The specification generally relates to compounds of Formula (I):
The specification generally relates to compounds of Formula (I):
The specification generally relates to compounds of Formula (I):
and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.
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 31/502 - Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
The disclosure relates to methods and compositions for the treatment of systemic lupous erythematosus (SLE). Specifically, the disclosure relates to methods comprising administering to a subject a type I IFN receptor inhibitor.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 specification relates to compounds of Formula (1):
The specification relates to compounds of Formula (1):
The specification relates to compounds of Formula (1):
and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
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
Disclosed are dendrimers of formula (I):
Disclosed are dendrimers of formula (I):
Disclosed are dendrimers of formula (I):
and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising the dendrimer of formula (I) and methods of using the same for treating cancer.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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 47/60 - 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 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
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
A compound with the Formula (I): A-B-C wherein A is of the following formula (II): where X1is C-RA16-105-65-105-10 heterocyclyl and their use as PCSK9 inhibitors.
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
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 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
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 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present disclosure relates to a system and method for use in performing clinical endpoint adjudication to provide: efficient, automated clinical event classification and medical review triage; reduce the time to identify clinical events; a unified, consistent process for classification of clinical events; and proactive identification of events in near real-time.
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
G06F 40/40 - Processing or translation of natural language
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
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
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 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
There is provided a new and improved synthetic route for the synthesis of the compound 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (Formula (I)) that is readily scalable for commercial production.
There is provided a new and improved synthetic route for the synthesis of the compound 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (Formula (I)) that is readily scalable for commercial production.
There is provided a new and improved synthetic route for the synthesis of the compound 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (Formula (I)) that is readily scalable for commercial production.
Also provided are important intermediate compounds that are formed in the new and improved synthetic route for the synthesis of the compound of formula (I).
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
A pharmaceutical formulation which comprises Compound 1, one or more pharmaceutical fillers, one or more pharmaceutical disintegrants, and one or more pharmaceutical lubricant.
Methods for treating and/or preventing HFpEF and/or at least one disease, disorder, and/or condition associated therewith in patients by the use of dapagliftozin and compositions comprising the same are disclosed.
Disclosed are methods for treating solid tumors with an anti-PD-L1 antibody and an anti-CTLA- 4 antibody concurrently with chemoradiation therapy (cCRT).
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
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
A pharmaceutical formulation which comprises Compound 1, one or more pharmaceutical fillers, one or more pharmaceutical disintegrants, and one or more pharmaceutical lubricant.
A pharmaceutical composition comprising: (a) one or more of a first pellet comprising i. a first core, and ii. a first coating on the first core, wherein the first coating comprises a mineralocorticoid receptor (MR) modulator and a first binder; and (b) one or more of a second pellet comprising i. a second core, and ii. a second coating on the second core, wherein the second coating comprises an SGLT2 inhibitor, wherein the SGLT2 inhibitor is about 5% to about 20% by weight of the second pellet, wherein the composition comprises about 20% to about 50% by weight of the mineralocorticoid receptor (MR) modulator; and about 1% to about 10% by weight of the SGLT2 inhibitor. Said compositions for use in the treatment of chronic kidney disease or heart failure.
Provided herein are system, apparatus, article of manufacture, method and/or computer program product embodiments, and/or combinations and sub-combinations thereof, for providing interactive exploration and analysis of cellular environments represented within MIF images. An embodiment includes a pipeline configured to generate an interactive visualization with selectable icons that represent cells in an MIF image by identifying identifying cells in the MIF image and generating a graph of the MIF image based on coordinates and the properties of the identified cells, with each node in the graph corresponding to the cells as well as neighboring cells. The graph may be transformed into embeddings and generating an interactive visualization of the graph based on the embeddings. Selectable icons in the interactive visualization correspond to nodes in the graph.
