Formulations of fluorinated stilbene suitable for PET imaging

The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.

FORMULATIONS OF FLUORINATED STILBENE SUITABLE FOR PET IMAGING

The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention. 1. A pharmaceutical formulation comprising:Lipophilic Amyloid beta ligand stilbene and suitable salts thereof,Ethanol,Polyether,Ascorbic acid, andSodium ascorbate.2. The pharmaceutical formulation according to wherein the lipophilic Amyloid beta ligand stilbene is Methyl-[4-((F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine or mixture of Methyl-[4-((F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine and Methyl-[4-((18F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine claim 1 , and suitable salts thereof.3. The pharmaceutical formulation according to and defined as follows:0.03 GBq/mL to 5 GBq/mL Methyl-[4-((18F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine,8% v/v to 25% v/v Ethanol,10% w/v to 25% w/v Poly(ethylene glycol),0.01% to 3% w/v Ascorbic acid, and0.01% to 20% w/v Sodium ascorbate.4. The pharmaceutical formulation according to and defined as follows:0.03 GBq/mL to 5 GBq/mL Methyl-[4-((18F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine,15% v/v Ethanol,20% w/v PEG 400,0.44% w/v Ascorbic acid, and2.88% w/v Sodium ascorbate.5. The pharmaceutical formulation according to defined as follows0.01 μg/mL to 5 μg/mL Methyl-[4-((F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine or mixture of Methyl-[4-((F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine and Methyl-[4-((18F)-2-{4-[2-(2-propoxy-ethoxy)-ethoxy]-phenyl}-vinyl)-phenyl]-amine, and suitable salts thereof,8% v/v to 25% v/v Ethanol,10% w/v to 25% w/v Poly(ethylene glycol),0.01% to ...

TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAFENIB

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof but without hydrophobic silica and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising regorafenib , a hydrate , solvate or pharmaceutically acceptable salt of regorafenib , or a polymorph thereof as active agent and at least one pharmaceutically acceptable vehicle wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle and wherein the composition does not contain hydrophobic silica.2. The pharmaceutical composition of wherein the composition does not contain any stabilizer including colloidal silica claim 1 , hydrophilic or hydrophobic silicas.3. The pharmaceutical composition of containing regorafenib monohydrate as active agent.4. The pharmaceutical composition of wherein the active agent is in a solid form.5. The pharmaceutical composition of wherein the active agent is in a crystalline form.6. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.7. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.8. The pharmaceutical composition of wherein the pharmaceutically acceptable vehicle is selected from the group comprising oleoyl polyethyleneglycol gylcerides claim 1 , linoleoyl polyethyleneglycol gylcerides claim 1 , lauroyl polyethyleneglycol gylcerides claim 1 , liquid paraffin claim 1 , light liquid paraffin claim 1 , soft paraffin (vaseline) claim 1 , hard paraffin claim 1 , castor oil claim 1 , peanut oil claim 1 , sesame oil claim 1 , middle chain trigylcerides claim 1 , cetylstearylalcohols claim 1 , wool fat claim 1 , glycerol ...

Topical Ophthalmological Pharmaceutical Composition containing Pazopanib

The present invention relates to topical ophthalmological pharmaceutical compositions containing pazopanib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising pazopanib , a hydrate , solvate or pharmaceutically acceptable salt of pazopanib , or a polymorph thereof as active agent and at least one non-aqueous pharmaceutically acceptable vehicle and optionally at least one pharmaceutically acceptable excipient.2. The pharmaceutical composition of wherein the active agent is pazopanib hydrochloride.3. The pharmaceutical composition of which does not contain regorafenib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of regorafenib or a polymorph thereof.4. The pharmaceutical composition of which only contains pazopanib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of pazopanib or a polymorph thereof as single and only active agent and no other active agent.5. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.6. The pharmaceutical composition of wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle.7. The pharmaceutical composition of wherein the active agent is in a solid form.8. The pharmaceutical composition of wherein the active agent is in a crystalline form.9. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.10. The pharmaceutical composition of wherein the pharmaceutically acceptable vehicle is selected from the group comprising oleoyl polyethyleneglycol gylcerides claim 1 , linoleoyl polyethyleneglycol gylcerides claim 1 , lauroyl polyethyleneglycol gylcerides claim 1 , liquid ...

