Curcumin-based compounds are described herein. The disclosed compounds contain a curcumin mimic moiety linked to an anti-inflammatory drug via an amino acid linker. These compounds show anticancer and/or anti-inflammatory activities, and may have a higher potency compared to the free curcumin mimic alone and/or the free anti-inflammatory drug alone. Pharmaceutical compositions containing the compounds and methods of using the compounds or pharmaceutical composition thereof for treating cancer and/or inflammation diseases/disorders are also described.
Provided herein are compounds of formula I or an enantiomer, solvate, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating inflammatory disease, cardiovascular disease, and cancer.
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
Compositions and methods of their use to detect and treat anti-PD1 therapy resistance are provided herein. Compositions that immunospecifically bind and deplete dysfunctional T cells are provided. The dysfunctional T cells that are depleted include CD38+PD-1+ T cells, CD38+CD8+ T-cells, or both. The dysfunctional T cells can be depleted, for example, by administering an antibody or fusion protein that specifically binds to dysfunctional T cells and promotes their depletion. In one embodiment the antibody is a bispecific antibody that can be specific for CD38 and CD8, or it can be specific for CD38 and PD-1. Also disclosed is a method of detecting and treating anti-PD1 therapy resistance by measuring the amount of CD38+PD1+CD8 T cells in blood or tissue samples obtained from a subject prior to anti-PD1 therapy and administering an anti-CD38/CD8 or anti-CD38/PD-1 depleting/blocking antibody to the subject prior to anti-PD1 therapy.
G01N 15/01 - Investigating characteristics of particlesInvestigating permeability, pore-volume or surface-area of porous materials specially adapted for biological cells, e.g. blood cells
Boston Scientific Neuromodulation Corporation (USA)
Augusta University Research Institute, Inc. (USA)
Inventor
Moffitt, Michael A.
Blake, David
Abstract
A system for stimulation of a nucleus basalis of Meynert (NBM) of a patient includes an implantable electrical stimulation lead including electrodes and configured for implantation of at least one of the electrodes adjacent to or within the NBM of the patient; and an implantable pulse generator coupleable to the implantable electrical stimulation lead and configured for delivering electrical stimulation to the NBM through at least one of the electrodes of the implantable electrical stimulation lead, the implantable pulse generator including at least one processor configured to, upon user request, during an initial stimulation period, which is at least 1 month in duration and has a start and an end, increase over time at least one of a duration or an amplitude of the electrical stimulation from an initial value at the start of the initial stimulation period to a final value at the end of the initial stimulation period.
Antibodies and antigen binding fragments thereof are provided that immunospecifically bind to PD-1 and induce or promote an immune response that activates immune cell proliferation or activity. Contrary to the existing paradigm that PD-1 exclusively promotes a suppressive immune response, the disclosed antibodies and antigen binding fragments thereof, immunospecifically bind to PD-1 and cause an activating signal to be delivered to the immune cell that activates the immune cell rather than suppressing the immune cell. In one embodiment, the disclosed antibodies and antigen binding fragments thereof specifically bind to PD-1 expressed on immune cells. The binding of the disclosed antibodies and antigen binding fragments thereof to PD-1 on immune cells causes an activating signal to be transmitted into the immune cell, for example a signal that enhances or promotes cytokine production and/or activation of immune cell proliferation.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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
7.
INHALANT CANNABIDIOL (CBD) IN THE TREATMENT OF GLIOBLASTOMA
A method of reducing tumor size in a subject in need thereof, comprising administering to the subject an effective amount of cannabidiol effective to inhibit tumor growth.
It has been discovered that PIK3δ (PIK3delta) selectively modulates the activation and proliferation of natural Tregs. Methods of modulating immune responses by modulating PIK3δ bioavailability or biological activity are provided.
A method for reducing tumor size in a subject having lung cancer, comprising administering to the subject an effective amount of a pharmaceutical composition comprising an effective amount of a inhalant cannabinoid to inhibit lung tumor growth.
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
10.
CANNABIDIOL FOR TREATING NEURODEGENERATIVE DISEASES
A method of reducing symptoms of a neurodegenerative disease comprising administering an effective amount of cannabidiol to a subject in need thereof to improved cognitive function and ameliorated the pathophysiology of the neurodegenerative disease.
A61K 31/00 - Medicinal preparations containing organic active ingredients
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
Bispecific aptamers having a first end that specifically binds to a first tumor specific marker, tumor antigen, or viral protein and a second end that specifically binds to a second tumor specific marker, tumor antigen, or viral protein are provide. The bispecific aptamers can be used to treat cancer or virally infected cells. Generally, the bispecific aptamers bind to two surface proteins, preferably different proteins, on the same cell. In a preferred embodiment the bispecific aptamers bind to two different tumor markers, tumor antigens, tumor specific proteins and combinations thereof.
It has been found that the prodrug 1-(butyryloxy)ethyl-5-amino-4-oxopentanoate (AN-233), an oral active conjugate of BA (histone deacetylase inhibitor) and ALA (heme precursor), is useful for the treatment of hemoglobinopathies including but not limited to sickle cell disease and thalassemias. In one embodiment, AN-233 activates γ-globin transcription, induces HbF expression, produces an anti-sickling effect, or combinations thereof when administered to a subject in need thereof.
THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPT. OF VETERANS AFFAIRS (USA)
Inventor
Weintraub, Neal L.
Romero Lucas, Maritza J.
Lucas, Rudolf
Schally, Andrew
Cai, Renzhi
Abstract
Provided herein are compositions and methods of use thereof for the treatment of metabolic disease such as diabetes and obesity. One embodiment provides a method of treating a metabolic disease or syndrome in a subject in need thereof by administering to the subject a therapeutically effective amount of a growth hormone releasing hormone (GHRH) antagonist or a pharmaceutical composition comprising the GHRH antagonist to reduce triglyceride-rich-lipoproteins (TRL) in the subject to treat the metabolic condition or syndrome.
Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.
C07D 317/60 - 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
C07C 69/66 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
C07D 311/06 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
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
15.