G06T 11/20 - Drawing from basic elements, e.g. lines or circles
G06F 3/04817 - Interaction techniques based on graphical user interfaces [GUI] based on specific properties of the displayed interaction object or a metaphor-based environment, e.g. interaction with desktop elements like windows or icons, or assisted by a cursor's changing behaviour or appearance using icons
G06T 7/62 - Analysis of geometric attributes of area, perimeter, diameter or volume
G06V 20/69 - Microscopic objects, e.g. biological cells or cellular parts
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
19.
PROCESS FOR THE PREPARATION OF SUBSTITUTED PYRROLOPYRIMIDINES AND INTERMEDIATES
There is provided a new and improved synthetic route for the synthesis of the compound 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (Formula (I)) that is readily scalable for commercial production. (I) Also provided are important intermediate compounds that are formed in the new and improved synthetic route for the synthesis of the compound of formula (I).
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
The current disclosure provides novel therapeutic methods for treating SCLC and other neuroendocrine cancers by evaluating the biomarker SLFN11. Aspects of the disclosure relate to a method for treating a subject with small cell lung cancer (SCLC) or with a neuroendocrine cancer, the method comprising administering a combination of lurbinectedin and an ATR inhibitor to a subject that has had been determined to be negative for SLFN11 expression or have low SLFN11 expression in a biological sample from the subject.
A method of treating liver cirrhosis in a subject in need thereof. The method includes administering to the subject a composition. The composition includes a therapeutically effective amount of zibotentan and dapagliflozin.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 9/00 - Medicinal preparations characterised by special physical form
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
27.
MTA-COOPERATIVE PRMT5 INHIBITORS FOR USE IN THE TREATMENT OF CANCER
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 31/438 - 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 being spiro-condensed with carbocyclic or heterocyclic ring systems
The specification generally relates to compounds of Formula (I), (Ia), and (Ib) and pharmaceutically acceptable salts thereof, where X, Y1, Y2, Y3, Y4, and Y5and X1, X2, r, and q, have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO, and are thereby particularly useful in the treatment or prophylaxis of diseases or conditions in which modulation of the activity of the enzyme myeloperoxidase (MPO) is desirable, including diseases with inflammatory, cardiovascular, respiratory, renal, hepatic and/or neurological components, as well as neutrophilic driven diseases.
C07D 473/22 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one sulfur atom
Composition comprising a therapeutically effective amount of zibotentan and dapagliflozin for use in a method of treating liver cirrhosis in a subject in need thereof.
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
The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
C07D 235/06 - Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
A61K 47/36 - Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE (France)
SORBONNE UNIVERSITÉ (France)
ASTRAZENECA AB (Sweden)
Inventor
Dieu-Nosjean, Marie-Caroline
Germain, Claire
Hammond, Scott Alan
Steele, Keith
Abstract
The present invention relates to the field of prognostic of lung cancer. In this study, the inventors used extensive gene expression profiling and flow cytometry for an integrative analysis of the phenotypes of the B cells and CD4+ T cells from tumors and blood of NSCLC patients by TLS-B density. They showed that TIL B cells and TIL CD4+ T cells are more highly activated in tumors than in the periphery and that they express all the ligand/receptor pairs necessary for B/T interactions and two-way co-stimulation. Moreover, a high density of TLS-B cells is associated with higher frequencies of activated CD4+ T cells and lower frequencies of both immune checkpoint (ICP)-expressing CD4+ T cells and regulatory CD4+ T cells (Tregs) in the intratumor CD4+ T cell compartment. High densities of TLS-B cells together with low densities of FoxP3+ CD3+ Tregs in NSCLC tumors consistently identified the group of patients with the best clinical outcome. Overall, these results suggest that TLS-B cells promote the development of protective CD4+ T cell-mediated immune responses. Thus, the present invention relates to a method for determining the TLS (Tertiary Lymphoid Structures) status of a patient suffering from a lung cancer and thus the survival time of said patient.
