Abrégé

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.

Classes IPC  ?

• F26B 3/06 - Procédés de séchage d'un matériau solide ou d'objets impliquant l'utilisation de chaleur par convection, c. à d. la chaleur étant transférée d'une source de chaleur au matériau ou aux objets à sécher par un gaz ou par une vapeur, p.ex. l'air le gaz ou la vapeur s'écoulant à travers le matériau ou les objets à sécher
• F26B 9/06 - Machines ou appareils pour le séchage d'un matériau solide ou d'objets au repos animés uniquement d'une agitation locale; Aération des placards ou armoires d'appartements dans des tambours ou chambres fixes
• F26B 21/12 - Commande, p.ex. régulation des paramètres de l'alimentation en gaz du débit

Abrégé

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.

Classes IPC  ?

• C07C 237/26 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle autre qu'un cycle aromatique à six chaînons du squelette carboné d'un cycle faisant partie d'un système cyclique condensé formé par au moins quatre cycles, p.ex. tétracycline

Abrégé

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.

Classes IPC  ?

• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres

Abrégé

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.

Classes IPC  ?

• C07F 5/02 - Composés du bore
• A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c. à d. le conjugué entier étant un co-médicament, p.ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
• A61K 47/60 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique macromoléculaire, p.ex. une molécule oligomérique, polymérique ou dendrimérique obtenu par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyurées ou polyuréthanes le composé organique macromoléculaire étant un oligomère, un polymère ou un dendrimère de polyoxyalkylène, p.ex. PEG, PPG, PEO ou polyglycérol
• A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c. à d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
• A61K 47/66 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant une protéine, un peptide ou un acide polyaminé l’agent de modification étant un système de pré-ciblage impliquant un peptide ou une protéine pour cibler des cellules spécifiques
• A61K 47/69 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament le conjugué étant caractérisé par sa forme physique ou sa forme galénique, p.ex. émulsion, particule, complexe d’inclusion, stent ou kit
• A61K 49/00 - Préparations pour examen in vivo

Abrégé

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.

Classes IPC  ?

• A61K 9/16 - Agglomérés; Granulés; Microbilles
• A61K 47/18 - Amines; Amides; Urées; Composés d’ammonium quaternaire; Acides aminés; Oligopeptides ayant jusqu’à cinq acides aminés
• A61M 15/00 - Inhalateurs
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrène; Leurs dérivés, p.ex. stéroïdes contenant des hétérocycles, p.ex. danazol, stanozolol, pancuronium ou digitogénine
• A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides  contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle

Abrégé

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.

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p.ex. rifampine, thiothixène
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p.ex. nucléosides, nucléotides  contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
• A61K 47/24 - Composés organiques, p.ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant des atomes autres que des atomes de carbone, d'hydrogène, d'oxygène, d'halogènes, d'azote ou de soufre, p.ex. cyclométhicone ou phospholipides
• A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine

Abrégé

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.

Classes IPC  ?

• G01B 7/04 - Dispositions pour la mesure caractérisées par l'utilisation de techniques électriques ou magnétiques pour mesurer la longueur, la largeur ou l'épaisseur spécialement adaptés pour mesurer la longueur ou la largeur d'objets en mouvement
• G01B 7/06 - Dispositions pour la mesure caractérisées par l'utilisation de techniques électriques ou magnétiques pour mesurer la longueur, la largeur ou l'épaisseur pour mesurer l'épaisseur

Abrégé

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.

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/16 - Agglomérés; Granulés; Microbilles
• A61K 47/18 - Amines; Amides; Urées; Composés d’ammonium quaternaire; Acides aminés; Oligopeptides ayant jusqu’à cinq acides aminés
• A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine

Abrégé

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.

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• C07D 319/08 - Dioxanes-1, 3; Dioxanes-1, 3 hydrogénés condensés avec des carbocycles ou avec des systèmes carbocycliques
• A61P 11/08 - Bronchodilatateurs

Produits et services

Electromechanical machines for chemical industry. Spray drying apparatus; apparatus for drying of particulates.

