The present invention provides antibodies that specifically bind to CD123. The invention further relates to immunoconjugates (e.g., antibody-drug conjugates, or ADCs) comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and ADCs for the treatment of a condition associated with cells expressing CD123 (e.g., cancer or autoimmune disease).
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Benaroya Research Institute at Virginia Mason (USA)
Inventor
Franklin, Edward Michael
Fennell, Brian Joseph
Stack, Edwina Catherine
Mosyak, Lidia
Apgar, James Reasoner
Chabot, Jeffrey Raymond
Khor, Bernard
Mikita, Thomas Jay
Chaparro-Riggers, Javier Fernando
Abstract
Provided herein are antibodies (including antigen-binding fragments thereof) that specifically bind to MIGIS-α, including for example without limitation, bispecific MIGIS-α/CD3 antibodies, other related antibodies, related nucleic acids, uses, and associated methods thereof. The disclosure also provides processes for making, preparing, and producing antibodies disclosed herein, including antibodies that bind to one or both of MIGIS-α and CD3.
C07K 16/42 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against immunoglobulins (anti-idiotypic antibodies)
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 disclosure provides CARs (CARs) that specifically bind to CD70. The disclosure further relates to engineered immune cells comprising such CARs, CAR-encoding nucleic acids, and methods of making such CARs, engineered immune cells, and nucleic acids. The disclosure further relates to therapeutic methods for use of these CARs and engineered immune cells comprising these CARs for the treatment of a condition associated with malignant cells expressing CD70 (e.g., 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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 40/11 - T-cells, e.g. tumour infiltrating lymphocytes [TIL] or regulatory T [Treg] cellsLymphokine-activated killer [LAK] cells
The invention relates to antibodies, and antigen-binding fragments thereof, that specifically bind TFPI and inhibit an activity thereof. Such antibodies and fragments are useful for treating bleeding disorders and shortening clotting time.
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
and pharmaceutically acceptable salts thereof, wherein A, L, X, Y and p are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may modulate the activity of antigens of interest and may be useful in inducing or enhancing an immune response against diseases, disorders and conditions mediated by antigens of interest.
The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
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 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
7.
METHODS AND DOSING REGIMENS COMPRISING A CDK2 INHIBITOR FOR THE TREATMENT OF CANCER
The disclosure provides methods of treating cancer in a subject in need thereof comprising administering to the subject a therapeutically effective amount of PF-07104091, as a monotherapy or in combination with an endocrine therapy agent and/or a CDK4/6 inhibitor.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
Solid Forms of 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, 1,3-Dihydroxy-2-(hydroxymethyl)propan-2-amine Salt
The invention provides solid forms of 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl) propan-2-amine salt for example, Form 1 or Form 2; as well as pharmaceutical compositions, and the uses thereof in treating diseases, conditions or disorders modulated by GLP-1R in a mammal, such as a human.
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 31/4545 - 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
9.
MELANOCORTIN 4 RECEPTOR ANTAGONISTS AND USES THEREOF
Described herein are compounds of Formula I: I and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R7, RF, t1, Y1, and Y2 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
Described herein are compounds of Formula I: I and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R7, RF, t1, Y1, and Y2 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
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 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
In one aspect, the invention relates to an immunogenic composition comprising modified O-polysaccharide molecules derived from E. coli lipopolysaccharides and conjugates thereof. Multivalent vaccines may be prepared by combining two or more monovalent immunogenic compositions for different E. coli serotypes. In one embodiment, the modified O-polysaccharide molecules are produced by a recombinant bacterium that includes a wzz gene.
The present invention relates to compounds of Formula (I):
The present invention relates to compounds of Formula (I):
or pharmaceutically acceptable salts thereof, wherein Ring A, Ring B, R1—R16, n and p are defined herein. The novel nitrogen-linked benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth, such as cancer, in patients.
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
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated 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
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
This invention relates to compositions that include a polypeptide derived from E. coli or a fragment thereof; and modified O-polysaccharide molecules derived from E. coli lipopolysaccharides and conjugates thereof, and methods of use thereof.
