
A61P 37/00 - Drugs for immunological or allergic disorders
C07C 35/18 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic containing six-membered rings with unsaturation at least in the ring
C07C 247/10 - Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated and containing rings
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 309/36 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/09 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
C07C 43/23 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
C07C 247/06 - Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated and containing rings
