In one aspect, a process for the preparation of vilanterol ((R)-4-(2-((6-(2-((2,6-dichlorobenzyl)oxy)ethoxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol; Compound VI) or a pharmaceutically acceptable salt thereof, comprises the following steps wherein steps A to B(i) are carried out as a one-pot or telescoped process: A) coupling the compound (5R)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3-oxazolidin-2-one (Compound II) with 2-[2-(6-bromohexyloxy)-ethoxymethyl]-1,3-dichlorobenzene (Compound III) in the presence of a base, in an organic solvent; and B) (i) adding a base to the reaction mixture formed in step A to remove the oxazolidinone protecting group, to form Compound V; (ii) converting Compound V to vilanterol (compound VI) or a pharmaceutically acceptable salt thereof. In another aspect, a process for the preparation of vilanterol ((R)-4-(2-((6-(2-((2,6-dichlorobenzyl)oxy)ethoxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol; Compound VI) or a pharmaceutically acceptable salt thereof, comprises coupling the compound (5R)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3-oxazolidin-2-one (Compound II) with 2-[2-(6-bromohexyloxy)-ethoxymethyl]-1,3-dichlorobenzene (Compound III) and converting the product formed to vilanterol or a pharmaceutically acceptable salt thereof, wherein during the process either no, or only one, intermediate compound is isolated.
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 213/02 - 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 involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
The present invention relates to a method for drying the residual solvent content of a pharmaceutical product or powder. The present disclosure describes a method that allows fast drying of fine and cohesive pharmaceutical powders enabling it uses for batch, semi-continuous and continuous operation.
F26B 3/06 - Drying solid materials or objects by processes involving the application of heat by convection, i.e. heat being conveyed from a heat source to the materials or objects to be dried by a gas or vapour, e.g. air the gas or vapour flowing through the materials or objects to be dried
F26B 9/06 - Machines or apparatus for drying solid materials or objects at rest or with only local agitationDomestic airing cupboards in stationary drums or chambers
A method for synthesizing 9-aminomethyl tetracycline compounds is disclosed. The method comprises a) reacting minocycline and an hydroxymethylamide derivative to form a 2,9-(methylamide-substituted) minocycline and a 2-(methylamidesubstituted) minocycline; b) reacting the 2,9-(methylamide-substituted) minocycline from step a) and an amine or diamine to form a 9-aminomethyl tetracycline intermediate; and c) reacting the 9-aminomethyl tetracycline intermediate from step b) and an aldehyde in the presence of a reducing agent to form a 9-aminomethyl tetracycline compound; or d) reacting the 9-aminomethyl tetracycline intermediate from step b) and an alkyl halide or an alkyl reagent to form a 9-aminomethyl tetracycline compound. Step b) may be operated in the absence of a hydrogenation reaction. The method may be a semi continuous or continuous flow process.
C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
The invention provides a process to reduce the particle size of ivermectin wherein the process comprises incorporating ivermectin particles in a wet or liquid medium and subjecting the medium comprising the particles to mixing in a high shear mixer.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC50 in the low nanomolar range.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/66 - 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 the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
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
The present invention describes a dry powder inhaler pharmaceutical composition comprising one or more active pharmaceutical ingredients (API) coated with one or more force control agents (FCA) with optimized aerodynamic performance by micronizing crystalline API particles to the respirable range and coating the particles with a force control agent. The present invention also id pharmaceutical composition, and its use in medicine.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
7.
DRY POWDER INHALER PHARMACEUTICAL COMPOSITION OF COATED CRYSTALLINE DRY POWDER FOR INHALATION
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
8.
CRYSTALLINE PHARMACEUTICAL COMPOSITION FOR INHALATION COMPRISING SUGAR AND LIPID COMPOSITE PARTICLES AND PROCESS FOR MANUFACTURE
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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
9.
CRYSTALLINE PHARMACEUTICAL COMPOSITION FOR INHALATION COMPRISING SUGAR AND LIPID COMPOSITE PARTICLES AND PROCESS FOR MANUFACTURE
The present invention describes a pharmaceutical composition comprising composite particles with a controlled aerodynamic particle size distribution, wherein the composite particles comprise one or more active pharmaceutical ingredients (API), at least one sugar and at least one lipid. A process for manufacturing the pharmaceutical composition comprises the steps of: a. Blending API and one or more excipients comprising at least one sugar or at least one lipid, or both at least one sugar and at least one lipid, into a homogeneous powder; b. Reducing the particle size distribution of the blend. The micronized pharmaceutical composition allows for the delivery of crystalline stable API with better aerodynamic properties than the micronized API alone, as well asimproved downstream processing and stability properties.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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
10.
A METHOD AND DEVICE FOR DETERMINING THICKNESS AND SOLID FRACTION OF A PHARMACEUTICAL TABLET USING NON-INVASIVE PROCESS ELECTRICAL TOMOGRAPHY
The present invention relates to a device for obtaining capacitance measurements for use in determining the relative permittivity and thickness of a pharmaceutical tablet. The invention further relates to a method of determining the relative permittivity and thickness of a pharmaceutical tablet using one or more capacitance sensors. The device and method may be part of a pharmaceutical tableting unit or a pharmaceutical tableting method.
G01B 7/04 - Measuring arrangements characterised by the use of electric or magnetic techniques for measuring length, width, or thickness specially adapted for measuring length or width of objects while moving
G01B 7/06 - Measuring arrangements characterised by the use of electric or magnetic techniques for measuring length, width, or thickness for measuring thickness
11.
INHALATION COMPOSITE AND CARRIER BASED FORMULATION COMBINATION
An inhalable pharmaceutical composition comprises: (i) Spray dried cohesive composite active particles, each composite active particle comprising an active pharmaceutical ingredient (API) material and an excipient; and, (ii) carrier particles Wherein the composite active particles and the carrier particles are blended in a physical mixture. A process of preparing the pharmaceutical composition comprises the steps of: i) providing a solution of an active pharmaceutical ingredient (API) material and a solution of an excipient, which may be separate solutions or a combined solution, and spray drying to provide cohesive composite active particles, wherein each composite active particle comprises an active pharmaceutical ingredient (API) material and an excipient; ii) blending the spray dried cohesive composite active particles with carrier particles to form a physical mixture. The composition may be used in a dry powder inhaler (DPI), particularly a reservoir DPI device.
