Abstract

The present disclosure provides for in-vitro generated cardiomyocytes, as well as methods of using such cardiomyocytes or variants thereof. The present disclosure also relates to methods of cell co-culture models of cardiac disorders, as well as methods of using such models or variants thereof.

IPC Classes  ?

• C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

An implant is provided comprising a substrate having one or more nanoceria coatings coated at least partially thereon, wherein the one or more nanoceria coatings comprise surface cerium having a 3+/4+ oxidation state ratio such that the one or more nanoceria coatings exhibit catalase mimetic activity, superoxide dismutase mimetic activity, or both. Methods are provided for forming a nanoceria coating. The coating has nanoceria having a surface cerium 3+/4+ oxidation state ratio such that such that the coating exhibits catalase mimetic activity, superoxide dismutase mimetic activity, or both. Also disclosed is a method of reducing degradation of an implant by placing nanoceria in proximity to a bone-implant interface.

IPC Classes  ?

• A61L 27/30 - Inorganic materials
• A61L 27/04 - Metals or alloys
• A61L 27/10 - Ceramics or glasses
• A61L 27/14 - Macromolecular materials
• A61L 27/54 - Biologically active materials, e.g. therapeutic substances
• C25D 13/02 - Electrophoretic coating characterised by the process with inorganic material
• C25D 13/12 - Electrophoretic coating characterised by the process characterised by the article coated
• C25D 13/18 - Electrophoretic coating characterised by the process using modulated, pulsed or reversing current
• C25D 15/00 - Electrolytic or electrophoretic production of coatings containing embedded materials, e.g. particles, whiskers, wires

Abstract

This disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof that are useful for treating a disease associated with TGR5.

IPC Classes  ?

• C07D 235/18 - BenzimidazolesHydrogenated benzimidazoles with aryl radicals directly attached in position 2
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/423 - Oxazoles condensed with carbocyclic rings
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61P 35/00 - Antineoplastic agents
• C07D 263/57 - Aryl or substituted aryl radicals
• C07D 277/66 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
• C07D 471/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems

Abstract

Described herein are compounds capable of modulating the level of activity of Serine/threonine protein kinase 3 (STK3) or serine/threonine protein kinase 4 (STK4), compositions, and methods of using these compounds and compositions.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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 471/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 495/04 - Ortho-condensed systems
• 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

Abstract

Described herein are compositions and methods useful for treating a soft bone disease, or for treating hypophosphatasia comprising administering a viral vector comprising a mineral-targeted alkaline phosphatase under the control of a tissue non-specific promotor to the subject in an intramuscular injection to a muscle, wherein administering the viral vector treats the soft bone disease. The compositions disclosed herein are suitable for administration to a subject.

IPC Classes  ?

• C12N 9/16 - Hydrolases (3.) acting on ester bonds (3.1)
• A61K 38/46 - Hydrolases (3)
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
• C12N 15/86 - Viral vectors

Abstract

Composition and methods of use to treat ZBTB11 associated disorders such as cancer comprising compounds as described herein that effect ZBTB11 degradation.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/454 - 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

Abstract

Described herein are compounds which are inhibitors of oncogenic and wild-type SHP2 and methods of treatment using SHP2 inhibitors.

IPC Classes  ?

• 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
• A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• C07C 65/40 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
• C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 307/56 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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 333/64 - Oxygen atoms
• 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 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

Abstract

Described herein are solid forms of sodium 4-chloro-3'-(((2-cyclopentyl-1-oxoisoindolin-5-yl)oxy)methyl)-[1,1'-biphenyl]-3-carboxylate and its pharmaceutical composition for the treatment of disease.

IPC Classes  ?

• C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• 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

Abstract

Provided herein are metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising said modulators, and methods of using said modulators and pharmaceutical compositions comprising said modulators.

IPC Classes  ?

• C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• A61K 31/4245 - Oxadiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
• A61P 25/32 - Alcohol-abuse
• A61P 25/34 - Tobacco-abuse
• A61P 25/36 - Opioid-abuse
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• 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 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/12 - 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

Abstract

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
• A61P 25/32 - Alcohol-abuse
• A61P 25/34 - Tobacco-abuse
• A61P 25/36 - Opioid-abuse
• C07H 13/08 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings

Abstract

Addiction to particular metabolic pathways is common to tumor cells. Disclosed herein are compounds and methods to modulate metabolic signaling facilitated by a glutaryl-CoA dehydrogenase (GCDH) protein for the treatment of cancer. In some embodiments, the compounds can reduce GCDH protein expression or activity and reduce the progression of cancers expressing GCDH.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61P 35/00 - Antineoplastic agents

Abstract

Described herein are methods and compositions for diagnosing, treating, or ameliorating symptoms of cancer, including Acute Myeloid Leukemia or acute lymphoblastic leukemia, with an inhibitor of SGF29.

IPC Classes  ?

• C12N 9/22 - Ribonucleases
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

Disclosed are compositions and methods useful for targeting molecules to activated macrophages, such as tumor associated macrophages. The compositions and methods are based on peptide sequences, such as AMT peptides, that home to activated macrophages. The disclosed homing to activated macrophages is useful for delivering therapeutic and detectable agents to cells and tissues where immune system effects or inflammation are occurring.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• A61K 38/00 - Medicinal preparations containing peptides
• 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

Abstract

This invention relates generally to methods for determining a subject having or is suspected of having a subtype of colorectal cancer and methods for treating the subject.

IPC Classes  ?

• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• 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

Abstract

Disclosed herein are methods for promoting increased mitochondrial mass and function by providing a consumable composition. Some embodiments provided include, for example, administering a compound of Formula (I) or compound of Formula (II). Some embodiments provide the composition is formulated as a dietary supplement, food ingredient or additive, a medical food, nutraceutical or pharmaceutical composition.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• 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
• A61P 3/00 - Drugs for disorders of the metabolism

Abstract

Described herein are EphA4 receptor antagonists, pharmaceutical compositions containing EphA4 antagonists, and methods and uses of treating an EphA4-based disease, disorder or pathology in an individual using EphA4 receptor antagonists.

IPC Classes  ?

• C07K 7/02 - Linear peptides containing at least one abnormal peptide link
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 47/40 - CyclodextrinsDerivatives thereof
• 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
• A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• A61P 7/04 - AntihaemorrhagicsProcoagulantsHaemostatic agentsAntifibrinolytic agents
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 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

Abstract

The present application provides, inter alia, a compound of Formula (I): The present application provides, inter alia, a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Y, Ar, X1, X2, X3, R1, R2, R3, R4, R5, and R6 are as described herein. Methods of making these compounds and methods of using these compound for treating diseases such as cancer are also provided.

IPC Classes  ?

• C07D 498/08 - Bridged systems
• A61P 35/00 - Antineoplastic agents
• C07D 251/66 - Derivatives of melamine in which a hetero atom is directly attached to a nitrogen atom of melamine
• 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - 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 487/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems

Abstract

Provided herein are, inter alia, compositions that bind to a PDZI domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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
• A61P 35/04 - Antineoplastic agents specific for metastasis
• C07D 495/14 - Ortho-condensed systems

Abstract

A method for inhibiting activity of a human blood protein vitronectin is disclosed. The method includes administering a composition that inhibits activity of a calcium and hydroxyapatite binding site of the human blood protein vitronectin. An ophthalmic composition is also disclosed. The composition includes: an effective amount of an organic compound having a molecular weight of less than 1,000 Daltons; and one or more selected from the group consisting of a thickening agent, a pH adjustor, a wetting agent, a stabilizer, a solubilize, a preservative, a refreshing agent, and an ointment base.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans

Abstract

Provided herein are methods for using HNF4α agonists and pharmaceutical compositions thereof for reducing body weight, maintaining body weight, reducing diet induced weight gain, reducing mitochondrial stress, treating diseases or disorders such as inflammation, diabetes, nonalcoholic fatty liver disease (NAFLD) or nonalcoholic steatohepatitis (NASH) in a subject.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/04 - AnorexiantsAntiobesity agents
• C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
• C12Q 1/6851 - Quantitative amplification

Abstract

Methods of treating cancer comprising targeting the FBXO7/EYA2-SCFFBXW7 axis, such as via EYA2 Tyr phosphatase inhibitors. As EYA2 acts downstream of SCFFBXW7, FBXO7/EYA2 inhibitors can be effective in blocking immune escape pathways and immunotherapy resistance in Fbxw7 mutant tumors. Furthermore, FBXO7/EYA2 inhibitors can be effective in mitigating AXL signaling and associated immune evasion, thus enhancing antitumor immune responses.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 38/46 - Hydrolases (3)
• A61K 49/00 - Preparations for testing in vivo
• A61P 35/00 - Antineoplastic agents
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing

Abstract

Provided herein are compounds, compositions, and methods for lowering expression levels of runt-related transcription factor 1 (RUNX1) in a cell, tissue or animal. Further provided are methods of improving memory and cognitive functioning in individuals with Down syndrome (DS) using an antisense compound targeted to a RUNX1 nucleic acid. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders. Further provided are methods of decreasing inflammation and slowing cognitive decline in individuals with dementia.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
• A61K 31/7125 - Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
• 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
• C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

Described herein are compositions and methods useful for detecting and treating pathologies associated with ATF in hepatocytes. A method of detecting a condition, a method of inhibiting a protein, a method of inhibiting a gene, and a method of treatment are disclosed herein. The present disclosure includes, but is not limited to, the development and testing of Atf6-specific short, synthetic, single-stranded antisense oligodeoxynucleotides (ASOs) in vitro and in vivo and future screening for ATF6 inhibitors.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• 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 31/4545 - 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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 49/00 - Preparations for testing in vivo
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating/preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: 3 represent the same meanings as in the claims.

IPC Classes  ?

• 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 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/423 - Oxazoles condensed with carbocyclic rings
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/444 - 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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 27/02 - Ophthalmic agents
• 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 405/12 - 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 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 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 498/08 - Bridged systems

Abstract

This present disclosure provides methods and pharmaceutical compositions for cell reprogramming and a pharmaceutical composition comprising the reprogrammed cells. In certain embodiments, the method of reprogramming a cell comprises reducing the expression of at least one barrier gene selected from the group consisting of ATF7IP, JUNB, ZNF207, Sp7, FOXA1, HEXIM2, SMARCA5, SOX15, CHST2 or NCEH1, or if the barrier gene is ATF7IP or SOX15, then the expression of a second barrier gene is also reduced. In another embodiment, the reprogramming method comprises reducing the expression of at least two barrier genes selected from the group consisting of ATF7IP, JUNB, ZNF207 and Sp7.

IPC Classes  ?

• C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
• A61K 35/30 - NervesBrainEyesCorneal cellsCerebrospinal fluidNeuronal stem cellsNeuronal precursor cellsGlial cellsOligodendrocytesSchwann cellsAstrogliaAstrocytesChoroid plexusSpinal cord tissue
• A61K 35/34 - MusclesSmooth muscle cellsHeartCardiac stem cellsMyoblastsMyocytesCardiomyocytes
• C12N 5/0793 - Neurons
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

e.ge.g., HFB 2050 hNSCs) or progenitors thereof.

