The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A, R1 and R3 are as described herein, as well as compositions and methods of using such compounds.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61P 9/00 - Drugs for disorders of the cardiovascular system
Provided herein are compounds for inhibiting peripheral myelin protein 22 (PMP22) mRNA. Also provided herein are methods of using such compounds for the treatment of Charcot-Marie-Tooth disease.
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 compound
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
The present disclosure is directed to a method of treating glioblastoma in a subject in need thereof comprising administering to said subject an efficient amount of a radiopharmaceutical compound. The present disclosure is also directed to methods of treating glioblastoma in a subject in need thereof comprising administering to said subject an efficient amount of a radiopharmaceutical compound in combination with a step of irradiating the subject with an efficient dose of ionizing radiations, and optionally, with a therapeutically efficient amount of an alkylating agent, preferably temozolomide.
Pharmaceutical compositions for oral administration comprising the drug substance (S)-1'-chloro-8-(difluoromethoxy)-8',8'-difluoro-6-(trifluoromethyl)-7',8'-dihydro-3H,6'H-spiro[imidazo[1,2- ]pyridine-2,5'-isoquinoline], or a pharmaceutically acceptable salt thereof, or a free form thereof are described. Further, processes for preparing said pharmaceutical 5 compositions for oral administration and uses of said pharmaceutical compositions in the manufacture of a medicament are described.
The invention relates to a pharmaceutical combination comprising a TEAD inhibitor in combination with a first and optionally a second therapeutically active agent. The present invention also relates to methods of treating cancer involving administering to a subject in need thereof the TEAD inhibitor in combination with the first and optionally the second therapeutically active agent.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/351 - 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 not condensed with another ring
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The invention relates to a TEAD inhibitor or a pharmaceutically acceptable salt thereof for use in the treatment of cancer, wherein the TEAD inhibitor is administered on each of the first 3 days of a 7 day treatment cycle, and wherein the treatment comprises at least two treatment cycles.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
The present invention generally relates to crystalline polymorphic forms of the biaryl YAP/TAZ-TEAD protein-protein interaction inhibitors 4-((2S,4S)-5-Chloro-6-fluoro-2-phenyl-2-((S)-pyrrolidin-2-yl)-2,3-dihydrobenzofuran-4-yl)-5-fluoro-6-(2-hydroxyethoxy)-N-methylnicotinamide and 2-((2S,3S,4S)-5-Chloro-6-fluoro-3-methyl-2-((methylamino)methyl)-2-phenyl-2,3-dihydrobenzofuran-4-yl)-3-fluoro-4-methoxybenzamide and salts thereof, as well as methods of using the forms in the treatment of cancer.
C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
The invention concerns ofatumumab for use in the treatment or prevention of pediatric multiple sclerosis (MS). According to the invention, ofatumumab is administered during a loading dose regimen at weeks 0, 1, 2 of the dosage regimen; and ofatumumab is administered during a maintenance dose regimen starting at week eight of the dosage regimen and continuing thereafter every six weeks.
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 25/28 - 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
A61P 37/00 - Drugs for immunological or allergic disorders
11.
METHODS OF MAKING CHIMERIC ANTIGEN RECEPTOR-EXPRESSING CELLS
The invention provides methods of making immune effector cells (for example, T cells, NK cells) that express a chimeric antigen receptor (CAR), and compositions generated by such methods.
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
Provided herein are compounds and compositions for treating, managing or preventing coronaviral related diseases. In particular, provided herein are compounds which are inhibitors of SARS-CoV-2 main protease (Mpro), pharmaceutical compositions comprising such compounds, method for synthesizing such compounds and methods of using such compounds and compositions for the treatment, management or prevention of coronaviral related diseases.
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
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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
13.
SUBSTITUTED PYRIDONE COMPOUNDS USEFUL TO TREAT ORTHOMYXOVIRUS INFECTIONS
The disclosure provides compounds of Formula (I): (I) as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.
A61K 31/4412 - Non-condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
C07D 401/10 - 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 carbon chain containing aromatic 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
C07D 405/10 - 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 aromatic rings
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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/10 - 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 aromatic 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
C07D 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure relates to the field of pharmacy, particularly to an NLRP3 inhibitor for use in the treatment of osteoarthritis. The disclosure also relates to an NLRP3 inhibitor or a pharmaceutical combination comprising an NLRP3 inhibitor, and at least one further therapeutic agent, for use in the treatment of osteoarthritis; to a method for the treatment of osteoarthritis that involves administering an NLRP3 inhibitor or the combination; and to the use of an NLRP3 inhibitor or the combination for the manufacture of a medicament for the treatment of osteoarthritis.
The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof, and the therapeutic uses of said compound. The present invention further provides a pharmaceutical composition comprising said compound.