The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
C07D 235/06 - Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
A61K 47/36 - Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
The present invention provides a pharmaceutical tablet formulation of tenapanor that is chemically stable and soluble comprising greater than about 6% w/w of amorphous tenapanor in its bis-HCl form, an acidifying agent, an antioxidant, a disintegrant, a lubricant, a glidant, a filler, and an immediate release coating, wherein the total chloride content of the active ingredient is greater than 5.82% and the particle diameter distribution D50 is from about from about 18 μm to about 22 μm.
The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof,
The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof,
The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof,
that inhibit dipeptidyl peptidase 1 (DPP1) activity. Methods provided herein are useful for prophylaxis, increasing the lung function in a patient, and/or and/or decreasing the rate of pulmonary exacerbation in a patient. In one embodiment, the compound of Formula (I) is (2S)—N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide.
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
A61K 9/00 - Medicinal preparations characterised by special physical form
35.
METHODS FOR DETECTING METABOLITES USING A MICROFLUIDIC-BASED CE-MS SYSTEM
The present disclosure relates to methods of detecting metabolites using a microfluidic capillary electrophoresis-mass spectrometry (CE-MS) system. The metabolites can be useful to diagnosis diseases or disorders, as well as to monitor therapeutic efficacy of compounds used to treat these diseases or disorders.
The present disclosure relates to a therapeutic combination comprising (i) a recombinant poxvirus comprising in its genome a heterologous nucleic acid sequence encoding interleukin-12 (IL-12) and (ii) a PD-1 inhibitor or PD-L1 inhibitor. Methods of treating cancer and methods of enhancing a tumor-specific immune response comprising administering the therapeutic combination are also provided.
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 methods for treating ischemic events in a patient, especially ST-segment elevation myocardial infarction and acute ischemic stroke, by administrating a recombinant apyrase protein in conjunction with a P2Y12 inhibitor.
C07K 14/47 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from humans from vertebrates from mammals
The disclosure relates to methods and compositions for the treatment of Systemic Lupus Erythematosus (SLE). The disclosure particular relates to the treatment of flares in SLE across multiple organ domains.
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 9/00 - Medicinal preparations characterised by special physical form
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 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 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to azaquinolone compounds of Formula (I), and their use in medicine.
The present invention relates to azaquinolone compounds of Formula (I), and their use in medicine.
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
43.
EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITORS IN COMBINATION WITH HGF-RECEPTOR INHIBITORS FOR THE TREATMENT OF CANCER
The specification relates to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) for use in the treatment of cancer, wherein the EGFR TKI is administered in combination with an inhibitor of c-MET.
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A method of assessing a wound in a subject is provided. The method comprises obtaining one or more optical coherence tomography images of the wound and analysing the one or more optical coherence tomography images using a deep learning model that has been trained to classify pixels in an optical coherence tomography image of a wound between a plurality of classes comprising a plurality of classes associated with different types of wound tissue, thereby obtaining for each image analysed, an indication of the location of tissue likely to belong to each of the different types of wound tissue in the respective image.
A61B 5/00 - Measuring for diagnostic purposes ; Identification of persons
G06V 10/764 - Arrangements for image or video recognition or understanding using pattern recognition or machine learning using classification, e.g. of video objects
G06T 7/55 - Depth or shape recovery from multiple images
This disclosure relates to an Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor (TKI) and an anti-EGFR/cMET antibody molecule for use in combination in the treatment of cancer (for example, non-small cell lung cancer [NSCLC]).
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 31/501 - Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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 disclosure relates to methods and compositions for the treatment of patients that are resistant to immuno-oncology therapies. Specifically, the disclosure relates to methods comprising administering to a subject in need thereof at least one of an antisense compound targeted to signal transducer and activator of transcription 3 (STAT3), a receptor tyrosine kinase inhibitor with selectivity for vascular endothelial growth factor receptor 1-3 (VEGFR1-3) and c-kit, a PI3Kγ inhibitor, an inhibitor of epidermal growth factor receptor, an inhibitor of programmed death-ligand 1 (PD-L1), an inhibitor of cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), and/or chemotherapy agent.