IPC Classes  ?

• A61K 35/30 - NervesBrainEyesCorneal cellsCerebrospinal fluidNeuronal stem cellsNeuronal precursor cellsGlial cellsOligodendrocytesSchwann cellsAstrogliaAstrocytesChoroid plexusSpinal cord tissue
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 25/00 - Drugs for disorders of the nervous system
• C12N 5/0797 - Stem cellsProgenitor cells

Abstract

Described and provided herein are compositions and methods useful for modulating PSGL1 (e.g., inhibiting PSGL1 negative regulation of the immune response). In certain instances, the inhibition and/or modulation of PSGL1 is achieved by utilizing a partially glycosylated PSGL1 fusion protein. As described herein, modulating (e.g., inhibiting) PSGL1 is useful for promoting (e.g., increasing) immune cell (e.g., T cell) function (e.g., inhibiting T cell exhaustion and/or increasing the number of CD8 + or CD4+ T cells). Moreover modulating (e.g., inhibiting) PSGL1 is useful for treating a tumor.

IPC Classes  ?

• 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 38/00 - Medicinal preparations containing peptides
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants

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.

IPC Classes  ?

• C07K 14/71 - ReceptorsCell surface antigensCell surface determinants for growth factorsReceptorsCell surface antigensCell surface determinants for growth regulators
• A61K 38/00 - Medicinal preparations containing peptides
• 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
• C07K 14/705 - ReceptorsCell surface antigensCell surface determinants
• C07K 14/715 - ReceptorsCell surface antigensCell surface determinants for cytokinesReceptorsCell surface antigensCell surface determinants for lymphokinesReceptorsCell surface antigensCell surface determinants for interferons
• C07K 19/00 - Hybrid peptides

Abstract

The present disclosure provides compositions and methods for prevention or treatment of hearing loss. In some examples, a composition for preventing or treating hearing loss comprises at least one compound that activates AMPK in at least one hair cell.

IPC Classes  ?

• 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 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61P 27/16 - Otologicals

Abstract

Methods and compositions related to treating flavivirus are described.

IPC Classes  ?

• C07K 16/10 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from viruses from RNA viruses
• A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
• 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

Abstract

Various embodiments relate to compounds and methods useful for preventing or treating a cancer in a subject. The method may include administering to a subject a composition according to any of the embodiments described herein in an amount effective to inhibit metastatic activity or tumor growth in the subject.

IPC Classes  ?

• C07D 295/155 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4

Abstract

Tyramine containing hydroxycinnamic acid amide derivatives are provided as are methods of using the same in modulating metabolism and addressing the underlying pathogenesis of metabolic disorders, such as nonalcoholic fatty liver disease, nonalcoholic steatohepatitis and type II diabetes mellitus.

IPC Classes  ?

• C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
• C07D 239/80 - Oxygen atoms

Abstract

Disclosed are peptides and peptidomimetics that in some embodiments include the amino acid sequence KRGARST or (SEQ ID NO: 1), AKRGARSTA or (SEQ ID NO: 2), or CKRGARSTC (SEQ ID NO: 3). Also disclosed are conjugates and compositions that onclude the peptides and/or peptidomimetics, methods for directing a moiety to tumor lymphatic vasculature, methods for imaging tumor lymphatic vasculature, methods for reducing or inhibiting tumor metastasis, methods for reducing the number of tumor lymphatic vessels, methods for treating cancer, methods for treating a disease or disorder associated with a gC1q/p32 receptor biological activity, methods for detecting the presence of a gC1q/p32 receptor, methods for detecting interactions between gC1q/p32 receptors and the presently disclosed conjugates and compositions, methods for delivering the presently disclosed conjugates and compositions to gC1q/p32 receptors, methods for assessing gC1q/p32 receptor levels in cells, methods for identifying subjects having diseases associated with gC1q/p32 receptor biological activities, and methods for screening for compounds that interact with gC1q/p32 receptors.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• A61K 38/00 - Medicinal preparations containing peptides
• 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 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 49/18 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

Described herein are peptides, compositions, and methods for diagnosing, detecting, imaging, monitoring, preventing, treating, or ameliorating diseases or disorders including cancer, inflammatory disorder, and autoimmune disease.

IPC Classes  ?

• A61K 49/00 - Preparations for testing in vivo
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

This disclosure relates to cardiogenic mesoderm formation regulators and methods of use thereof, e.g., generating a multipotent cardiovascular progenitor cell by overexpressing Id1, Id2, Id3, Id4, Evx1, and/or Grrp1 in a stem cell.

IPC Classes  ?

• C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

Disclosed herein include methods, compositions, and kits suitable for use in treatment and/or prevention of RNA viral infections. In some embodiments, the method comprises modulation of host factors related to RNA viral infection using compounds, compositions and kits disclosed herein. There are provided, some embodiments, compounds modulating host factors that govern SARS-CoV-2 replication. Disclosed herein include the use of compounds, compositions and kits disclosed herein to prevent and/or treat SARS-CoV-2 infection, for example by modulating the SARS-CoV-2 life cycle.

IPC Classes  ?

• 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Disclosed herein are methods of diagnosing and treating MYC-driven cancers by detecting a PVT1 splice variant in a biological sample from a subject.

IPC Classes  ?