SYNTHESIS OF NSAID CONJUGATES AS ANTI-INFLAMMATORY AGENTS USING THE MOLECULAR HYBRIDIZATION
Described are synthetic compounds having anti-inflammatory properties and optionally analgesic properties. These compounds are derivatives of FDA-approved anti-inflammatory, such as ibuprofen and indomethacin, and can be formed using reactions under microwave irradiation. Generally, the compounds contains a moiety of the parent drug, a triazolyl heterocycle, and a substituted or unsubstituted aryl group. In some forms, the compounds show anti-inflammatory properties and optionally analgesic properties with similar or higher efficiencies compared with their respective parent drugs, with additional advantages including no or reduced adverse effects (e.g., without ulcerogenic liability in the gastric) and/or selective inhibition of COX-2 over COX-1. Pharmaceutical compositions suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical formulation can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. Methods for preventing or treating an inflammatory disease or disorder in a subject are also disclosed.
C07D 263/30 - 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
16.
THORACIC SPINAL NERVE NEUROMODULATION THERAPY FOR GASTROINTESTINAL SYMPTOMS
Systems and methods for neuromodulation therapy with repetitive magnetic stimulation of paraspinal regions have been developed for the treatment and prevention of gastroparesis. The methods identify a minimal electromagnetic intensity threshold required to elicit a motor response of 10 μV at a preferred location within the mid-thoracic region of a subject, and then deliver repetitive magnetic stimulation to the subject at a maximum 150% of the threshold value. Typically, the methods administer about 1,200 stimulations in groups of about 300 pulses having a frequency of about 1 Hz, with a rest period of about 5 minutes between pulses. Typically, the methods repeat the stimuli about twice a day for a period of around 5 days.
Methods and compositions for treating neurodegenerative diseases are provided. In one embodiment, the method includes administering gangliosides into the brain of a mammal in need of such treatment. The gangliosiges are preferably GM1 and GD3 gangliosides. The gangliosides are intranasally administered in an amount effective to delay and/or prevent disease progression, and to increase the resilience of brains by promoting adult neurogenesis by gangliosides.
A61K 31/7032 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyl-diacylglycerides, lactobionic acid, gangliosides
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
18.
OSTEOPONTIN MONOCLONAL ANTIBODIES FOR CANCER AND OSTEOPOROSIS IMMUNOTHERAPY
The US Government as represented by the Department of Veterans Affairs (USA)
Inventor
Liu, Kebin
Klement, John
Redd, Priscilla S.
Abstract
Antibodies and antigen binding fragments thereof that immunospecifically bind OPN (OPN) and inhibit OPN activity are provided herein. The disclosed antibodies and antigen binding fragments are useful for modulating signal transduction through OPN proteins. The antibodies and antigen-binding fragments are useful for the treatment or prevention of cancer, osteoporosis, or other immune diseases.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Pharmaceutical formulations for nasal administration are disclosed. The pharmaceutical formulation contains a green tea catechin derivative (such as an epigallocatechin-3-gallate-palmitate); and preferably further includes a carbohydrate (such as a polysaccharide); and a pharmaceutically acceptable carrier. The pharmaceutical formulation has a viscosity sufficient to maintain the green tea catechin derivative in contact with nasal epithelial cells optionally for at least about 30 minutes in the presence of mucus. Also described are methods of using the nasal formulations for preventing, reducing, and/or treating neurological damages caused by exposure to a virus, such as a SARS-CoV-2. For example, the disclosed pharmaceutical formulations can treat or prevent one or more symptoms of long COVID in an infected subject, and/or repair the damaged nasal epithelial cells, neuroepithelial cells, vascular cells, and/or neurons and restore their functions in a subject recovered from a COVID infection, such as the olfactory function of these cells.
Antibodies and antigen binding fragments thereof are provided that immunospecifically bind to PD-1 and induce or promote an immune response that activates immune cell proliferation or activity. Contrary to the existing paradigm that PD-1 exclusively promotes a suppressive immune response, the disclosed antibodies and antigen binding fragments thereof, immunospecifically bind to PD-1 and cause an activating signal to be delivered to the immune cell that activates the immune cell rather than suppressing the immune cell. In one embodiment, the disclosed antibodies and antigen binding fragments thereof specifically bind to PD-1 expressed on immune cells. The binding of the disclosed antibodies and antigen binding fragments thereof to PD-1 on immune cells causes an activating signal to be transmitted into the immune cell, for example a signal that enhances or promotes cytokine production and/or activation of immune cell proliferation.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
An engineered targeting exosome comprising; a modified Lamp2b peptide, a targeting peptide or antibody; and a Fc portion of IgG2b. The targeting peptide or antibody detects a target protein within a cell and precisely delivers the exosome to cells expressing the target protein and the Fc portion of IgGb2 induces antibody-dependent cell-mediated cytotoxicity (ADCC) events in cells expressing the target protein. Also disclosed are methods of using the engineered targeting exosome to detect and/or deplete cells expressing the target protein.
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 35/22 - UrineUrinary tract, e.g. kidney or bladderIntraglomerular mesangial cellsRenal mesenchymal cellsAdrenal gland
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
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
G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances
22.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEURONAL INJURIES
The US Government as Represented by the Department of Veterans Affairs (USA)
Inventor
Caldwell, Ruth
Abstract
Pathological retinal neovascularization is a common micro-vascular complication in several retinal diseases including retinopathy of prematurity (ROP), diabetic retinopathy, age related macular degeneration and central vein occlusion. Disclosed herein are compositions and methods useful for the treatment or prevention of retinal neovascularization and related diseases in a subject in need thereof. Exemplary methods include administering a composition including PEGylated arginase 1 to a subject in need thereof to promote reparative angiogenesis and decrease retinal neovascularization in the eye.
