Abstract

The present invention refers to a microemulsion, particularly suitable for ophthalmic applications such as treatment of dry eye syndrome, which comprises at least one oily component, an aqueous phase, at least one non-ionic surfactant, at least one polysaccharide, a salt or a derivative thereof, and at least one cross-linking agent. Moreover, the present invention relates to a process of manufacturing a microemulsion according to the invention, as well as its use in ophthalmic applications or as a carrier.

IPC Classes  ?

• A61K 9/107 - Emulsions
• A61P 27/04 - Artificial tearsIrrigation solutions
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

IPC Classes  ?

• C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
• C07B 49/00 - Grignard reactions
• C07B 43/08 - Formation or introduction of functional groups containing nitrogen of cyano groups
• C07B 43/04 - Formation or introduction of functional groups containing nitrogen of amino groups
• C07B 31/00 - Reduction in general
• C07B 37/12 - Diels-Alder reactions
• C07D 498/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
• A61P 25/36 - Opioid-abuse
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The present invention refers to a microemulsion, particularly suitable for ophthalmic applications such as treatment of dry eye syndrome, which comprises at least one oily component, an aqueous phase, at least one non-ionic surfactant, at least one polysaccharide, a salt or a derivative thereof, and at least one cross-linking agent. Moreover, the present invention relates to a process of manufacturing a microemulsion according to the invention, as well as its use in ophthalmic applications or as a carrier.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/107 - Emulsions
• A61K 47/02 - Inorganic compounds
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61P 27/04 - Artificial tearsIrrigation solutions

Abstract

The present invention refers to a microemulsion, particularly suitable for ophthalmic applications such as treatment of dry eye syndrome, which comprises at least one oily component, an aqueous phase, at least one non-ionic surfactant, at least one polysaccharide, a salt or a derivative thereof, and at least one cross-linking agent. Moreover, the present invention relates to a process of manufacturing a microemulsion according to the invention, as well as its use in ophthalmic applications or as a carrier.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/107 - Emulsions
• A61K 47/02 - Inorganic compounds
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61P 27/04 - Artificial tearsIrrigation solutions

Abstract

The present application refers to an electrochemically activated salt solution (EGAS), its production, and its use for treating infections.

IPC Classes  ?

• A61K 33/22 - Boron compounds
• A61K 33/20 - Elemental chlorineInorganic compounds releasing chlorine
• A61K 33/42 - PhosphorusCompounds thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions
• A61P 31/12 - Antivirals
• A61P 31/04 - Antibacterial agents
• A61P 27/02 - Ophthalmic agents
• C25B 1/26 - ChlorineCompounds thereof
• C25B 11/02 - ElectrodesManufacture thereof not otherwise provided for characterised by shape or form

Abstract

The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolicoxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

IPC Classes  ?

• C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms

Abstract

The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of the baine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

IPC Classes  ?

• C07D 498/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings

Abstract

The present invention relates to a new path to synthesize crystalline Tafamidis polymorphs starting from a Tafamidis acetic acid adduct. In addition, this invention relates to a process to synthesize Tafamidis (2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid * (2R,3R,4R,5S)-6-(methyl-amino)-hexane-1,2,3,4,5-pentol), new Tafamidis crystalline polymorphs, a pharmaceutical compositions comprising the new crystalline polymorphs and to the therapeutic use of such new polymorphs.

IPC Classes  ?

• C07D 263/57 - Aryl or substituted aryl radicals

Abstract

The present application refers to an electrochemically activated salt solution (EGAS), its production, and its use for treating infections.

IPC Classes  ?

• A61K 33/20 - Elemental chlorineInorganic compounds releasing chlorine
• A61K 9/08 - Solutions
• A61K 33/00 - Medicinal preparations containing inorganic active ingredients
• A61P 27/02 - Ophthalmic agents
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• C25B 1/26 - ChlorineCompounds thereof

Abstract

The present application refers to an electrochemically activated salt solution (EGAS), its production, and its use for treating infections.

IPC Classes  ?

• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 31/12 - Antivirals
• A61P 31/22 - Antivirals for DNA viruses for herpes viruses
• A61K 33/20 - Elemental chlorineInorganic compounds releasing chlorine

Abstract

RRRSS)-6-(methyl-amino)-hexane-1,2,3,4,5-pentol), new Tafamidis crystalline polymorphs, a pharmaceutical compositions comprising the new crystalline polymorphs and to the therapeutic use of such new polymorphs.

IPC Classes  ?