• 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

Abstract

Stress responses involve corticotropin releasing factor (CRF), the two cognate receptors (CRF1 and CRF2) and the CRF-binding protein (CRFBP). Utilizing a novel cell-based assay, a C-terminal CRFBP fragment [CRFBP(10 kD)] was found to potentiates CRF-intracellular Ca2+ release, demonstrating that CRFBP possesses excitatory roles in addition to the inhibitory role established by the N-terminal fragment of CRFBP [CRFBP(27 kD)]. This interaction was CRF2-specific, as CRF1 responses were not potentiated by CRFBP(10 kD). As there were currently no small molecule ligands available that selectively interact with either CRFBP or CRF2, a cell-based assay was miniaturized, wherein CRFBP(10 kD) was fused as a chimera with CRF2α, that allowed us to a perform a high-throughput screen (HTS) of approximately 350,000 small molecules. This resulted in the identification of negative allosteric modulators (NAMs) of the CRFBP(10 kD)-CRF2 complex that blunt CRF-induced potentiation of N-Methyl-D-aspartic acid receptor (NMDAR)-mediated synaptic transmission in dopamine neurons in the ventral tegmental area (VTA). These results provide the first evidence of specific roles for CRF2 and CRFBP in the modulation of neuronal activity and suggest that NMDARs in the VTA may be a target for the treatment of stress and substance abuse disorders such as alcohol use disorder.

IPC Classes  ?

• A61K 31/4245 - Oxadiazoles
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

The present disclosure provides compounds and compositions that are useful as MYC protein modulators and methods of using the same for treating MYC-mediated diseases or disorders.

IPC Classes  ?

• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/51 - Thiamines, e.g. vitamin B1
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• 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 31/5355 - Non-condensed oxazines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 239/74 - QuinazolinesHydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
• 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 403/04 - 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 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 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 413/14 - 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 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
• C07D 471/04 - Ortho-condensed systems
• C07D 487/14 - Ortho-condensed systems

Abstract

Described herein are methods of prognosing/diagnosing an estrogen receptor positive (ER+) breast cancer in an African American subject. Also described herein are methods of treating an estrogen receptor positive (ER+) breast cancer in an African American subject.

IPC Classes  ?

• 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Provided are methods and compositions for detecting cognitive disorders such as Schizophrenia. Demonstrated herein is collapsing response mediator protein-2 (CRMP2) as a biomarker for detecting Schizophrenia in peripheral blood sample.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

Methods and compositions related to treating pancreatic cancer are described.

IPC Classes  ?

• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• A61K 47/66 - 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 a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 35/00 - Antineoplastic agents
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

Compositions and methods useful for delivery of targeted therapies for pulmonary arterial hypertension, sepsis, cancer and cachexia. The compositions and methods are based on peptide pharmacophores that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. Peptide pharmacophores may selectively target tumor vasculature, regenerating tissue, wounded tissue, inflamed tissue, fibrotic tissue, remodeled tissue, tissue characterized by elevated heparanase levels, and have the ability to internalize into such diseased cells.

IPC Classes  ?

• A61K 38/12 - Cyclic peptides
• 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
• A61K 31/18 - Sulfonamides
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 38/55 - Protease inhibitors
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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
• 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
• G01N 33/15 - Medicinal preparations
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 9/12 - Antihypertensives
• A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
• G16B 35/00 - ICT specially adapted for in silico combinatorial libraries of nucleic acids, proteins or peptides
• G16C 20/60 - In silico combinatorial chemistry
• 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
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61P 35/00 - Antineoplastic agents
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• G16B 35/10 - Design of libraries
• G16B 35/20 - Screening of libraries

Abstract

Described herein are compositions and methods useful for hair follicle generation comprising transplanting human pluripotent stem cell-derived hair follicle bulge stem cells, wherein the developmental and molecular requirements for the generation of hair follicle following transplantation is ensured.

IPC Classes  ?

• A61K 35/36 - SkinHairNailsSebaceous glandsCerumenEpidermisEpithelial cellsKeratinocytesLangerhans cellsEctodermal cells
• A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
• C12N 5/071 - Vertebrate cells or tissues, e.g. human cells or tissues
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

Disclosed herein are methods and compositions engineered to modulate ephrin type-A receptor 2 (EphA2), including novel compositions comprising one or more dimeric peptide units that binds to a EphA2, wherein the dimeric peptide comprises two or more homologous sequences or fragments thereof, wherein the two or more homologous sequences or fragments thereof, individually, comprise one or more binding sites for the EphA2 with unexpectedly high specificity and binding affinity. The compositions described herein can be attenuated to treat subjects suffering from diseases and/or conditions.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure relates to immunofluorescence detection of epigenetic markers and automated cell imaging by a machine learning to profile and quantify the “epigenetic state” of individual cells.

IPC Classes  ?

• C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving viable microorganisms
• G16B 30/00 - ICT specially adapted for sequence analysis involving nucleotides or amino acids

Abstract

Disclosed herein are methods for identifying a subject as having serrated colorectal cancer (CRC), and models of human serrated CRC. Also provided herein are methods for treating serrated CRC in the subject.

IPC Classes  ?

• A61K 38/47 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
• A61P 35/00 - Antineoplastic agents

Abstract

Provided herein are methods and compositions for inhibition of FBXO44 protein or expression in order to enhance immunotherapy treatment for cancer.

IPC Classes  ?

• 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides

Abstract

Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

IPC Classes  ?