1. In one aspect, a process for the preparation of vilanterol ((R)-4-(2-((6-(2-((2,6- dichlorobenzyl)oxy)ethoxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol; Compound VI) or a pharmaceutically acceptable salt thereof, comprises the following steps wherein steps A to B(i) are carried out as a one-pot or telescoped process: A) coupling the compound (5R)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3- oxazolidin-2-one (Compound II) with 2-[2-(6-bromohexyloxy)-ethoxymethyl]-1,3- dichlorobenzene (Compound III) in the presence of a base, in an organic solvent; and B) (i) adding a base to the reaction mixture formed in step A to remove the oxazolidinone protecting group, to form Compound V; (ii) converting Compound V to vilanterol (compound VI) or a pharmaceutically acceptable salt thereof. In another aspect, a process for the preparation of vilanterol ((R)-4-(2-((6-(2-((2,6-dichlorobenzyl)oxy)ethoxy)hexyl)amino)-1-hydroxyethyl)-2-(hydroxymethyl)phenol; Compound VI) or a pharmaceutically acceptable salt thereof, comprises coupling the compound (5R)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3- oxazolidin-2-one (Compound II) with 2-[2-(6-bromohexyloxy)-ethoxymethyl]-1,3- dichlorobenzene (Compound III) and converting the product formed to vilanterol or a pharmaceutically acceptable salt thereof, wherein during the process either no, or only one, intermediate compound is isolated.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
C07D 319/08 - 1,3-DioxanesHydrogenated 1,3-dioxanes condensed with carbocyclic rings or ring systems
The invention provides a process to reduce the particle size of ivermectin wherein the process comprises incorporating ivermectin particles in a wet or liquid medium and subjecting the medium comprising the particles to mixing in a high shear mixer.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The invention provides a process to reduce the particle size of ivermectin wherein the process comprises incorporating ivermectin particles in a wet or liquid medium and subjecting the medium comprising the particles to mixing in a high shear mixer.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
Electromechanical machines for chemical industry, namely, chemical particle spray drying apparatus, for drying pharmaceutical preparations and chemical particles used in the manufacture of pharmaceuticals Spray drying apparatus for chemical particles; apparatus for drying of particulates for use in the manufacture of pharmaceuticals
18.
METHOD FOR SYNTHESIZING 9-AMINOMETHYL TETRACYCLINE COMPOUNDS
A method for synthesizing 9-aminomethyl tetracycline compounds is disclosed. The method comprises a) reacting minocycline and an hydroxymethylamide derivative to form a 2,9-(methylamide-substituted) minocycline and a 2-(methylamide-substituted) minocycline; b) reacting the 2,9-(methylamide-substituted) minocycline from step a) and an amine or diamine to form a 9-aminomethyl tetracycline intermediate; and c) reacting the 9-aminomethyl tetracycline intermediate from step b) and an aldehyde in the presence of a reducing agent to form a 9-aminomethyl tetracycline compound; or d) reacting the 9-aminomethyl tetracycline intermediate from step b) and an alkyl halide or an alkyl reagent to form a 9-aminomethyl tetracycline compound. Step b) may be operated in the absence of an hydrogenation reaction. The method may be a semi continuous or continuous flow process. Optionally, in a semi continuous flow process, two of steps a), b) and c) or d) may be carried without the use of batch reactors and without the need to isolate intermediate products between the reaction steps, for example steps b) and c) or steps b) and d) may operate in a continuous manner with the 9-aminomethyl tetracycline intermediate formed in step b) being used directly in step c) or d). The 9-aminomethyl tetracycline compound formed in step c) or d) may be omadacycline.
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
19.
METHOD FOR SYNTHESIZING 9-AMINOMETHYL TETRACYCLINE COMPOUNDS
A method for synthesizing 9-aminomethyl tetracycline compounds is disclosed. The method comprises a) reacting minocycline and an hydroxymethylamide derivative to form a 2,9-(methylamide-substituted) minocycline and a 2-(methylamide-substituted) minocycline; b) reacting the 2,9-(methylamide-substituted) minocycline from step a) and an amine or diamine to form a 9-aminomethyl tetracycline intermediate; and c) reacting the 9-aminomethyl tetracycline intermediate from step b) and an aldehyde in the presence of a reducing agent to form a 9-aminomethyl tetracycline compound; or d) reacting the 9-aminomethyl tetracycline intermediate from step b) and an alkyl halide or an alkyl reagent to form a 9-aminomethyl tetracycline compound. Step b) may be operated in the absence of an hydrogenation reaction. The method may be a semi continuous or continuous flow process. Optionally, in a semi continuous flow process, two of steps a), b) and c) or d) may be carried without the use of batch reactors and without the need to isolate intermediate products between the reaction steps, for example steps b) and c) or steps b) and d) may operate in a continuous manner with the 9-aminomethyl tetracycline intermediate formed in step b) being used directly in step c) or d). The 9-aminomethyl tetracycline compound formed in step c) or d) may be omadacycline.
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
The present invention contemplates the use of inhaled ivermectin for use in various viruses and parasitic infections (treatment and/or prophylaxis) that are present or manifest in the lungs or respiratory tract. Exemplary dosing, formulations, devices, and processing techniques are also disclosed herein.
The present invention relates to a novel process for the preparation of anticholinergic agents/drugs, such as umeclidinium bromide, tiotropium bromide, glycopyrronium bromide, aclidinium bromide, ipratropium bromide (V) in continuous flow mode in the presence of one or more polar protic solvents. The anticholinergic drugs are in a form suitable for use in inhalation in the treatment of respiratory diseases such as asthma or chronic obstructive pulmonary disease (COPD).
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
42 - Scientific, technological and industrial services, research and design
Goods & Services
Development of pharmaceutical products and drug products;
research on pharmaceutical products and drug products;
research and development of processes for the pharmaceutical
industry; technological research and pharmaceutical testing
aimed to optimize processes for the pharmaceutical industry;
research and development services for the pharmaceutical
industry.
