Formulations and methods of using mitochondrially targeted antioxidants (SkQ) to improve dry eye conditions in subjects having a tear production of ≥7 mm measured by a Schirmer's test are provided. The methods provide benefits to the population-specific group of subjects but do not provide benefits to subjects having a tear production of <7 mm, as measured by a Schirmer's test.
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
Methods for enhancing weight loss, or preventing or treating obesity or other conditions related thereto, such as diabetes, involve administering a GLP-1 agonist together with, or prior to, administering a mitochondrial uncoupler. Use of the uncoupler increases weight loss and enhances treatment of obesity and obesity-related medical conditions, such as by preventing weight regain after cessation of administration of the GLP-1 agonist.
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 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
3.
MITOCHONDRIA-TARGETED ANTIOXIDANTS FOR USE IN THE TREATMENT OF CELL BALLOOONING-ASSOCIATED DISEASES, SUCH AS NON-ALCOHOLIC FATTY LIVER DISEASE (NAFLD) AND NON-ALCOHOLIC STEATOHEPATITIS (NASH)
Methods and compositions for treating and preventing cell ballooning and other diseases or medical conditions are provided. The diseases or medical conditions are characterized by cell degeneration or cell death as a part of the disease pathogenesis. Cell ballooning is a condition associated with storage of excess fat in the liver. nutritional or biochemical imbalance, damage to mitochondria, ATP depletion, or virus infection. A mitochondrially targeted antioxidant compound is administered to a subject in need thereof, whereby excess fat is metabolized.
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
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
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
4.
MITOCHONDRIA-TARGETED ANTIOXIDANTS FOR USE IN THE TREATMENT OF CELL BALLOOONING-ASSOCIATED DISEASES, SUCH AS NON-ALCOHOLIC FATTY LIVER DISEASE (NAFLD) AND NON-ALCOHOLIC STEATOHEPATITIS (NASH)
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
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
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
5.
Contact Lenses And Other Eye-Contacting Matrices Carrying Mitochondrially-Targeted Antioxidants
The present inventor has discovered how to adsorb a mitochondrially targeted compound (MTC) of general formula I on contact lenses and other matrices prior to the application of lenses or other matrix on the eye surface. After such matrix is positioned on the eye, MTC is translocated from the lens into cornea cells of the eye providing cornea protective effect and thus reducing side effects of contact lens application.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
Formulations and methods of using mitochondrially targeted antioxidants (SkQ) to improve dry eye conditions in subjects having a tear production of ≥ 7 mm measured by a Schirmer's test are provided. The methods provide benefits to the population-specific group of subjects but do not provide benefits to subjects having a tear production of < 7 mm, as measured by a Schirmer's test.
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 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61K 9/00 - Medicinal preparations characterised by special physical form
Mitochondrially targeted antioxidants are used to prevent and treat severe inflammatory conditions including viral infection (such as COVID-19), systemic shock, trauma, burns, surgery associated with significant tissue damage, toxic damage, and damage associated with autoimmune reactions.
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
8.
POLYMER MATRIXES FOR DIFFERENT COMPOSITIONS OF MITOCHONDRIALLY TARGETED ANTIOXIDANTS
A composition containing amitochodrially-targeted antioxidant of the SkQ type and a polyacrylate, agarose, agar-agar orhyaluronic acid polymer useful for production of pharmaceutical, medicinal and cosmetic compositions having good stability. Such compositions may usefully also include lactic acid.
Mitochondrially targeted antioxidants are used to prevent and treat severe inflammatory conditions including viral infection (such as COVID-19), systemic shock, trauma, burns, surgery associated with significant tissue damage, toxic damage, and damage associated with autoimmune reactions.
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 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
Here are described SkQ compounds containing cations of various types: alkyl(triphenyl)phosphonium cation, quaternary ammonium cations, including pH -dependent and permanent cations of rhodamines, berberine and palmatine alkaloids.
A method for providing to a mammal a neuroprotective effect against a brain pathology that is associated with reactive oxygen species originating from mitochondria (mROS). The method includes the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to provide said neuroprotective effect. The SkQ mitochondria-targeted antioxidant may be administered either prophylactically or for treatment with respect to brain pathologies other than brain trauma or stroke, and may be administered for treatment of brain trauma or stroke.
A61K 31/35 - 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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
The present disclosure provides methods of preventing activation of neutrophils with mitochondrially targeted antioxidants. Also disclosed are methods of preventing or treating different inflammatory diseases and inflammation-related conditions with MTAs.