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 31/454 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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 31/541 - Non-condensed thiazines containing further heterocyclic rings
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 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
The invention relates to bivalent bispecific monoclonal antibodies (bbmAb) or variants thereof for use in the treatment or for use in alleviating the symptoms of hidradenitis suppurativa in a subject.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The present invention relates to a pharmaceutical combination comprising a KRAS G12C inhibitor and one or more therapeutic agents which is selected from an agent targeting the MARK pathway or an agent targeting parallel pathways; and pharmaceutical compositions comprising the same. The invention also relates to KRAS G12C inhibitors alone or said combinations for use in methods of treating a cancer or a tumor, in particular wherein the cancer or tumor is KRAS G12C mutant.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/4439 - Non-condensed pyridines; Hydrogenated 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 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention provides anti-lgE antibodies formulated as stable aqueous pharmaceutical compositions, suitable for injection. An aqueous pharmaceutical composition of the invention includes a sugar (trehalose), a buffering agent (histidine), and a surfactant (polysorbate 20). The aqueous pharmaceutical compositions are useful for delivery of a high concentration of the antibody (at least 50 mg/ml) active ingredient to a patient without high levels of antibody aggregation and without a high level of sub-visible particulate matter.
The application relates to compounds of formula (I), pharmaceutical compositions comprising them and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta- thalassemia.
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 31/454 - 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 31/4545 - 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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
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
The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): (I) wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.
The present disclosure provides compositions and methods of restoring or enhancing visual function in an individual by administering to the individual a pharmaceutical composition comprising a recombinant adeno-associated viral (rAAV) vector having a polynucleotide sequence that encodes a medium wavelength cone opsin (MW-opsin). The MW-opsin is expressed in a retinal cell in the individual, thereby restoring or enhancing visual function.
The present disclosure relates to dosing regimens and combinations comprising N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide or a pharmaceutically acceptable salt thereof, and their use for the treatment of breakpoint cluster region-abelson protein (BCR-ABL) mediated diseases or disorders.
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/5025 - Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
23.
TREATMENT FOR SYSTEMIC LUPUS ERYTHEMATOSUS USING ANTI-BAFFR ANTIBODIES
The present disclosure relates to methods for treating Systemic Lupus Erythematosus (SLE) using an anti-BAFFR antibody or binding fragment thereof, e.g., ianalumab. Also disclosed herein are anti-BAFFR antibodies or binding fragments thereof, e.g., ianalumab, for treating SLE patients, as well as medicaments, dosing regimens, pharmaceutical formulations, dosage forms, and kits for use in the disclosed uses and methods.
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
A61P 37/00 - Drugs for immunological or allergic disorders
24.
TREATMENT FOR LUPUS NEPHRITIS USING ANTI-BAFFR ANTIBODIES
The present disclosure relates to methods for treating Lupus Nephritis (LN) using an anti-BAFFR antibody or binding fragment thereof, e.g., ianalumab. Also disclosed herein are anti-BAFFR antibodies or binding fragments thereof, e.g., ianalumab, for treating LN patients, as well as medicaments, dosing regimens, pharmaceutical formulations, dosage forms, and kits for use in the disclosed uses and methods.
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
A61P 37/00 - Drugs for immunological or allergic disorders
Alpelisib Formulation The invention features a granular formulation comprising an internal phase consisting of free flowing granules including alpelisib, or a pharmaceutically acceptable salt thereof, as active pharmaceutical ingredient and at least one pharmaceutically acceptable carrier material, and preferably in addition an external phase without said API comprising at least one pharmaceutically acceptable carrier material; and related invention embodiments.
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
26.
IPTACOPAN FOR THE TREATMENT OF ATYPICAL HEMOLYTIC UREMIC SYNDROME
Described herein are methods of treating atypical hemolytic uremic syndrome (aHUS) with the Factor B inhibitor LNP023 (iptacopan) or a pharmaceutically acceptable salt thereof, e.g. iptacopan hydrochloride.
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
27.
DEUBIQUITINASE-TARGETING CHIMERAS AND RELATED METHODS
Described herein are bifunctional compounds, as well as pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof, that function to recruit certain deubiquitinases to a target protein for modulation (e.g., stabilization) of the target protein, as well as methods of use thereof.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
28.
METHODS FOR THE ADMINISTRATION OF ADAMTS BINDING IMMUNOGLOBULINS
Disclosed herein are methods and dosage regimens for the treatment of osteoarthritis (e.g., knee osteoarthritis). The methods and dosage regimens comprise administration of an ADAMTS5 inhibiting polypeptide in a therapeutically effective amount.
The disclosure provides, at least in part, to a method for producing high titer lentiviral vectors, and for producing lentiviral particles carrying a transgene of interest and under satisfactory safety conditions. The disclosure also provides at least in part, methods of purification of such lentiviral particle, e.g., from a cell culture. The disclosure also provides a formulation to lentiviral preparations that maintain structural integrity of the viral vector during purification, storage, and gene transfer events.