• C07D 263/57 - Aryl or substituted aryl radicals
• A61P 25/00 - Drugs for disorders of the nervous system
• A61K 31/423 - Oxazoles condensed with carbocyclic rings

Abstract

The present invention relates to a catalytic composition comprising at least 7 different elements selected from the group consisting of the elements defined by the intersection of the second to the sixth period and the first to the sixteenth group of the periodic table of the elements, whereby technetium is excluded, and a matrix component. A method for use of the catalytic composition is also provided.

IPC Classes  ?

• B01J 23/00 - Catalysts comprising metals or metal oxides or hydroxides, not provided for in group
• C01B 3/32 - Production of hydrogen or of gaseous mixtures containing hydrogen by reaction of gaseous or liquid organic compounds with gasifying agents, e.g. water, carbon dioxide, air
• C10G 2/00 - Production of liquid hydrocarbon mixtures of undefined composition from oxides of carbon

Goods & Services

Commercial consultancy and assistance before authorizing authorities. Transport; packaging and storage of merchandise. Treatment of materials. Scientific and technological services as well as research and design services relating thereto; scientific and technological consultancy and assistance before authorizing authorities, industrial analysis and research services; biological research services; chemical analysis; chemical research; chemistry services; quality control; research and development of new products for others. Medical services; veterinary services; hygienic and beauty care for human beings or animals; pharmacy advice, medical and pharmaceutical consultancy and assistance before authorizing authorities. Legal services and representation, intellectual property consultancy; intellectual property licensing.

Goods & Services

Custom synthesis and manufacturing of active pharmaceutical ingredients, intermediates thereof and finished dosage forms, especially for pharmaceutical use Commercial consultancy and assistance before authorizing authorities Transport of pharmaceutical products; Warehousing services, namely, packaging, storage and distribution of pharmaceutical products Scientific and technological services, namely, research and design in the field of pharmaceuticals and active pharmaceutical ingredients; scientific and technological consultancy in the field of pharmaceuticals, namely, rendering technical assistance to authorizing authorities to obtain related market authorization, industrial research and analysis in the field of pharmaceuticals and active pharmaceutical ingredients; biological research services; chemical analysis; chemical research, chemistry services, namely, synthesis and manufacturing of active pharmaceutical ingredients, intermediates thereof and finished dosage forms, for pharmaceutical research use; analysis and quality control for others of pharmaceuticals and their manufacturing process; research and development of new pharmaceutical products for others Medical services; veterinary services; hygienic and beauty care for human beings or animals; pharmacy advice, medical and pharmaceutical consultancy and assistance before authorizing authorities Legal services and representation, intellectual property consultancy; intellectual property licensing

Abstract

The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.

IPC Classes  ?

• C07C 401/00 - Irradiation products of cholesterol or its derivativesVitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
• C07C 317/18 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
• C07C 323/12 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated

Abstract

The present invention refers to a microemulsion formulation suitable for preventing assembly of amphiphilic drug molecules which may cause hypersensitivity reactions and other unwanted side effects.

IPC Classes  ?

• A61K 9/107 - Emulsions
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• 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 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

Abstract

The present invention refers to an oil-in-water emulsion for ophthalmic application comprising at least one prostaglandin as active agent and a surfactant component comprising a combination of at least two non-ionic surfactants. The emulsion is suitable for medical applications, particularly for the treatment of glaucoma, and has an increased chemical stability of the prostaglandin active agent so to allow long-term storage also at room temperature.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/107 - Emulsions
• C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins

Abstract

The present application refers to pharmaceutical preparations comprising an active ingredient and a carrier wherein the carrier comprises an aqueous electrochemically activated salt solution.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61L 2/03 - Electric current, e.g. electrolysis