The present invention contemplates the use of inhaled ivermectin for use in various viruses and parasitic infections (treatment and/or prophylaxis) that are present or manifest in the lungs or respiratory tract. Exemplary dosing, formulations, devices, and processing techniques are also disclosed herein.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 9/00 - Medicinal preparations characterised by special physical form
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 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
The present invention relates to a method for drying the residual solvent content of a pharmaceutical product or powder. The present disclosure describes a method that allows fast drying of fine and cohesive pharmaceutical powders enabling it uses for batch, semi-continuous and continuous operation.
F26B 3/06 - Drying solid materials or objects by processes involving the application of heat by convection, i.e. heat being conveyed from a heat source to the materials or objects to be dried by a gas or vapour, e.g. air the gas or vapour flowing through the materials or objects to be dried
F26B 9/06 - Machines or apparatus for drying solid materials or objects at rest or with only local agitationDomestic airing cupboards in stationary drums or chambers
The present invention relates to a method for drying the residual solvent content of a pharmaceutical product or powder. The present disclosure describes a method that allows fast drying of fine and cohesive pharmaceutical powders enabling it uses for batch, semi-continuous and continuous operation.
F26B 3/06 - Drying solid materials or objects by processes involving the application of heat by convection, i.e. heat being conveyed from a heat source to the materials or objects to be dried by a gas or vapour, e.g. air the gas or vapour flowing through the materials or objects to be dried
The invention provides methods, compositions, and kits containing a pharmaceutical composition, for treating meibomian gland dysfunction, dry eye disease, and related disorders.
42 - Scientific, technological and industrial services, research and design
Goods & Services
Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of processes for the pharmaceutical industry; technological research and pharmaceutical testing aimed to optimize processes for the pharmaceutical industry; research and development services for the pharmaceutical industry
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of processes for the pharmaceutical industry; technological research and pharmaceutical testing aimed to optimize processes for the pharmaceutical industry; research and development services for the pharmaceutical industry.
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 9/00 - Medicinal preparations characterised by special physical form
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
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical ingredients; compositions for medical and
veterinarian use; medical diagnostic compositions; chemical
products for pharmaceutical use. Development of pharmaceutical products and drug products;
research on pharmaceutical products and drug products;
research and development of processes for the pharmaceutical
industry; optimization of processes for the pharmaceutical
industry (term considered too vague by the International
Bureau - Rule 13 (2) (b) of the Regulations); research and
development services for the pharmaceutical industry.
32.
Amorphous Form of Chelating Agents and Process for Preparing them
An amorphous form of a chelating agent is provided, in particular wherein the chelating agent comprises ethylenediaminetetraacetic acid/edetic acid (EDTA), diethylenetriaminepentaacetic acid/pentetic acid (DTPA), nitrilotriacetic acid (NTA), amino tris(methylenephosphonic acid) (ATMP), ethylenediamine tetramethylene phosphonic acid (EDTMP), 1-hydroxyethane 1,1-diphosphonic acid (HEDP), ethylenediaminedisuccinic acid (EDDS), iminodisuccinic acid (IDS), hydroxamic acid, oxalic acid, galactaric acid, metaphosphoric acid, or phytic acid, or a salt of any one or more of the above acids, or a mixture of two or more of any of the above acids or salts thereof.
An amorphous form of a chelating agent is provided, in particular wherein the chelating agent comprises ethylenediaminetetraacetic acid/edetic acid (EDTA), diethylenetriaminepentaacetic acid/pentetic acid (DTPA), nitrilotriacetic acid (NTA), amino tris(methylenephosphonic acid) (ATMP), ethylenediamine tetramethylene phosphonic acid (EDTMP), 1-hydroxyethane 1,1-diphosphonic acid (HEDP), ethylenediaminedisuccinic acid (EDDS), iminodisuccinic acid (IDS), hydroxamic acid, oxalic acid, galactaric acid, metaphosphoric acid, or phytic acid, or a salt of any one or more of the above acids, or a mixture of two or more of any of the above acids or salts thereof.
A process for preparing an amorphous form of a chelating agent comprises the steps of:
a) Dissolving the chelating agent in a suitable solvent;
b) Optionally purifying the solution;
c) Isolating an amorphous form of the chelating agent;
d) Optionally post drying or conditioning the amorphous form of the chelating agent.
C07C 229/16 - 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 only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
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 invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.
The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.
The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.
42 - Scientific, technological and industrial services, research and design
Goods & Services
Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of processes for the pharmaceutical industry; optimization of processes for the pharmaceutical industry; research and development services for the pharmaceutical industry.
A ligand drug conjugate comprising a) a targeting ligand; b) a cleavable bridge; and a bromodomain and extraterminal (BET) inhibitor is provided. The targeting ligand may comprise a cancer targeting ligand. The BET inhibitor may comprise I-BET762, (+)-JQ1, MS417, OXT015, (2), RVX-208, (3), OXFBD02, OXFBD03, I-BET151, (4), PFI-1, I-BET726, MS436, XD14 or a modified BET inhibitor. Modified BET inhibitors are also provided, including RT48 ((S) -2- (6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-4-yl)-1-(4-(dimethylamino) piperidin-1-yl) ethan-1-one) and RT53 ((S) -2- (6- (4-chlorophenyl) -8-methoxy-1-methyl-4H-benzo[f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-4-yl) -N-(4- (4- (dimethylamino) piperidin-1-yl) phenyl) acetamide). A pro-drug of a BET inhibitor is also provided. A method of preparing a ligand drug conjugate according to the invention is also provided. The method comprises i) functionalising a BET inhibitor with a tertiary amine to form a modified BET inhibitor according to the invention; ii) bonding the modified BET inhibitor formed in step i) to a cleavable bridge; and iii) bonding the cleavable bridge bound to the modified BET inhibitor formed in step ii) to a targeting ligand. A ligand drug conjugate according to the invention for use as a medicament is also provided.
