70 results about "Treprostinil" patented technology

Provided are treprostinil derivatives with a reduced ability to form undesired impurities in a pharmaceutical formulation, such as a dry powder formulation, further containing a carboxyl group containing inactive ingredient, such as fumaryl diketopiperazine.

The present disclosure encompasses combinations of ralinepag with a cGMP-elevating agent or prostanoid such as riociguat, treprostinil, or iloprost for treating PAH. The disclosed combination therapy provides for advantages such as improved efficacy, improved safety, reduced doses and / or frequency of ralinepag and / or riociguat, reduced doses and / or frequency of ralinepag and / or treprostinil, and reduced doses and / or frequency of ralinepag and / or iloprost. In some embodiments, the clinical effectiveness of a reduced dose combination is additive or synergistic compared to that provided by the corresponding ralinepag, riociguat, treprostinil, and / or iloprost monotherapies.

The present invention relates to the field of chemical medicine, and provides a treprostinil derivative represented by formula I, an isomer or a pharmaceutically acceptable salt thereof, and each group is defined in the specification. The compound as shown in the formula I, the isomer or the pharmaceutically acceptable salt thereof can stay in the lung for a long time and slowly release treprostinil with an effective concentration after being administered through the lung, and can be used for treating pulmonary hypertension diseases and pulmonary fibrosis diseases. The compound as shown in the formula I and the isomer or pharmaceutically acceptable salt thereof provided by the invention are administered through lungs, so that the administration dosage can be greatly reduced, lower administration frequency and wider treatment window can be provided, systemic side effects and local lung irritation can be reduced, and the safety of medicines and the medication tolerance of patients can be greatly improved; and a new treatment choice is provided for patients with pulmonary hypertension and pulmonary fibrosis. # imgabs0 #

A process for manufacturing a Treprostinil-diketopiperazone dry powder for pharmaceutical use by spray drying a suspension without need to dissolve Treprostinil in an alcohol solution prior to processing. In some embodiments, the dry powder is for oral inhalation for pulmonary delivery using a dry powder inhaler.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

The present invention relates to a new prostacyclin for treating pulmonary hypertension. Specifically, the compound of the present invention has the structure as represented by formula (I), wherein the definition of each group and substituent is as described in the description. Compared with treprostinil and a salt thereof, the compound of the present invention has better right ventricular systolic pressure (RVSP) and a better Fulton index.

The present disclosure provides a liquid propellant-free pharmaceutical preparation including treprostinil. The pharmaceutical preparation can undergo a better nebulization effect in a soft mist inhaler than the existing treprostinil preparations. In addition, the active substance in the pharmaceutical preparation is stable during a storage period of 1 to 2 years or longer.

The present invention provides treprostinil or a pharma- ceutically acceptable salt or derivative thereof for use in a method of treating pulmonary hypertension in a subject diagnosed with or at risk of developing pulmonary hypertension, the treatment comprising the steps of: i) administering to the subject a first liquid composition comprising a first concentration of treprostinil or a pharma- ceutically acceptable salt or derivative thereof in aerosolized form for a first treatment period; and ii) administering to the subject a second liquid composition comprising a second concentration of treprostinil or a pharma- ceutically acceptable salt or derivative thereof in aerosolized form for a second treatment period following the first treatment period, wherein the second concentration of treprostinil or a pharma- ceutically acceptable salt or derivative thereof in the second liquid composition is higher than the first concentration of treprostinil or a pharma- ceutically acceptable salt or derivative thereof in the first liquid composition, and wherein the first and second liquid compositions are aerosolized and administered to the subject using a soft mist inhaler.

Compositions and methods for treating chronic obstructive pulmonary disease, interstitial lung disease, asthma, bronchitis, pneumonia, cystic fibrosis, pulmonary edema, sarcoidosis, idiopathic pulmonary fibrosis, pulmonary arterial hypertension, acute respiratory distress syndrome, and respiratory syncytial virus in a patient are presented. Embodiments of the composition include a combination of diethylcarbamazine (DEC) and a prostacyclin analogue, such as Beraprost, Beraprost sodium, Iloprost, Treprostinil, Treprostinil Palmitil, and Cicaprost. Other embodiments include fluvoxamine and / or a phosphodiesterase (PDE) inhibitor. Some embodiments of the composition are in the form of an aerosol, include a propellent, or are in an inhalation delivery device.