C12N 9/78 - Hydrolases (3.) acting on carbon to nitrogen bonds other than peptide bonds (3.5)
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
One aspect of the invention relates to a method for screening SANS for a living subject comprising obtaining 3D images or 3D quantitative measurements of at least one optic nerve sheath of the living subject at rest and with a provocative maneuver, respectively, prior to a spaceflight, wherein the 3D images or the 3D quantitative measurements obtained at rest is used as a baseline; evaluating the 3D images or the 3D quantitative measurements obtained at rest and with the provocative maneuver; and determining if the living subject is at risk of developing the SANS based on the evaluation of the 3D images or the 3D quantitative measurements.
Compositions and methods for determining the presence of free monoclonal immunoglobulin light chains in biological samples with improved resolution and sensitivity are described. The methods detect subjects who have or are at risk of neoplastic monoclonal gammopathies and identify residual/minimal residual disease in subjects who have received therapy for neoplastic monoclonal gammopathies. The methods include immunofixation electrophoresis modified by applying undiluted or concentrated biological samples, washing/blotting of gels to enhance removal of residual proteins, and staining for free light chains with antisera specific to free light chains. Kits including compositions required for the methods are also provided.
Provided herein are compounds that inhibit phosphodiesterase 5 (PDE5) and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating gastrointestinal diseases and disorders such as intestinal cancers and inflammatory bowel disease.
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
26.
CANNABIDIOL AS A THERAPEUTIC MODALITY FOR COVID-19
Compositions and methods for treating or reducing symptoms of COVID-19 are provided herein. An exemplary method includes administering to the subject an effective amount of cannabidiol to reduce acute respiratory distress syndrome caused by COVID-19.
Enteral formulations containing including therapeutically effective amount carbon monoxide, and methods of use thereof, for treatment of ocular diseases and disorders are provided. The formulations can be administered in a subject in need thereof in an effective amount to reduce or prevent an ocular disease in the subject, and thus reduce one or more symptoms of disease, disorder, or illness associated with the disease. In some embodiments, the formulation is administered orally.
Compositions and methods for treating leukemia are provided herein. One embodiment provides a method of treating leukemia in a subject in need thereof by administering to a subject in need thereof a composition that selectively inhibits Akt3 by an amount effective to reduce the immune suppressive response in the subject. In one embodiment, the Akt3 inhibitors include, but are not limited to, compounds 1-31 and Formulas I-III.
Embodiments of the present systems and methods may provide improved, automated monitoring of brain function. In embodiments, a multimodal, multi-sensor monitoring device may provide to monitoring of the full spectrum of brain function. In an embodiment, a system for monitoring brain function of a subject may include an apparatus for mounting a plurality of stimulus and response sensors on a head of the subject, including a cognizance stimuli-sensor suite, a physiologic sensor suite, and advance monitoring devices such as a transcranial Doppler puck, an electroencephalograph monitor, and an optic nerve sheath parameter sensor.
Pyrazinamide (PZA) conjugates and hybrids are provided herein. The PZA conjugates are useful for treating bacterial infections. In one embodiment, the PZA conjugates are useful for treating tuberculosis.
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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 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
A61P 31/06 - Antibacterial agents for tuberculosis
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
31.
COMPOSITIONS AND METHODS FOR INHIBITING TUMOR-INDUCED IMMUNE SUPPRESSION
It has been discovered that the cyclic peptide EnnA inactivates the Hsp90 chaperone pathway, but without activating an extensive heat shock response and overexpression of anti-apoptotic proteins. Mechanistically distinct, EnnA inhibits Hsp90 and destabilize PDL-1 and IDO, two major immune checkpoints mediating tumor-induced immune suppression. The provided herein show that EnnA profoundly modulates the cytokine signature of cancer cells and promotes a cytokine profile that favors an immune attack on tumor cells. This translates into highly efficacious anti-tumor activity in vivo, which, when combined with a single dose of chemotherapy, completely reduced the tumor burden in experimental animals and instilled highly efficient immune memory against the primary tumor.
A method of reducing tumor size in a subject in need thereof, comprising administering to the subject an effective amount of cannabidiol effective to inhibit tumor growth.
Disclosed herein are compositions and methods for ovulation induction in females in need thereof. Current methods for inducing ovulation have unpleasant side effects and are expensive. The disclosed compositions and methods are safe, efficacious, and inexpensive. An exemplary method of inducing ovulation includes steps of monitoring ovarian follicle development and size during the follicular phase of the menstrual cycle; and administering to the subject a pharmaceutical composition including progesterone or ioidentical progesterone in an amount effective to increase the plasma concentration of progesterone to between about 0.1 ng/ml to about 1 ng/ml when the follicle reaches a size of at least 15 mm.
A61K 31/57 - 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
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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
Compositions and methods for treating or reducing symptoms of acute respiratory distress syndrome (ARDS) generally and COVID-19 infection in particular are provided herein. An exemplary method includes administering to the subject an effective amount of cannabichromene to reduce acute respiratory distress syndrome caused by ARDS generally and COVID-19 infection in particular.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 9/00 - Medicinal preparations characterised by special physical form
A method for removing bodily fluid includes drawing bodily fluid that has accumulated in excess, converting the drawn fluid from bulk liquid form to aerosol form, and disposing of the aerosol via evaporation of liquid droplets and absorption and/or diffusion of vapor. Conversion from bulk liquid to aerosol may include collecting the bulk liquid fluid in a reservoir, conveying the bulk liquid bodily fluid to an atomizer, converting the bulk liquid fluid into an aerosol having ultrafine droplets, and ejecting the aerosol into a subcutaneous space for disposal via evaporation of liquid droplets and absorption and/or diffusion of vapors. The method may be performed with a subcutaneous atomizer that may be controlled locally or by an external transmitter for effecting a conversion and mist rate to keep pace with the accumulation of excess bodily fluid.
THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPT. OF VETERANS AFFAIRS (USA)
Inventor
Weintraub, Neal L.
Romero Lucas, Maritza J.