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
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active pharmaceutical ingredients in the nature of pharmaceutical preparations, which are used for the prevention and treatment of disorders of the skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems of humans or animals; compositions for medical and veterinarian use, namely, chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals; medical diagnostic compositions, namely medical diagnostic reagents; chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of new products in the pharmaceutical industry; Consulting services in the field of design and development of engineering processes for the pharmaceutical industry; research in the field of optimizing of manufacturing processes for the pharmaceutical industry
42.
Spray drying process with continuous preparation of spray solution
The present invention discloses a spray drying process characterized by continuous preparation and immediate spray drying of a solution comprising at least one active pharmaceutical ingredient and/or at least one excipient, and at least one solvent. The said active pharmaceutical ingredient(s) and solvent(s) are combined, alone or along with one or more excipients to form a first suspension. Said suspension is continuously fed to an intensifier pump that pushes said suspension through at least one micro-reaction chamber and/or at least one micro-channel where the suspension's solid(s) component(s) is(are) dissolved into said solvent(s) by means of high energy mixing I forced contact at micro, nano and molecular level to form a solution stream. The said solution stream is then immediately and continuously fed to the spray dryer through at least one atomization nozzle, drying said atomized stream to obtain solid particles and collecting said solid particles. Single component particles or multi-component particles, particulate amorphous solid dispersion and pharmaceutical compositions are also disclosed. The present invention also discloses amorphous solid dispersions obtained by the method of the invention as well as pharmaceutical compositions containing the same.
Amorphous ivermectin is provided, suitably in isolated solid form, and is suitably free of any additives or a support matrix, such as a solid dispersion. Also provided is a pharmaceutical formulation, for animal including human or veterinary use, comprising the amorphous ivermectin of the invention, and a pharmaceutically-acceptable carrier therefor. Also provided is a medical device incorporating amorphous ivermectin according to the invention, or a medical device incorporating a pharmaceutical formulation according to the invention described herein. A method of preparing amorphous ivermectin comprises the steps of preparing a solution of ivermectin in at least one solvent; removing the solvent by feeding the solution to a spray dryer and collecting particles of ivermectin. Amorphous ivermectin as disclosed herein may be used as a medicament, in particular to treat conditions such as a medical condition caused by internal nematode infections including but not limited to onchocerciasis (river blindness), filariasis (elephantiasis), strongyloidiasis or demodicosis.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention relates to a novel process for the preparation of anticholinergic agents/drugs, such as umeclidinium bromide, tiotropium bromide, glycopyrronium bromide, aclidinium bromide, ipratropium bromide (V) in continuous flow mode in the presence of one or more polar protic solvents. The anticholinergic drugs are in a form suitable for use in inhalation in the treatment of respiratory diseases such as asthma or chronic obstructive pulmonary disease (COPD).
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
The present invention relates to a novel process for the preparation of anticholinergic agents/drugs, such as umeclidinium bromide, tiotropium bromide, glycopyrronium bromide, aclidinium bromide, ipratropium bromide (V) in continuous flow mode in the presence of one or more polar protic solvents. The anticholinergic drugs are in a form suitable for use in inhalation in the treatment of respiratory diseases such as asthma or chronic obstructive pulmonary disease (COPD).
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical Ingredients; Compositions for medical and veterinarian use; medical diagnostic compositions; Chemical products for pharmaceutical use. Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; Research and development of processes for the pharmaceutical industry; optimization of processes for the pharmaceutical industry; Research and development services for the pharmaceutical industry.
48.
Process for the preparation of umeclidinium bromide
The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of
pharmaceuticals. Compositions for medical and veterinarian use; medical
diagnostic compositions; chemical products for
pharmaceutical use; chemical preparations for the
prevention, diagnosis, treatment or improvement of
conditions and disorders; pharmaceutical ingredients. Development of pharmaceutical products and drug products;
research on pharmaceutical products and drug products;
research and development of manufacturing processes for the
pharmaceutical industry; optimization of processes for the
pharmaceutical industry; research and development services
for the pharmaceutical industry; research and development
services for medical purposes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of
pharmaceuticals. Compositions for medical and veterinarian use; medical
diagnostic compositions; chemical products for
pharmaceutical use; chemical preparations for the
prevention, diagnosis, treatment or improvement of
conditions and disorders; pharmaceutical ingredients. Development of pharmaceutical products and drug products;
research on pharmaceutical products and drug products;
research and development of manufacturing processes for the
pharmaceutical industry; optimization of processes for the
pharmaceutical industry; research and development services
for the pharmaceutical industry; research and development
services for medical purposes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of pharmaceuticals for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Compositions for medical and veterinarian use, namely, chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals; diagnostic preparations for medical purposes; chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of new products in the pharmaceutical industry; consulting services in the field of design and development of engineering processes for the pharmaceutical industry; research and development services in the pharmaceutical field; research and development services in the field of pharmaceuticals, chemical preparations, vaccines, medicines, antibodies, new products in the medical field
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Active chemical ingredients for use in the manufacture of pharmaceuticals.
