The present invention relates to a compound for use in a method of treating chronic obstructive pulmonary disease (COPD) in a patient suffering from COPD, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein: the patient is resistant to improvements in lung function; and treating COPD comprises (i) improving the symptoms of COPD in the patient and/or (ii) improving the quality of life of the patient. In some aspects, the compound is in an inhalable pharmaceutical composition.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
Provided herein are pharmaceutical compositions and methods for providing blood plasma concentrations of ensifentrine to specific patient group populations including those with modified renal or hepatic impairment. In some aspects, the compound is in an inhalable pharmaceutical composition.
A61K 47/00 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
3.
PHARMACEUTICAL COMPOSITIONS OF ENSIFENTRINE FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE
Provided herein are pharmaceutical compositions and methods for treating COPD or COPD exacerbations in subjects suffering from, for example, moderate COPD, or subjects with decreased eosinophil concentrations, or are suffering from chronic bronchitis. Also provided herein are methods of increasing trough lung function in subjects suffering from moderate COPD. In some aspects, the compound is in an inhalable pharmaceutical composition.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
The present invention relates to a compound for use in a method of treating chronic obstructive pulmonary disease (COPD) in a patient suffering from COPD, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein: the patient is resistant to improvements in lung function; and treating COPD comprises (i) improving the symptoms of COPD in the patient and/or (ii) improving the quality of life of the patient. In some aspects, the compound is in an inhalable pharmaceutical composition.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
5.
PHARMACEUTICAL COMPOSITIONS OF ENSIFENTRINE FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE
Provided herein are pharmaceutical compositions and methods for providing blood plasma concentrations of ensifentrine to specific patient group populations including those with modified renal or hepatic impairment.
Provided herein are pharmaceutical compositions and methods for treating COPD or COPD exacerbations in subjects suffering from, for example, moderate COPD, or subjects with decreased eosinophil concentrations, or are suffering from chronic bronchitis. Also provided herein are methods of increasing trough lung function in subjects suffering from moderate COPD.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The disclosure relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt % to 0.60 wt % of 1,3-bis(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6, 1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt % to 0.50 wt % of a biuret impurity of formula (A) relative to the total weight of ensifentrine. Further disclosed herein are liquid pharmaceutical compositions comprising the particulate composition, and a process 10 for producing the particulate composition are also described.
The present invention relates to a compound for use in a method of preventing or treating bronchiectasis in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the bronchiectasis is non-cystic fibrosis (non-CF) bronchiectasis. The invention also relates to a compound for use in a method of treating bronchiectasis in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the method comprises treating the bronchiectasis by (a) reducing the frequency of cough in the patient and/or (b) reducing sputum production and/or facilitating clearance of mucus from the lungs in the patient.
The present invention relates to a compound for use in treating chronic obstructive pulmonary disease (CORD) in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the patient has a blood eosinophil count of < 300 cells/μL.
The present disclosure relates to a compound for use in treating chronic obstructive pulmonary disease (COPD) in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the patient has a blood eosinophil count of <300 cells/μL, <150 cells/μL, or <100 cells/μL.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances; Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes; Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services; provision of medical information and services; information provided to patients and healthcare professionals concerning pharmaceutical products, vaccines, medical diseases and disorders and related treatments; Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
36 - Services financiers, assurances et affaires immobilières
Produits et services
Health insurance information, namely, providing information regarding prescription drug insurance coverage, prior authorizations, administration of claims procedures, co-pays, and appeals for physicians and patients; Financial administration of a patient assistance program for eligible patients to purchase prescription drugs at reduced prices, and providing information related thereto
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of cardiovascular, central nervous system, pulmonary, respiratory, autoimmune diseases and disorders for human use; Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma Scientific research for medical purposes in the field of the treatment of cardiovascular, central nervous system, pulmonary, respiratory, autoimmune diseases and disorders; Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma Medical treatment services for the treatment of cardiovascular, central nervous system, pulmonary, respiratory, autoimmune diseases and disorders; Provision of medical information and services; Information provided to patients and healthcare professionals concerning pharmaceutical products, vaccines, medical diseases and disorders and related treatments; Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; Provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma
The disclosure relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt % to 0.60 wt % of 1,3-bis(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt % to 0.50 wt % of a biuret impurity of formula (A) relative to the total weight of ensifentrine. Further disclosed herein are liquid pharmaceutical compositions comprising the particulate composition, and a process for producing the particulate composition are also described.