A61K 31/662 - Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Medicines, namely, pharmaceutical preparations for the treatment of age-related disorders such as glaucoma, cataracts, age-related macular degeneration, diabetes, and cardio-vascular disorders
14.
Oral formulations of mitochondrially-targeted antioxidants and their preparation and use
Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
The present disclosure provides methods of preventing activation of neutrophils with mitochondrially targeted antioxidants.. Also disclosed are methods of preventing or treating different inflammatory diseases and inflammation-related conditions with MTAs.
A method for providing to a mammal a neuroprotective effect against a brain pathology that is associated with reactive oxygen species originating from mitochondria (mROS). The method includes the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to provide said neuroprotective effect. The SkQ mitochondria-targeted antioxidant may be administered either prophylactically or for treatment with respect to brain pathologies other than brain trauma or stroke, and may be administered for treatment of brain trauma or stroke.
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 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/00 - Drugs for disorders of the nervous system
20.
Pharmaceutical compositions useful for preventing and treating cancer
Disclosed is a method of treating a cancer on a mammal, comprising administering to the mammal in need thereof a therapeutically effective amount of a compound
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 31/352 - 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 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
21.
ORAL FORMULATIONS OF MITOCHONDRIALLY-TARGETED ANTIOXIDANTS AND THEIR PREPARATION AND USE
Provided are stable liquid and solid formulations of oxidized and reduced mitochondria-targeted antioxidants, and methods of their preparation and use.
The present disclosure provides purified pharmaceutical preparations comprising oxidized SkQ1, wherein no individual impurity exceeds 1.5%, the total impurity content of the preparation does not exceed 4.0%, and the content of reduced SkQ1 is not greater than 10%, the structure of oxidized SkQ1 being:
C07C 46/06 - Preparation of quinones by oxidation giving rise to quinoid structures of at least one hydroxy group on a six-membered aromatic ring
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
23.
Method for moderately increasing the proton conductivity of biological membranes with the aid of mitochondria-targeted delocalized cations
The invention relates to biology and medicine, in particular, can be used in medicine for preparation of a pharmaceutical composition for specific, self-regulating uncoupling of mitochondria. The invention may be useful in treatment of diseases and conditions associated with violation of cellular metabolism, in treatment of obesity including its pathological forms, as well as in treatment of diseases associated with increased formation of free radicals and reactive oxygen species. In addition, the invention may be used in biotechnology for stimulation of growth of yeast and microorganisms as well as for stimulation of development of tissues and organs of plant and animal origin.
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
24.
Use of mitochondrially-addressed compounds for preventing and treating cardiovascular diseases
The invention relates to pharmacology and medicine, in particular to a class of mitochondrially-addressed compounds which can be used in the pharmaceutical compositions of medicinal agents (preparations) for preventing and treating cardiovascular diseases and diseases and pathological conditions caused by disturbed blood circulation or oxygen supply to tissues and organs.
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
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 39/06 - Free radical scavengers or antioxidants
25.
Pharmaceutical and cosmetic compositions for accelerated healing of wounds and other surface damages
This invention relates to biology and medicine and in particular it can be used in medicine for preparation of pharmaceutical composition that can accelerate wound healing by means of directed transport of biologically active substances (bioactive compounds) to the mitochondria, using hydrogen electrochemical potential in mitochondria. Besides, this invention relates to a certain method of influencing on the organism by means of said directed transport of required biologically active substances.
A61Q 17/00 - Barrier preparationsPreparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
The invention relates to pharmacology, medicine and gerontology, in particular to a class of chemical structures (1) which can be used in compositions, in the form of geroprotectors, for extending the life time, decelerating, stopping or for reversing the process of the entirety of the organism's dysfunctions causing the mammal ageing and for preventing and treating particular senile diseases.
The invention relates to pharmacology, medicine and oncology, in particular, to a class of chemical compounds, the structure of which corresponds to formula (I) and which can be used in pharmaceutical compositions for preventing and treating an extended range of oncological diseases, including, in the form of an anti-tumoral preparation and a preparation which is used for combined therapy of oncological diseases.
A01N 31/08 - Oxygen or sulfur directly attached to an aromatic ring system
A01N 57/26 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds
A01N 27/00 - Biocides, pest repellants or attractants, or plant growth regulators containing hydrocarbons
A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