Provided herein are novel compounds comprising a GLP-1 compound and a fatty acid or fatty acid derivative, the manufacture of said novel compounds and the use thereof.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 compound
A61P 5/48 - Drugs for disorders of the endocrine system of the pancreatic hormones
The invention concerns ofatumumab for use in the treatment of multiple sclerosis (MS), wherein patients are treated who are of Asian race. The invention further relates to ofatumumab for use in the treatment of multiple sclerosis, wherein the treatment is ethnically insensitive. The invention further relates to ofatumumab for use in the treatment of multiple sclerosis, wherein patients having certain genetic or physiological risk factors are treated.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular 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
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
32.
ANTIBODY DRUG CONJUGATES AND METHODS FOR MAKING THEREOF
This application discloses microorganisms and methods of producing GNAQ/GNA11 inhibitors and methods of making antibody drug conjugates of anti-PMEL17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor. The disclosure also relates to formulations comprising antibody drug conjugates of anti-PMEL17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor and methods of treating or preventing cancer using the formulations.
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 11/00 - Drugs for disorders of the respiratory system
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 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 413/10 - 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 aromatic 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
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
35.
FOLATE RECEPTOR-TARGETED RADIOTHERAPEUTIC AGENTS AND THEIR USE
The present disclosure relates to folate receptor-targeted radiotherapeutic compounds and their use. The present disclosure relates to folate receptor-targeted radiolabeled imaging conjugates and their use. The present disclosure also relates to pharmaceutical compositions of the compounds and conjugates described herein, methods of making and methods of using the same.
2-((4-((S)-2-(4-CHLORO-2-FLUOROPHENYL)-2-METHYLBENZO[D][1,3]DIOXOL-4-YL)PIPERIDIN-1-YL)METHYL)-1-(((S)-OXETAN-2-YL)METHYL)-1H-IMIDAZOLE DERIVATIVES AS ACTIVATORS OF THE GLP1 RECEPTOR FOR THE TREATMENT OF OBESITY
The present invention relates to compounds of formula (I) as activators of glucagon-like peptide 1 (GLP1) receptor for the treatment of obesity, type 2 diabetes mellitus, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, one or more diabetic complications, diabetic nephropathy, dyslipidemia, non- alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hypertension, atherosclerosis, peripheral arterial disease, stroke, cardiomyopathy, atrial fibrillation, heart failure, coronary heart disease and neuropathy. Preferred compounds are e.g. 2-((4-((S)-2-(4-chloro-2-fluorophenyl) -2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)- oxetan-2-yl)methyl)-1H-imidazole derivatives and similar compounds, such as e.g. C-1, C-2, C-3, C-4 and other 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 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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
The present disclosure relates to the field of diagnostic methods, and more particularly prostate cancer imaging. In particular, the disclosure relates to a radiopharmaceutical PSMA-binding compound for use in determining the presence and/or localization of PSMA-positive tumors in a subject in need thereof, wherein said subject has been diagnosed with biochemical recurrence, particularly after radical prostatectomy or radiotherapy, and wherein said radiopharmaceutical compound is the compound of formula (III).
The present disclosure provides a compound of formula (I), or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the disclosure, and its therapeutic uses. The present disclosure further provides a combination of pharmacologically active agents and a pharmaceutical composition.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic rings
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/536 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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
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
A61P 25/00 - Drugs for disorders of the nervous system
39.
NEW PROCESS FOR THE SYNTHESIS OF 5-{5-CHLORO-2-[(3S)-3- [(MORPHOLIN-4-YL)METHYL]-3,4-DIHYDROISOQUINOLINE-2(1H)- CARBONYL]PHENYL}-1,2-DIMETHYL-1H-PYRROLE-3-CARBOXYLIC ACID DERIVATIVES AND ITS APPLICATION FOR THE PRODUCTION OF PHARMACEUTICAL COMPOUNDS
The present invention relates to a new process for preparing 5-{5-chloro-2-[(3S)-3- [(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1H)-carbonyl]phenyl}-1,2-dimethyl- 1H-pyrrole-3 -carboxylic acid derivatives and its application for the production of pharmaceutical compounds.
C07D 401/10 - 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 carbon chain containing aromatic rings
C07D 207/34 - 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
C07D 217/16 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
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 disclosure relates to compounds of formula (I) and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta-hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
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
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.
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
The present invention relates to the field of pharmacy, particularly to a pharmaceutical composition for oral administration comprising a pharmaceutical composition for oral administration comprising: (a) an inert substrate, and (b) a mixture comprising N-(3-(6-amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, or a pharmaceutically acceptable salt thereof, or a free form thereof, and at least one binder. The present invention also relates to a process for preparing said pharmaceutical composition for oral administration; and to the use of said pharmaceutical composition in the manufacture of a medicament.