• C07D 277/82 - Nitrogen atoms
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles 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 in position 2
• C07D 513/04 - Ortho-condensed systems

Abstract

Provided herein are methods and compositions for diagnosing, treating, or ameliorating symptoms of cancer, including melanoma, with inhibitors of PRMTS and immune response regulators in combination with checkpoint inhibitor therapy.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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 35/00 - Antineoplastic agents
• C12N 9/22 - Ribonucleases

Abstract

Provided herein are compounds that modulate the activity of melanoma inhibitor of apoptosis (ML-IAP) protein, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
• A61P 35/00 - Antineoplastic agents

Abstract

The ubiquitin ligase, RNF5, regulates the gut microbiota composition and influences the immune checkpoint response to tumors. RNF5 deficient animals exhibit significant inhibition of tumor development as well as an altered gut microbiota composition. Methods of treating cancer by administering to a subject one or more selected bacterial species and/or one or more prebiotics that promote the growth of one or more selected bacterial species are disclosed. Also disclosed are methods of treating cancer by administering to a subject one or more selected bacterial species and/or one or more prebiotics that promote the growth of one or more selected bacterial species in combination with one or more anti-cancer agents.

IPC Classes  ?

• A61K 35/74 - Bacteria
• A61P 35/00 - Antineoplastic agents
• A61K 31/7004 - Monosaccharides having only carbon, hydrogen and oxygen atoms
• A61K 31/7008 - Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
• A61K 31/7024 - Esters of saccharides
• A61K 31/733 - Fructosans, e.g. inulin
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

A method for modulating metabolism is provided which includes the step of providing a consumable composition including an extract containing a compound of Formula I to a subject in need thereof thereby modulating the subject's metabolism and addressing the underlying pathogenesis of metabolic disorders, such as nonalcoholic fatty liver disease, nonalcoholic steatohepatitis and type II diabetes mellitus.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• 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

Abstract

The present disclosure provides compositions and methods for treating acute myeloid leukemia (AML) using a histone deacetylase (HDAC) inhibitor alone or incombination with a RING finger protein 5 (RNF5) inhibitor and/or a retinoblastoma binding protein 4 (RBBP4) inhibitor. Moreover, RNF5 and/or RBBP4 expression or protein levels in a patient can be measured and used to inform individualized treatment options and dosing regiments. For example, AML patients with lower levels of either RNF5 or RBBP4 may be stratified and treated with one or more HDAC inhibitors leading to improved therapeutic results.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 38/15 - DepsipeptidesDerivatives thereof
• A61K 31/365 - Lactones
• A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/69 - Boron compounds
• 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
• C12Q 1/6851 - Quantitative amplification
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

Disclosed herein are methods for promoting in¬ creased mitochondrial mass and function by providing a consum¬ able composition. Some embodiments provided include, for exam¬ ple, administering a compound of Formula (I) or compound of For¬ mula (II). Some embodiments provide the composition is formulat¬ ed as a dietary supplement, food ingredient or additive, a medical food, nutraceutical or pharmaceutical composition.

IPC Classes  ?

• A61K 31/015 - Hydrocarbons carbocyclic
• A61K 31/13 - Amines, e.g. amantadine
• A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
• A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine

Abstract

Disclosed herein are compounds and methods to inhibit metabolic signaling facilitated by glutaryl CoA dehydrogenase (GCDH) for the treatment of melanoma. In some embodiments, the compounds can reduce GCDH protein expression and reduce the progression of melanoma expressing GCDH.

IPC Classes  ?

• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
• A61P 35/00 - Antineoplastic agents
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells

Abstract

Methods are disclosed for treating periodontal disease, peri-implantitis, or to preserve a tooth socket in a subject. These methods include selecting a subject with periodontal disease, peri-implantitis, or in need of tooth socket preservation; and locally administering into the periodontium of the subject a therapeutically effective amount of a tissue-nonspecific alkaline phosphatase (TNAP) polypeptide, or a nucleic acid molecule encoding the recombinant TNAP polypeptide. Methods are also disclosed for i) promoting alveolar bone regeneration in the subject; ii) increasing attachment of a periodontal ligament to a root surface of a tooth in the subject; iii) increasing cementum formation; and/or iv) increasing mineralization in a tooth in the subject. Pharmaceutical compositions are also disclosed that are of use in these methods.

IPC Classes  ?

• A61K 38/46 - Hydrolases (3)
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

In some embodiments, the present disclosure provides a compound of Formula (I), as described herein, or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the compound of Formula (I), and methods of treating, e.g., metabolic diseases using the compound of Formula (I) are also provided.

IPC Classes  ?

• 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 9/12 - Antihypertensives

Abstract

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• C07C 65/40 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
• A61P 25/32 - Alcohol-abuse
• A61P 25/34 - Tobacco-abuse
• A61P 25/36 - Opioid-abuse
• C07C 49/84 - Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
• C07C 65/24 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
• C07C 217/22 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by carbon atoms having at least two bonds to oxygen atoms
• C07C 255/30 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same unsaturated acyclic carbon skeleton
• C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• C07C 311/17 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
• C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• C07C 311/55 - Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea having sulfur atoms of the sulfonylurea groups bound to acyclic carbon atoms
• C07C 317/18 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
• C07C 321/28 - Sulfides, hydropolysulfides, or polysulfides having thio groups bound to carbon atoms of six-membered aromatic rings
• C07C 323/12 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07D 213/55 - AcidsEsters
• C07D 213/80 - AcidsEsters in position 3
• C07D 213/08 - Preparation by ring-closure
• C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
• C07D 271/10 - 1,3,4-OxadiazolesHydrogenated 1,3,4-oxadiazoles
• C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
• 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 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/04 - 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 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 417/10 - 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 aromatic rings

Abstract

Disclosed herein are methods of inhibiting nuclear pore complex assembly and inducing nuclear pore complex disassembly. Methods to screen for agents that inhibit nuclear pore assembly or induce nuclear pore complex disassembly are also disclosed.

IPC Classes  ?

• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• A61K 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution
• C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Described herein are compounds which are inhibitors of oncogenic and wild-type SHP2 and methods of treatment using SHP2 inhibitors.

IPC Classes  ?

• 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
• A61K 9/06 - OintmentsBases therefor
• A61K 9/08 - Solutions
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 35/00 - Antineoplastic agents
• C07C 65/40 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
• C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 307/56 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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 333/64 - Oxygen atoms
• C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/06 - 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

Abstract

Described herein are methods of treating atherosclerosis, including administering a tissue-nonspecific alkaline phosphatase (TNAP) inhibitor to a patient. Described herein are also methods of reducing microcalcifications in an atherosclerotic plaque, including administering a TNAP inhibitor to a patient. Described herein are also methods of preventing, arresting, or reducing the development of plaque calcifications in a patient, including administering a TNAP inhibitor to a patient.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material

Abstract

Provided herein are compounds that modulate the activity of melanoma inhibitor of apoptosis (ML-IAP) protein, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure is directed to compounds, compositions, formulations and methods of use thereof in the treatment and prevention of ULK mediated diseases, including cancer.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• 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

Abstract

Provided herein are methods of treating diseases, including cancer, with ULK inhibitors, both as monotherapies and in combination with other therapeutic agents.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Provided herein are small molecule modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• C07D 487/04 - Ortho-condensed systems
• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
• C07D 498/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems

Abstract

Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.

IPC Classes  ?

• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• A61K 31/245 - Amino benzoic acid types, e.g. procaine, novocaine
• A61K 31/415 - 1,2-Diazoles
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/42 - Oxazoles
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
• 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 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/50 - PyridazinesHydrogenated pyridazines
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• C07D 213/40 - Acylated substituent nitrogen atom
• C07D 213/56 - Amides
• C07D 213/643 - 2-PhenoxypyridinesDerivatives thereof
• C07D 213/73 - Unsubstituted amino or imino radicals
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
• C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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 249/04 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles
• C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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 277/28 - Radicals substituted by nitrogen atoms
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• 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 405/12 - 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/12 - 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
• C07D 471/04 - Ortho-condensed systems
• C07D 498/08 - Bridged systems

Abstract

Provided herein are compounds that modulate the activity of inhibitor of apoptosis (IAPs) proteins, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

IPC Classes  ?

• 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
• A61P 35/00 - Antineoplastic agents
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

IPC Classes  ?

• C07D 243/14 - 1,4-BenzodiazepinesHydrogenated 1,4-benzodiazepines
• A61K 31/4196 - 1,2,4-Triazoles
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• C07D 217/06 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
• 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 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 285/08 - 1,2,4-ThiadiazolesHydrogenated 1,2,4-thiadiazoles
• 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 233/54 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• 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 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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 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 243/12 - 1,5-BenzodiazepinesHydrogenated 1,5-benzodiazepines
• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
• C07D 275/02 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
• C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
• C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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 277/26 - Radicals substituted by sulfur atoms
• C07D 307/38 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
• C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/02 - 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
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 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 413/14 - 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 417/10 - 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 aromatic rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Described herein are compounds capable of modulating the level of activity of Serine/threonine protein kinase 3 (STK3) or serine/threonine protein kinase 4 (STK4), compositions, and methods of using these compounds and compositions.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure is directed to compounds, compositions, formulations and methods of use thereof in the treatment and prevention of ULK mediated diseases, including cancer.

IPC Classes  ?

• A61K 31/529 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
• A61K 31/282 - Platinum compounds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 498/08 - Bridged systems

Abstract

Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of LMPTP, compositions, and methods of using these compounds and compositions.

IPC Classes  ?

• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
• 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 9/08 - Solutions
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 9/06 - OintmentsBases therefor
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

This invention relates generally to methods for determining a subject having or is suspected of having a subtype of colorectal cancer and methods for treating the subject.

IPC Classes  ?

• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase

Abstract

Described herein are methods and compositions for diagnosing, treating, or ameliorating symptoms of cancer, including MYC-driven and KRAS-driven cancer, with therapeutic HNB polypeptides. In some embodiments, disclosed herein are compositions comprising a synthetic nucleic acid sequence encoding a Plasmacytoma variant translocation 1_217 (PVT1_217) splice variant micropeptide, wherein the PVT1_217 splice variant micropeptide comprises at least 10 contiguous amino acids that are identical to a peptide encoded by a short open reading frame (shORF) located at the junction of Exon 3 and Exon 4 of human PVT 1_217.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• A61P 35/00 - Antineoplastic agents

Abstract

Models and methods related to targeting binding immunoglobulin protein (BiP) are described, where the models and methods allow identification and analysis of protein folding and misfolding.

IPC Classes  ?

• A01K 67/027 - New or modified breeds of vertebrates

Abstract

Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Provided herein are agonists of the apelin receptor of Formula (I): for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 487/04 - Ortho-condensed systems

Abstract

A method for inhibiting activity of a human blood protein vitronectin is disclosed. The method includes administering a composition that inhibits activity of a calcium and hydroxyapatite binding site of the human blood protein vitronectin. An ophthalmic composition is also disclosed. The composition includes: an effective amount of an organic compound having a molecular weight of less than 1,000 Daltons; and one or more selected from the group consisting of a thickening agent, a pH adjustor, a wetting agent, a stabilizer, a solubilize, a preservative, a refreshing agent, and an ointment base.

IPC Classes  ?