Abrégé

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.

Classes IPC  ?

• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine

Abrégé

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.

Classes IPC  ?

• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine

Produits et services

(1) Electromechanical machines for chemical industry. (2) Spray drying apparatus; apparatus for drying of particulates.

Produits et services

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

Abrégé

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.

Classes IPC  ?

• C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
• C07C 231/14 - Préparation d'amides d'acides carboxyliques par formation de groupes carboxamide combinée avec des réactions n'impliquant pas les groupes carboxamide
• C07C 237/26 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle autre qu'un cycle aromatique à six chaînons du squelette carboné d'un cycle faisant partie d'un système cyclique condensé formé par au moins quatre cycles, p.ex. tétracycline

Abrégé

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.

Classes IPC  ?

• C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
• C07C 231/14 - Préparation d'amides d'acides carboxyliques par formation de groupes carboxamide combinée avec des réactions n'impliquant pas les groupes carboxamide
• C07C 237/26 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle autre qu'un cycle aromatique à six chaînons du squelette carboné d'un cycle faisant partie d'un système cyclique condensé formé par au moins quatre cycles, p.ex. tétracycline

Abrégé

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.

Classes IPC  ?

• A61K 31/365 - Lactones
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
• A61P 31/12 - Antiviraux
• A61P 33/00 - Agents antiparasitaires

Abrégé

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).

Classes IPC  ?

• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation

Produits et 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.

Abrégé

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.

Classes IPC  ?

• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
• A61K 47/02 - Composés inorganiques
• A61K 47/12 - Acides carboxyliques; Leurs sels ou anhydrides
• A61K 47/18 - Amines; Amides; Urées; Composés d’ammonium quaternaire; Acides aminés; Oligopeptides ayant jusqu’à cinq acides aminés
• A61K 47/24 - Composés organiques, p.ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant des atomes autres que des atomes de carbone, d'hydrogène, d'oxygène, d'halogènes, d'azote ou de soufre, p.ex. cyclométhicone ou phospholipides

Abrégé

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.

Classes IPC  ?

• F26B 3/06 - Procédés de séchage d'un matériau solide ou d'objets impliquant l'utilisation de chaleur par convection, c. à d. la chaleur étant transférée d'une source de chaleur au matériau ou aux objets à sécher par un gaz ou par une vapeur, p.ex. l'air le gaz ou la vapeur s'écoulant à travers le matériau ou les objets à sécher
• F26B 9/06 - Machines ou appareils pour le séchage d'un matériau solide ou d'objets au repos animés uniquement d'une agitation locale; Aération des placards ou armoires d'appartements dans des tambours ou chambres fixes
• F26B 21/12 - Commande, p.ex. régulation des paramètres de l'alimentation en gaz du débit

Abrégé

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.

Classes IPC  ?

• F26B 3/06 - Procédés de séchage d'un matériau solide ou d'objets impliquant l'utilisation de chaleur par convection, c. à d. la chaleur étant transférée d'une source de chaleur au matériau ou aux objets à sécher par un gaz ou par une vapeur, p.ex. l'air le gaz ou la vapeur s'écoulant à travers le matériau ou les objets à sécher
• F26B 21/12 - Commande, p.ex. régulation des paramètres de l'alimentation en gaz du débit

Produits et services

Electromechanical machines for chemical industry. Spray drying apparatus; apparatus for drying of particulates.

Abrégé

The invention provides methods, compositions, and kits containing a pharmaceutical composition, for treating meibomian gland dysfunction, dry eye disease, and related disorders.

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/05 - Phénols
• A61K 31/745 - Polymères d'hydrocarbures
• A61P 27/02 - Agents ophtalmiques
• A61P 27/04 - Larmes artificielles; Solutions d'irrigation

Produits et 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

Produits et 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.

