Abstract

The present invention provides complexes of a specialized pro-resolving mediator (SPM), or a salt, ester, or amide thereof, and a cyclodextrin (CD), wherein the SPM is a hydroxylated, polyunsaturated fatty acid derived from arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid, or docosapentaenoic acid, 20 or 22 carbon atoms in length, with 4, 5 or 6 conjugated double bonds arranged in diene, triene, or tetraene systems or combinations thereof; and related compositions and methods.

IPC Classes  ?

• A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit

Abstract

The present invention relates to compositions comprising resolvins and their use in methods of treating immune-mediated inflammatory disease.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/315 - Zinc compounds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to compositions comprising resolvins and their use in methods of treating cancer.

IPC Classes  ?

• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

The present invention provides complexes of a specialized pro-resolving mediator (SPM), or a salt, ester, or amide thereof, and a cyclodextrin (CD), wherein the SPM is a hydroxylated, polyunsaturated fatty acid derived from arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid, or docosapentaenoic acid, 20 or 22 carbon atoms in length, with 4, 5 or 6 conjugated double bonds arranged in diene, triene, or tetraene systems or combinations thereof; and related compositions and methods.

IPC Classes  ?

• A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
• A61K 31/00 - Medicinal preparations containing organic active ingredients
• 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

Abstract

The present invention relates to compositions comprising resolvins and their use in methods of treating cancer.

IPC Classes  ?

• A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated

Abstract

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both. Provided are pharmaceutical compositions adapted to deliver the compounds the lower gastrointestinal tract and methods of using same as monotherapy in the treatment of inflammatory diseases or disorders of the lower gastrointestinal tract, and in combination therapy with 5-aminosalicylate.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/62 - 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
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

Abstract

The present invention relates to compounds of Formulas I-IV and compositions comprising same, including pharmaceutical compositions. The compounds of Formulas I-IV represent new salt forms of specialized pro-resolving mediators (“SPMs”) which include lipoxins, resolvins, protectins, and their aspirin-triggered counterparts. The SPM salts described here contain at least one or two SPM molecules ionically bound to at least one basic function that is provided by a scaffold as described in Formulas I-IV. Also provided are methods for pharmaceutical and non-pharmaceutical uses of such compounds and compositions describing same.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/62 - 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
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

Abstract

The present invention relates to compounds of Formulas I- IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/62 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated

Abstract

The present invention relates to compounds of Formulas I- IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/12 - Antidiarrhoeals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/62 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof

Abstract

The present invention relates to compounds which are salts of specialized pro-resolving mediators (referred to herein as “SPMs”) which include lipoxins, resolvins, protectins, and their aspirin-triggered counterparts. The SPM salts described here contain at least one or two SPM molecules ionically bound to at least one basic function that is provided by a scaffold moiety as described herein, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• 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
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• 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]
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to compounds of Formula IV, compositions comprising same, and their use in therapy 2 are as defined herein.

IPC Classes  ?

• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/03 - Peptides having up to 20 amino acids in an undefined or only partially defined sequenceDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 47/62 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
• A61K 47/54 - 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 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• A61P 1/12 - Antidiarrhoeals
• 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]
• C07C 229/26 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups

Abstract

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• C07C 229/76 - Metal complexes of amino carboxylic acids
• A61K 31/191 - Acyclic acids having two or more hydroxy groups, e.g. gluconic acid
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• 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]
• C07C 59/42 - Unsaturated compounds containing hydroxy or O-metal groups

Abstract

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/62 - 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
• 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]

Abstract

The present invention provides compounds of Formula I and Formula II, and related compositions and methods.

IPC Classes  ?

• C07C 229/76 - Metal complexes of amino carboxylic acids
• C07K 5/068 - Dipeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

The present invention provides compounds of Formula I and related compositions and methods. Formula (I). R1 and R2each refer to a branched or unbranched carbon chain of from 1 to 20 carbons having at least one basic function; R1 and R2 are the same or different; X1 and X2 are independently selected from H and -CO-Z, where Z is a peptide moiety incorporating from 1 to 5 amino acids, or a pharmaceutically acceptable salt thereof; X1 and X2 are the same or different; M is a divalent metal cation selected from magnesium (Mg2 +), calcium (Ca2+), and zinc (Zn2+); A and B are each a molecule having at least one acidic function, either A or B, but not both, may be absent, and when both A and B are present, A and B may be the same or different. In a particular embodiment, at least one of "A" and "B" or both are fatty acids. A representative example of the application is the compound Magnesium Lysinate bis docosapentaenoic acid shown hereafter, Formula; The complexes of the application are intended for pharmaceutical compositions or as food additive, notably to treat conditions responsive to treatment with polyunsaturated fatty acids.