• A61P 27/02 - Ophthalmic agents
• C07K 14/78 - Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

Abstract

A method for inhibiting activity of a human blood protein vitronectin is disclosed. The method includes administering a composition that inhibits activity of a calcium and hydroxyapatite binding site of the human blood protein vitronectin. An ophthalmic composition is also disclosed. The composition includes: an effective amount of an organic compound having a molecular weight of less than 1,000 Daltons; and one or more selected from the group consisting of a thickening agent, a pH adjustor, a wetting agent, a stabilizer, a solubilize, a preservative, a refreshing agent, and an ointment base.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 27/02 - Ophthalmic agents
• C07K 14/78 - Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]

Abstract

Provided herein are compositions comprising a vaccine composition and an agent that triggers metabolic reprogramming of B cells and methods of using the agent that triggers metabolic reprogramming of B cells to increase effectiveness of the vaccine by increasing memory B cell population. One aspect of the disclosure includes a method of increasing the effectiveness of a vaccine in a subject, which comprises administering a B cell metabolic reprogramming agent to the subject in a dose and schedule configured to increase the effectiveness of the vaccine, wherein the subject is administered with the vaccine.

IPC Classes  ?

• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
• A61K 39/145 - Orthomyxoviridae, e.g. influenza virus

Abstract

The present invention relates to the seminal discovery that P-selectin glycoprotein ligand-1 (PSGL-1) modulates the immune system and immune responses. Specifically, the present invention provides PSGL-1 agonists and antagonists which increase the survival of multifunctional T cells and viral clearance. The present invention further provides methods of treating infectious diseases, cancer and immune and inflammatory diseases and disorders using a PSGL-1 modulator.

IPC Classes  ?

• 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 14/705 - ReceptorsCell surface antigensCell surface determinants

Abstract

Described herein are compositions and methods useful for detecting and treating pathologies associated with ATF in hepatocytes. A method of detecting a condition, a method of inhibiting a protein, a method of inhibiting a gene, and a method of treatment are disclosed herein. The present disclosure includes, but is not limited to, the development and testing of Atf6-specific short, synthetic, single-stranded antisense oligodeoxynucleotides (ASOs) in vitro and in vivo and future screening for ATF6 inhibitors.

IPC Classes  ?

• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/4245 - Oxadiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• 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 31/4545 - 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 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61J 1/16 - Holders for containers
• A61P 35/00 - Antineoplastic agents
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

Provided herein are small molecule inhibitors of CXCR6 receptor, compositions comprising the compounds, and methods of using the compounds and compositions. The compounds are 9-azbicyclo[3.3.1]nonane or 9-diazbicyclo[3.3.1]nonane derivatives, whose synthesis is also described. Also provided are method of treating a disease or condition (such as, cancer) mediated by CXCR6/CXCL16 signaling pathway in a mammal.

IPC Classes  ?

• C07D 451/14 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantaneCyclic acetals thereof

Abstract

This present disclosure provides methods and pharmaceutical compositions for cell reprogramming and a pharmaceutical composition comprising the reprogrammed cells. In certain embodiments, the method of reprogramming a cell comprises reducing the expression of at least one barrier gene selected from the group consisting of ATF7IP, JUNB, ZNF207, Sp7, FOXA1, HEXIM2, SMARCA5, SOX15, CHST2 or NCEH1, or if the barrier gene is ATF7IP or SOX15, then the expression of a second barrier gene is also reduced. In another embodiment, the reprogramming method comprises reducing the expression of at least two barrier genes selected from the group consisting of ATF7IP, JUNB, ZNF207 and Sp7.

IPC Classes  ?

• A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
• A61K 35/30 - NervesBrainEyesCorneal cellsCerebrospinal fluidNeuronal stem cellsNeuronal precursor cellsGlial cellsOligodendrocytesSchwann cellsAstrogliaAstrocytesChoroid plexusSpinal cord tissue
• A61K 35/33 - Fibroblasts
• A61K 35/34 - MusclesSmooth muscle cellsHeartCardiac stem cellsMyoblastsMyocytesCardiomyocytes
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
• C12N 5/0793 - Neurons
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

This present disclosure provides methods and pharmaceutical compositions for cell reprogramming and a pharmaceutical composition comprising the reprogrammed cells. In certain embodiments, the method of reprogramming a cell comprises reducing the expression of at least one barrier gene selected from the group consisting of ATF7IP, JUNB, ZNF207, Sp7, FOXA1, HEXIM2, SMARCA5, SOX15, CHST2 or NCEH1, or if the barrier gene is ATF7IP or SOX15, then the expression of a second barrier gene is also reduced. In another embodiment, the reprogramming method comprises reducing the expression of at least two barrier genes selected from the group consisting of ATF7IP, JUNB, ZNF207 and Sp7.

IPC Classes  ?

• A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
• A61K 35/30 - NervesBrainEyesCorneal cellsCerebrospinal fluidNeuronal stem cellsNeuronal precursor cellsGlial cellsOligodendrocytesSchwann cellsAstrogliaAstrocytesChoroid plexusSpinal cord tissue
• A61K 35/33 - Fibroblasts
• A61K 35/34 - MusclesSmooth muscle cellsHeartCardiac stem cellsMyoblastsMyocytesCardiomyocytes
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12N 5/077 - Mesenchymal cells, e.g. bone cells, cartilage cells, marrow stromal cells, fat cells or muscle cells
• C12N 5/0793 - Neurons
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Described herein are compositions and methods useful for treating a soft bone disease, or for treating hypophosphatasia comprising administering a viral vector comprising a mineral-targeted alkaline phosphatase under the control of a tissue non-specific promotor to the subject in an intramuscular injection to a muscle, wherein administering the viral vector treats the soft bone disease. The compositions disclosed herein are suitable for administration to a subject.

IPC Classes  ?