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 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
NN-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)-6- morpholinoquinoline-4-carboxamide; corresponding pharmaceutical compositions; uses to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits; and methods of preparation.
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
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
Compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, wherein R2, R3, R5, R6, R7, and R8 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
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 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
Compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5, and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)- mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
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
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
C12N 9/64 - Proteinases derived from animal tissue, e.g. rennin
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
C12N 9/06 - Oxidoreductases (1.), e.g. luciferase acting on nitrogen containing compounds as donors (1.4, 1.5, 1.7)
The present provides a method of treating ovarian cancer, breast cancer, gastrointestinal cancer, lung cancer, cancer of the brain or prostate cancer in a subject in need thereof, comprising administering to the subject a first amount of a selective PARP1 inhibitor or a pharmaceutically acceptable salt thereof, and a second amount of an ATR inhibitor or a pharmaceutically acceptable salt thereof. Also disclosed are compositions and kits comprising a PARP inhibitor and ATR inhibitor.
The disclosure generally relates to methods for treating cancer in a patient using durvalumab in combination with chemotherapy based on the patient's minimal residual status. Specifically, the disclosure relates to preventing or treating a recurrent tumor in a patient, wherein the patient is minimal residual disease-positive (MRD+), using durvalumab and chemotherapy.
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
Compounds having the structure of Formula (I):
Compounds having the structure of Formula (I):
Compounds having the structure of Formula (I):
and pharmaceutically acceptable salts thereof, wherein R2, R3, R5, R6, R7, and R8 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
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
58.
RXFP1 MODULATORS FOR TREATING RESISTANT HYPERTENSION OR HEART FAILURE WITH PULMONARY HYPERTENSION
The specification generally relates to uses of to uses of RXFP1 modulators, in particular methods of treating resistant hypertension and heart failure with pulmonary hypertension.
The specification generally relates to solid forms, for example, crystalline and amorphous forms, of (1S,4s)-4-(2-fluoro-4-methoxy-5-(((1S,2R,3S,4R)-3-(((1- methylcyclobutyl)methyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)phenoxy)-1- methylcyclohexane-1-carboxylic acid (Compound (I)). In particular, an amorphous form of Compound (I), solid dispersions and pharmaceutical compositions comprising such an amorphous form, and crystalline Form G of Compound (I).
C07C 237/52 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
60.
COMBINATIONS OF RXFP1 MODULATORS AND SGLT2 INHIBITORS
The specification generally relates to combinations of RXFP1 modulators and SGLT2 inhibitors, in particular pharmaceutical compositions comprising such combinations, and therapeutic methods using such combinations.
Provided herein are methods of purifying proteins of interest using continuous counter-current downstream processing. Also provided herein are methods of purifying proteins of interest using continuous counter-current affinity nanoparticle dialysis.
The present disclosure relates to a recombinant poxvirus comprising in its genome a heterologous nucleic acid sequence encoding interleukin-12 (IL-12). Methods for producing the recombinant poxvirus, compositions (e.g., pharmaceutical compositions) comprising the recombinant poxvirus, methods of treating cancer using the recombinant poxvirus, and kits comprising the recombinant poxvirus are provided.
The present invention relates to the treatment of melanoma in a patient, where the method includes administering to a patient who has or is suspected of having melanoma a therapeutically effective amount of tebentafusp; and a therapeutically effective amount of an immune checkpoint inhibitor. In particular, patients may have metastatic melanoma that is refractory to treatment with an anti-PD(L)1 inhibitor in the metastatic setting or where the patient's melanoma is relapsed following treatment with an anti-PD(L)1 inhibitor.
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
65.