Abrégé

The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating rosacea.

Classes IPC  ?

• A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. carbomères
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes ; Huiles, graisses ou cires naturelles ou naturelles modifiées, p.ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
• A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
• A61K 31/65 - Tétracyclines 

Produits et 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.

Abrégé

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.

Classes IPC  ?

• C07C 229/16 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe amino et un seul groupe carboxyle liés au squelette carboné l'atome d'azote du groupe amino étant lié de plus à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons à des atomes de carbone de radicaux hydrocarbonés substitués par des groupes amino ou carboxyle, p.ex. acide éthylènediaminetétra-acétique, acides iminodiacétiques
• A61K 47/54 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique
• A61K 9/16 - Agglomérés; Granulés; Microbilles
• C07C 227/40 - Séparation; Purification

Produits et services

Antibiotics; ocular rosacea treatment preparations; blepharitis treatment preparations; dry eye treatment preparations; meibomian gland dysfunction treatment preparations; ocular surface inflammation treatment preparations; pharmaceutical preparations for eye care; pharmaceutical preparations for ophthalmic purposes; medicated eye-washes; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.

Abrégé

The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.

Classes IPC  ?

• A61K 31/65 - Tétracyclines 
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/06 - Onguents; Excipients pour ceux-ci
• A61K 47/06 - Composés organiques, p.ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
• A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. carbomères
• A61P 27/02 - Agents ophtalmiques

Abrégé

The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.

Classes IPC  ?

• A61K 31/65 - Tétracyclines 
• A61P 27/02 - Agents ophtalmiques
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/06 - Onguents; Excipients pour ceux-ci
• A61K 9/10 - Dispersions; Emulsions
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 47/06 - Composés organiques, p.ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
• A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. carbomères

Abrégé

The invention provides methods, compositions, and kits containing a minocycline topical suspension, for treating meibomian gland dysfunction and related disorders.

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/10 - Dispersions; Emulsions
• A61K 31/65 - Tétracyclines 
• A61P 27/04 - Larmes artificielles; Solutions d'irrigation

Produits et 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.

Produits et services

(1) Antibiotics; ocular rosacea treatment preparations; blepharitis treatment preparations; dry eye treatment preparations; meibomian gland dysfunction treatment preparations; ocular surface inflammation treatment preparations; pharmaceutical preparations for eye care, namely ocular rosacea treatment preparations; pharmaceutical preparations for eye care, namely blepharitis treatment preparations; pharmaceutical preparations for eye care, namely dry eye treatment preparations; pharmaceutical preparations for eye care, namely meibomian gland dysfunction treatment preparations; pharmaceutical preparations for eye care, namely ocular surface inflammation treatment preparations; medicated eye-washes.

Produits et services

Antibiotics; ocular rosacea treatment preparations; blepharitis treatment preparations; dry eye treatment preparations; meibomian gland dysfunction treatment preparations; ocular surface inflammation treatment preparations; pharmaceutical preparations for eye care; pharmaceutical preparations for ophthalmic purposes; medicated eye-washes; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes

Abrégé

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.

Classes IPC  ?

• A61K 47/54 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique
• A61P 35/00 - Agents anticancéreux

Produits et 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

Abrégé

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.

Classes IPC  ?

• A61K 9/16 - Agglomérés; Granulés; Microbilles
• F26B 5/00 - Procédés de séchage d'un matériau solide ou d'objets n'impliquant pas l'utilisation de chaleur

Produits et services

Antibiotics; ocular rosacea treatment preparations; blepharitis treatment preparations; dry eye treatment preparations; meibomian gland dysfunction treatment preparations; ocular surface inflammation treatment preparations; pharmaceutical preparations for eye care; pharmaceutical preparations for ophthalmic purposes; medicated eye-washes; chemical preparations for medical purposes; chemico-pharmaceutical preparations; medicines for human purposes.

Abrégé

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.