Goods & Services

(1) Synthetic human pharmaceutical and veterinary preparations for the treatment of cancer, ophthalmic, cardiovascular, neurological [neurological disorders, namely degenerative neurological diseases of various etiology, brain or spine injury of various etiology], respiratory, digestive and inflammatory diseases [inflammatory diseases, namely inflammatory connective tissue disease, inflammatory skin diseases, inflammatory diseases of the eye]; synthetic adjuvants, namely recombinant proteins or vaccines for human and veterinary use; amino acids for medical purposes; synthetic surgical anaesthetics for human and veterinary use; synthetic analgesics; synthetic anthelmintics; synthetic antibiotics; synthetic biological preparations to produce generic medicines for human or veterinary use, specifically recombinant proteins or monoclonal antibodies; synthetic chemical preparations to produce generic medicines for human or veterinary use for the treatment of cancer, ophthalmic, cardiovascular, neurological [neurological disorders, namely degenerative neurological diseases of various etiology, brain or spine injury of various etiology], respiratory, digestive and inflammatory diseases [inflammatory diseases, namely inflammatory connective tissue disease, inflammatory skin diseases, inflammatory diseases of the eye]; synthetic chemical reagents to produce generic medicines for human or veterinary use; synthetic chemico-pharmaceutical preparations to produce generic medicines for human or veterinary use for the treatment of cancer, ophthalmic, cardiovascular, neurological [neurological disorders, namely degenerative neurological diseases of various etiology, brain or spine injury of various etiology], respiratory, digestive and inflammatory diseases [inflammatory diseases, namely inflammatory connective tissue disease, inflammatory skin diseases, inflammatory diseases of the eye]; synthetic ferments to produce generic medicines for human or veterinary use; synthetic hormones to produce generic medicines for human or veterinary use; synthetic medicinal infusions for human or veterinary use for the treatment of cancer, ophthalmic, cardiovascular, neurological [neurological disorders, namely degenerative neurological diseases of various etiology, brain or spine injury of various etiology], respiratory, digestive and inflammatory diseases [inflammatory diseases, namely inflammatory connective tissue disease, inflammatory skin diseases, inflammatory diseases of the eye]; synthetic medicines for dental purposes, namely topical and surgical anaesthetics; synthetic generic medicines for human or veterinary purposes for the treatment of cancer, ophthalmic, cardiovascular, neurological [neurological disorders, namely degenerative neurological diseases of various etiology, brain or spine injury of various etiology], respiratory, digestive and inflammatory diseases [inflammatory diseases, namely inflammatory connective tissue disease, inflammatory skin diseases, inflammatory diseases of the eye]; radiological contrast substances for medical purposes; steroids. (1) Scientific and technological services and research and design relating thereto in the field of chemico-pharmaceutical preparations; industrial analysis and research services in the field of chemico-pharmaceutical preparations; design and development of computer hardware and software; legal services; biological research services; chemical analysis; chemical research; intellectual property consultancy; licensing of intellectual property; quality control of human and veterinary pharmaceutical preparations; chemical and pharmaceutical research and development for others; veterinary services; pharmacy advice.

Abstract

The present invention refers to an oil-in-water emulsion for ophthalmic application comprising at least one prostaglandin as active agent and a surfactant component comprising a combination of at least two non-ionic surfactants. The emulsion is suitable for medical applications, particularly for the treatment of glaucoma, and has an increased chemical stability of the prostaglandin active agent so to allow long-term storage also at room temperature.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/557 - Eicosanoids, e.g. leukotrienes
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• 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

Abstract

The present invention refers to an oil-in-water emulsion for ophthalmic application comprising at least one prostaglandin as active agent and a surfactant component comprising a combination of at least two non-ionic surfactants. The emulsion is suitable for medical applications, particularly for the treatment of glaucoma, and has an increased chemical stability of the prostaglandin active agent so to allow long-term storage also at room temperature.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• 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 31/557 - Eicosanoids, e.g. leukotrienes
• 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

Goods & Services

Pharmaceutical and veterinary products; sanitary preparations for medical purposes; dietetic substances adapted for medical use; adjuvants for medical purposes; amino acids for medical purposes; anaesthetics; analgesics; vermifuges; antibiotics; barks for pharmaceutical purposes; biological preparations for medical purposes; chemical preparations for pharmaceutical purposes; chemical reagents for medical or veterinary purposes; chemical-pharmaceutical preparations; ferments for pharmaceutical purposes; hormones for medical purposes; medicinal infusions; medicines for dental purposes; medicines for human purposes; pharmaceutical preparations; pills for pharmaceutical purposes; radiological contrast substances for medical purposes; steroids. Transport; packaging and storage of goods. Treatment of materials. Scientific and technological services and related research and design services; industrial analysis and research services; design and development of computers and software; legal services; biological research; chemical analysis; chemical research; chemistry services; intellectual property consultancy; granting of intellectual property licenses; quality control; research and development of new products for third parties. Medical services; veterinary services; hygienic and beauty care for human beings or animals; pharmacy advice.

Goods & Services

(1) Scientific and technological services and research and design relating thereto in the field of chemico-pharmaceutical preparations; industrial analysis and research services in the field of chemico-pharmaceutical preparations; design and development of computer hardware and software; biological research services; chemical analysis; chemical research; quality control of human and veterinary pharmaceutical preparations; chemical and pharmaceutical research and development for others. (2) Veterinary services; pharmacy advice. (3) Legal services; intellectual property consultancy; licensing of intellectual property.