The present disclosure relates to methods for reducing the oxidation level of cysteine residues in recombinant polypeptides such as anti-IL-17 antibodies during cell culture (e.g., a preparation of secukinumab antibodies) that have been recombinantly produced by mammalian cells. Also provided are purified preparations of recombinant polypeptides such as anti-IL-17 antibodies or antigen binding fragments thereof produced by such methods, e.g, purified preparations of secukinumab. Also provided are purified preparations of recombinant polypeptides produced by such methods wherein the level of active recombinant polypeptide in the preparation is high.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
44.
RADIOLABELLED ALPHA-V BETA-3 AND/OR ALPHA-V BETA-5 INTEGRINS ANTAGONIST FOR USE AS THERAGNOSTIC AGENT
The present disclosure relates to ?v?3 and/or ?v?5 integrins antagonist radiopharmaceuticals and their use in a theragnostic approach for selection and therapy of human subjects with tumors overexpressing ?v?3 and/or ?v?5 integrins. In particular, the present disclosure relates to a pharmaceutical composition of ?v 177Lu radiolabeled ?v?3 and/or ?v?5 integrins antagonist, for use in treating tumors overexpressing ?v?3 and/or ?v?5 integrins in a human subject eligible for said treatment, wherein said subject has been selected for the treatment by PET/CT or PET/MRI or SPECT/CT or SPECT/MRI imaging with the same ?v?3 and/or ?v?5 integrins antagonist but with 68-Ga as radiometal for use as imaging agent.
The present disclosure relates to a compound of Formula (I): (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R1 through R8 are as defined herein, and methods of making and using the same.
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
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 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
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
46.
PHARMACEUTICAL COMBINATIONS COMPRISING A KRAS G12C INHIBITOR AND USES OF A KRAS G12C INHIBITOR FOR THE TREATMENT OF CANCERS
It relates to a pharmaceutical combination comprising a KRAS G12C inhibitor, in particular 1- {6- [ (4M) -4- (5-Chloro-6-methyl-1H-indazol-4-yl) -5-methyl-3- (1-methyl -1H-indazol-5-yl) -1H-pyrazol-1-yl] -2-azaspiro [3.3] heptan-2-yl} prop- 2-en-1-one (Compound A) and one or more therapeutically active agents selected from a SHP2 inhibitor (e.g. TNO155) and a PD-1 inhibitor; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of a cancer or a tumor, in particular wherein the cancer or tumor is KRAS G12C mutated.
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
47.
USE OF MGLUR5 ANTAGONISTS FOR TREATING GAMBLING DISORDER
The present invention relates to the use of mavoglurant in the treatment of gambling disorder. The present invention also relates to the use of mavoglurant in the treatment of gaming disorder.
The invention relates to the mavoglurant, or a pharmaceutically acceptable salt thereof: in the treatment of substance use disorder, wherein the substance is an amphetamine-type stimulant; in a treatment in the reduction of substance use by a substance use disorder patient, wherein the substance is an amphetamine-type stimulant; in a treatment to prevent relapse into substance use by a substance use disorder patient, wherein the substance is an amphetamine-type stimulant; in a treatment to promote substance abstinence by a substance use disorder patient, wherein the substance is an amphetamine-type stimulant; in the treatment of the symptoms of depression or anxiety associated with substance use disorder, wherein the substance is an amphetamine-type stimulant.
The invention relates to a dosage regimen of Compound (I), or a pharmaceutically acceptable salt thereof, for the treatment of diseases or disorders mediated by negative allosteric modulation or inhibition of NR2B-NMDA receptor including, but not limited to, major depressive disorder, treatment resistant depression and suicidality. The invention also relates to the use of Compound (I), or a pharmaceutically acceptable salt thereof, in the treatment of major depressive disorder in patients with suicidal ideation with intent.
A61K 31/40 - 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
A61P 25/00 - Drugs for disorders of the nervous system
Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody- drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody- drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
51.
MCL-1 INHIBITOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
Anti-CD48 antibody-drug conjugates are disclosed. The anti-CD48 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD48 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
Disclosed herein are antibodies, antigen binding fragments thereof, and antibody drug conjugates thereof that bind human CD48. Also disclosed are pharmaceutical compositions comprising the antibodies, antigen binding fragments thereof, and antibody drug conjugates thereof; and methods of making and using such pharmaceutical compositions for treating cancer in a patient in need of treatment.
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
53.