This invention relates generally to devices, systems, and methods for performing biological assays by using indicators that modify one or more optical properties of the assayed biological samples. The subject methods include generating a reaction product by carrying out a biochemical reaction on the biological sample introduced into a device and reacting the reaction product with an indicator capable of generating a detectable change in an optical property of the biological sample to indicate the presence, absence, or amount of analyte suspected to be present in the sample.
G01N 21/25 - ColourSpectral properties, i.e. comparison of effect of material on the light at two or more different wavelengths or wavelength bands
G01N 21/27 - ColourSpectral properties, i.e. comparison of effect of material on the light at two or more different wavelengths or wavelength bands using photo-electric detection
G01N 21/77 - Systems in which material is subjected to a chemical reaction, the progress or the result of the reaction being investigated by observing the effect on a chemical indicator
G01N 21/78 - Systems in which material is subjected to a chemical reaction, the progress or the result of the reaction being investigated by observing the effect on a chemical indicator producing a change of colour
G01N 35/00 - Automatic analysis not limited to methods or materials provided for in any single one of groups Handling materials therefor
The present disclosure provides deuterated compounds that are inducers of KLF2 and pharmaceutical compositions comprising the same. The present disclosure further provides method of treating an inflammatory disease or endothelial dysfunction comprising administering a therapeutically effective amount of the deuterated compounds disclosed herein.
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
C07B 59/00 - Introduction of isotopes of elements into organic compounds
The invention relates to compounds of Formula I″
The invention relates to compounds of Formula I″
The invention relates to compounds of Formula I″
wherein R, R1, R2, R3, p, q and q′ are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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
16.
Dosing Regime For Treatment of Chronic Hand Eczema
Method for treating moderate to severe chronic hand eczema in a subject in need thereof, which method comprises the step of administering to said subject a therapeutically effective amount of the compound of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide, or a pharmaceutically acceptable salt thereof.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
17.
Crystalline form of (2R)-2-(5-fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(pyrimidin-2-yl)-3,4-dihydro-1H-spiro[1,8-naphthyridine-2,3-pyrrolidin]-1-yl]propan-1-one
Described herein is a crystalline form of (2R)-2-(5-fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(pyrimidin-2-yl)-3,4-dihydro-1H-spiro[1,8-naphthyridine-2,3-pyrrolidin]-1-yl]propan-1-one having a powder X-ray diffraction pattern comprising at least one characteristic peak, in terms of 2θ at a copper wavelength, selected from 8.7±0.2, 11.1±0.2, and 13.3±0.2.
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
18.
Amorphous Form of (S)-2-(5-((3-Ethoxypyridin-2-YL)Oxy)Pyridin-3-YL)-N-(Tetrahydrofuran-3-YL)Pyrimidine-5-Carboxamide
Solid forms of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide, including crystalline forms and an amorphous form, in addition to pharmaceutical compositions, processes for preparing, and their use to treat diseases, conditions and disorders modulated by the activity of the diacylglycerol acyltransferase 2 (DGAT2) in a mammal such as a human are described herein.
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 31/506 - PyrimidinesHydrogenated 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
The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable organic or inorganic acid salt thereof, a pharmaceutically acceptable organic or inorganic acid, a pharmaceutically acceptable beta- or gamma-cyclodextrin and water, that is a clear solution, with the proviso that the organic or inorganic acid (including a salt thereof) is not a sulphonic acid. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.
The present disclosure relates to the treatment of cancer and/or cancer-associated disease. Certain aspects relate to the treatment of an individual having cancer or cancer-associated disease by administering to the individual a combination therapy of a first therapeutic agent that is an EZH2 inhibitor, a second therapeutic agent that is a CDK inhibitor, and a third therapeutic agent that is a selective estrogen receptor degrader.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
wherein Y1a, Y1b, Y2a, Y2b, Y2c, Y2d, Y2e, Y2f, Y2g, Y2h and Y2i are as defined herein and to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may be useful in the treatment of coronavirus infections and coronavirus infection related disorders.