Lucas, Rudolf
Schally, Andrew
Cai, Renzhi
Abstract
Provided herein are compositions and methods of use thereof for the treatment of metabolic disease such as diabetes and obesity. One embodiment provides a method of treating a metabolic disease or syndrome in a subject in need thereof by administering to the subject a therapeutically effective amount of a growth hormone releasing hormone (GHRH) antagonist or a pharmaceutical composition comprising the GHRH antagonist to reduce triglyceride-rich-lipoproteins (TRL) in the subject to treat the metabolic condition or syndrome.
Chimeric antigen receptor T cell (CARTs) compositions and methods of their use are provided. One embodiment provides a chimeric antigen receptor T cell composition including 8F8 chimeric antigen receptor T cells. Another embodiment provides a chimeric antigen receptor T cell composition including 6G11 chimeric antigen receptor T cells. Still another embodiment provide a chimeric antigen receptor T cell composition including 12D7 chimeric antigen receptor T cells. The disclosed CARTs can be used to treat cancer, for example hepatocellular carcinoma.
A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
BOSTON SCIENTIFIC NEUROMODULATION CORPORATION (USA)
AUGUSTA UNIVERSITY RESEARCH INSTITUTE, INC. (USA)
Inventor
Moffitt, Michael, A.
Blake, David
Abstract
A system for stimulation of a nucleus basalis of Meynert (NBM) of a patient includes an implantable electrical stimulation lead including electrodes and configured for implantation of at least one of the electrodes adjacent to or within the NBM of the patient; and an implantable pulse generator coupleable to the implantable electrical stimulation lead and configured for delivering electrical stimulation to the NBM through at least one of the electrodes of the implantable electrical stimulation lead, the implantable pulse generator including at least one processor configured to, upon user request, during an initial stimulation period, which is at least 1 month in duration and has a start and an end, increase over time at least one of a duration or an amplitude of the electrical stimulation from an initial value at the start of the initial stimulation period to a final value at the end of the initial stimulation period.
Boston Scientific Neuromodulation Corporation (USA)
Augusta University Research Institute, Inc. (USA)
Inventor
Moffitt, Michael A.
Blake, David
Abstract
A system for stimulation of a nucleus basalis of Meynert (NBM) of a patient includes an implantable electrical stimulation lead including electrodes and configured for implantation of at least one of the electrodes adjacent to or within the NBM of the patient; and an implantable pulse generator coupleable to the implantable electrical stimulation lead and configured for delivering electrical stimulation to the NBM through at least one of the electrodes of the implantable electrical stimulation lead, the implantable pulse generator including at least one processor configured to, upon user request, during an initial stimulation period, which is at least 1 month in duration and has a start and an end, increase over time at least one of a duration or an amplitude of the electrical stimulation from an initial value at the start of the initial stimulation period to a final value at the end of the initial stimulation period.
A method of reducing symptoms of a neurodegenerative disease comprising administering an effective amount of cannabidiol to a subject in need thereof to improved cognitive function and ameliorated the pathophysiology of the neurodegenerative disease.
A61K 31/06 - Phenols the aromatic ring being substituted by nitro groups
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
Methods and compositions for treating neurodegenerative diseases are provided. In one embodiment, the method includes administering gangliosides into the brain of a mammal in need of such treatment. The gangliosiges are preferably GM1 and GD3 gangliosides. The gangliosides are intranasally administered in an amount effective to delay and/or prevent disease progression, and to increase the resilience of brains by promoting adult neurogenesis by gangliosides.
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61K 31/7032 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyl-diacylglycerides, lactobionic acid, gangliosides
A61K 9/00 - Medicinal preparations characterised by special physical form
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.
C07C 69/66 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
C07D 317/60 - 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 311/06 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
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
44.
Platform insert for bowl, bowl with platform, and methods of using the same
GEORGIA SOUTHERN UNIVERSITY RESEARCH AND SERVICE FOUNDATION, INC. (USA)
Inventor
Baniasadi, Mahmoud
Alleyne, Jr., Cargill H
Abstract
A filament platform insert for insertion into a bowl includes a plurality protruding stages and a plurality of recesses that are each formed in arcuate shapes to form a plurality of arcuate filament channels. An access channel extending along the platform insert, between a top and bottom, and between a rear and front, provides access for insertion of a finger or tool for manipulating an endovascular filament stored in the filament channel. The platform insert is dimensioned such that alignment of multiple such platforms will form filament raceways within a bowl for the coiled reception and storage of multiple endovascular filaments, with each filament reliably isolated from one another. In an alternative configuration, an endovascular filament bowl may be made to have the filament platform as a monolithic component thereof.
B65D 25/10 - Devices to locate articles in containers
B65D 85/04 - Containers, packaging elements or packages, specially adapted for particular articles or materials for annular articles for coils of wire, rope or hose
45.
HYBRID CURCUMIN CONJUGATES AND METHODS OF USE THEREOF
THE US GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS (USA)
Inventor
Panda, Siva S.
Thangaraju, Muthusamy
Lokeshwar, Balakrishna L.
Abstract
Hybrid curcumin-based conjugates and methods of use thereof are provided. Pharmaceutical compositions including an effective amount of one or more curcumin conjugates are also provided. In particular embodiments, the compositions are formulated for oral delivery. The conjugates and pharmaceutical compositions thereof can be administered to a subject in need thereof to treat cancer.
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
Antibodies and antigen binding fragments thereof are provided that immunospecifically bind to PD-1, preferably human or mouse PD-1, and induce or promote an immune response that activates immune cell proliferation or activity. Contrary to the existing paradigm that PD-1 exclusively promotes a suppressive immune response, the disclosed antibodies and antigen binding fragments thereof, immunospecifically bind to PD-1 and cause an activating signal to be delivered to the immune cell that activates the immune cell rather than suppressing the immune cell. In one embodiment, the disclosed antibodies and antigen binding fragments thereof specifically bind to PD-1 expressed on immune cells. The binding of the disclosed antibodies and antigen binding fragments thereof to PD-1 on immune cells causes an activating signal to be transmitted into the immune cell, for example a signal that enhances or promotes cytokine production and/or activation of immune cell proliferation. Immune cells that express PD-1, include but are not limited to B and T cells as well as myeloid-derived cells. In one embodiment, the immune cell is a T cell, preferably a CD8+ T cell.