Classes IPC  ?

• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61K 9/16 - Agglomérés; Granulés; Microbilles

Abrégé

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).

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p.ex. quinuclidine
• A61P 11/06 - Antiasthmatiques

Abrégé

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).

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p.ex. quinuclidine
• A61P 11/06 - Antiasthmatiques

Produits et 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.

Abrégé

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.

Classes IPC  ?

• C07D 471/08 - Systèmes pontés
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• C07D 211/62 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p.ex. radicaux ester ou nitrile liés en position 4
• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation

Produits et 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.

Produits et 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.

Produits et 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

Produits et 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.

Produits et 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

Abrégé

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.

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61P 11/06 - Antiasthmatiques
• A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
• A61K 31/138 - Aryloxyalkylamines, p.ex. propranolol, tamoxifène, phénoxybenzamine
• C07C 213/10 - Séparation; Purification; Stabilisation; Emploi d'additifs
• C07C 215/60 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes hydroxy liés à des atomes de carbone d'au moins un cycle aromatique à six chaînons et des groupes amino liés à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du avec des groupes amino reliés au cycle aromatique à six chaînons, ou au système cyclique condensé contenant ce cycle, par l'intermédiaire de chaînes carbonées qui sont substituées de plus par des groupes hydroxy avec des groupes hydroxy et le cycle aromatique à six chaînons, ou le système cyclique condensé contenant ce cycle, liés au même atome de carbone de la chaîne carbonée la chaîne ayant deux atomes de carbone entre les groupes amino et le cycle aromatique à six chaînons ou le système cyclique condensé contenant ce cycle

Abrégé

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°.

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61P 11/06 - Antiasthmatiques
• A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
• A61K 31/138 - Aryloxyalkylamines, p.ex. propranolol, tamoxifène, phénoxybenzamine
• C07C 213/10 - Séparation; Purification; Stabilisation; Emploi d'additifs
• C07C 215/60 - Composés contenant des groupes amino et hydroxy liés au même squelette carboné ayant des groupes hydroxy liés à des atomes de carbone d'au moins un cycle aromatique à six chaînons et des groupes amino liés à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du avec des groupes amino reliés au cycle aromatique à six chaînons, ou au système cyclique condensé contenant ce cycle, par l'intermédiaire de chaînes carbonées qui sont substituées de plus par des groupes hydroxy avec des groupes hydroxy et le cycle aromatique à six chaînons, ou le système cyclique condensé contenant ce cycle, liés au même atome de carbone de la chaîne carbonée la chaîne ayant deux atomes de carbone entre les groupes amino et le cycle aromatique à six chaînons ou le système cyclique condensé contenant ce cycle

Abrégé

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.

Classes IPC  ?

• C07C 227/40 - Séparation; Purification
• C07C 229/16 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe amino et un seul groupe carboxyle liés au squelette carboné l'atome d'azote du groupe amino étant lié de plus à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons à des atomes de carbone de radicaux hydrocarbonés substitués par des groupes amino ou carboxyle, p.ex. acide éthylènediaminetétra-acétique, acides iminodiacétiques
• C07C 229/76 - Complexes métalliques d'acides aminocarboxyliques

Abrégé

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.

Classes IPC  ?

• C07C 227/40 - Séparation; Purification
• C07C 229/16 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe amino et un seul groupe carboxyle liés au squelette carboné l'atome d'azote du groupe amino étant lié de plus à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons à des atomes de carbone de radicaux hydrocarbonés substitués par des groupes amino ou carboxyle, p.ex. acide éthylènediaminetétra-acétique, acides iminodiacétiques
• C07C 229/76 - Complexes métalliques d'acides aminocarboxyliques

Abrégé

50 in the low nanomolar range.

Classes IPC  ?