36 - Services financiers, assurances et affaires immobilières
Produits et services
Health insurance information, namely, providing information regarding prescription drug insurance coverage, prior authorizations, administration of claims procedures, co-pays, and appeals for physicians and patients; Financial administration of a patient assistance program for eligible patients to purchase prescription drugs at reduced prices, and providing information related thereto
The present invention relates to a process for producing a sterile liquid pharmaceutical composition suitable for administration by inhalation comprising ensifentrine particles, wherein the process comprises: (a) heating ensifentrine particles at a temperature of from 100° C. to 220° C. to obtain sterile ensifentrine particles; and (b) combining the sterile ensifentrine particles with a sterile liquid vehicle to produce the sterile liquid pharmaceutical composition suitable for administration by inhalation. A process for producing an ampule comprising the sterile liquid pharmaceutical composition is also described.
36 - Services financiers, assurances et affaires immobilières
Produits et services
Health insurance information, namely, providing information regarding prescription drug insurance coverage, prior authorizations, administration of claims procedures, co-pays, and appeals for physicians and patients; financial administration of a patient assistance program for eligible patients to purchase prescription drugs at reduced prices, and providing information related thereto.
36 - Services financiers, assurances et affaires immobilières
Produits et services
Health insurance information, namely, providing information regarding prescription drug insurance coverage, prior authorizations, administration of claims procedures, co-pays, and appeals for physicians and patients; financial administration of a patient assistance program for eligible patients to purchase prescription drugs at reduced prices, and providing information related thereto.
19.
PHARMACEUTICAL COMPOSITIONS COMPRISING RPL554 IN HFA-134A FOR ADMINISTRATION BY INHALATION
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) a suspension of particles comprising 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554); and (ii) a diluent which is 1,1,1,2-tetrafluoroethane (HFA-134a), wherein the liquid pharmaceutical composition is substantially free of surfactant. The invention also relates to a pressurised metered dose inhaler comprising the liquid pharmaceutical composition.
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
The disclosure relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt % to 0.60 wt % of 1,3-bis(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt % to 0.50 wt % of a biuret impurity of formula (A) relative to the total weight of ensifentrine. Further disclosed herein are liquid pharmaceutical compositions comprising the particulate composition, and a process for producing the particulate composition are also described.
The invention relates to a particulate composition comprising ensifentrine, wherein the particulate composition further comprises: from greater than 0.00 wt% to 0.60 wt% of 1,3-bis(2-(2-(mesitylimino)-9, 10-dimethoxy-4-oxo-6,7-dihydro-2H- pyrimido[6,1-a]isoquinolin-3(4H)-yl)ethyl)urea (BMIQU) relative to the total weight of ensifentrine; and from 0.00 wt% to 0.50 wt% of a biuret impurity of formula (A) relative to the total weight of ensifentrine. A liquid pharmaceutical composition comprising the particulate composition, and a process for producing the particulate composition are also described.
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 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
36 - Services financiers, assurances et affaires immobilières
Produits et services
Health insurance information, namely, providing information regarding prescription drug insurance coverage, prior authorizations, administration of claims procedures, co-pays, and appeals for physicians and patients; financial administration of a patient assistance program for eligible patients to purchase prescription drugs at reduced prices, and providing information related thereto.
The invention relates to a liquid pharmaceutical composition comprising a dose of a compound which is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the liquid pharmaceutical composition provides a blood plasma concentration of ensifentrine after administration by inhalation to a human subject having COPD, which blood plasma concentration of ensifentrine has: a mean Cmax Of from about 400 pg/mL to about 720 pg/mL; and/or a mean AUC0-tau of from about 2000 pg/mL*h to about 3000 pg/mL*h; and/or a mean Tmax at from about 0.6 hours to about 1.5 hours. The invention also provides a method of treating COPD.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
41 - Éducation, divertissements, activités sportives et culturelles
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Medical education and training services, namely, conducting classes and workshops and training to support patients undergoing medical therapy and treatment in the fields of health, wellness, healthcare, pharmaceuticals, pharmaceutical access, drug safety and drug compatibility and treatment of individuals, adherence to pharmaceutical protocols, and the diagnostic, prophylactic and therapeutic properties of pharmaceuticals. Providing patient support programs offering medical information to patients undergoing medical therapy and treatment for the purpose of evaluating therapeutic treatment options in the nature of providing a website featuring medical information; patient support program providing disease awareness and disease management information and materials, in the nature of providing a website featuring medical information to improve understanding by patients and caregivers about pharmaceutical information; and patient support program in the nature of health counselling relating to the treatment of respiratory disease; providing medical information.