C07B 59/00 - Introduction of isotopes of elements into organic compounds
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
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
A blister package is disclosed herein. The blister package includes a body, a plurality of pockets, and a top seal. The body has a top surface and a bottom surface opposite the top surface. The plurality of pockets is formed in the body. Each of the plurality of pockets extend below the top surface of the body. Each pocket of the plurality of pockets is configured to hold a pharmaceutical. The plurality of pockets is arranged in a manner that defines at least one dose. The plurality of pockets for the at least one dose includes a first pocket in parallel with a second pocket, and a third pocket perpendicular to the first pocket and the second pocket. The top seal is configured to interface with the body. The top seal is configured to hold the pharmaceutical in each respective pocket.
A61J 1/03 - Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
B65D 75/36 - Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents one sheet or blank being recessed and the other formed of relatively stiff flat sheet material, e.g. blister packages
The disclosure provides a method of treating cancer comprising administering to a subject in need thereof with a therapeutically effective amount of PF-07220060. The disclosure also provides a method of treating cancer comprising administering to a subject in need thereof with a therapeutically effective amount of PF-07220060 and an endocrine therapy agent.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
This disclosure relates to combination therapies for use in treating cancer, comprising a CDK2 inhibitor of Formula (I) and a selective CDK4 inhibitor of Formula (II), each as further described herein, optionally in further combination with an additional anti-cancer agent.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
The invention relates to compounds of Formula (I)-(III) and pharmaceutically acceptable salts thereof to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds the present invention may be useful in the treatment, prevention, suppression and amelioration diseases, disorders and conditions such as cancers.
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 31/553 - 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
The present invention provides antibodies that specifically bind to CD70 (Cluster of Differentiation 70). The invention further provides bispecific antibodies that bind to CD70 and another antigen (e.g., CD3). The invention further relates to antibody encoding nucleic acids, and methods of obtaining such antibodies (monospecific and bispecific). The invention further relates to therapeutic methods for use of these antibodies for the treatment of CD70-mediated pathologies, including 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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates), kits comprising said immunogenic compositions and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/385 - Haptens or antigens, bound to carriers
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
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
C08H 1/00 - Macromolecular products derived from proteins
This disclosure relates to a crystalline form of 4-[(1R)-1-aminopropyl]-2-{6-[(5S)-5-methyl-6,7-dihydro-5H-pyrro-lo[2,1-c][1,2,4]triazol-3-yl]pyridin-2-yl}-6-[(2R)-2-methylpyrrolidin-1-yl]-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin- 1-one (PF-07265028) free base and method of making thereof. The disclosure also relates to pharmaceutical compositions comprising this crystalline form, and to methods of using the crystalline form and such compositions for the treatment of abnormal cell growth, such as cancer, in a mammal.
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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
33.
CALICHEAMICIN DERIVATIVES AND ANTIBODY DRUG CONJUGATES THEREOF
The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.
C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Systems and methods for performing biological assays are provided herein. The systems and methods determine one or more characteristics of a nucleic acid amplification sample based on a modified optical property of the sample.
Embodiments disclosed herein may provide digital medicine support for predicting and mitigating side effects of bispecific antibody treatment (e.g., Pfizer's Elranatamab) for myeloma patients. The side effects may include cytokine release syndrome (CRS), infection (e.g., sepsis), neurotoxicity (e.g., peripheral neuropathy), cytopenia (e.g., neutropenia), etc. These side effects may be predicted based on passive collection of data from patient wearables, patient entered data on healthcare application, and other data such as bloodwork data. Trained machine learning models may be used for predicting the side effects. As the side effects may be predicted before their onsets, a proactive intervention may be feasible to improve the healthcare outcomes for myeloma patients.
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
G16H 50/50 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for simulation or modelling of medical disorders
The present invention provides compounds of Formula XA-1, XA-2, XA-3, XA-4, XA-5, or XA-6, or metabolites of Compound 1 or metabolites of a compound of Formula I, PA-I, or PA-III, including compositions and salts thereof, which are useful in the prevention and/or treatment of a disease or disorder such as T2DM, obesity, or NASH, as well as analytical methods related to the administration of Compound 1 or a compound of Formula I, PA-1, or PA-III.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
37.