(2) Compositions for medical and veterinarian use, namely, anti-inflammatory compositions, antiallergic compositions, medicinal compositions for use in oncology, tumor suppressing compositions, antibacterials, antidotes to counteract poisons, antibiotics, medicinal compositions for use in oncology, anti-cancer compositions, antiseptic compositions, cardiovascular treatment compositions, compositions for the diagnosis and treatment of disorders relating to sexual reproduction and fertility, pain relief compositions, respiratory treatment compositions, pulmonary treatment compositions; medical diagnostic compositions, namely, diagnostic reagents for veterinary purposes, diagnostic reagents for medical purposes, diagnostic reagents for medical diagnostic use, clinical diagnostic reagents, diagnostic chemical reagents for medical purposes, diagnostic preparations for clinical laboratory use, diagnostic preparations for medical laboratory use; chemical products for pharmaceutical use, namely, diagnostic chemical reagents for medical purposes, anti-inflammatory preparations, antiallergic medicines, medicinal preparations for use in oncology, tumor suppressing agents, antibacterials, antidotes to counteract poisons, antibiotics, medicinal preparations for use in oncology, anti-cancer preparations, antiseptic preparations, cardiovascular treatment preparations, preparations for the diagnosis and treatment of disorders relating to sexual reproduction and fertility, pain relief preparations, diagnostic biomarkers for use in assessment of chemical respiratory sensitizers for medical use, respiratory treatment preparations, pulmonary treatment preparations; chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, diagnostic chemical reagents for medical purposes, anti-inflammatory preparations, antiallergic medicines, medicinal preparations for use in oncology, tumor suppressing agents, antibacterials, antidotes to counteract poisons, antibiotics, medicinal preparations for use in oncology, anti-cancer preparations, antiseptic preparations, cardiovascular treatment preparations, preparations for the diagnosis and treatment of disorders relating to sexual reproduction and fertility, pain relief preparations, respiratory treatment preparations, pulmonary treatment preparations. (1) Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of manufacturing processes for the pharmaceutical industry; technological research and pharmaceutical testing aimed to optimise processes for the pharmaceutical industry; research and product development services for medical purposes; research and development of new products for others for medical purposes; research and development of pharmaceutical preparations and medicines for medical purposes; pharmaceutical research and development services for medical purposes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of pharmaceuticals for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Compositions for medical and veterinarian use, namely, chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals; diagnostic preparations for medical purposes; chemical products for pharmaceutical use, namely, chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders, all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals; pharmaceutical active ingredients, namely, sold as a component ingredient of pharmaceutical preparations, and pharmaceutical preparations and compounds, all of the foregoing for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders; all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; research and development of new products in the pharmaceutical industry; Consulting services in the field of design and development of engineering processes for the pharmaceutical industry; research and development services in the pharmaceutical field; research and development services in the field of pharmaceuticals, chemical preparations, vaccines, medicines, antibodies, new products in the medical field
54.
Amorphous form of vilanterol trifenatate and processes for the preparation thereof
The present invention relates to an amorphous form of vilanterol trifenatate, processes for its preparation and its use in pharmaceutical formulations for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the invention relates to an amorphous form of vilanterol trifenatate, characterized by the X-ray powder diffraction (XRPD) pattern, obtained using copper K-alpha1 radiation.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 215/60 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
55.
Crystalline forms of vilanterol trifenatate and processes for their preparation
The present invention relates to new crystalline forms of vilanterol trifenatate, processes for their preparation, and their use in a pharmaceutical composition for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the present invention relates to a crystalline form of vilanterol trifenatate characterised in that the form has an XRPD pattern as defined herein having characteristic diffraction angles (2-theta or 20 (°)) falling within or at each end of one or more of the following ranges: (a) 3 to 5°, such as 3.8 to 4.4°; and/or (b) 7 to 9.9°, such as 7 to 8.5°; and/or (c) 12 to 13.3°, such as 12 to 13.3′; and/or (d) 16.4 to 17.3°, such as 16.4 to 17.3′; and/or (e) 26.8 to 28.3°, such as 26.8 to 28.3°.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 215/60 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
56.
AMORPHOUS FORM OF CHELATING AGENTS AND PROCESS FOR PREPARING THEM
An amorphous form of a chelating agent is provided, in particular wherein the chelating agent comprises ethylenediaminetetraacetic acid/edetic acid (EDTA), diethylenetriaminepentaacetic acid/pentetic acid (DTPA), nitrilotriacetic acid (NTA), amino tris(methylenephosphonic acid) (ATMP), ethylenediamine tetramethylene phosphonic acid (EDTMP), 1-hydroxyethane 1,1-diphosphonic acid (HEDP), ethylenediaminedisuccinic acid (EDDS), iminodisuccinic acid (IDS), hydroxamic acid, oxalic acid, galactaric acid, metaphosphoric acid, or phytic acid, or a salt of any one or more of the above acids, or a mixture of two or more of any of the above acids or salts thereof. A process for preparing an amorphous form of a chelating agent comprises the steps of: a) Dissolving the chelating agent in a suitable solvent; b) Optionally purifying the solution; c) Isolating an amorphous form of the chelating agent; d) Optionally post drying or conditioning the amorphous form of the chelating agent.
C07C 229/16 - 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 only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
C07C 229/76 - Metal complexes of amino carboxylic acids
57.
Boronated multifunctional targeting drug conjugates, their uses and methods for their preparation
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/66 - 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 the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of pharmaceuticals; pharmaceutical Ingredients. Compositions for medical and veterinarian use; medical diagnostic compositions; Chemical products for pharmaceutical use; Chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders. Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; Research and development of manufacturing processes for the pharmaceutical industry; optimization of processes for the pharmaceutical industry; Research and development services for the pharmaceutical industry; research and development services for medical purposes.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Active chemical ingredients for use in the manufacture of pharmaceuticals; pharmaceutical Ingredients. Compositions for medical and veterinarian use; medical diagnostic compositions; Chemical products for pharmaceutical use; Chemical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders. Development of pharmaceutical products and drug products; research on pharmaceutical products and drug products; Research and development of manufacturing processes for the pharmaceutical industry; optimization of processes for the pharmaceutical industry; Research and development services for the pharmaceutical industry; research and development services for medical purposes.
60.
A NOVEL FORM OF IVERMECTIN AND A PROCESS FOR MAKING IT
Amorphous ivermectinis provided, suitably in isolated solid form, and is suitably free of any additives or a support matrix, such as a solid dispersion. Also provided is a pharmaceutical formulation, for animal including human or veterinary use, comprising the amorphous ivermectin of the invention, and a pharmaceutically-acceptable carrier therefor. Also provided is a medical device incorporating amorphous ivermectin according to the invention, or a medical device incorporating a pharmaceutical formulation according to the invention described herein. A method of preparing amorphous ivermectin comprises the steps of preparing a solution of ivermectin in at least one solvent; removing the solvent by feeding the solution to a spray dryer and collecting particles of ivermectin. Amorphous ivermectin as disclosed herein may be used as a medicament, in particular to treat conditions such as a medical condition caused by internal nematode infections including but not limited to onchocerciasis (river blindness), filariasis (elephantiasis), strongyloidiasis or demodicosis.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07H 17/08 - Hetero rings containing eight or more ring members, e.g. erythromycins
61.