The present invention relates to a compound for use in treating moderate COPD in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
The present invention relates to a compound for use in a method for decreasing the frequency and/or severity of chronic obstructive pulmonary disease (COPD) exacerbations in a patient suffering from COPD, wherein the compound is ensifentrine or a pharmaceutically acceptable salt thereof. The present invention also relates to a compound for use in a method for treating chronic obstructive pulmonary disease (COPD) in a patient, wherein: the compound is ensifentrine or a pharmaceutically acceptable salt thereof; and the patient is susceptible to COPD exacerbations.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a compound for use in a method of increasing trough lung function in a patient suffering from chronic obstructive pulmonary disease (COPD), wherein the compound is ensifentrine or a pharmaceutically acceptable salt thereof. The invention also relates to a compound for use in treating chronic obstructive pulmonary disease (COPD) in a patient, wherein: the compound is ensifentrine or a pharmaceutically acceptable salt thereof and the patient is susceptible to disturbed sleep.
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a process for producing a sterile liquid pharmaceutical composition suitable for administration by inhalation comprising ensifentrine particles, wherein the process comprises: (a) heating ensifentrine particles at a temperature of from 100° C. to 220° C. to obtain sterile ensifentrine particles; and (b) combining the sterile ensifentrine particles with a sterile liquid vehicle to produce the sterile liquid pharmaceutical composition suitable for administration by inhalation. A process for producing an ampule comprising the sterile liquid pharmaceutical composition is also described.
The invention relates to a liquid pharmaceutical composition comprising a dose of a compound which is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the liquid pharmaceutical composition provides a blood plasma concentration of ensifentrine after administration by inhalation to a human subject having COPD, which blood plasma concentration of ensifentrine has: a mean Cmax of from about 400 pg/mL to about 720 pg/mL; and/or a mean AUC0-tau of from about 2000 pg/mL*h to about 3000 pg/mL*h; and/or a mean Tmax at from about 0.6 hours to about 1.5 hours. The invention also provides a method of treating COPD.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a compound for use in a method of treating idiopathic pulmonary fibrosis in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the compound to the patient by inhalation. The present invention relates to a compound for use in a method of treating pulmonary fibrosis in a patient by improving lung function, or by preventing or reducing a reduction in lung function, which compound is ensifentrine or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the compound to the patient by inhalation.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. (1) Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
(2) Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. (1) Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
(2) Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
43.
ENSIFENTRINE (RPL-554) FOR THE TREATMENT OF MODERATE CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
The present invention relates to a compound for use in treating moderate COPD in a patient, which compound is ensifentrine or a pharmaceutically acceptable salt thereof.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a compound for use in a method of increasing trough lung function in a patient suffering from chronic obstructive pulmonary disease (COPD), wherein the compound is ensifentrine or a pharmaceutically acceptable salt thereof. The invention also relates to a compound for use in treating chronic obstructive pulmonary disease (COPD) in a patient, wherein: the compound is ensifentrine or a pharmaceutically acceptable salt thereof; and the patient is susceptible to disturbed sleep.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a compound for use in a method for decreasing the frequency and/or severity of chronic obstructive pulmonary disease (COPD) exacerbations in a patient suffering from COPD, wherein the compound is ensifentrine or a pharmaceutically acceptable salt thereof. The present invention also relates to a compound for use in a method for treating chronic obstructive pulmonary disease (COPD) in a patient, wherein: the compound is ensifentrine or a pharmaceutically acceptable salt thereof; and the patient is susceptible to COPD exacerbations.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
41 - Éducation, divertissements, activités sportives et culturelles
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Medical education and training services, namely, conducting classes and workshops and training to support patients undergoing medical therapy and treatment in the fields of health, wellness, healthcare, pharmaceuticals, pharmaceutical access, drug safety and drug compatibility and treatment of individuals, adherence to pharmaceutical protocols, and the diagnostic, prophylactic and therapeutic properties of pharmaceuticals. Providing patient support programs offering medical information to patients undergoing medical therapy and treatment for the purpose of evaluating therapeutic treatment options in the nature of providing a website featuring medical information; patient support program providing disease awareness and disease management information and materials, in the nature of providing a website featuring medical information to improve understanding by patients and caregivers about pharmaceutical information; and patient support program in the nature of health counselling relating to the treatment of respiratory disease; providing medical information.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
49.