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
Provided herein are compounds of formula I or an enantiomer, solvate, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating inflammatory disease, cardiovascular disease, and cancer.
C07D 487/02 - 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 two hetero rings
Disclosed herein are engineered polyfunctional CD4+ T cells/CAR T cells and methods of their use for the treatment of cancers. One embodiment provides a method of producing polyfunctional CD4+ T cells by constitutively activating STAT5A in the cells to induce a polyfunctional phenotype. Also provided is a method of reversing exhaustion in tumor-specific CD4+ T cells by engineering the cells to express Fos, Jun, Nr4a1, or combinations thereof but not express Tox, Pdcd1, Ctla4, Haver2, Lag3, Tigit, Slam6, Nrf4a2, and administering the engineered cells to a subject.
Compounds and compositions for selectively modulating Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
50.
Human alpha fetoprotein-specific t cell receptors and uses thereof
Disclosed herein as ibuprofen hybrid conjugates and methods of their use to reduce inflammation, pain, and fever. The ibuprofen conjugates have potent anti-inflammatory and analgesic properties with low potential for ulcerogenic activity. An exemplary compound is an ibuprofen-amino acid-4-aminophenol hybrid. Also disclosed are methods of treating or reducing inflammation, pain, and fever in a subject.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
Provided herein are compounds that inhibit phosphodiesterase 5 (PDE5) and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating gastrointestinal diseases and disorders such as intestinal cancers and inflammatory bowel disease.
Compositions and methods for treating or reducing symptoms of COVID-19 are provided herein. An exemplary method includes administering to the subject an effective amount of cannabidiol to reduce acute respiratory distress syndrome caused by COVID-19.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
Methods for inducing CD8+ T cells to express a CD62LhiCD44lo naïve-like phenotype are provided. One embodiment provides a pharmaceutical composition containing CD8+ T cells induced to express a CD62LhiCD44lo naïve-like phenotype and optionally an excipient. The CD8+ T cells can be induced by contacting them with an effective amount of a MEK1/2 inhibitor. An exemplary MEK1/2 inhibitor is Selumetinib. The induced CD8+ cells can be used to treat cancer, reduce tumor burden, or treat infections in a subject in need thereof.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Compositions and methods for treating leukemia are provided herein. One embodiment provides a method of treating leukemia in a subject in need thereof by administering to a subject in need thereof a composition that selectively inhibits Akt3 by an amount effective to reduce the immune suppressive response in the subject. In one embodiment, the Akt3 inhibitors include, but are not limited to, compounds 1-31 and Formulas I-III.
The application provides methods of prognosing and classifying uterine serous carcinoma (USC) patients into poor survival groups or good survival groups and for predicting response to therapy by way of a multigene signature. The application also includes kits and computer products for use in the methods of the application.
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
G16B 25/10 - Gene or protein expression profilingExpression-ratio estimation or normalisation
G16B 5/00 - ICT specially adapted for modelling or simulations in systems biology, e.g. gene-regulatory networks, protein interaction networks or metabolic networks
57.
ENHANCING GERMICIDAL ACTIVITIES OF ALCOHOL BY COMPOUNDS DERIVED FROM PLANTS
Compositions and methods of rapidly killing, inactivating, or otherwise reducing alcohol-resistant human pathogens such as nonenveloped viruses and spores are disclosed. The methods typically include contacting a surface or objected suspected of being contaminated with a pathogen with an effective amount of one or more of the disclosed alcohol-based germicidal compositions including plant-derived compounds such as glycerol, citric acid, and green tea polyphenols, either water soluble or lipid-soluble. The compositions and methods can be used in a variety of applications, for example, to decontaminate a food or a foodstuff, to prevent pathogenic transmission, or to decontaminate a device or surface contaminated with a pathogen.
Compositions and methods of rapidly killing, inactivating, or otherwise reducing the spores such as bacterial spores are disclosed. The methods typically include reducing or preventing spore reactivation comprising contacting spores with an effective amount of one or more green tea polyphenols (GTP), one or more modified green tea polyphenols (LTP), or a combination thereof. In a preferred embodiment, the LTP is (-)-epigallocatechin-3-gallate (EGCG) esterified at the 4' position with stearic acid, EGCG esterified at the 4' position with palmitic acid, or a combination thereof. The compositions and methods can be used in a variety of applications, for example, to increase the shelf-life of a food or a foodstuff, to reduce or delay the spoilage of a food or a foodstuff, or to decontaminate a device contaminated with spores.
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
It has been discovered that even mild changes in cerebrospinal fluid (CSF) pressure or intracranial pressure (ICP) can be detected immediately as evidenced by distortions in the ONS surface structure. Further, the changes in the ONS persist after the CSF pressure has returned to normal. The stability of ONS distortions provides a means of detecting transient changes in brain pressure even when the use of the diagnostic ultrasound is delayed. One embodiment provides systems and methods for detecting or diagnosing brain injury by detecting distortions or deformations of the ONS, preferably using ultrasound.
A61B 5/00 - Measuring for diagnostic purposes Identification of persons
A61B 5/03 - Measuring fluid pressure within the body other than blood pressure, e.g. cerebral pressure
A61B 6/50 - Apparatus or devices for radiation diagnosisApparatus or devices for radiation diagnosis combined with radiation therapy equipment specially adapted for specific body partsApparatus or devices for radiation diagnosisApparatus or devices for radiation diagnosis combined with radiation therapy equipment specially adapted for specific clinical applications
A61B 8/00 - Diagnosis using ultrasonic, sonic or infrasonic waves
A61B 5/055 - Detecting, measuring or recording for diagnosis by means of electric currents or magnetic fieldsMeasuring using microwaves or radio waves involving electronic [EMR] or nuclear [NMR] magnetic resonance, e.g. magnetic resonance imaging
A61B 6/00 - Apparatus or devices for radiation diagnosisApparatus or devices for radiation diagnosis combined with radiation therapy equipment
Disclosed herein are compositions and methods for ovulation induction in females in need thereof. Current methods for inducing ovulation have unpleasant side effects and are expensive. The disclosed compositions and methods are safe, efficacious, and inexpensive. An exemplary method of inducing ovulation includes steps of monitoring ovarian follicle development and size during the follicular phase of the menstrual cycle; and administering to the subject a pharmaceutical composition including progesterone or bioidentical progesterone in an amount effective to increase the plasma concentration of progesterone to between about 0.1 ng/ml to about 1 ng/ml when the follicle reaches a size of at least 15 mm.