A NOVEL FORM OF IVERMECTIN AND A PROCESS FOR MAKING IT
Amorphous ivermectinis provided, suitably in isolated solid form, and is suitably free of any additives or a support matrix, such as a solid dispersion. Also provided is a pharmaceutical formulation, for animal including human or veterinary use, comprising the amorphous ivermectin of the invention, and a pharmaceutically-acceptable carrier therefor. Also provided is a medical device incorporating amorphous ivermectin according to the invention, or a medical device incorporating a pharmaceutical formulation according to the invention described herein. A method of preparing amorphous ivermectin comprises the steps of preparing a solution of ivermectin in at least one solvent; removing the solvent by feeding the solution to a spray dryer and collecting particles of ivermectin. Amorphous ivermectin as disclosed herein may be used as a medicament, in particular to treat conditions such as a medical condition caused by internal nematode infections including but not limited to onchocerciasis (river blindness), filariasis (elephantiasis), strongyloidiasis or demodicosis.
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07H 17/08 - Hetero rings containing eight or more ring members, e.g. erythromycins
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
62.
A SPRAY DRYING PROCESS WITH CONTINUOUS PREPARATION OF SPRAY SOLUTION
The present invention discloses a spray drying process characterized by continuous preparation and immediate spray drying of a solution comprising at least one active pharmaceutical ingredient and/or at least one excipient, and at least one solvent. The said active pharmaceutical ingredient(s) and solvent(s) are combined, alone or along with one or more excipients to form a first suspension. Said suspension is continuously fed to an intensifier pump that pushes said suspension through at least one micro-reaction chamber and/or at least one micro-channel where the suspension's solid(s) component(s) is(are) dissolved into said solvent(s) by means of high energy mixing / forced contact at micro, nano and molecular level to form a solution stream. The said solution stream is then immediately and continuously fed to the spray dryer through at least one atomization nozzle, drying said atomized stream to obtain solid particles and collecting said solid particles. Single component particles or multi-component particles, particulate amorphous solid dispersion and pharmaceutical compositions are also disclosed. The present invention also discloses amorphous solid dispersions obtained by the method of the invention as well as pharmaceutical compositions containing the same.
The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
64.
A SPRAY DRYING PROCESS WITH CONTINUOUS PREPARATION OF SPRAY SOLUTION
The present invention discloses a spray drying process characterized by continuous preparation and immediate spray drying of a solution comprising at least one active pharmaceutical ingredient and/or at least one excipient, and at least one solvent. The said active pharmaceutical ingredient(s) and solvent(s) are combined, alone or along with one or more excipients to form a first suspension. Said suspension is continuously fed to an intensifier pump that pushes said suspension through at least one micro-reaction chamber and/or at least one micro-channel where the suspension's solid(s) component(s) is(are) dissolved into said solvent(s) by means of high energy mixing / forced contact at micro, nano and molecular level to form a solution stream. The said solution stream is then immediately and continuously fed to the spray dryer through at least one atomization nozzle, drying said atomized stream to obtain solid particles and collecting said solid particles. Single component particles or multi-component particles, particulate amorphous solid dispersion and pharmaceutical compositions are also disclosed. The present invention also discloses amorphous solid dispersions obtained by the method of the invention as well as pharmaceutical compositions containing the same.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosacea treatment
preparations; pharmaceutical preparations for skin care;
chemical preparations for medical purposes;
chemico-pharmaceutical preparations; medicines for human
purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosacea treatment
preparations; pharmaceutical preparations for skin care;
chemical preparations for medical purposes;
chemico-pharmaceutical preparations; medicines for human
purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosacea treatment
preparations; pharmaceutical preparations for skin care;
chemical preparations for medical purposes;
chemico-pharmaceutical preparations; medicines for human
purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosacea treatment
preparations; pharmaceutical preparations for skin care;
chemical preparations for medical purposes;
chemico-pharmaceutical preparations; medicines for human
purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Antibiotics; acne treatment preparations; rosacea treatment preparations; pharmaceutical preparations for skin care for the treatment of acne; pharmaceutical preparations for skin care for the treatment of rosacea; pharmaceutical preparations for skin care for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemical preparations for medical purposes for the treatment of acne; chemical preparations for medical purposes for the treatment of rosacea; chemical preparations for medical purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemico-pharmaceutical preparations for the treatment of acne; chemico-pharmaceutical preparations for the treatment of rosacea; chemico-pharmaceutical preparations for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; medicines for human purposes for the treatment of acne; medicines for human purposes for the treatment of rosacea; medicines for human purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Antibiotics; acne treatment preparations; rosacea treatment preparations; pharmaceutical preparations for skin care for the treatment of acne; pharmaceutical preparations for skin care for the treatment of rosacea; pharmaceutical preparations for skin care for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemical preparations for medical purposes for the treatment of acne; chemical preparations for medical purposes for the treatment of rosacea; chemical preparations for medical purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemico-pharmaceutical preparations for the treatment of acne; chemico-pharmaceutical preparations for the treatment of rosacea; chemico-pharmaceutical preparations for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; medicines for human purposes for the treatment of acne; medicines for human purposes for the treatment of rosacea; medicines for human purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Antibiotics; acne treatment preparations; rosacea treatment preparations; pharmaceutical preparations for skin care for the treatment of acne; pharmaceutical preparations for skin care for the treatment of rosacea; pharmaceutical preparations for skin care for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemical preparations for medical purposes for the treatment of acne; chemical preparations for medical purposes for the treatment of rosacea; chemical preparations for medical purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemico-pharmaceutical preparations for the treatment of acne; chemico-pharmaceutical preparations for the treatment of rosacea; chemico-pharmaceutical preparations for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; medicines for human purposes for the treatment of acne; medicines for human purposes for the treatment of rosacea; medicines for human purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Antibiotics; acne treatment preparations; rosacea treatment preparations; pharmaceutical preparations for skin care for the treatment of acne; pharmaceutical preparations for skin care for the treatment of rosacea; pharmaceutical preparations for skin care for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemical preparations for medical purposes for the treatment of acne; chemical preparations for medical purposes for the treatment of rosacea; chemical preparations for medical purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; chemico-pharmaceutical preparations for the treatment of acne; chemico-pharmaceutical preparations for the treatment of rosacea; chemico-pharmaceutical preparations for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; medicines for human purposes for the treatment of acne; medicines for human purposes for the treatment of rosacea; medicines for human purposes for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections.