IPC Classes  ?

• C07F 3/02 - Magnesium compounds
• A61K 31/7135 - Compounds containing heavy metals
• A61K 33/00 - Medicinal preparations containing inorganic active ingredients
• C07F 3/04 - Calcium compounds
• C07F 3/06 - Zinc compounds

Abstract

The present invention relates to compounds of Formula I, compositions containing same, and methods of use.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C07C 57/03 - Monocarboxylic acids
• C11C 3/00 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis

Abstract

Provided herein are tri-salt compounds comprising a compound having two acidic functional groups and one basic functional groups (e.g., aspartate or glutamate), metformin, and polyunsaturated fatty acids, such as eicosapentaenoate or docosahexaenoate. The salts can be used in the treatment of diabetes, diabetes with concomitant dyslipidemia (e.g. , high triglycerides) and diabetes exacerbated cardiovascular complications, such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke. The compounds of this invention are also useful in treating obesity.

IPC Classes  ?

• C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
• C07C 279/02 - GuanidineSalts, complexes or addition compounds thereof
• C07C 277/08 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
• A61K 31/205 - Amine addition salts of organic acidsInner quaternary ammonium salts, e.g. betaine, carnitine
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/06 - Antiarrhythmics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Disclosed herein are highly soluble and bioavailable ω-3 fatty acid salts. These fatty acid salts have high bioavailability when administered orally. They are also used for relatively high concentration intravenous dosage forms that can be used for the treatment of atrial defibrillation. These fatty acid salts can also be used to supplement food, drink and nutraceuticals with ω-3 polyunsaturated fatty acids.

IPC Classes  ?

• A61K 9/08 - Solutions
• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• 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
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/06 - Antiarrhythmics
• A23L 1/00 - Foods or foodstuffs; Their preparation or treatment (preservation thereof in general A23L 3/00)
• A23L 1/30 - containing additives (A23L 1/308 takes precedence);;

Abstract

The present invention is directed to a combination therapy comprising metformin eicosapentaenoate or metformin docosahexaenoate, or a mixture thereof, and an antihyperglycemic agent or an antihyperlipidemic agent, or a pharmaceutically-acceptable salt or prodrug thereof, or a pharmaceutically-acceptable salt of said prodrug. The invention further relates to methods of treating a metabolic disorder selected from the group consisting of type 2 diabetes (T2D), pre-diabetes, obesity, metabolic syndrome, hypertrilipidemia and T2D complications such as neuropathy, nephropathy, retinopathy, cataracts and cardiovascular complications, including cardiac arrhythmia, myocardial infarction, stroke, and cardiomyopathy in diabetic patients.

IPC Classes  ?

• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• C07C 279/22 - Y being a hydrogen or a carbon atom, e.g. benzoylguanidines
• C07C 57/03 - Monocarboxylic acids
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/06 - Antihyperlipidemics
• A61P 9/06 - Antiarrhythmics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Provided herein are diamine salts of eicosapentaenoic acid and docosahexaenoic acid, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and the uses of such compounds as agents for treating dyslipidemia, cardiovascular diseases such as cardiac arrhythmia, cardiac ischemia, myocardial infarction, cardiomyopathy, and stroke and obesity.

IPC Classes  ?

• C07C 215/10 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
• C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
• C07C 57/03 - Monocarboxylic acids
• C07C 215/40 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton with quaternised nitrogen atoms bound to carbon atoms of the carbon skeleton
• C07C 211/10 - Diaminoethanes
• C07C 211/62 - Quaternary ammonium compounds
• C07C 209/00 - Preparation of compounds containing amino groups bound to a carbon skeleton
• C07D 295/02 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
• C07D 295/023 - PreparationSeparationStabilisationUse of additives
• A61K 31/19 - Carboxylic acids, e.g. valproic acid
• A61K 31/205 - Amine addition salts of organic acidsInner quaternary ammonium salts, e.g. betaine, carnitine
• 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 31/495 - 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
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/06 - Antiarrhythmics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
• C11C 3/00 - Fats, oils or fatty acids obtained by chemical modification of fats, oils or fatty acids, e.g. by ozonolysis
• C11C 1/00 - Preparation of fatty acids from fats, fatty oils, or waxesRefining the fatty acids

Goods & Services

Development of pharmaceutical preparations and medicines

Abstract

A composition which includes a salt of metformin and the use of the composition for treatment of or use in prediabetes, diabetes, lowering triglycerides and/or other conditions in mammals.

IPC Classes  ?

• A01N 37/52 - 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 containing groups, e.g. carboxylic acid amidines
• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)