Topical Ophthalmological Pharmaceutical Composition containing Axitinib

The present invention relates to topical ophthalmological pharmaceutical compositions containing axitinib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising axitinib , a hydrate , solvate or pharmaceutically acceptable salt of axitinib , or a polymorph thereof as active agent and at least one pharmaceutically acceptable vehicle and optionally at least one pharmaceutically acceptable excipient.2. The pharmaceutical composition of which does not contain regorafenib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of regorafenib or a polymorph thereof.3. The pharmaceutical composition of which only contains axitinib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of axitinib or a polymorph thereof as single and only active agent and no other active agent.4. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.5. The pharmaceutical composition of comprising further pharmaceutically acceptable excipients like stabilizers claim 1 , surfactants claim 1 , polymer base carriers like gelling agents claim 1 , organic co-solvents claim 1 , pH active components claim 1 , osmotic active components and preservatives.6. The pharmaceutical composition of wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle.7. The pharmaceutical composition of wherein the active agent is in a solid form.8. The pharmaceutical composition of wherein the active agent is in a crystalline form.9. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.10. The pharmaceutical composition of wherein the pharmaceutically acceptable ...

TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING CEDIRANIB

The present invention relates to topical ophthalmological pharmaceutical compositions containing cediranib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising ceridanib , a hydrate , solvate or pharmaceutically acceptable salt of ceridanib , or a polymorph thereof as active agent and at least one pharmaceutically acceptable vehicle and optionally at least one pharmaceutically acceptable excipient.2. The pharmaceutical composition of which does not contain regorafenib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of regorafenib or a polymorph thereof.3. The pharmaceutical composition of which only contains ceridanib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of ceridanib or a polymorph thereof as single and only active agent and no other active agent.4. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.5. The pharmaceutical composition of comprising further pharmaceutically acceptable excipients like stabilizers claim 1 , surfactants claim 1 , polymer base carriers like gelling agents claim 1 , organic co-solvents claim 1 , pH active components claim 1 , osmotic active components and preservatives.6. The pharmaceutical composition of wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle.7. The pharmaceutical composition of wherein the active agent is in a solid form.8. The pharmaceutical composition of wherein the active agent is in a crystalline form.9. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.10. The pharmaceutical composition of wherein the pharmaceutically acceptable ...

TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING SUNITINIB

The present invention relates to topical ophthalmological pharmaceutical compositions containing sunitinib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising sunitinib , a hydrate , solvate or pharmaceutically acceptable salt of sunitinib , or a polymorph thereof as active agent and at least one pharmaceutically acceptable vehicle and optionally at least one pharmaceutically acceptable excipient.2. The pharmaceutical composition of which does not contain regorafenib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of regorafenib or a polymorph thereof.3. The pharmaceutical composition of which only contains sunitinib claim 1 , a hydrate claim 1 , solvate or pharmaceutically acceptable salt of sunitinib or a polymorph thereof as single and only active agent and no other active agent.4. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.5. The pharmaceutical composition of comprising further pharmaceutically acceptable excipients like stabilizers claim 1 , surfactants claim 1 , polymer base carriers like gelling agents claim 1 , organic co-solvents claim 1 , pH active components claim 1 , osmotic active components and preservatives.6. The pharmaceutical composition of wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle.7. The pharmaceutical composition of wherein the active agent is in a solid form.8. The pharmaceutical composition of wherein the active agent is in a crystalline form.9. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.10. The pharmaceutical composition of wherein the pharmaceutically acceptable ...

TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAGENIB

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. 1. A topical ophthalmological pharmaceutical composition comprising regorafenib , a hydrate , solvate or pharmaceutically acceptable salt of regorafenib , or a polymorph thereof as active agent and at least one pharmaceutically acceptable vehicle wherein the composition is a suspension comprising the active agent suspended in the applicable pharmaceutically acceptable vehicle.2. The pharmaceutical composition of containing regorafenib monohydrate as active agent.3. The pharmaceutical composition of wherein the active agent is in a solid form.4. The pharmaceutical composition of wherein the active agent is in a crystalline form.5. The pharmaceutical composition of wherein the active agent is in a microcrystalline form.6. The pharmaceutical composition of wherein the concentration of the active agent in the pharmaceutical composition is from 0.01 to 10% by weight of the total amount of the composition.7. The pharmaceutical composition of wherein the pharmaceutically acceptable vehicle is selected from the group comprising oleoyl polyethyleneglycol gylcerides claim 1 , linoleoyl polyethyleneglycol gylcerides claim 1 , lauroyl polyethyleneglycol gylcerides claim 1 , liquid paraffin claim 1 , light liquid paraffin claim 1 , soft paraffin (vaseline) claim 1 , hard paraffin claim 1 , castor oil claim 1 , peanut oil claim 1 , sesame oil claim 1 , middle chain trigylcerides claim 1 , cetylstearylalcohols claim 1 , wool fat claim 1 , glycerol claim 1 , propylene glycol claim 1 , polyethyleneglycols (PEG) or a mixture of those claim 1 , water or a mixture thereof.8. The pharmaceutical composition of based on a non-aqueous vehicle.9. The pharmaceutical composition of based on a hydrophobic vehicle.10. ...

TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAFENIB

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof but without hydrophobic silica and its process of preparation and its use for treating ophthalmological disorders.

Topical ophthalmological pharmaceutical composition containing regorafenib

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.

TYPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAFENIB

La presente invención se refiere a composiciones farmacéuticas oftalmológicas que contienen regorafenib, un hidrato, solvato, metabolito o sal aceptables desde el punto de vista farmacéutico del mismo o un polimorfo del mismo pero sin sílice hidrofóbica y su procedimiento de preparación y su uso para tratar trastornos oftalmológicos

Topical ophthalmological pharmaceutical composition comprising regorafenib, a hydrate, solvate or a salt thereof, or a polymorph thereof and at least one vehicle; procedure to elaborate it; and procedure to treat or prevent an ophthalmological disorder selected from retinitis pigmentosa, glaucoma and cataracts, among others.

Acceptable fluorinated stilbene formulations for PET imaging

Formulación farmacéutica que comprende - estilbeno ligando de amiloide beta lipófilo y sales aceptables del mismo, - etanol (8% v/v a 25% v/v), - poliéter (10% p/v a 25% p/v), - ácido ascórbico (0,01% p/v a 1,5% p/v), y - ascorbato de sodio (1,5% p/v a 5% p/v). Pharmaceutical formulation comprising - stilbene beta lipophilic amyloid ligand and acceptable salts thereof, - ethanol (8% v / va 25% v / v), - polyether (10% w / v 25% w / v), - ascorbic acid (0.01% w / v 1.5% w / v), and - sodium ascorbate (1.5% w / w 5% w / v).

topical ophthalmic pharmaceutical composition containing regorefenib

TYPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAFENIB

La presente invención se refiere a composiciones farmacéuticas oftalmológicas tópicas que contienen regorafenib, un hidrato, solvato o sal farmacéuticamente aceptable del mismo o un polimorfo del mismo y su procedimiento de preparación y su uso para el tratamiento de trastornos oftalmológicos. The present invention relates to topical ophthalmic pharmaceutical compositions containing regorafenib, a pharmaceutically acceptable hydrate, solvate or salt thereof or a polymorph thereof and its preparation process and its use for the treatment of ophthalmic disorders.

Formulations of fluorinated stilbene suitable for pet imaging

The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.

Topical ophthalmological pharmaceutical composition containing regorafenib

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.

Formulations of fluorinated stilbene suitable for pet imaging

Topical ophthalmological pharmaceutical composition containing pazopanib

The present invention relates to topical ophthalmological pharmaceutical compositions containing pazopanib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.