73.
Method of production of inhalable composite particles using a three-fluid nozzle
A method of preparing a pharmaceutical formulation which is suitable for inhalation, the method comprising: providing a solution comprising a first solvent or mixture of solvents and a poorly water soluble active agent; providing a second solution comprising a second solvent or mixture of solvents and an excipient. The first and second solvents or mixture of solvents are removed by simultaneously drying both solutions in a spray dryer equipped with a three-fluid nozzle to produce particles comprising an active agent and an excipient.
e. Optionally collecting a powdered form of the complex.
The described process has high throughput with higher yields of complexation in less time than prior art methods.
The complexes obtained by the invention are characterized by having enhanced dissolution and/or bioavailability of the active pharmaceutical ingredient in body fluids.
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
The present invention relates to an amorphous form of vilanterol trifenatate, processes for its preparation and its use in pharmaceutical formulations for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the invention relates to an amorphous form of vilanterol trifenatate, characterised by the X-ray powder diffraction (XRPD) pattern, obtained using copper K-alpha1 radiation, depicted in Figure 1.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical and veterinary products, medication for
humans and animals; chemical preparations for the
pharmaceutical purposes; pharmaceutical compositions;
veterinary preparations. Medical devices.
77.
CRYSTALLINE FORMS OF VILANTEROL TRIFENATATE AND PROCESSES FOR THEIR PREPARATION
The present invention relates to new crystalline forms of vilanterol trifenatate, processes for their preparation, and their use in a pharmaceutical composition for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the present invention relates to a crystalline form of vilanterol trifenatate characterised in that the form has an XRPD pattern as defined herein having characteristic diffraction angles (2-theta or 2.THETA. (.degree.)) falling within or at each end of one or more of the following ranges: (a) 3 to 5.degree., such as 3.8 to 4.4.degree.; and/or (b) 7 to 9.9.degree., such as 7 to 8.5.degree.; and/or (c) 12 to 13.3.degree., such as 12 to 13.3.degree.; and/or (d) 16.4 to 17.3.degree., such as 16.4 to 17.3.degree.; and/or (e)26.8 to 28.3.degree., such as 26.8 to 28.3.degree.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
78.
AMORPHOUS FORM OF VILANTEROL TRIFENATATE AND PROCESSES FOR THE PREPARATION THEREOF
The present invention relates to an amorphous form of vilanterol trifenatate, processes for its preparation and its use in pharmaceutical formulations for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the invention relates to an amorphous form of vilanterol trifenatate, characterised by the X-ray powder diffraction (XRPD) pattern, obtained using copper K-alpha1 radiation, depicted in Figure 1.
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
79.
NEW CRYSTALLINE FORMS OF VILANTEROL TRIFENATATE AND PROCESSES FOR THEIR PREPARATION
The present invention relates to new crystalline forms of vilanterol trifenatate, processes for their preparation, and their use in a pharmaceutical composition for the treatment of respiratory diseases, particularly for the treatment of asthma and chronic obstructive pulmonary disease. In particular, the present invention relates to a crystalline form of vilanterol trifenatate characterised in that the form has an XRPD pattern as defined herein having characteristic diffraction angles (2-theta or 2Θ (°)) falling within or at each end of one or more of the following ranges: (a) 3 to 5°, such as 3.8 to 4.4°; and/or (b) 7 to 9.9°, such as 7 to 8.5°; and/or (c) 12 to 13.3°, such as 12 to 13.3°; and/or (d) 16.4 to 17.3°, such as 16.4 to 17.3°; and/or (e)26.8 to 28.3°, such as 26.8 to 28.3°
C07C 217/08 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes, namely, for treatment of damaged skin and tissue; chemico-pharmaceutical preparations for dermatologic use and chemico-pharmaceutical preparations for treating skin disorders; medicines for human purposes, namely, medicines for treating skin diseases in humans and medicinal preparations for treating rosacea in humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes, namely, for treatment of damaged skin and tissue; chemico-pharmaceutical preparations for dermatologic use and chemico-pharmaceutical preparations for treating skin disorders; medicines for human purposes, namely, medicines for treating skin diseases in humans and medicinal preparations for treating rosacea in humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes, namely, for treatment of damaged skin and tissue; chemico-pharmaceutical preparations for dermatologic use and chemico-pharmaceutical preparations for treating skin disorders; medicines for human purposes, namely, medicines for treating skin diseases in humans and medicinal preparations for treating rosacea in humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes, namely, for treatment of damaged skin and tissue; chemico-pharmaceutical preparations for dermatologic use and chemico-pharmaceutical preparations for treating skin disorders; medicines for human purposes, namely, medicines for treating skin diseases in humans and medicinal preparations for treating rosacea in humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Antibiotics; acne treatment preparations; rosácea treatment preparations; pharmaceutical preparations for skin care; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.
88.
Polymorphic forms of minocycline base and processes for their preparation
Described are new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and Form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.
C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug;a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins);and a targeting unit. A B- complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate- receptor-positive MDA-MB-231 cancer cells, having an IC50 in the low nanomolar range.