DIGITAL MEDICINE COMPANION FOR TREATING AND MANAGING SKIN DISEASES
A digital medicine companion for managing skin diseases (e.g., atopic dermatitis, psoriasis) may include patient wearable devices passively collecting patient data, patient user devices with healthcare applications for the patient to enter health related data, central analytics for flare prediction and disease progress tracking, and a clinician dashboard. For flare prediction, a prediction tool may be trained using the ground truth of recorded flare occurrences for the trained model to predict whether observed scratch events may result in a flare. Upon predicting a likely flare, alert notifications may be generated, e.g., for a clinician and/or the patient. Furthermore, a baseline may be established based on the data passively gathered from the wearables and actively gathered from the patient user devices. The continuously collected data may be compared against the established baseline. Upon detecting a significant deviation, alerts may be sent to the patient and/or the clinician.
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
G16H 80/00 - ICT specially adapted for facilitating communication between medical practitioners or patients, e.g. for collaborative diagnosis, therapy or health monitoring
38.
Modulators of STING (Stimulator of Interferon Genes)
Provided herein are compounds of the general formula (I):
Provided herein are compounds of the general formula (I):
Provided herein are compounds of the general formula (I):
and pharmaceutically acceptable salts thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates) and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
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
41.
GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE RECEPTOR ANTAGONISTS AND USES THEREOF
Described herein are compounds of Formula I:
Described herein are compounds of Formula I:
Described herein are compounds of Formula I:
and their pharmaceutically acceptable salts, wherein R1, R2, R3, L1, T1, T2, T3, T4, t1, and t2 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and/or T2DM.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
42.
N-SUBSTITUTED-DIOXOCYCLOBUTENYLAMINO-3-HYDROXY-PICOLINAMIDES USEFUL AS CCR6 INHIBITORS
The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B)
The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B)
The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B)
or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - 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
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
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
43.
LILRB1 and LILRB2 ANTIBODIES AND METHODS OF USE THEREOF
The invention is directed to Anti-LILRB1 and anti-LILRB2 bispecific antibodies, anti-LILRB1 antibodies, and anti-LILRB2 antibodies, their uses and pharmaceutical compositions 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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates), kits comprising said immunogenic compositions and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/385 - Haptens or antigens, bound to carriers
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
45.
COMBINATION THERAPY COMPRISING A PKC INHIBITOR AND A C-MET INHIBITOR
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The invention relates to compounds of Formula (I)-(III) and pharmaceutically acceptable salts thereof to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds the present invention may be useful in the treatment, prevention, suppression and amelioration diseases, disorders and conditions such as cancers.
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 31/553 - 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
The invention relates to substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof that can activate adenosine 5′-monophosphate-activated protein kinase (AMPK). The invention further relates to pharmaceutical compositions comprising AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof and at least one pharmaceutically acceptable excipient, and methods of treating a condition comprising administering AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof.
This invention provides a polypeptide derived from E. coli or a fragment thereof, including compositions and methods thereof. In one embodiment, the compositions comprise a polypeptide derived from E. coli or a fragment thereof, and modified O-polysaccharide molecules derived from E. coli lipopolysaccharides or conjugates thereof. In a further aspect, the compositions further comprise modified O-polysaccharide molecules derived from Klebsiella pneumoniae or conjugates thereof.
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates), kits comprising said immunogenic compositions and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
Vectors and nucleic acid constructs for improved antibody production are provided. Also provided are methods of making and using the vectors and constructs.
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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
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
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
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
Methods for producing a compound of Formula I, Formula I, wherein R1 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 8 to 20 carbon atoms; R3 is a hydrocarbon group; n is an integer from 2 to 5, m is an integer from 30 to 70, and L is a linker. The method includes: a) contacting a fatty acid having a chemical formula of R1—COOH and a primary amine having a chemical formula of R2—NH2 to form an amide having a chemical formula of R1—C(O)—NH—R2; b) contacting the amide with a reducing agent to form a secondary amine having a chemical formula of R1—CH2—NH—R2; and c) contacting the secondary amine with a polyolefin-glycol compound to form the compound of Formula I. Intermediates produced in the method, salts of compound of Formula I and of intermediates.