STERILIZATION PROCESS OF STERILE LIQUID PHARMACEUTICAL COMPOSITION COMPRISING ENSIFENTRINE
The present invention relates to a process for producing a sterile liquid pharmaceutical composition suitable for administration by inhalation comprising ensifentrine particles, wherein the process comprises: (a) heating ensifentrine particles at a temperature of from 100C to 220C to obtain sterile ensifentrine particles; and (b) combining the sterile ensifentrine particles with a sterile liquid vehicle to produce the sterile liquid pharmaceutical composition suitable for administration by inhalation. A process for producing an ampule comprising the sterile liquid pharmaceutical composition is also described.
A61L 2/00 - Procédés ou appareils de désinfection ou de stérilisation de matériaux ou d'objets autres que les denrées alimentaires ou les lentilles de contactAccessoires à cet effet
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
52.
LIQUID PHARMACEUTICAL COMPOSITION COMPRISING ENSIFENTRINE AND GLYCOPYRROLATE
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) ensifentrine particles; (ii) glycopyrrolate; and (iii) a diluent, which diluent comprises water, wherein: the glycopyrrolate is dissolved in the diluent; the concentration of glycopyrrolate is less than or equal to 5.0 mg/mL; and the pH of the liquid pharmaceutical composition is from 3.0 to 6.0. The invention also relates to a nebuliser comprising the liquid pharmaceutical composition.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
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
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment
of respiratory conditions and disease, namely, chronic
obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the
research and development of pharmaceutical preparations for
the treatment of respiratory conditions and disease, in
particular, chronic obstructive pulmonary disease, cystic
fibrosis and asthma. Medical treatment services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma; provision of
medical information and services in the field of respiratory
conditions and disease, namely, chronic obstructive
pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. (1) Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
(2) Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. (1) Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
(2) Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. (1) Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
(2) Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Scientific research for medical purposes, namely, the research and development of pharmaceutical preparations for the treatment of respiratory conditions and disease, in particular, chronic obstructive pulmonary disease, cystic fibrosis and asthma. Medical treatment services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma; provision of medical information and services in the field of respiratory conditions and disease, namely, chronic obstructive pulmonary disease, cystic fibrosis and asthma.
The present invention relates to a dry powder pharmaceutical composition suitable for administration by inhalation comprising: (i) ensifentrine particles; (ii) coarse lactose particles having a Dv50 of from 40 μm to 80 μm; and (iii) fine lactose particles having a Dv50 of from 5 μm to 10 μm, wherein: the fine lactose particles are present in an amount of from 0.1 wt % to 6.0 wt % relative to the total weight to the dry powder pharmaceutical composition. Also provided is a dry powder inhaler comprising the dry powder pharmaceutical composition and medical use of the dry powder pharmaceutical composition.
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i) ensifentrine particles; (ii) glycopyrrolate; and (iii) a diluent, which diluent comprises water, wherein: the glycopyrrolate is dissolved in the diluent; the concentration of glycopyrrolate is less than or equal to 5.0 mg/mL; and the pH of the liquid pharmaceutical composition is from 3.0 to 6.0. The invention also relates to a nebuliser comprising the liquid pharmaceutical composition.
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
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
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a leukotriene receptor antagonist. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a CFTR potentiator or a CFTR corrector.
A61K 31/443 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'oxygène comme hétéro-atome du cycle
The present invention relates to a dry powder pharmaceutical composition suitable for administration by inhalation comprising: (i) ensifentrine particles; (ii) coarse lactose particles having a Dv50 of from 40 µm to 80 µm; and (iii) fine lactose particles having a Dv50 of from 5 µm to 10 µm, wherein: the fine lactose particles are present in an amount of from 0.1 wt% to 6.0 wt% relative to the total weight to the dry powder pharmaceutical composition. Also provided is a dry powder inhaler comprising the dry powder pharmaceutical composition and medical use of the dry powder pharmaceutical composition.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances. Scientific research for medical purposes. Medical services; provision of medical information and services; information provided to patients and healthcare professionals concerning pharmaceutical products, vaccines, medical diseases and disorders and related treatments.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and diseases, and, in particular, chronic obstructive pulmonary disease, asthma and COVID-19 Scientific research for medical purposes in the fields of respiratory conditions and diseases and, in particular, chronic obstructive pulmonary disease, asthma and COVID-19
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances for the treatment of respiratory conditions and diseases and, in particular, chronic obstructive pulmonary disease, asthma and COVID-19 Scientific research for medical purposes Medical services; provision of medical information and services; information provided to patients and healthcare professionals concerning pharmaceutical products, vaccines, medical diseases and disorders and related treatments
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations and substances. Scientific research for medical purposes. Medical services; provision of medical information and services; information provided to patients and healthcare professionals concerning pharmaceutical products, vaccines, medical diseases and disorders and related treatments.