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
(1) Active ingredients for the pharmaceutical industry, namely, chemical additives for use in the manufacture of human and animal pharmaceuticals
(2) Pharmaceutical and veterinary products, medication for humans and animals, namely, corticosteroids, antibiotics, pharmaceutical preparations for reducing cholesterol, parasiticides, hormones for medical purposes, medical imaging contrast media; pharmaceutical and veterinary formulations for humans and animals, namely, corticosteroids, antibiotics, pharmaceutical preparations for reducing cholesterol, parasiticides, hormones for medical purposes, medical imaging contrast media
(3) Medical devices, namely, inhalers for therapeutic use
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical and veterinary products, namely pharmaceutical and veterinary preparations and compositions for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders; all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals; medication for humans and animals, namely medicines for the treatment of , inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders; all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management; chemical preparations for the pharmaceutical purposes, namely pharmaceutical preparations for the prevention, diagnosis, treatment or improvement of conditions and disorders, namely, inflammatory, allergical, oncological, degenerative, genetic, traumatic, tumoural, pressure, poisoning, mutation, sepsis, psychiatric, obese, eating, addictive, sexual, sleep, and infectious conditions and disorders, namely, bacterial, viral, fungal or parasitic conditions and disorders; all of the above related to skin, musculo-skeletal, cardiac, neurological, cellular, vascular, hematological, respiratory, digestive, genital, urinary, reproductive, sensorial, metabolic, endocrine, lymphatic, immune or nervous systems, as well as pain management, for use by humans or animals Medical devices for use in treating conditions and disorders of the respiratory system
92.
Process for the preparation of intermediates useful in the preparation of non-ionic contrast agents
The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.
B01J 19/18 - Stationary reactors having moving elements inside
C07C 227/04 - Formation of amino groups in compounds containing carboxyl groups
C07C 227/18 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
B01J 19/00 - Chemical, physical or physico-chemical processes in generalTheir relevant apparatus
C07C 17/12 - Preparation of halogenated hydrocarbons by replacement by halogens of hydrogen atoms in the ring of aromatic compounds
C07C 22/04 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings
C07C 229/62 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino groups and at least two carboxyl groups bound to carbon atoms of the same six-membered aromatic ring
C07C 233/69 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
C07C 237/46 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and at least three atoms of bromine or iodine, bound to carbon atoms of the same non-condensed six-membered aromatic ring
93.
PROCESS FOR THE PREPARATION OF UMECLIDINIUM BROMIDE
The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1 -bromo-2- chloroethane in the presence of an organic base in a solvent to form ethyl 1 -(2-chloroethyl)piperidine- 4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1 -(2- chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1 -azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1 -azabicyclo[2.2.2]octane-4- carboxylate (III) with phenyl lithium in a solvent to form 1 -azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1 -azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1 -[2-(phenylmethyl)oxy]ethyl]-1 - azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1 - azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1 -[2-(phenylmethyl)oxy]ethyl]-1 -azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1 -(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
94.
PROCESS FOR THE PREPARATION OF UMECLIDINIUM BROMIDE
The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1 -(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1 -azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyOmethanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyOmethyl]-1 42-(phenylmethypoxy]ethyl]-1 -azoniabicyclo[2.2.2]octane bromide (l),umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1 42-(phenylmethypoxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1 -(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide, wherein the solvent is selected from cyclic ethers such as tetrahydrofuran, aromatic solvents, such as toluene, ketones such as acetone and protic solvents such as water or combinations thereof, optionally wherein the solvent is water is also disclosed. Umeclidinium bromide obtainable from the disclosed processes, ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) and pharmaceutical compositions are also disclosed.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
The present invention discloses a method to continuously manufacture micro- and/or nanoparticles of single component particles or multi-component particles such as particulate amorphous solid dispersions or particulate co-crystals. The continuous method comprises the steps of 1. preparing a first solution comprising at least one component and at least one solvent and a second solution comprising at least one anti-solvent of the at least one component comprised in the first solution, 2. mixing said first solution and said second solution by means of microfluidization to produce a suspension by precipitation or co-precipitation, 3. feeding said suspension to a filtration system to obtain a concentrate stream, 4. feeding said concentrate stream to a spray dryer, 5. atomizing said concentrate stream using at least one atomization nozzle, 6. drying said atomized concentrate stream to obtain particles, and 7. collecting said particles. Single component particles or multi-component particles, particulate amorphous solid dispersions, particulate co-crystals and pharmaceutical compositions are also disclosed.
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
B01D 63/00 - Apparatus in general for separation processes using semi-permeable membranes
B05B 1/02 - Nozzles, spray heads or other outlets, with or without auxiliary devices such as valves, heating means designed to produce a jet, spray, or other discharge of particular shape or nature, e.g. in single drops
B05B 12/14 - Arrangements for controlling deliveryArrangements for controlling the spray area for supplying a selected one of a plurality of liquids or other fluent materials to a single spray outlet
F26B 3/12 - Drying solid materials or objects by processes involving the application of heat by convection, i.e. heat being conveyed from a heat source to the materials or objects to be dried by a gas or vapour, e.g. air the gas or vapour carrying the materials or objects to be dried with it in the form of a spray
F26B 17/10 - Machines or apparatus for drying materials in loose, plastic, or fluidised form, e.g. granules, staple fibres, with progressive movement with movement performed by fluid currents, e.g. issuing from a nozzle
A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2θ, 10.4±0.2° 2θ, 13.2±0.2° 2θ, 13.8±0.2° 2θ, 19.9±0.2° 2θ, 20.3±0.2° 2θ, 20.8±0.2° 2θ, 24.2±0.2° 2θ, 25.7±0.2° 2θ, 26.1±0.2° 2θ, 29.2±0.2° 2θ, 30.8±0.2° 2θ. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical and veterinary products, medication for humans and animals; active ingredients for the pharmaceutical industry; pharmaceutical and veterinary formulations. Medical Devices.
99.
Polymorphic forms of minocycline base and processes for their preparation
The present invention concerns new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.
C07C 237/26 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
The present invention provides co-crystals of glycopyrronium bromide with lactose. The glycopyrronium bromide and lactose in the novel co-crystals are present in a stoichiometric ratio of from about 1 :2 to 2: 1. These are characterized by XRD and DSC. Processes for preparing the novel co-crystals are also provided. The co-crystals are also disclosed for use as a medicament, in particular, for treatment of respiratory complaints, such as chronic pulmonary obstructive disease (COPD), bronchitis and asthma. Pharmaceutical compositions comprising the co-crystals as active ingredient are also presented.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
