Disclosed is a method of reducing plasma level of macrophage migratory inhibitory factor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61P 11/00 - Drugs for disorders of the respiratory system
2.
TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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
A injectable pharmaceutical compositions consists of a buffered aqueous solution comprising (a) about 5% w/v to about 15% w/v sulfobutylether-β-cyclodextrin (SBE-β-CD), and about 0.05% w/v to about 0.5% w/v ibudilast, or (b) about 5% w/v to about 25% w/v polyoxyl castor oil, and about 1% w/v to about 5% w/v ibudilast.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A injectable pharmaceutical compositions consists of a buffered aqueous solution comprising (a) about 5% w/v to about 15% w/v sulfobutylether-β-cyclodextrin (SBE-P- CD), and about 0.05% w/v to about 0.5% w/v ibudilast, or (b) about 5% w/v to about 25% w/v polyoxyl castor oil, and about 1% w/v to about 5% w/v ibudilast.
Disclosed is a method of treating post-COVID condition(s) in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
6.
IBUDILAST FOR USE IN THE TREATMENT OF POST-COVID CONDITIONS
A method of treating post-COVID condition(s) in a patient in need thereof includes administering to the patient a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
A method of preventing metastasis of a cancer in a patient in need thereof includes administering to the patient a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
Disclosed herein are compositions and methods for treating glioblastoma in a patient in need thereof by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo [l,5-a] pyridine) or a pharmaceutically acceptable salt thereof, and an immune checkpoint inhibitor.
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 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Disclosed herein are compositions and methods for treating glioblastoma in a patient in need thereof by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof, and an immune checkpoint inhibitor.
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 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 9/00 - Medicinal preparations characterised by special physical form
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK (USA)
Inventor
Matsuda, Kazuko
Ambrosini, Grazia
Schwartz, Gary K.
Rai, Alex J.
Abstract
A method of preventing metastasis of a cancer in a patient in need thereof includes administering to the patient a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 35/04 - Antineoplastic agents specific for metastasis
The Trustees of Columbia University in the City of New York (USA)
Inventor
Matsuda, Kazuko
Ambrosini, Grazia
Schwartz, Gary K.
Rai, Alex J.
Abstract
A method of preventing metastasis of a cancer in a patient in need thereof includes administering to the patient a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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
Described herein are methods for decreasing triglyceride synthesis and/or decreasing triglyceride accumulation in the liver of a subject, wherein the methods comprise administering to the subject a compound of Formula (I):
a metabolite thereof, or a pharmaceutically acceptable salt thereof.
Described herein are methods for decreasing triglyceride synthesis and/or decreasing triglyceride accumulation in the liver of a subject, wherein the methods comprise administering to the subject a compound of Formula (I): a metabolite thereof, or a pharmaceutically acceptable salt thereof.
A method of treating chemical-induced lung injury in a subject in need thereof includes administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61P 11/00 - Drugs for disorders of the respiratory system
Disclosed is a method of treating chemical-induced lung injury in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 11/00 - Drugs for disorders of the respiratory system
16.
Treatment of progressive neurodegenerative disease with ibudilast
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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
Disclosed is a method of reducing plasma level of macrophage migratory inhibitory factor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
Disclosed is a method of reducing plasma level of macrophage migratory inhibitory factor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of ibudilast, or a pharmaceutical salt thereof.
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 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61P 11/00 - Drugs for disorders of the respiratory system
19.
IBUDILAST ORAL FORMULATIONS AND METHODS OF USING SAME
This disclosure is directed to ibudilast higher dosage oral formulations, such as tablet or capsule formulations, and the corresponding methods of treatment.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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
20.
Ibudilast oral formulations and methods of using same
This disclosure is directed to ibudilast higher dosage oral formulations, such as tablet or capsule formulations, and the corresponding methods of treatment.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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
21.
Methods and dosing regimens using ibudilast and a second agent for cancer therapy
Methods and dosing regimens for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof and at least one or more other therapeutic agent.
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
The present disclosure relates generally to methods for treating neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing neurodegenerative diseases, including their progressive forms and their associated symptoms by administering a combination of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) and riluzole, or pharmaceutically acceptable salts of one or both thereof.
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 31/428 - Thiazoles condensed with carbocyclic rings
A61K 9/00 - Medicinal preparations characterised by special physical form
This disclosure is directed to methods of treating ophthalmic disease/disorder or injury associated with neurodegenerative disease/disorder, such as progressive multiple sclerosis, or a neuro-ophthalmologic disorder in human patients using ibudilast.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
A61P 25/28 - 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 9/00 - Medicinal preparations characterised by special physical form
24.
METHODS OF TREATING OPHTHALMIC DISEASE/DISORDER OR INJURY WITH IBUDILAST
This disclosure is directed to methods of treating ophthalmic disease/disorder or injury associated with neurodegenerative disease/disorder, such as progressive multiple sclerosis, or a neuro-ophthalmologic disorder in human patients using ibudilast.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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
25.