Methods for producing a compound of Formula I, Formula I, wherein R1 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 8 to 20 carbon atoms; R3 is a hydrocarbon group; n is an integer from 2 to 5, m is an integer from 30 to 70, and L is a linker. The method includes: a) contacting a fatty acid having a chemical formula of R1—COOH and a primary amine having a chemical formula of R2—NH2 to form an amide having a chemical formula of R1—C(O)—NH—R2; b) contacting the amide with a reducing agent to form a secondary amine having a chemical formula of R1—CH2—NH—R2; and c) contacting the secondary amine with a polyolefin-glycol compound to form the compound of Formula I. Intermediates produced in the method, salts of compound of Formula I and of intermediates.
C08G 69/40 - Polyamides containing oxygen in the form of ether groups
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
The present invention provides compositions comprising a recombinant AAV (rAAV) vector and one or more pharmaceutically acceptable excipients. The compositions have improved stability as compared to other rAAV compositions.
The present invention relates to a method for identifying a candidate therapeutic for a disease caused by infection with a human cytomegalovirus (HCMV) having a glycoprotein B (gB) polypeptide, comprising contacting the HCMV gB polypeptide comprising a druggable region with a compound, wherein binding of said compound indicates a candidate therapeutic. The present invention also relates to candidate therapeutics comprising modulators and inhibitors of HCMV activity and pharmaceutical compositions comprising said modulators and inhibitors and methods of use thereof.
The present disclosure provides solid forms of 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, and methods of preparing and using the same.
Selectively vented biological assay devices and methods of performing biological assays with such devices are provided herein. Disclosed devices include a selective venting clement having passively tunable porosity. The methods include controlling fluid flow within the subject devices with the selective venting element.
The invention relates to immunogenic compositions comprising a capsular polysaccharide (CP) from Streptococcus agalactiae, commonly referred to as group B Streptococcus (GBS), conjugated to a carrier protein, and optionally including an aluminum-based adjuvant. The invention further relates to methods for inducing an immune response in subjects against GBS and/or for reducing or preventing invasive GBS disease in subjects using the compositions disclosed herein. The resulting antibodies can be used to treat or prevent GBS infection via passive immunotherapy.
This invention relates to compounds of Formula (I)
This invention relates to compounds of Formula (I)
and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - 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
59.
CETYLTRIMETHYLAMMONIUM BROMIDE (CTAB) AS A LYSIS AND FLOCCULATION REAGENT IN GENE THERAPY DOWNSTREAM PROCESSES
The present disclosure describes improved methods for use in purifying biological products made by host cells. In some embodiments, the improved methods comprise one or more steps of lysing host cells to release the biological product and precipitating host cell DNA, using a detergent such as cetyltrimethylammonium bromide (CTAB). In some embodiments, the biological product is a vaccine, or a viral vector for gene therapy, such as an AAV vector or a lentiviral vector.
The invention provides antibodies, and antigen-binding fragments thereof, that specifically bind to CXCR5. The antibodies can be afucosylated and exhibit increased ADCC compared with the otherwise identical fucosylated antibodies. The invention includes uses, and associated methods of using the antibodies.
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
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
C12N 15/62 - DNA sequences coding for fusion proteins
61.
PRODUCTION OF ADENO-ASSOCIATED VIRUS VECTOR IN INSECT CELLS
The present disclosure relates to compositions and methods for the optimal large-scale production of rAAV vectors using the baculovirus expression vector system in insect cells.
Devices and methods for modifying optical properties of biological samples or aspects thereof are provided. The subject methods include generating a reaction product with a device and reacting the reaction product to sufficiently modify an optical property to allow detection of the modified optical property.
G01N 21/78 - Systems in which material is subjected to a chemical reaction, the progress or the result of the reaction being investigated by observing the effect on a chemical indicator producing a change of colour
This invention provides a recombinant Escherichia coli (E. coli) host cell for producing a Klebsiella pneumoniae (K. pneumoniae) O-antigen, wherein the E. coli host cell comprises a polynucleotide encoding the K. pneumoniae O-antigen, including methods of producing and purifying the K. pneumoniae O-antigen.