• C07F 5/02 - Composés du bore
• A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c. à d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
• A61K 47/66 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant une protéine, un peptide ou un acide polyaminé l’agent de modification étant un système de pré-ciblage impliquant un peptide ou une protéine pour cibler des cellules spécifiques
• A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c. à d. le conjugué entier étant un co-médicament, p.ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
• A61K 47/60 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique macromoléculaire, p.ex. une molécule oligomérique, polymérique ou dendrimérique obtenu par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyurées ou polyuréthanes le composé organique macromoléculaire étant un oligomère, un polymère ou un dendrimère de polyoxyalkylène, p.ex. PEG, PPG, PEO ou polyglycérol
• A61K 47/69 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament le conjugué étant caractérisé par sa forme physique ou sa forme galénique, p.ex. émulsion, particule, complexe d’inclusion, stent ou kit
• A61K 49/00 - Préparations pour examen in vivo

Produits et 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.

Produits et 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.

Abrégé

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.

Classes IPC  ?

• C07D 493/22 - Composés hétérocycliques contenant des atomes d'oxygène comme uniques hétéro-atomes dans le système condensé dans lesquels le système condensé contient au moins quatre hétérocycles
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61P 33/00 - Agents antiparasitaires
• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p.ex. érythromycines

Abrégé

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.

Classes IPC  ?

• C07D 493/22 - Composés hétérocycliques contenant des atomes d'oxygène comme uniques hétéro-atomes dans le système condensé dans lesquels le système condensé contient au moins quatre hétérocycles
• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p.ex. érythromycines
• A61P 33/00 - Agents antiparasitaires
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p.ex. leucoglucosane, hespéridine, érythromycine, nystatine

Abrégé

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.

Classes IPC  ?

• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 9/16 - Agglomérés; Granulés; Microbilles
• B01J 19/00 - Procédés chimiques, physiques ou physico-chimiques en général; Appareils appropriés

Abrégé

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.

Classes IPC  ?

• C07D 471/08 - Systèmes pontés
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• C07D 211/62 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p.ex. radicaux ester ou nitrile liés en position 4
• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation

Abrégé

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.

Classes IPC  ?

• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 9/16 - Agglomérés; Granulés; Microbilles
• B01J 19/00 - Procédés chimiques, physiques ou physico-chimiques en général; Appareils appropriés

Produits et 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.

Produits et 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.

Produits et 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.

Produits et 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.

Produits et 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

Produits et 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.

Produits et 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

Produits et 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.

Abrégé

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.

Classes IPC  ?

• A61K 9/16 - Agglomérés; Granulés; Microbilles
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/50 - Microcapsules
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 31/56 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrène; Leurs dérivés, p.ex. stéroïdes

Abrégé

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.

Classes IPC  ?

• A61K 47/69 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament le conjugué étant caractérisé par sa forme physique ou sa forme galénique, p.ex. émulsion, particule, complexe d’inclusion, stent ou kit
• A61K 9/16 - Agglomérés; Granulés; Microbilles
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 47/40 - Cyclodextrines; Leurs dérivés
• A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p.ex. rifampine, thiothixène

Abrégé

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.

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61K 31/133 - Amines, p.ex. amantadine ayant des groupes hydroxyle, p.ex. sphingosine
• A61P 11/06 - Antiasthmatiques

Produits et services

Pharmaceutical and veterinary products, medication for humans and animals; chemical preparations for the pharmaceutical purposes; pharmaceutical compositions; veterinary preparations. Medical devices.

Abrégé

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. (°)) 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°

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61K 31/133 - Amines, p.ex. amantadine ayant des groupes hydroxyle, p.ex. sphingosine
• A61P 11/06 - Antiasthmatiques

Abrégé

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.

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61K 31/133 - Amines, p.ex. amantadine ayant des groupes hydroxyle, p.ex. sphingosine
• A61P 11/06 - Antiasthmatiques

Abrégé

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°

Classes IPC  ?