• A61K 38/46 - Hydrolases (3)
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
• A61P 3/00 - Drugs for disorders of the metabolism
• C12N 9/16 - Hydrolases (3.) acting on ester bonds (3.1)
• C12N 15/86 - Viral vectors

Abstract

Described herein are methods and compositions for treating, reducing, or ameliorating cancer in a subject, comprising administering compositions comprising mucin and/or inulin. In some aspects, described herein is a method of enhancing anti-cancer immunity comprising: (a) administering to a subject a composition comprising mucin, wherein the subject has been identified as having a gut microbiome comprising one more microbial taxa that are members of a Clostridium cluster XIVa or an Actinobacteria phylum; and (b) altering the gut microbiome in the subject, wherein administration of the composition causes an enhanced anti-cancer immunity in the subject.

IPC Classes  ?

• 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
• A61P 35/00 - Antineoplastic agents
• A61K 31/733 - Fructosans, e.g. inulin

Abstract

A method for modulating metabolism is provided which includes the step of providing a consumable composition including an extract containing a compound of Formula I to a subject in need thereof thereby modulating the subject's metabolism and addressing the underlying pathogenesis of metabolic disorders, such as nonalcoholic fatty liver disease, nonalcoholic steatohepatitis and type II diabetes mellitus.

IPC Classes  ?

• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• 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

Abstract

Disclosed herein are compositions and pharmaceutical formulations comprising a functionally selected β-arrestin-biased NTSR1 ligand (such as SBI-553 and SBI-810) and methods of using those compositions and pharmaceutical formulations for treating and/or preventing pain.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• C07D 239/94 - Nitrogen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

Methods and compositions related to type 2 diabetes therapy are described, where the methods and compositions relieve ER stress in pancreatic islet cells. The present disclosure provides methods and compositions for reducing hepatic steatosis, e.g., associated with Type 2 diabetes (T2D). In one aspect, the present disclosure provides a method of reducing hepatic steatosis, e.g., associated with T2D, in a subject in need thereof.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• 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 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• C12N 15/86 - Viral vectors

Abstract

Methods and compositions for treating acute brain injury and acute nervous system injury, which include administering to a subject suffering from an acute brain injury or an acute nervous system injury, a therapeutically effective amount of a composition comprising the amino acid sequence CAQK (SEQ ID NO:4).

IPC Classes  ?

• 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 9/51 - Nanocapsules
• C07K 5/103 - Tetrapeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• A61K 47/62 - 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 a protein, peptide or polyamino acid
• 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
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy

Abstract

Described herein are methods and compositions for diagnosing, treating, or ameliorating symptoms of cancer, including pancreatic cancer and melanoma, with ASNS synthetic lethal partners.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 38/46 - Hydrolases (3)
• 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
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 38/50 - Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
• A61P 35/00 - Antineoplastic agents
• A61P 17/00 - Drugs for dermatological disorders
• A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes

Abstract

The present disclosure relates to proinsulin misfolding in beta cells as it relates to glucose intolerance associated with type 2 diabetes (T2D).

IPC Classes  ?

• G01N 33/74 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving hormones
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

The present disclosure provides compositions and methods for prevention or treatment of hearing loss. In some examples, a composition for preventing or treating hearing loss comprises at least one compound that activates AMPK in at least one hair cell.

IPC Classes  ?

• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• 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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

Abstract

Described herein are small molecule agonists of dopamine receptor D1 that inhibit YAP/TAZ, compositions, and methods of using these compounds and compositions. The methods of using such compounds in the treatment of conditions, diseases, or disorders associated with fibrotic disease are described herein.

IPC Classes  ?

• C07D 221/18 - Ring systems of four or more rings
• C07D 471/04 - Ortho-condensed systems
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue

Abstract

Described are platforms, systems, and methods for screening patients. In one aspect, a computer-implemented method comprises: receiving, from a cellular imaging device, image data comprising calcium kinetic features of neuronal cultures derived from a patient; processing the image data through a machine-learning model to determine a diagnosis for the patient based on the calcium kinetic features, the machine-learning model trained using neuronal calcium data; and providing the diagnosis a user interface.

IPC Classes  ?

• G06T 7/00 - Image analysis
• G06N 20/20 - Ensemble learning
• G06V 10/774 - Generating sets of training patternsBootstrap methods, e.g. bagging or boosting
• G06V 10/776 - ValidationPerformance evaluation
• G06V 20/69 - Microscopic objects, e.g. biological cells or cellular parts
• G16C 20/70 - Machine learning, data mining or chemometrics
• G16H 70/40 - ICT specially adapted for the handling or processing of medical references relating to drugs, e.g. their side effects or intended usage

Abstract

Disclosed herein include methods, compositions, and kits suitable for use in treatment and/or prevention of RNA viral infections. In some embodiments, the method comprises modulation of host factors related to RNA viral infection using compounds, compositions and kits disclosed herein. There are provided, some embodiments, compounds modulating host factors that govern SARS-CoV-2 replication. Disclosed herein include the use of compounds, compositions and kits disclosed herein to prevent and/or treat SARS-CoV-2 infection, for example by modulating the SARS-CoV-2 life cycle.

IPC Classes  ?

• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

Disclosed herein are methods for identifying a subject as having serrated colorectal cancer (CRC), and models of human serrated CRC. Also provided herein are methods for treating serrated CRC in the subject.

IPC Classes  ?

• C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.

IPC Classes  ?

• A61K 47/66 - 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 a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
• B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Abstract

The present disclosure relates to immunofluorescence detection of epigenetic markers and automated cell imaging by a machine learning to profile and quantify the "epigenetic state" of individual cells.

IPC Classes  ?

• G06T 7/00 - Image analysis