The present invention provides antibodies and antibody-drug conjugates that bind to the extra domain B splice variant of fibronectin 1 and methods for preparing and using the same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present disclosure relates to compositions comprising RNA molecules encoding an antigen derived from influenza, wherein the RNA may be formulated in a lipid nanoparticle (LNP), and wherein the composition further includes a polypeptide antigen derived from respiratory syncytial virus (RSV) and/or RNA molecules encoding an antigen derived from RSV, wherein the RSV RNA may be may be formulated in an LNP. The present disclosure further relates to the use of the RNA molecules, RNA-LNPs and compositions for the prevention of influenza and RSV infection-induced illness.
The present disclosure relates to hMPV F, PIV3 F and PIV1 F protein mutants, nucleic acids or vectors encoding a hMPV F, PIV3 F and PIV1 F protein mutant, compositions comprising a hMPV F, PIV3 F and PIV1 F protein mutant or nucleic acid, and uses of the hMPV F, PIV3 F and PIV1 F protein mutants, nucleic acids or vectors, and compositions.
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
The invention relates to compounds of Formula (I)
and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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 or sparfloxacin
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
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 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/12 - 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 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 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 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
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
Sanford Burnham Prebys Medical Discovery Institute (USA)
PFIZER INC. (USA)
Inventor
Ware, Carl F.
Sedy, John
Aivazian, Tigran
Miller, Brian
Crellin, Natasha K.
Abstract
The present invention is based on the seminal discovery that BTLA agonist fusion proteins modulate an immune response. Specifically, the present invention provides fusion proteins that bind BTLA enhancing BTLA signaling. The present invention further provides methods of treating cancer and immune and inflammatory diseases and disorders with a BTLA agonist fusion protein as described herein.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
An object of the present invention is to provide immunogenic compositions for protection against S. pneumoniae, in particular against S. pneumoniae serogroup 10A and 39, while limiting the number of conjugates. The present invention therefore relates to new immunogenic compositions for use in pneumococcal vaccines and to vaccination of human subjects, in particular infants and elderly, against pneumoccocal infections using said immunogenic compositions.
Described herein are 3-fluoro-4-hydroxybenzamide-containing inhibitors and/or degraders, and pharmaceutical compositions containing 3-fluoro-hydroxybenzamide-containing inhibitors and/or degraders. In some embodiments, the 3-fluoro-4-hydroxybenzamide-containing compounds of the disclosure can be used to treat a condition, for example, nonalcoholic fatty liver disease and nonalcoholic steatohepatitis.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic 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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
71.
COMPOSITIONS AND METHODS FOR ELICITING AN IMMUNE RESPONSE AGAINST CLOSTRIDIUM DIFFICILE
In one aspect, the invention relates to an immunogenic composition that includes a Clostridium difficile toxoid A and/or a C. difficile toxoid B, and methods of use thereof. In another aspect, the invention relates to a method for eliciting an immune response in a human against a C. difficile infection. The method includes administering to the human an effective dose of a composition, which includes a C. difficile toxoid, wherein the composition is administered at least two times, wherein the second administration is about 30 days after the first administration, and wherein the immune response against C. difficile toxin A and/or toxin B is sustained.
Provided herein are Claudin 18.2 binding agents and chimeric antigen receptors (CARs) comprising a Claudin 18.2 binding molecule that specifically binds to Claudin 18.2; and immune cells comprising these Claudin 18.2-specific CARs, e.g., CAR-T cells. Also provided are methods of making and using Claudin 18.2-specific CARs and Claudin 18.2 binding agents, and immune cells comprising Claudin 18.2-specific CARs.
A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
A61K 39/00 - Medicinal preparations containing antigens or antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
73.
COMBINATION THERAPY COMPRISING A PKC INHIBITOR AND A MEK INHIBITOR
The present invention provides for CD80-Fc fusion proteins that have therapeutic and diagnostic use, and methods for making thereof. The present invention further relates to variant CD80 polypeptides. The present invention also provides for CD80-Fc fusion proteins for use in the treatment of 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
The present disclosure provides methods for producing a compound having a chemical formula of Formula I, wherein R3 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 1 to 30 carbon atoms; R3 is a i′) lincar or branched or cyclic. ii′) saturated or unsaturated, and iii′) substituted or unsubstituted hydrocarbon group: and L1, L2 and L3 independently are linkers.