A61K 31/57 - 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
A61K 9/00 - Medicinal preparations characterised by special physical form
Antibodies and antigen binding fragments thereof that immunospecifically bind OPN (OPN) and inhibit OPN activity are provided herein. The disclosed antibodies and antigen binding fragments are useful for modulating signal transduction through OPN proteins. The antibodies and antigen-binding fragments are useful for the treatment or prevention of cancer, osteoporosis, or other immune diseases.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
An aptamer platform capable of efficiently delivering and silencing one, two or more genes in vivo or in vitro is provided. Methods of using the aptamer compositions for selectively targeting cells to down-regulate the expression of multiple genes are also provided.
Methods of using one or more fumaric acid esters or pharmacologically active salts, derivatives, analogues, or prodrugs thereof to increase expression of fetal hemoglobin (HbF) are disclosed. The methods typically include administering to a subject an effective amount of one or more fumaric acid esters optionally in combination or alternation with hydroxyurea to induce HbF expression in the subject in an effective amount to reduce one or more symptoms of a sickle cell disorder, a hemoglobinopathy, or a beta-thalassemia, or to compensate for a genetic mutation is the human beta-globin gene (HBB) or an expression control sequence thereof. Pharmaceutical dosage units and dosage regimes for use in the disclosed methods are also provided.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/573 - 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 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
Chimeric antigen receptor T cell (CARTs) compositions and methods of their use are provided. One embodiment provides a chimeric antigen receptor T cell composition including 8F8 chimeric antigen receptor T cells. Another embodiment provides a chimeric antigen receptor T cell composition including 6G11 chimeric antigen receptor T cells. Still another embodiment provide a chimeric antigen receptor T cell composition including 12D7 chimeric antigen receptor T cells. The disclosed CARTs can be used to treat cancer, for example hepatocellular carcinoma.
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
Antibodies and antigen binding fragments thereof are provided that immunospecifically bind to PD-1, preferably human or mouse PD-1, and induce or promote an immune response that activates immune cell proliferation or activity. Contrary to the existing paradigm that PD-1 exclusively promotes a suppressive immune response, the disclosed antibodies and antigen binding fragments thereof, immunospecifically bind to PD-1 and cause an activating signal to be delivered to the immune cell that activates the immune cell rather than suppressing the immune cell. In one embodiment, the disclosed antibodies and antigen binding fragments thereof specifically bind to PD-1 expressed on immune cells. The binding of the disclosed antibodies and antigen binding fragments thereof to PD-1 on immune cells causes an activating signal to be transmitted into the immune cell, for example a signal that enhances or promotes cytokine production and/or activation of immune cell proliferation. Immune cells that express PD-1, include but are not limited to B and T cells as well as myeloid-derived cells. In one embodiment, the immune cell is a T cell, preferably a CD8+ T cell.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
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
University of Georgia Research Foundation, Inc. (USA)
Augusta University Research Institute (USA)
Inventor
Kennedy, Eileen J.
Cowell, John
Abstract
As disclosed herein, stapled peptides targeting the interaction interface between proteins that maintain the integrity of Wiskott-Aldrich syndrome protein family member 3 (WASF3) leads to destabilization of WASF3 and suppression of invasion. Disclosed are stapled peptides that inhibit the binding of Cytoplasmic FMR1-interacting protein 1 (CYFIP1) to either WASF3 or NCK-associated protein (NCKAP1). Also disclosed are methods for treating or suppressing invasion and metastasis of a cancer in a subject that involve administering to the subject a therapeutically effective amount of a stapled peptide disclosed herein.
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
Compounds and compositions for selectively modulating Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
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
Compositions and methods for supporting health, especially renal health, comprising ketonic agents that recapitulate beneficial effects of ketosis by exogenously administered agents. The agents include BHB, analogs thereof, and GPR109A agonists. The agents may further include crystal precipitation inhibitors which synergistically improve treatment of certain renal conditions. The agents may be used in dietary supplements and therapeutic compositions for the treatment of cystic kidney diseases such as polycystic kidney disease, ciliopathies, and other conditions.
A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
THE BOARD OF REGENTS OF THE UNIVERSITY SYSTEM OF GEORGIA BY AND ON BEHALF OF AUGUSTA UNIVERSITY (USA)
Inventor
Weimbs, Thomas
Torres, Jacob
Thangaraju, Muthusamy
Abstract
Compositions and methods for supporting health, especially renal health, comprising ketonic agents that recapitulate beneficial effects of ketosis by exogenously administered agents. The agents include BHB, analogs thereof, and GPR109A agonists. The agents may further include crystal precipitation inhibitors which synergistically improve treatment of certain renal conditions. The agents may be used in dietary supplements and therapeutic compositions for the treatment of cystic kidney diseases such as polycystic kidney disease, ciliopathies, and other conditions.
Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Bispecific aptamers having a first end that specifically binds to a first tumor specific marker, tumor antigen, or viral protein and a second end that specifically binds to a second tumor specific marker, tumor antigen, or viral protein are provide. The bispecific aptamers can be used to treat cancer or virally infected cells. Generally, the bispecific aptamers bind to two surface proteins, preferably different proteins, on the same cell. In a preferred embodiment the bispecific aptamers bind to two different tumor markers, tumor antigens, tumor specific proteins and combinations thereof.