COMBINATION OF IBUDILAST AND INTERFERON-BETA AND METHODS OF USING SAME
This disclosure is directed to methods of alleviating the negative effects of, treating, or slowing the progression of progressive multiple sclerosis in human patients using ibudilast and interferon-beta.
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
This disclosure is directed to methods of alleviating the negative effects of, treating, or slowing the progression of progressive multiple sclerosis in human patients using ibudilast and interferon-beta.
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
27.
Treatment of progressive neurodegenerative disease with ibudilast
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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
Methods of suppressing myeloid-derived suppressor cells (MDSCs), reducing immune suppression, reducing regulatory T-cell count and increasing CD4+ T-cell count in cancer patients using ibudilast.
Methods and dosing regimens for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof and at least one or more other therapeutic agent.
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
Methods and dosing regimens for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5- a]pyridine) or a pharmaceutically acceptable salt thereof and at least one or more other therapeutic agent.
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 9/00 - Medicinal preparations characterised by special physical form
Compositions and methods for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
32.
METHODS OF TREATING GLIOBLASTOMA MULTIFORME USING IBUDILAST
Compositions and methods for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[l,5- a]pyridine) or a pharmaceutically acceptable salt thereof.
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 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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 31/4439 - 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
C07D 231/54 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
The present disclosure relates generally to methods for treating neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing neurodegenerative diseases, including their progressive forms and their associated symptoms by administering a combination of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) and riluzole, or pharmaceutically acceptable salts of one or both thereof.
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 31/428 - Thiazoles condensed with carbocyclic rings
A61K 9/00 - Medicinal preparations characterised by special physical form
Alcoholism, and symptoms and negative effects thereof may be treated using ibudilast or a pharmaceutically acceptable salt thereof. Patients diagnosed with alcohol use disorder and who exhibit symptoms of depression and/or dysphoric mood can be treated using ibudilast or a pharmaceutically acceptable salt thereof.
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
A therapeutic use of trans-geranylgeranylacetone and its analogs is described, along with methods of inhibiting, reducing, or treating fibrosis, by administering the trans isomer of geranylgeranylacetone or an analog thereof.
The present disclosure relates generally to methods for treating progressive neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing progressive neurodegenerative diseases, including their progressive forms and its associated symptoms by administration of a combination of geranylgeranylacetone (teprenone), ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine), and riluzole (insert chemical name?), or pharmaceutically acceptable salts thereof.
Geranylgeranylacetone and its analogs and a phenoxyalkylcarboxylic acid are described, along with methods of inhibiting, reducing, or treating fibrosis, by administering the trans isomer of geranylgeranylacetone or an analog thereof with a phenoxyalkylcarboxylic acid, salt, or ester thereof.
Provided herein are methods of inhibiting or treating non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), advanced NASH, non-alcoholic fatty liver disease, conditions leading to or arising from them, and/or negative effects of each of the above by administering ibudilast or a pharmaceutically acceptable salt thereof in combination with an effective amount of telmisartan or an ester thereof or a pharmaceutically acceptable salt of each thereof.
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 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
39.
COMBINATION OF IBUDILAST AND RILUZOLE AND METHODS OF USING SAME
The present disclosure relates generally to methods for treating neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing neurodegenerative diseases, including their progressive forms and their associated symptoms by administering a combination of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) and riluzole, or pharmaceutically acceptable salts of one or both thereof.
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 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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
40.
A COMBINATION OF GERANYLGERANYLACETONE AND IBUDILAST AND METHODS OF USING SAME
The present invention relates generally to methods for treating progressive neurodegenerative diseases, including their progressive forms. In particular, the present invention pertains to methods of treating or preventing progressive neurodegenerative diseases and its associated symptoms by administration of a combination of geranylgeranylacetone (teprenone) and ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine), or pharmaceutically acceptable salts thereof.
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
C07C 49/203 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
A compound of Formula (I) or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein Formula (I), m, n, X1 and X2 are as defined herein, is useful for inhibiting, reducing, or treating fibrosis, conditions leading to or arising from it, and/or negative effects of each thereof.
2 are as defined herein, is useful for inhibiting, reducing, or treating fibrosis, conditions leading to or arising from it, and/or negative effects of each thereof.
A compound of Formula (I):
2 are as defined herein, is useful for inhibiting or treating advanced nonalcoholic steatohepatitis, conditions leading to or arising from it, and/or negative effects of each thereof.
C07C 323/22 - 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 doubly-bound oxygen atoms bound to the same carbon skeleton
44.
METHOD OF TREATING ADVANCED NON-ALCOHOLIC STEATOHEPATITIS
A compound of Formula (I): or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X1 and X2 are as defined herein, is useful for inhibiting or treating advanced nonalcoholic steatohepatitis, conditions leading to or arising from it, and/or negative effects of each thereof.
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A compound of Formula (I) or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X1 and X2 are as defined herein, is useful for inhibiting or treating idiopathic pulmonary fibrosis, conditions leading to or arising from it, and/or negative effects of each thereof.