BISPECIFIC ANTIBODIES FOR USE IN TREATMENT OF NLRC4-GOF INFLAMMASOMAPATHY
The invention relates to bivalent bispecific monoclonal antibodies (bbmAb) or variants thereof for use in the treatment or for use in alleviating the symptoms of an NLRC4 inflammasomopathy, such as an NLRC4-GOF inflammasomopathy in a subject in need thereof. This invention also relates to bivalent bispecific monoclonal antibodies (bbmAb) or variants thereof for use in the treatment or for use in alleviating the symptoms of AIFEC in a subject in need thereof.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
This disclosure provides methods for treating a B-cell lymphoma, by administering a CD 19 CAR therapy as described herein, in combination with a BCL2 inhibitor as described herein.
The present disclosure provides CD19 binding molecules that specifically bind to CD19, including monospecific, bispecific and trispecific binding molecules, conjugates comprising the CD19 binding molecules, and pharmaceutical compositions comprising the CD19 binding molecules and the conjugates. The disclosure further provides methods of using the C19 binding molecules to treat diseases and disorders associated with expression of CD19. The disclosure yet further provides recombinant host cells engineered to express the CD19 binding molecules and methods of producing the CD19 binding molecules by culturing the host cells under conditions in which the CD19 binding molecules are expressed.
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 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
The present disclosure provides combinations of anti-CD19 agents and B cell targeting agents and methods of treating subjects having B cell malignancies with combinations of anti-CD19 agents and a B cell targeting agents.
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 novel pyridine-N oxide substituted 2-formamido (N-phenyl and N-pyridyl) acetamide compounds that are Interleukin-17 (IL-17) inhibitors, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by IL-17.
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 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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 413/12 - 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 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to the treatment and/or prevention of atopic dermatitis or a related condition. More specifically, the invention relates to the administration of an IL-18 antagonist, e.g., an anti-IL-18 antibody or a fragment thereof, to treat or prevent atopic dermatitis or a related condition in a subject in need thereof.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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
59.
NEW CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR COMPOUND
Provided are crystalline forms of a KRAS G12C inhibitor compound and to processes for their preparation. Furthermore, provided is pharmaceutical composition comprising said crystalline forms, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition can be used as a medicament, in particular for the treatment of cancer, and KRAS G12C-mutant cancer.
The invention relates to compounds of Formula I: Formula (I) or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for method for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of cryptosporidiosis by administering such a compound.
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
A61P 33/02 - Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
The invention relates to a mouse double minute 2 (MDM2) inhibitor for use in the treatment and/or prevention of a hematologic neoplasm relapse after hematopoietic cell transplantation (HCT) in a patient. In embodiments, the hematologic neoplasm is a leukaemia, preferably acute myeloid leukaemia (AML). Preferably, the patient received an allogeneic T cell transplantation, either together with the HCT and/or after HCT, such as at the time point of MDM2 administration. Furthermore, the invention relates to a pharmaceutical composition comprising a MDM2 inhibitor and an exportin 1 (XPO-1) inhibitor for use in the treatment and/or prevention of a hematologic neoplasm relapse after hematopoietic cell transplantation (HCT) in a patient according to any of the preceding claims.
A61K 31/40 - 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
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 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
The present invention relates to tricyclic compounds comprising a diazepinone moiety which are effective in inhibiting Sppl2a (signal peptide peptidase like protease 2a), to pharmaceutical compositions containing such inhibitors, and to methods of using such inhibitors and compositions.
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
Aspects of this disclosure relate generally to the use of biomaterials for the in vivo generation of CAR expressing cells. In some embodiments, the biomaterials comprise one or more of a cell recruitment composition, a viral vector, and/or a cell activation agent.
A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 R2, R4 and X1 are defeined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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
65.
QUINOLINE COMPOUNDS AND COMPOSITIONS FOR INHIBITING EZH2
The invention disclosed herein relates to aza-quinoline compounds of Formula (I), pharmaceutical compositions comprising such compounds; and the use of such compounds for treating a disease or condition mediated by Enhancer of Zeste Homolog 2 (EZH2), Polycomb Repressive Complex 2 (PRC2), or a combination thereof.
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to anti-BAFFR antibodies or binding fragments thereof, alone or in combination with BTK inhibitors, for use in the treatment of CLL. Specifically, the invention relates to a pharmaceutical combination comprising a BTK inhibitor, or a pharmaceutically acceptable salt thereof, and an anti-BAFFR antibody or binding fragment thereof, and their use in the treatment of CLL. The invention also relates to a method for the treatment of CLL that involves administering the combination; and to the use of the combination for the manufacture of a medicament for the treatment of CLL.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61P 35/02 - Antineoplastic agents specific for leukemia
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 disclosure relates to anti-BAFFR antibodies and binding fragments thereof, alone or in combination with additional agents, for use in the treatment of B cell malignancies, for example a B-cell non-Hodgkin's lymphoma.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61P 35/02 - Antineoplastic agents specific for leukemia
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
68.