Formulations of fluorinated stilbene suitable for pet imaging

The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.

Formulations of fluorinated stilbene suitable for pet imaging

fluorinated stilbene formulations suitable for pet imaging

resumo patente de invenção: "formulações de estilbeno fluorado adequadas para imagiologia pet". a presente invenção refere-se à formulações de estilbeno com capacidade ligante a beta amiloide lipofílico e mais particularmente a formulações que são capazes de ser administradas parenteralmente, por exemplo, de forma intravenosa, em que o estilbeno com capacidade ligante a beta amiloide lipofílico é um estilbeno fluorado. ademais, a invenção é direcionada a um método para a filtração estéril de formulações adequadas para imagiologia pet de mamíferos de acordo com a invenção. patent summary: "fluorinated stilbene formulations suitable for pet imaging". The present invention relates to lipophilic beta amyloid-binding stilbene formulations and more particularly to formulations which are capable of being administered parenterally, for example intravenously, wherein the lipophilic beta-amyloid-binding stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for mammalian pet imaging according to the invention.

Topical ophthalmological pharmaceutical composition containing sunitinib

The present invention relates to topical ophthalmological pharmaceutical compositions containing sunitinib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.

Topical ophthalmological pharmaceutical composition containing regorafenib

The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders.

Formulación farmacéutica de polvo seco para inhalación y proceso de preparación

La presente invención se refiere a formulaciones farmacéuticas de polvo seco, que comprenden ácido (5S)-{[2-(4-carboxifenil)etil][2-(2-{[3-cloro-4’-(trifluorometil)bifenil-4-il]metoxi}fenil)etil]-amino}-5,6,7,8-tetrahidroquinolin-2-carboxílico de fórmula (1), preferiblemente en forma de una de sus sales o solvatos o hidratos, preferiblemente ácido (5S)-{[2-(4-carboxifenil)etil][2-(2-{[3-cloro-4’-(trifluorometil)bifenil-4-il]metoxi}fenil)etil]-amino}-5,6,7,8-tetrahidroquinolin-2-carboxílico monohidrato I de fórmula (1-M-I) o ácido (5S)-{[2-(4-carboxifenil)etil][2-(2-{[3-cloro-4’-(trifluorometil)bifenil-4-il]metoxi}fenil)etil]-amino}-5,6,7,8-tetrahidroquinolin-2-carboxílico monohidrato II de fórmula (1-M-II) en combinación con un portador de lactosa, que comprende lactosa monohidrato como mezcla de lactosa gruesa y lactosa fina, y al proceso de manufactura de dichas formulaciones farmacéuticas de polvo seco y su aplicación para usar en el tratamiento de trastornos cardiopulmonares, tales como hipertensión arterial pulmonar (PAH), hipertensión pulmonar tromboembólica crónica (CTEPH) e hipertensión pulmonar (PH) asociada con enfermedad pulmonar crónica (PH grupo 3) tal como hipertensión pulmonar en la enfermedad pulmonar obstructiva crónica (PH-EPOC) e hipertensión pulmonar con neumonía intersticial idiopática (PH-IIP).

Treatment of cardiopulmonary disorders

The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the ...

Treatment of cardiopulmonary disorders

The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (PAH), chronic tromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 µg, preferably 480 to 2000 µg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of ...

Pharmaceutical dry powder inhalation formulation

The present invention relates to pharmaceutical dry powder formulations, comprising (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid monohydrate (II) of formula (I-M-II) in combination with a lactose carrier, comprising lactose monohydrate as a mixture of coarse lactose and fine lactose, and to the process of manufacturing such pharmaceutical dry powder formulations and its application for use in the treatment of cardiopulmonary disorders, such as pulmonary arterial hypertension (PAH), chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP).

Treatment of cardiopulmonary disorders

Pharmaceutical dry powder inhalation formulation

Treatment of cardiopulmonary disorders

The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic tromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the ...

Treatment of cardiopulmonary disorders

The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (PAH), chronic tromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 µg, preferably 480 to 2000 µg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4'-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of ...