A compound of Formula (I), or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof wherein: m is an integer from 2 to 5 inclusive; and n is an integer from 3 to 8 inclusive; and X1 and X2 are each independently sulfur, oxygen, a sulfinyl group or a sulfonyl group, provided that X1 and X2 are not simultaneously oxygen. Such a compound may be useful for treating, inhibiting, or preventing the progression of amyotrophic lateral sclerosis, primary lateral sclerosis, or familial amyotrophic lateral sclerosis, or a symptom of each thereof.
A compound of Formula (I) or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X1 and X2 are as defined herein, is useful for inhibiting liver steatosis, lobular inflammation, hepatic ballooning and hepatic scarring.
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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
48.
Methods for reducing triglyceride, total cholesterol and low density lipoprotein blood levels
A compound of Formula (I):
2 are as defined herein, is useful for reducing blood levels of one or more of triglycerides (TG), total cholesterol (TC) and low density lipoprotein (LDL) in human subjects.
Alcoholism, and symptoms and negative effects thereof may be treated using ibudilast or a pharmaceutically acceptable salt thereof. Abstinence from alcohol consumption may be maintained using ibudilast or a pharmaceutically acceptable salt thereof. Withdrawal from alcohol may be facilitated and negative effects thereof reduced by using ibudilast or a pharmaceutically acceptable salt thereof.
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 31/4439 - 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
A compound of Formula (I): or a metabolite thereof, or an ester of the compound of Formula (I) or the metabolite thereof, or a pharmaceutically acceptable salt of each thereof, wherein m, n, X1 and X2 are as defined herein, is useful for reducing blood levels of one or more of triglycerides (TG), total cholesterol (TC) and low density lipoprotein (LDL) in human subjects.
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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
A compound of Formula (I):
2 are as defined herein, is useful for inhibiting liver steatosis, lobular inflammation, hepatic ballooning and hepatic scarring.
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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 31/4439 - 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
54.
Method of treating non-alcoholic fatty liver disease and steatohepatitis
A compound of Formula (I):
2 are as defined herein, is useful for treating non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).
MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent.
The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.
MN-029 di-hydrochloride (MN-029.2HC1, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
57.
Treatment of acute exacerbation of asthma and reduction of likelihood of hospitalization of patients suffering therefrom
The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
A01N 37/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
A61K 31/21 - Esters, e.g. nitroglycerine, selenocyanates
58.
TREATING HUMAN MALE COPD PATIENTS WITH ORAL BEDORADRINE
A method of treating a human male patient is disclosed. Enterally administering bedoradrine or a pharmaceutically acceptable salt thereof to a human male patient who is suffering from a medical condition that is responsive to bedoradrine or a pharmaceutically acceptable salt thereof, is useful and benefits human males versus human females. A preferred mode of administration is oral administration.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2 -isopropylpyrazolo[1,5-a]pyridine).
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
A61P 25/00 - Drugs for disorders of the nervous system
60.
Methods and compositions for the treatment of irritable bowel syndrome
A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I:
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 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I.
C07C 235/00 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
C07D 211/06 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
62.
COMPOSITIONS, METHODS, AND DEVICES FOR THE TREATMENT OF DYSMENORRHEA
A method for a prevention and/or treatment of dysmenorrhea or amelioration of a symptom thereof in a subject, comprising administering to said subject an effective amount of a compound of formula I.
The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one, (S)-AV1013, is a candidate therapeutic for treating neuroathic pain, addiction behavior and drug withdrawal symptoms. Also described are methods for preparing and using (S)-AV1013, its pharmaceutically acceptable salts as well as pharmaceutically acceptable formulations of the same.
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
65.
Treatment of progressive neurodegenerative disease with ibudilast
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
66.
TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 25/28 - 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
67.
Substituted pyrazolo[1,5-a]pyridine compounds and their methods of use
The invention concerns a method of treatment or prophylaxis of depression by administering a phenylethanolaminocyclohexylphenyl compound of a general formula (I) in which R1 represents hydrogen or halogen; R2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted with lower alkylaminocarbonyl which may be substituted with lower alkoxy, lower alkoxy substituted with cyclic aminocarbonyl of 4 to 6 carbon atoms, lower alkoxycarbonyl or carboxy; R3 represents hydrogen, hydroxy, lower alkoxy or lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups; R2 and R3 may be bonded to each other to form methylenedioxy substituted with carboxy or lower alkoxycarbonyl; and m and n are 0 or 1, and their pharmacologically acceptable metabolites or salts, which have selective stimulating activity and binding affinity for β3 adrenergic receptors.
The present invention is directed to the use of ibudilast for treating addictions, including drug and behavioral addictions. In particular, ibudilast is used to diminish the dopamine-mediated reward associated with addictions and to treat withdrawal syndromes after discontinuance of addictive drug use or behavior.
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
70.
Method for treating neuropathic pain and associated syndromes