COMBINATION OF A BCL-2 INHIBITOR AND A HYPOMETHYLATING AGENT FOR TREATING CANCERS, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF
A combination comprising a Bcl-2 inhibitor with a hypomethylating agent, uses in the treatment of cancers and pharmaceutical compositions thereof. The Bcl-2 inhibitor is 5-(5-chloro-2- {[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydroisoquinolin-2(1H)-yl]carbonyl}phenyl)-N-(5- cyano-1,2-dimethyl-1H-pyrrol-3-yl)-N-(4-hydroxyphenyl)-1,2-dimethyl-1H-pyrrole-3- carboxamide and the hypomethylating agent is selected from decitabine, azacitidine and guadecitabine.
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/706 - 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
A61K 31/708 - 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 containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
The invention relates to the use of mavoglurant, or a pharmaceutically acceptable salt thereof: in the reduction of opioid use by an opioid use disorder patient; in preventing relapse into opioid use by an opioid use disorder patient; in the promotion of opioid abstinence by an opioid use disorder patient; in the treatment of the symptoms of depression or anxiety associated with opioid use disorder.
The present disclosure provides anti-BTC antibodies, methods of producing said antibodies, pharmaceutical compositions comprising said antibodies, and methods of using said antibodies. The present disclosure also provides multi-specific binding molecules, e.g., bispecific antibodies, comprising a BTC binding moiety and an anti-VEGF binding moiety.
The present invention relates to a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme:. wherein LG, A, n, m and p are as defined in the Summary of the Invention, said manufacture including the manufacture and use of a compound of the formula VI; wherein R1 is a secondary amino protecting group and R5 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl or unsubstituted or substituted aryl.
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 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
72.
PROCESS FOR THE MANUFACTURE OF 1,4-DISUBSTITUTED PYRIDAZINE COMPOUNDS
The invention relates to a novel process, novel process step(s) and novel intermediate(s) useful for the preparation of 1,4-disubstituted pyridazine compounds, such as 5-(1 H-Pyrazol-4-yl)-2-(6- ((2,2,6,6-tetramethylpiperidin-4-yl)oxy)pyridazin-3-yl)phenol.
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
73.
METHODS OF TREATING THYROID EYE DISEASE AND GRAVES' ORBITOPAHY USING INTERLEUKIN-17 (IL-17) ANTAGONISTS
The present disclosure relates to methods for treating Thyroid Eye Disease (e.g., Graves' Orbitopathy) using Interleukin (IL)-17 antagonists, e.g., secukinumab. Also disclosed herein are IL-17 antagonists, e.g., IL-17 antibodies, such as secukinumab, for treating patients having Thyroid Eye Disease (e.g., Graves' Orbitopathy), as well as medicaments, dosing regimens, pharmaceutical formulations, dosage forms, and kits for use in the disclosed uses and methods.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
The present disclosure relates to dosing regimens comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione compounds or pharmaceutical compositions, pharmaceutical formulations, or combinations comprising the same; and methods of using such compounds, combinations, and compositions in the treatment or prevention IKAROS Family Zinc Finger 2 (IKZF2)-dependent diseases or disorders or where reduction of IKZF2 or IKZF4 protein levels can ameliorate a disease, for example, the treatment of cancers.
METHYL 2-(FLUOROMETHYL)-5-OXO-4-PHENYL-4,5,6,7-TETRAHYDRO-1H-CYCLOPENTA[B]PYRIDINE-3-CARBOXYLATES AND METHYL 2-(FLUOROMETHYL)-5-OXO-4-PHENYL-1,4,5,7-TETRAHYDROFURO[3,4-B]PYRIDINE-3-CARBOXYLATES AS CAV1.2 ACTIVATORS
The present disclosure provides for a compound according to formula (I) or a pharmaceutically acceptable salt thereof as Cav1.22 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, or early repolarization syndrome.
A61K 31/4355 - 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 oxygen as a ring hetero atom
A61P 25/00 - Drugs for disorders of the nervous system
C07D 221/04 - Ortho- or peri-condensed ring systems
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
76.
METHYL 2-METHYL-5-OXO-1,4,5,7-TETRADHYDROFURO[3,4-B]PYRIDINE-3-CARBOXYL ATE COMPOUNDS AS CAV1.2 ACTIVATORS
The present disclosure provides for a compound according to formula (I) or a pharmaceutically acceptable salt thereof as Cav1.2 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, and early repolarization syndrome.
A61K 31/4355 - 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 oxygen as a ring hetero atom
A61P 25/00 - Drugs for disorders of the nervous system
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
77.
TREATMENT OF FOOD ALLERGY USING ANTI-IGE ANTIBODIES
The present disclosure relates to methods for modifying the course of a disease or disorder involving IgE, in particular an IgE mediated food allergy to one or more allergens, in subjects having such disease or condition.