METHODS OF TREATING MELANOMA USING TEBENTAFUSP AND IMMUNE CHECKPOINT INHIBITORS
The present invention relates to the treatment of melanoma in a patient, where the method includes administering to a patient who has or is suspected of having melanoma a therapeutically effective amount of tebentafusp; and a therapeutically effective amount of an immune checkpoint inhibitor. In particular, patients may have metastatic melanoma that is refractory to treatment with an anti-PD(L)1 inhibitor in the metastatic setting or where the patient's melanoma is relapsed following treatment with an anti-PD(L)1 inhibitor.
The present specification relates to novel physical forms of a indazole-5-carboxamide derivative, as well as solvate and salt forms of the same compound. A process for the preparation of the compound and uses of the new physical forms are also provided.
An example embodiment may involve obtaining an observation of demographic values, comorbidity values, vital sign values, and/or blood test values of an individual, wherein the individual was diagnosed with portal hypertension and/or cirrhosis; applying a machine learning model to the observation, wherein the machine learning model was trained with a training data set, wherein the training data set contains observations of corresponding demographic values, comorbidity values, vital sign values, blood test values, and/or disease progression values for a plurality of individuals diagnosed with portal hypertension and/or cirrhosis, and wherein the machine learning model is configured to provide a prediction of: (i) a hazard ratio of whether the individual is expected to exhibit progression to a condition related to portal hypertension or cirrhosis, and/or (ii) a period of time between that of the new observation and a further diagnosis of the condition; and providing the prediction based on the observation.
G16H 20/00 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance
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
G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
G16H 50/50 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT 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 mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
G16H 40/67 - ICT specially adapted for the management or administration of healthcare resources or facilities; ICT specially adapted for the management or operation of medical equipment or devices for the operation of medical equipment or devices for remote operation
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
C12N 9/00 - Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
71.
BIOMARKERS FOR PREDICTING OVERALL SURVIVAL IN RECORRENT/METASTATIC HEAD AND NECK SQUAMOUS CELL CARCINOMA
The present disclosure generally relates to methods for treating head and neck squamous cell carcinoma patients based on use of blood-based tumor mutation burden, PD-L1 expression, expression levels of immunomodulators, pro-angiogenesis markers and pro-inflammatory markers and/or identification of mutations in circulating tumor DNA.
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
G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for cancer
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 35/04 - Antineoplastic agents specific for metastasis
72.
AMINO HETEROAROMATIC COMPOUNDS USEFUL IN THE TREATMENT OF LIVER DISEASES
The specification relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of diseases such as liver disease.
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 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
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
An example embodiment may involve obtaining, by a computing system, an observation of demographic values of an individual, vital sign values of the individual, and blood test values of the individual; applying, by the computing system, a machine learning model to the observation, wherein the machine learning model was trained with a training data set, wherein the training data set contained observations of corresponding demographic values, vital sign values, blood test values, and either urine albumin-to-creatinine ratio (UACR) values or urine protein-to-creatinine ratio (UPR) values for a plurality of individuals, and wherein the machine learning model is configured to provide predictions of whether further observations are indicative of undiagnosed albuminuria or proteinuria; and providing, by the computing system, a prediction of whether the individual exhibits undiagnosed albuminuria or proteinuria based on the observation.
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
G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT 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 features methods of treating cancer with an immunomodulatory agent, such as an anti-PD-L1 antibody or an antigen-binding fragment thereof, and an antisense compound targeted to STAT3 in a subject in need thereof.
The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where A, Z, Y, RA, Linker and v have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in the prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where A, Z, Y, RA, Linker and v have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in the prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
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 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 409/04 - 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 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
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 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
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
The present disclosure relates, in general, to therapeutic combinations, and to corresponding methods of treatment, pharmaceutical compositions, and kits.
The specification relates to compounds of Formula (I):
The specification relates to compounds of Formula (I):
The specification relates to compounds of Formula (I):
and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of diseases such as liver disease.