73.
PHARMACEUTICAL COMPOSITIONS COMPRISING RPL554 IN HFA-134A FOR ADMINISTRATION BY INHALATION
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation comprising: (i)a suspension of particles comprising 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)- 3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554); and (ii) a diluent which is 1,1,1,2-tetrafluoroethane (HFA-134a),wherein the liquid pharmaceutical composition is substantially free of surfactant. The invention also relates to a pressurised metered dose inhaler comprising the liquid pharmaceutical composition.
The present invention relates to a novel nitrile derivative of a pyrimido[6,1-a]isoquinolin-4-one compound of formula (A). The invention further relates to a process for producing a compound of formula (A). The invention also relates to a process which comprises reducing a compound of formula (A). Compounds of the invention are useful in the production of compounds such as RPL554.
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention relates to a novel nitrile derivative of a pyrimido[6,1- a]isoquinolin-4-one compound of formula (A). The invention further relates to a process for producing a compound of formula (A). The invention also relates to a process which comprises reducing a compound of formula (A). Compounds of the invention are useful in the production of compounds such as RPL554. (A)
The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
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
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
A61K 31/46 - Aza-8-bicyclo[3.2.1]octaneSes dérivés, p. ex. atropine, cocaïne
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
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 oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a leukotriene receptor antagonist. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a CFTR potentiator or a CFTR corrector.
A61K 31/443 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'oxygène comme hétéro-atome du cycle
82.
SALT OF A PYRIMIDO[6,1-A]ISOQUINOLIN-4-ONE COMPOUND
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
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
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
A61K 31/46 - Aza-8-bicyclo[3.2.1]octaneSes dérivés, p. ex. atropine, cocaïne
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/46 - Aza-8-bicyclo[3.2.1]octaneSes dérivés, p. ex. atropine, cocaïne
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
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
The invention provides a compound for use in treating or preventing a disease or condition selected from cystic fibrosis, chronic obstructive pulmonary disease (COPD), asthma, mild pulmonary disease, bronchitis, bronchiectasis, idiopathic bronchiectasis, allergic bronchopulmonary aspergillosis, sinusitis, rhinosinusitis, CFTR-related metabolic syndrome (CRMS), pancreatitis, idiopathic chronic pancreatitis and Sjörgren's syndrome, or for use in preventing male infertility caused by congenital absence of the vas deferens, in a patient by modulating CFTR activity, which compound is 9,10-dimethoxy-2-(2,4,6- trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1- a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a composition comprising (i) 9,10-dimethoxy-2-(2,4,6- trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1- a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a leukotriene receptor antagonist. The invention also provides acomposition comprising (i) 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7- tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (ii) a CFTR potentiator or a CFTR corrector.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7- tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β2 -adrenergic receptor agonist.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7- tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
A liquid pharmaceutical composition for use in a pressurized metered dose inhaler (pMDI), which composition comprises a pharmaceutically acceptable addition salt of (i) carcainium, and (ii) sulfuric acid, hydrochloric acid, hydrobromic acid, maleic acid or 1-hydroxy-2-naphthoic acid(xinafoic acid).
A61K 9/72 - Préparations médicinales caractérisées par un aspect particulier à fumer ou inhaler
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 9/72 - Préparations médicinales caractérisées par un aspect particulier à fumer ou inhaler
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.
The invention is directed towards carcainium in the form of a salt having an anion An-, wherein An- is an anion of pharmaceutically acceptable acid for use in the treatment and/or suppression of cough, tussive attacks or tussive episodes in a patient.
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 9/72 - Préparations médicinales caractérisées par un aspect particulier à fumer ou inhaler
The invention is directed towards an inhalable composition comprising carcainium in the form of a salt having an anion An, wherein An is an anion of a pharmaceutically acceptable acid, which composition is a dry powder aerosol or a nebulized aerosol, and wherein the particles present in said aerosol have a mass median aerodynamic diameter (MMAD) of from about 3μηι to about 10μm.
A61K 9/72 - Préparations médicinales caractérisées par un aspect particulier à fumer ou inhaler
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinoIin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimetlioxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.