The disclosure provides compositions and methods for treating diseases such as cancer. The disclosure also relates to methods of making improved CART cell therapies, e.g., with reduced expression and/or a reduced biological activity of ZBTB32. The disclosure further provides ZBTB32 inhibitors, and methods of using the same alone or in combination with CART cell therapies.
Provided are dosing regimens of polyomavirus neutralizing antibodies and related methods and pharmaceutical compositions for treating polyomavirus infections.
The present disclosure provides recombinant adeno-associated virus (AAV) virions comprising: a) a variant capsid protein; and b) a heterologous nucleic acid comprising one or more nucleotide sequences encoding one or more heterologous gene products. The rAAV virions are useful for delivery of gene products to a retinal cell. The present disclosure provides methods of delivering a gene product to a retinal cell in an individual.
The present invention provides a compound of Formula (I): or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating a disease or condition mediated by mixed lineage leukemia 1 (MLL1).
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 31/53 - 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
C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
82.
DOSING REGIMENS FOR N-((5-FLUORO-2,3-DIHYDROBENZOFURAN-4-YL)METHYL)-8-(2-METHYLPYRIDIN-3-YL)-[1,2,4]TRIAZOLO[4,3-C]PYRIMIDIN-5-AMINE, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, FOR USE IN TREATING PRC2-MEDIATED DISEASES OR DISORDERS
The invention provided herein provides dosage and dosage regimens for N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine (Compound (1)), or a pharmaceutically acceptable salt thereof, Compound (1) for the treatment of PRC2-mediated diseases or disorders. In addition, the invention provides using such dosage and dosage regimens in methods for treating PRC2-mediated diseases or disorders.
Described herein is a crystalline hydrate form of LNP023 hydrochloride and to a process for its preparation. Furthermore, described herein is a pharmaceutical composition comprising the crystalline hydrate form of LNP023 hydrochloride, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition described herein can be used to treat a disease and disorder mediated by complement activation.
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
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
84.
PHARMACEUTICAL COMBINATION COMPRISING TNO155 AND NAZARTINIB
The present invention relates to a pharmaceutical combination comprising TNO155 and nazartinib; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of conditions in a SHP2 inhibitor combined with EGFR inhibition is beneficial in, for example, the treatment of cancers.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/506 - Pyrimidines; Hydrogenated 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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
This application discloses compositions and methods of treating follicular lymphoma using CCR7 antibody drug conjugates. Also disclosed herein are methods of treating cancer in a subject in need thereof, comprising administering to said subject an antibody drug conjugate, wherein the cancer expresses CCR7, wherein the antibody drug conjugate is administered to said subject at about 0.1 mg/kg to about 10 mg/kg.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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
The present invention relates to computer-implemented method for assessing a level of activity, including presence or an absence, of a disease in at least one eye of a patient, wherein the disease is a neovascular ocular disease. The method comprises the steps of receiving, via one or more input elements, a set of input patient data corresponding to the patient and comprising retinal images of the patient; applying a first algorithm for imaging data analysis to the retinal images to identify values of e anatomical variables of the patient's eye; applying a second algorithm to the values of anatomical variables identified, and to distinct clinical, non-image derived input patient data comprised in the set of input patient data, in order to consequently make an assessment of the level of activity of the disease in the eye of the patient, and/or of the progression or regression of the disease with respect to a level of activity formerly determined. Based on the assessment, a disease activity score is generated and output corresponding to the level of activity of the disease. The assessment of disease activity is used to adjust a dosing regimen of a drug for treatment of the patient's eye disease.
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
87.
COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2.ALPHA. A ND THEIR METHODS OF USE
The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease. The compounds are inhibitors or modulators of HIF2alpha.
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
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
88.
METHODS FOR RADIOLABELING PSMA BINDING LIGANDS AND THEIR KITS
The present invention relates to methods for labeling a PSMA binding ligand with a radioactive isotope, preferably 68Ga, 67Ga or 64Cu, said method comprising the steps of: i. providing a single vial comprising, in dried form, said PSMA binding ligand of the following formula (I): (I) at least one buffering agent, sodium chloride and a stabilizer against radiolytic degradation, ii. adding a solution of said radioactive isotope into said single vial, thereby obtaining a solution of said PSMA binding ligand of formula (I) with said radioactive isotope, iii. mixing the solution obtained in ii., and incubating it for a sufficient period of time for obtaining said PSMA binding ligand labelled with said radioactive isotope, and, iv. optionally, adjusting the pH of the solution.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
C07B 59/00 - Introduction of isotopes of elements into organic compounds
89.
METHODS FOR RADIOLABELLING PSMA BINDING LIGANDS AND THEIR KITS
The present disclosure relates to methods for radiolabelling PSMA binding ligands with a radioactive isotope, preferably 68Ga, 67Ga or 64Cu, and their kits.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
C07B 59/00 - Introduction of isotopes of elements into organic compounds
90.