• C07C 217/08 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés et des groupes amino liés à des atomes de carbone acycliques du même squelette carboné le squelette carboné étant acyclique et saturé ayant un seul groupe hydroxy éthérifié et un seul groupe amino liés au squelette carboné, qui n'est pas substitué par ailleurs l'atome d'oxygène du groupe hydroxy éthérifié étant lié de plus à un atome de carbone acyclique
• A61K 31/133 - Amines, p.ex. amantadine ayant des groupes hydroxyle, p.ex. sphingosine
• A61P 11/06 - Antiasthmatiques

Produits et 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

Produits et 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

Produits et 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

Produits et 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

Produits et 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.

Produits et 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.

Produits et 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.

Produits et 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.

Abrégé

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.

Classes IPC  ?

• C07C 237/26 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle autre qu'un cycle aromatique à six chaînons du squelette carboné d'un cycle faisant partie d'un système cyclique condensé formé par au moins quatre cycles, p.ex. tétracycline
• A61K 31/65 - Tétracyclines 

Abrégé

Tri-component multi-functional boronated complexes (B-complexes) of formula featuring reversible covalent bonds, 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.

Classes IPC  ?

• C07F 5/02 - Composés du bore
• A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c. à d. le conjugué entier étant un co-médicament, p.ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
• A61K 47/60 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique macromoléculaire, p.ex. une molécule oligomérique, polymérique ou dendrimérique obtenu par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyurées ou polyuréthanes le composé organique macromoléculaire étant un oligomère, un polymère ou un dendrimère de polyoxyalkylène, p.ex. PEG, PPG, PEO ou polyglycérol
• A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c. à d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
• A61K 31/69 - Composés du bore
• A61K 49/00 - Préparations pour examen in vivo

Abrégé

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.

Classes IPC  ?

• C07F 5/02 - Composés du bore
• A61K 31/69 - Composés du bore
• A61K 49/00 - Préparations pour examen in vivo
• A61K 47/55 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique l’agent de modification étant aussi un agent pharmacologiquement ou thérapeutiquement actif, c. à d. le conjugué entier étant un co-médicament, p.ex. un dimère, un oligomère ou un polymère de composés pharmacologiquement ou thérapeutiquement actifs
• A61K 47/60 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. les supports ou les additifs inertes; Agents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p.ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique macromoléculaire, p.ex. une molécule oligomérique, polymérique ou dendrimérique obtenu par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p.ex. polyurées ou polyuréthanes le composé organique macromoléculaire étant un oligomère, un polymère ou un dendrimère de polyoxyalkylène, p.ex. PEG, PPG, PEO ou polyglycérol
• A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c. à d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif

Produits et 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

Produits et 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

Abrégé

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.

Classes IPC  ?

• B01J 19/18 - Réacteurs fixes avec éléments internes mobiles
• C07C 227/04 - Formation de groupes amino dans des composés contenant des groupes carboxyle
• C07C 227/18 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions impliquant des groupes amino ou carboxyle, p.ex. hydrolyse d'esters ou d'amides, par formation d'halogénures, de sels ou d'esters
• C07C 231/02 - Préparation d'amides d'acides carboxyliques à partir d'acides carboxyliques ou à partir de leurs esters, anhydrides ou halogénures par réaction avec de l'ammoniac ou des amines
• C07C 231/12 - Préparation d'amides d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes carboxamide
• C07C 227/16 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions n'impliquant pas les groupes amino ou carboxyle
• B01J 19/00 - Procédés chimiques, physiques ou physico-chimiques en général; Appareils appropriés
• C07C 17/12 - Préparation d'hydrocarbures halogénés par remplacement par des halogènes d'atomes d'hydrogène dans le cycle de composés aromatiques
• C07C 22/04 - Composés cycliques contenant des atomes d'halogène liés à un atome de carbone acyclique ayant une insaturation dans les cycles contenant des cycles aromatiques à six chaînons
• C07C 229/62 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone de cycles aromatiques à six chaînons du même squelette carboné avec des groupes amino et carboxyle liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé avec des groupes amino et au moins deux groupes carboxyle liés à des atomes de carbone du même cycle aromatique à six chaînons
• C07C 233/69 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des atomes d'oxygène liés par des liaisons simples avec le radical hydrocarboné substitué lié à l'atome d'azote du groupe carboxamide par un atome de carbone acyclique d'un squelette carboné acyclique saturé
• C07C 237/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné ayant des atomes de carbone de groupes carboxamide, des groupes amino et au moins trois atomes de brome ou d'iode liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé

Abrégé

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.

Classes IPC  ?

• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
• C07D 211/62 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p.ex. radicaux ester ou nitrile liés en position 4

Abrégé

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.

Classes IPC  ?

• C07D 471/08 - Systèmes pontés
• C07D 211/62 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p.ex. radicaux ester ou nitrile liés en position 4

Abrégé

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.

Classes IPC  ?

• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
• C07D 211/62 - Atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p.ex. radicaux ester ou nitrile liés en position 4

Abrégé

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.

Classes IPC  ?

• B01D 9/00 - Cristallisation
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p.ex. poudres
• A61K 31/56 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrène; Leurs dérivés, p.ex. stéroïdes
• A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p.ex. azélastine, pentylènetétrazole
• B01D 63/00 - Appareils en général pour les procédés de séparation utilisant des membranes semi-perméables
• B01D 63/08 - Modules à membranes planes
• B05B 1/02 - Buses, têtes de pulvérisation ou autres dispositifs de sortie, avec ou sans dispositifs auxiliaires tels que valves, moyens de chauffage agencés pour produire un jet, un pulvérisat ou tout autre écoulement de forme ou de nature particulière, p.ex. sous forme de gouttes individuelles
• B05B 12/14 - Aménagements de commande de la distribution; Aménagements de réglage de l’aire de pulvérisation pour fournir à un orifice de pulvérisation unique, un liquide ou un autre matériau fluide choisi parmi plusieurs
• F26B 3/12 - Procédés de séchage d'un matériau solide ou d'objets impliquant l'utilisation de chaleur par convection, c. à d. la chaleur étant transférée d'une source de chaleur au matériau ou aux objets à sécher par un gaz ou par une vapeur, p.ex. l'air le gaz ou la vapeur entraînant le matériau ou les objets à sécher sous forme d'une pulvérisation
• F26B 17/10 - Machines ou appareils à mouvement progressif pour le séchage d'un matériau en vrac, à l'état plastique ou sous forme fluidisée, p.ex. granulés, fibres brutes le mouvement étant réalisé par des courants de fluides, p.ex. provenant d'une tuyère

Abrégé

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.

Classes IPC  ?

• C07D 453/02 - Composés hétérocycliques contenant des systèmes cycliques quinuclidine ou isoquinuclidine, p.ex. alcaloïdes de la quinine contenant des systèmes cycliques quinuclidine sans autre condensation
• A61P 11/08 - Bronchodilatateurs
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p.ex. quinuclidine
• A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
• B01D 9/00 - Cristallisation

Produits et services

Pharmaceutical and veterinary products, medication for humans and animals; active ingredients for the pharmaceutical industry; pharmaceutical and veterinary formulations. Medical Devices.

Abrégé

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.

Classes IPC  ?

• C07C 237/26 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle autre qu'un cycle aromatique à six chaînons du squelette carboné d'un cycle faisant partie d'un système cyclique condensé formé par au moins quatre cycles, p.ex. tétracycline
• A61K 31/65 - Tétracyclines 

Abrégé

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.

Classes IPC  ?

• C07D 207/12 - Atomes d'oxygène ou de soufre
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p.ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 13/06 - Antispasmodiques

Abrégé

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.

Classes IPC  ?

• C07D 207/12 - Atomes d'oxygène ou de soufre
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p.ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 13/06 - Antispasmodiques