The present disclosure provides methods for producing a compound having a chemical formula of Formula I, wherein R3 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 1 to 30 carbon atoms; R3 is a i′) lincar or branched or cyclic. ii′) saturated or unsaturated, and iii′) substituted or unsubstituted hydrocarbon group: and L1, L2 and L3 independently are linkers.
C07C 229/46 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 67/29 - Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by introduction of oxygen-containing functional groups
C07C 227/08 - Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid by reaction of ammonia or amines with acids containing functional groups
C07C 229/24 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one carboxyl group bound to the carbon skeleton, e.g. aspartic acid
This invention relates to compounds of general Formula I
This invention relates to compounds of general Formula I
and pharmaceutically acceptable salts thereof, in which R1, R2, R3a, R3b, and R4 are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The present invention provides, in part, compounds of Formula I:
The present invention provides, in part, compounds of Formula I:
The present invention provides, in part, compounds of Formula I:
or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
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 25/00 - Drugs for disorders of the nervous system
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
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
78.
IMMUNOGENIC COMPOSITIONS AND METHODS FOR ELICITING AN IMMUNE RESPONSE AGAINST CLOSTRIDIOIDES (CLOSTRIDIUM) DIFFICILE
The present invention relates to immunogenic compositions that comprise a Clostridioides difficile toxoid A and/or a C. difficile toxoid B, and an adjuvant, and methods of use thereof. The present invention further relate to a methods for eliciting an enhanced immune response in a human against a C. difficile infection. The methods include administering to the human an effective dose of an immunogenic composition, which includes a C. difficile toxoid and an adjuvant, wherein the composition is administered two times.
The present invention provides antibodies and antibody-drug conjugates that bind to the extra domain B splice variant of fibronectin 1 and methods for preparing and using the same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates) and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in Prevnar, Synflorix and/or Prevnar 13. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumoccocal infections using said novel immunogenic compositions.
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
Described herein are compounds of Formula I,
Described herein are compounds of Formula I,
wherein the variables are defined herein, their use as activators from AMPK, pharmaceutical compositions containing such compounds and their use to treat, for example, heart failure or peripheral vascular disease.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated 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
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 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
82.
Combination of Talazoparib and an Anti-Androgen for the Treatment of DDR Gene Mutated Metastatic Castration-Sensitive Prostate Cancer
This invention relates to combination therapies comprising talazoparib, or a pharmaceutically acceptable salt thereof, and an anti-androgen, or a pharmaceutically acceptable salt thereof, and associated pharmaceutical compositions, methods of treatment, and pharmaceutical uses for the treatment of metastatic castration-sensitive prostate cancer in subjects identified as having at least one DNA damage repair gene mutation.
Pharmacuetical Compounds Benzodiazepine derivatives of formula (I): wherein: R1 is H or F; R2 is selected from formula (II) and formula (III) R3 is C1-C6 alkyl which is unsubstituted or substituted by CF3, or is a monocyclic 4- to 6-membered heterocyclic group containing 1 or 2 heteroatoms selected from O, N and S; R4 is H or a group selected from —X, -alk-X, —CONR6R7, C═NNR6R7, —SO2R6 and —SO2NR6R7; R4 is a group selected from —X, -alk-X, —CONR6R7, —C═NNR6R7, —SO2R6 and —SO2R6R7; X is OH or a derivative of an OH group selected from α-amino carboxylic acid esters, carboxylic acid esters, carbonates, carbamates, ethers and phosphates: alk is C1-C6 alkylene which is unsubstituted or substituted by C3-C6 cycloalkyl; and R6 and R7 are each independently C1-C6 alkyl or C3-C6 cycloalkyl; and the pharmaceutically acceptable salts thereof are inhibitors of respiratory syncytial virus (RSV) and can therefore be used to treat or prevent an RSV infection.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
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 9/00 - Medicinal preparations characterised by special physical form
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 35/04 - Antineoplastic agents specific for metastasis
The invention relates to antibodies, or antigen-binding fragments thereof, that specifically binds to interferon beta (IFNβ). Such antibodies, or antigen-binding fragments thereof, are are useful for various therapeutic or diagnostic purposes.