DOSING REGIMEN FOR TREATING A DISEASE MODULATED BY CSF-1R
The present disclosure relates to the field of pharmacy, particularly to a CSF-1R inhibitor for use in the treatment of disease modulated by CSF-1R. For example, the disclosure relates to a CSF-1R inhibitor for use in the treatment of cancer or neurodegenerative diseases. The disclosure also relates to a CSF-1R inhibitor or a pharmaceutical combination comprising a CSF-1R inhibitor, or a pharmaceutically acceptable salt thereof, and an anti-PD-1 antibody mo!ecu!e, or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer; to a method for the treatment of cancer that involves administering a CSF-1R inhibitor or the combination; and to the use of a CSF-1R inhibitor or the combination for the manufacture of a medicament for the treatment of cancer.
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/00 - Drugs for disorders of the nervous system
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
Inventor
Neyts, Johan
Poon, Daniel
Pfister, Keith Bruce
Malpani, Yashwardhan R.
Jung, Young-Sik
Han, Soo Bong
Biswas, Bishyajit Kumar
Chakrasali, Prashant
Kim, Chonsaeng
Shin, Jin Soo
Kim, Hae Soo
Lee, Chong-Kyo
Abstract
The invention provides compounds of Formula (I): as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
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
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
Inventor
Neyts, Johan
Poon, Daniel
Pfister, Keith Bruce
Jung, Young-Sik
Han, Soo Bong
Malpani, Yashwardhan R.
Chakrasali, Prashant
Kim, Chonsaeng
Shin, Jin Soo
Kim, Hae Soo
Lee, Chong-Kyo
Lee, Sang-Ho
Abstract
This disclosure provides compounds of Formula (I), (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
93.
PHARMACEUTICAL COMPOSITIONS AND PHARMACEUTICAL PRODUCTS OF HETERODIMERIC HUMAN INTERLEUKIN-15 (HETIL-15)
The disclosure is directed to stable pharmaceutical compositions comprising a heterodimer complex of IL-15 and IL-15Ra and pharmaceutical products comprising such compositions. The disclosure is also directed to the use of these compositions (e.g. as part of a kit having instructions for use) and pharmaceutical products for the treatment of lymphopenia, cancer, or infectious disease.
The invention concerns ofatumumab for use in the treatment of multiple sclerosis (MS), wherein the treatment is a long-term treatment and wherein serum IgG level is maintained during the treatment. The invention further relates to B cell and/or T cell inhibitors for use in the treatment of MS, said treatment comprising monitoring serum IgG level and selecting ofatumumab as the B cell and/or T cell inhibitor if the serum IgG level decreases and/or said treatment comprising assessing the predisposition of the patient for an increased risk of infections and selecting ofatumumab as the B cell and/or T cell inhibitor if a predisposition is identified. The invention further relates to ofatumumab for use in the treatment of multiple sclerosis, wherein patients having a lowered serum IgG level are treated and/or wherein patients having risk factors associated with serum Ig levels, in particular serum IgG levels, are treated.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61P 25/00 - Drugs for disorders of the nervous system
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.
BIARYL DERIVATIVES AS YAP/TAZ-TEAD PROTEIN-PROTEIN INTERACTION INHIBITORS
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
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 403/04 - 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
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
C07D 405/10 - 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 aromatic rings
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
C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 413/04 - 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
C07D 417/04 - 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 two hetero rings directly linked by a ring-member-to-ring- member bond
The present disclosure provides salts of lipoic acid choline ester (LACE), crystalline forms thereof, and methods of use thereof. The present disclosure further provides pharmaceutical compositions of LACE salts and methods of use thereof.
The present invention relates generally to processes for production of heavily glycosylated recombinant proteins (e.g., mucins and mucin-like proteins, such as lubricin), the processes comprising culturing mammalian cells capable of producing a glycoprotein in a liquid medium in a system comprising one or more bioreactors, concentrating and purifying and formulating the glycoprotein, the purification comprising one or more steps of chromatography, an endonuclease step, and at least one step of viral inactivation. In certain aspects the invention relates to pharmaceutical compositions comprising purified recombinant human lubiricin, and methods of treating a subject in need thereof.
C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
The present invention relates to a pharmaceutical combination comprising dabrafenib, an Erk-inhibitor and a RAF inhibitor; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of conditions in which MAPK pathway inhibition is beneficial, for example, in the treatment of cancers.
The present invention relates to a pharmaceutical combination comprising dabrafenib, an Erk-inhibitor and a SHP2 inhibitor; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of conditions in which MAPK pathway inhibition is beneficial, for example, in the treatment of cancers.
The invention provides methods of making immune effector cells (for example, T cells, NK cells) that express a chimeric antigen receptor (CAR), and compositions generated by such methods.
patents