Provided are embodiments of creatine and creatine ethyl ester (CEE) salts where the anion is an artificial (non-saccharide) taste-modifier. These compounds represent stable white non-hygroscopic solids or semisolids that can readily dissolve in water and buffer solutions. Synthesis of novel creatine salts using environmentally safe solvents such as ethanol resulted in the formation of products in quantitative yields with sodium or potassium chloride as a byproduct. The creatine and creatine alkyl eater derivative salts are stable sweet-tasting compounds that are more palatable to a consumer than creatine or derivatives thereof.
C07C 279/14 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
A23L 27/00 - SpicesFlavouring agents or condimentsArtificial sweetening agentsTable saltsDietetic salt substitutesPreparation or treatment thereof
Several compounds have been discovered that modulate signal transduction through the PD-1 receptor. In certain embodiments, the compounds promote or induce an activating signal through the PD-1 receptor that activates a T cell. The compounds can bind to PD-1 and inhibit or prevent ligands from binding to PD-1 and thereby suppress inhibitory signal transduction through the PD-1 receptor.
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
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 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
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 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
Pyrazinamide (PZA) conjugates and hybrids are provided herein. The PZA conjugates are useful for treating bacterial infections. In one embodiment, the PZA conjugates are useful for treating tuberculosis.
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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 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
A61P 31/06 - Antibacterial agents for tuberculosis
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 9/00 - Medicinal preparations characterised by special physical form
76.
Compositions and methods for promoting hair growth
Compositions and methods for treating hair loss are provided. One embodiment provides a microneedle composition, which when administered to the skin of a subject promotes hair growth. The microneedle compositions include an effective amount of glucocorticoid-induced leucine zipper (GILZ) protein having an amino acid sequence that has 99 or 100% identity to SEQ ID NO: 1, or fragment thereof to promote hair growth when administered to the skin of the subject and a bioerodible, biodegradable, or biosorbable polymer, wherein the composition is formulated as bioerodible, biodegradable, or bioabsorbable microneedles. In one embodiment the GILZ protein or fragment thereof is conjugated to a cell penetrating peptide. The cell penetrating peptide can be TAT GRKKRRQRRRPQ (SEQ ID NO:4) or a variant thereof.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61M 37/00 - Other apparatus for introducing media into the bodyPercutany, i.e. introducing medicines into the body by diffusion through the skin
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
Glucocorticoid-induced leucine zipper protein (GILZ) peptide compositions and their methods of use in wound healing are disclosed herein. An exemplary GILZ peptide composition includes a GILZ fusion protein. The GILZ peptide compositions can be administered topically to wounds, for example in the form of a cream, ointment, or lotion. The GILZ peptide compositions can be used to treat acute wounds, induce wound healing in chronic wounds, and reduce scar formation.
A61L 26/00 - Chemical aspects of, or use of materials for, liquid bandages
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
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
78.
EGCG-PALMITATE COMPOSITIONS AND METHODS OF USE THEREOF
13030 group in at least one position. The modified green tea polyphenols can be used to prevent influenza viruses without coming into contact with the viral cell.
Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
A method for removing bodily fluid includes drawing bodily fluid that has accumulated in excess, converting the drawn fluid from bulk liquid form to aerosol form, and disposing of the aerosol via evaporation of liquid droplets and absorption and/or diffusion of vapor. Conversion from bulk liquid to aerosol may include collecting the bulk liquid fluid in a reservoir, conveying the bulk liquid bodily fluid to an atomizer, converting the bulk liquid fluid into an aerosol having ultrafine droplets, and ejecting the aerosol into a subcutaneous space for disposal via evaporation of liquid droplets and absorption and/or diffusion of vapors. The method may be performed with a subcutaneous atomizer that may be controlled locally or by an external transmitter for effecting a conversion and mist rate to keep pace with the accumulation of excess bodily fluid.
+ T-cells, or both. The dysfunctional T cells can be depleted, for example, by administering an antibody or fusion protein that specifically binds to dysfunctional T cells and promotes their depletion. In one embodiment the antibody is a bispecific antibody that can be specific for CD38 and CD8, or it can be specific for CD38 and PD-1. Also disclosed is a method of detecting and treating anti-PD1 therapy resistance by measuring the amount of CD38+PD1+CD8 T cells in blood or tissue samples obtained from a subject prior to anti-PD1 therapy and administering an anti-CD38/CD8 or anti-CD38/PD-1 depleting/blocking antibody to the subject prior to anti-PD1 therapy.
G01N 33/49 - Physical analysis of biological material of liquid biological material blood
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
G01N 15/01 - Investigating characteristics of particlesInvestigating permeability, pore-volume or surface-area of porous materials specially adapted for biological cells, e.g. blood cells
A method for removing bodily fluid includes drawing bodily fluid that has accumulated in excess, converting the drawn fluid from bulk liquid form to aerosol form, and disposing of the aerosol via evaporation of liquid droplets and absorption and/or diffusion of vapor. Conversion from bulk liquid to aerosol may include collecting the bulk liquid fluid in a reservoir, conveying the bulk liquid bodily fluid to an atomizer, converting the bulk liquid fluid into an aerosol having ultrafine droplets, and ejecting the aerosol into a subcutaneous space for disposal via evaporation of liquid droplets and absorption and/or diffusion of vapors. The method may be performed with a subcutaneous atomizer that may be controlled locally or by an external transmitter for effecting a conversion and mist rate to keep pace with the accumulation of excess bodily fluid.
Calprotectin inhibitors and derivatives thereof, and methods of using them for inhibiting or reducing metastatis and treating cancer are provided. The pharmaceutical formulations prepared from the compounds can be used in the treatment of cancer either as a single agent or in combination with at least one other cancer therapeutic, chemotherapeutic or anti-cancer agent.
Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
Compositions of alkaline salts and metabolic acid inducers and methods of use thereof are provided. The disclosed compositions may be used for stimulating vagal nerve efferent pathways, treating or preventing an inflammatory response or an autoimmune disorder, inhibiting or reducing one or more inflammatory M1 macrophages and/or one or more inflammatory neutrophils in the blood, promoting polarization of macrophages from a pro-inflammatory M1 state to an anti-inflammatory M2 state, and treating or preventing cardiovascular disease or metabolic disorders.