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
86.
METHODS OF ADMINISTERING LONG-ACTING GROWTH HORMONE POLYPEPTIDES
The subject matter described herein is directed to methods of treating growth hormone related disorders by administering a long-acting recombinant human growth hormone. In another embodiment, a long-acting recombinant human growth hormone is administered in a composition or the combination is administered separately to treat growth deficiency in a subject previously treated with a once daily rhGH therapy.
The present invention provides antibodies and antibody-drug conjugates that bind to the extra domain B splice variant of fibronectin 1 and methods for preparing and using the same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Method for treating vitiligo, including active and stable non-segmental vitiligo, using compounds and analogues which inhibit certain kinases including Janus Kinase (JAK), said method comprising the step of administering to the subject in need thereof 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one, or a pharmaceutically acceptable salt thereof.
Antibody compositions and methods for the purification of antibodies are provided. Purification methods provided involve the use of hydroxyapatite resin (HA) to separate an antibody of interest from one or more impurities.
C07K 16/06 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies from serum
C07K 1/16 - ExtractionSeparationPurification by chromatography
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 an oral solution formulation or an oral powder for constitution comprising 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazirt-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, or a lactate or malate salt thereof, and a buffer system comprising lactic acid or malic acid.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
91.
Solid state forms of (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide and uses thereof
The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
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
Described herein are compounds of Formula I,
Described herein are compounds of Formula I,
Described herein are compounds of Formula I,
wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.
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 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - 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 417/04 - 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 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
Methods of removing high molecular weight species, in particular aggregates, from antibody drug conjugate preparations, by contacting preparations of the antibody drug conjugate reaction mixture with a hydroxyapatite resin and selectively eluting the ADC from the resin using a gradient comprising sodium phosphate.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The invention relates to 4-((6-(2,2-Difluoroethyl)-8-(2-hydroxy-2-methylcyclopentyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)piperidine-1-sulfonamide or pharmaceutically acceptable salts thereof, to compositions containing them, to processes for their preparation, to intermediates used in such processes, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer. The disclosure also relates to its crystalline form 1, to pharmaceutical compositions comprising form 1, and to the use of form 1 for the treatment of cancers.
Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
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 31/506 - PyrimidinesHydrogenated 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
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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
96.
Colorimetric Detection of Nucleic Acid Amplification
Colorimetry is used to detect amplification reaction products. A sample is contacted with a reaction mix under conditions such that an amplification reaction occurs and produces an amplification reaction product if the sample contains a target nucleic acid template molecule. The reaction mix includes an enzyme for catalyzing the amplification reaction, and at least one halochromic agent. If the target nucleic acid template molecule is present, the amplification reaction changes the starting pH of the reaction mix to cause a detectable colorimetric change of the halochromic agent, thereby indicating the presence of the target nucleic acid. If the target nucleic acid template molecule is not present, the amplification reaction does not generate an adequate number of protons to sufficiently change the starting pH of the reaction mix to cause a detectable colorimetric change of the halochromic agent, thereby indicating that the amplification reaction product has not been produced.
The invention relates to benzimidazoles of Formula (I)
The invention relates to benzimidazoles of Formula (I)
The invention relates to benzimidazoles of Formula (I)
and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The invention relates to benzimidazoles of Formula (I)
and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.
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 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need 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
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
The invention relates to imidazopyridines of Formula (I)
The invention relates to imidazopyridines of Formula (I)
The invention relates to imidazopyridines of Formula (I)
and pharmaceutically acceptable salts thereof, wherein R0 to R5 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The invention relates to imidazopyridines of Formula (I)
and pharmaceutically acceptable salts thereof, wherein R0 to R5 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.
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
100.
Antibodies Specific for CD47, PD-L1, and Uses Thereof
Antibodies that specifically bind to CD47 and antibodies that specifically bind to PD-L1 are provided, as well as CD47/PD-L1 bispecific antibodies. Also provided are uses of these antibodies, and related compositions 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
patents