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 413/12 - 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 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 409/06 - 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 carbon chain containing only aliphatic carbon atoms
The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of diseases such as liver disease.
C07D 261/18 - Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/06 - 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 carbon chain containing only aliphatic carbon atoms
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 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 413/12 - 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 417/06 - 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 carbon chain containing only aliphatic carbon atoms
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
The disclosure relates to methods and compositions for the treatment of type I IFN mediated disease. Specifically, the disclosure relates to a subcutaneous dose of a type I IFN receptor inhibitor.
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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
80.
COMBINATION OF ZIBOTENTAN AND DAPAGLIFLOZIN FOR THE TREATMENT OF ENDOTHELIN RELATED DISEASES
The present disclosure relates to the endothelin receptor antagonist (ERA) zibotentan in combination with the sodium-dependent glucose cotransporter 2 (SGLT-2) inhibitor dapagliflozin for use in the treatment of certain endothelin related diseases.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
Disclosed are compounds of formula (Ia) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of formula (Ia) and methods of using the same for treating cancer or a respiratory inflammatory disease and inhibiting arginase:
3.
The specification relates to spirocyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative 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
83.
PHARMACEUTICAL COMPOSITIONS COMPRISING AN ANTISENSE OLIGONUCLEOTIDE FOR ORAL ADMINISTRATION
A pharmaceutical composition comprising A) one or more ASO or a pharmaceutically acceptable salt thereof; B) one or more permeation enhancer; C) one or more optional pharmaceutically acceptable excipient; and D) one or more optional coating. Said composition for use in the treatment, prevention, or amelioration of a disease associated with PCSK9 or PNPLA3 in a subject.
The present disclosure provides dosages and methods for treating a disease associated with proprotein convertase subtilisin/kexin type 9 (PCSK9). The present disclosure also provides unit dosages, dosing regimens and methods for treating a disease associated with PCSK9.
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R1, R2, R3, R4 and R5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
86.
COMPOSITIONS AND METHODS OF TREATING CANCER WITH CHIMERIC ANTIGEN RECEPTORS
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
The specification relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
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
88.
BICYCLIC HETEROAROMATIC COMPOUNDS FOR TREATING CANCER
The specification relates to compounds of Formula (I): (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
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 403/12 - 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
The specification relates to compounds of Formula (I): (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
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
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
This specification discloses the use of an ATR inhibitor, preferably in combination with a taxane, for the treatment of cancer in a particular subset of patients who have previously received immunotherapy.
Provided herein are methods of reducing exacerbations of asthma in an asthma patient with nasal polyposis, comprising administering to the patient an effective amount of the anti-interleukin-5 receptor (IL-5R) antibody benralizumab or an antigen-binding 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
The specification relates to compounds of Formula (I): (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
The present disclosure provides a method of treating asthma in a subject at risk of asthma exacerbation, and a method of as-needed treatment or prevention of bronchoconstriction in a subject, and/or prevention of exacerbation in a subject with asthma, comprising administering as needed to the subject a composition comprising therapeutically effective amounts of albuterol and budesonide, wherein the composition is administered via a metered dose inhaler, wherein the method reduces risk of severe asthma exacerbation by at least about 15% as compared to administration of a composition comprising a same dose of albuterol alone, as measured by time-to-first severe asthma exacerbation. Also provided is a pharmaceutical composition comprising: albuterol and budesonide in the form of particles; a suspension medium comprising a hydrofluoroolefins (HFO) propellant and/or a hydrofluorocarbon propellant (HFC), and a plurality of respirable suspending particles, wherein the particles of albuterol and budesonide associate with the plurality of respirable suspending particles.
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
The present disclosure relates to nucleic acids that comprise a nucleotide sequence encoding an immunoglobulin heavy chain, wherein the nucleotide sequences of at one or two introns in the immunoglobulin heavy chain are deleted. These nucleic acids are useful for increasing immunoglobulin expression.