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
An aptamer platform capable of efficiently delivering and silencing one, two or more genes in vivo or in vitro is provided. Methods of using the aptamer compositions for selectively targeting cells to down-regulate the expression of multiple genes are also provided.
A method for identifying drug resistant genes and compositions containing agents that downregulate these genes in combination with a cancer therapeutic.
Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 39/00 - Medicinal preparations containing antigens or antibodies
It has been discovered that the cyclic peptide EnnA inactivates the Hsp90 chaperone pathway, but without activating an extensive heat shock response and overexpression of anti-apoptotic proteins. Mechanistically distinct, EnnA inhibits Hsp90 and destabilize PDL-1 and IDO, two major immune checkpoints mediating tumor-induced immune suppression. The provided herein show that EnnA profoundly modulates the cytokine signature of cancer cells and promotes a cytokine profile that favors an immune attack on tumor cells. This translates into highly efficacious anti-tumor activity in vivo, which, when combined with a single dose of chemotherapy, completely reduced the tumor burden in experimental animals and instilled highly efficient immune memory against the primary tumor.
Methods are disclosed for viable preservation of biomaterials including both prokaryotic and eukaryotic cells/materials such as human cells and tissues at subzero and suprazero temperatures. One embodiment provides a method wherein initial desiccation and subsequent cooling of the biological samples is below their glass transition temperature (Tg) to achieve a stable glassy state without exposing the biomaterials to excessive osmotic/chemical stresses for long periods of time. Another embodiment provides a method that includes combining the initial desiccation with subsequent freeze-drying to achieve a glassy state of biomaterials. Another embodiment provides a desiccation medium with low salt, high osmolyte/glass former content and desiccation of biomaterials in a spherical droplet to avoid the edge effect.
Compositions for the inhibition of SUV39H1 methyltransferase activity and methods of use thereof are provided. The disclosed compositions may be used for treating certain types of cancer, inducing apoptosis in a cancer cell, increasing cell sensitivity to FasL-induced apoptosis, and overcoming cancer cell resistance to apoptosis and/or certain types of cancer immunotherapy.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
Antibodies and antigen binding fragments thereof are provided that immunospecifically bind to PD-1, preferably human or mouse PD-1, and induce or promote an immune response that activates immune cell proliferation or activity. Contrary to the existing paradigm that PD-1 exclusively promotes a suppressive immune response, the disclosed antibodies and antigen binding fragments thereof, immunospecifically bind to PD-1 and cause an activating signal to be delivered to the immune cell that activates the immune cell rather than suppressing the immune cell. In one embodiment, the disclosed antibodies and antigen binding fragments thereof specifically bind to PD-1 expressed on immune cells. The binding of the disclosed antibodies and antigen binding fragments thereof to PD-1 on immune cells causes an activating signal to be transmitted into the immune cell, for example a signal that enhances or promotes cytokine production and/or activation of immune cell proliferation. Immune cells that express PD-1, include but are not limited to B and T cells as well as myeloid-derived cells. In one embodiment, the immune cell is a T cell, preferably a CD8+ T cell.
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
Provided are embodiments of creatine and creatine ethyl ester (CEE) salts where the anion is an artificial (non-saccharide) taste-modifier. These compounds represent stable white non-hygroscopic solids or semisolids that can readily dissolve in water and buffer solutions. Synthesis of novel creatine salts using environmentally safe solvents such as ethanol resulted in the formation of products in quantitative yields with sodium or potassium chloride as a byproduct. The creatine and creatine alkyl eater derivative salts are stable sweet-tasting compounds that are more palatable to a consumer than creatine or derivatives thereof.
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
C07C 279/14 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
98.
Communication and skills training using interactive virtual humans
University of Florida Research Foundation, Incorporated (USA)
Inventor
Lok, Benjamin Chak Lum
Lind, David Scott
Cendan, Juan Carlos
Raij, Andrew Brian
Rossen, Brent H.
Kotranza, Aaron Andrew
Johnsen, Kyle John
Abstract
A system for providing interaction between a virtual human and a user, the system comprising: a tangible interface providing a physical interface between the user and the virtual human, an imaging system directed towards the physical interface to provide images of the user interacting with the tangible interface; a tracking system tracking at least one position or the user; a microphone capturing speech from the user; a simulation system receiving inputs from the tangible interface, the imaging system, the tracking system and the microphone, the simulation system generating output signals corresponding to the virtual human; and a display presenting the output signals to the user.
G09B 7/00 - Electrically-operated teaching apparatus or devices working with questions and answers
G09B 23/28 - Models for scientific, medical, or mathematical purposes, e.g. full-sized device for demonstration purposes for medicine
G06F 19/00 - Digital computing or data processing equipment or methods, specially adapted for specific applications (specially adapted for specific functions G06F 17/00;data processing systems or methods specially adapted for administrative, commercial, financial, managerial, supervisory or forecasting purposes G06Q;healthcare informatics G16H)
99.
Detection and treatment of LRP4-associated neurotransmission disorders
The present invention includes methods for the detection of neurotransmission or developmental disorders, including, but not limited to, myasthenia gravis that is seronegative for autoantibodies to the acetylcholine receptor (AChR) and/or muscle specific tyrosine kinase (MuSK), the method including detecting autoantibodies that bind to LRP4, or an epitope thereof. Also included are methods for the treatment of an individual suffering from a neurotransmission disorder, the method including detecting in a bodily fluid of the individual autoantibodies that bind to LRP4, or an epitope thereof, and administering to the patient an effective amount an immunosuppressant and/or another appropriate therapeutic modality. Also included are antibodies that bind to autoantibodies to LRP4 and kits for the detection of neurotransmission or developmental disorders.
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
G01N 33/567 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent utilising isolate of tissue or organ as binding agent
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
G01N 33/92 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving lipids, e.g. cholesterol
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 39/00 - Medicinal preparations containing antigens or antibodies