The present disclosure provides aerosol properties of a powder composition applied by a dry powder inhaler and a spray drying method. Also provided is a method for treating pulmonary hypertension (PH) in a patient comprising administering an effective amount of the powder composition once a day to the lung of the patient by inhalation with the dry powder inhaler. Further provided is a system for treating PH using the powder composition and the dry powder inhaler.

Provided are novel treprostinil salts as well as methods for making treprostinil salts.

The objective is to provide methods for treating interstitial lung disease, mitigating lung function decline in individuals with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in individuals suffering from ILD. [Solution] A method for treating pulmonary hypertension caused by a condition selected from chronic lung disease, hypoxia, and combinations thereof, comprising administering an effective amount of treprostinil, its prodrug, or a pharmaceutically acceptable salt thereof to a subject with pulmonary hypertension caused by a condition selected from chronic lung disease, hypoxia, and combinations thereof.

Provided are treprostinil derivatives with a reduced ability to form undesired impurities in a pharmaceutical formulation, such as a dry powder formulation, further containing a carboxyl group containing inactive ingredient, such as fumaryl dikctopiperazinc.

The invention relates to the technical field of health management, and discloses a pulmonary hypertension patient medication guidance system and method based on multi-modal adaptive fusion, and the system comprises a construction module which is used for training a support vector machine regression model through the sample data of each medication mode in each body weight interval, and obtaining a plurality of infusion parameter prediction models; the processing module is used for obtaining a target infusion parameter prediction model according to the medication mode and the weight value of the patient, and inputting the current hemodynamic index into the target infusion parameter prediction model to generate initial infusion parameters of treprostinil of the patient in the medication mode; and the guidance module is used for generating a medication guidance scheme of the patient in the medication mode based on the current cardiac function parameters, the environmental parameters and the genotype correction initial infusion parameters. According to the method, personalized medication guidance is provided for the pulmonary hypertension patients, the risks of adverse reaction or poor medication effect and the like caused by individual differences of the patients are reduced, and then doctors are assisted to make more scientific and reasonable medication decisions for the patients.

The invention relates to a treprostinil monohydrate crystal and a preparation method thereof. The present invention provides novel crystalline forms of treprostinil monohydrate, mixtures comprising the same, and methods of making the same.

Provided are methods of producing compounds, which are useful in synthesizing prostacyclin derivatives, such as treprostinil.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

Methods of treating of interstitial lung disease, reducing pulmonary function decline in a subject with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in a subject suffering from ILD are provided, wherein the methods include administration of treprostinil.

To provide prostacyclin compounds and compositions comprising the same.SOLUTION: Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.SELECTED DRAWING: None

This disclosure provides a dry powder composition of treprostol prodrug and a method of treating pulmonary hypertension (e.g., pulmonary arterial hypertension or PH associated with interstitial lung disease) in patients in need using said dry powder composition. The dry powder composition comprises: (a) about 0.5 wt% to about 5 wt% of a compound, its stereoisomers, or a pharmaceutically acceptable salt thereof; (b) about 10 wt% to about 61 wt% of leucine; and the remainder is (c) a sugar selected from the group consisting of trehalose and mannitol. The total of (a), (b), and (c) is 100 wt%, and R1 is tetradecyl, pentadecyl, hexadecyl, heptadecanyl, or octadecyl. The method of treating PH comprises administering an effective amount of the dry powder composition to the lungs of the patient by inhalation via a dry powder inhaler during an administration period.

The invention provides Treprostinil or a pharmaceutically acceptable salt or derivative thereof for use in a method of treatment of pulmonary hypertension in a subject being diagnosed with pulmonary hypertension or being at risk of developing pulmonary hypertension wherein the treatment comprises the steps of i) administering to said subject a first liquid composition comprising Treprostinil or a pharmaceutically acceptable salt or derivative thereof in a first concentration in aerosolized form for a first treatment period, and ii) administering to said subject a second liquid composition comprising Treprostinil or a pharmaceutically acceptable salt or derivative thereof in a second concentration in aerosolized form for a second treatment period following the first treatment period; wherein the second concentration of Treprostinil or a pharmaceutically acceptable salt or derivative thereof in the second liquid composition is higher than the first concentration of Treprostinil or a pharmaceutically acceptable salt or derivative thereof in the first liquid composition, and wherein the first and the second liquid compositions are aerosolized and administered to the subject using a soft mist inhaler.

A dry powder inhalation treatment for pulmonary arterial hypertension includes a dose of dry particles comprising greater than 25 micrograms of treprostinil enclosed in a capsule. The dry particles can include treprostinil, a wetting agent, a hydrophobicity modifying agent, a pH modifying agent and a buffer. A method of treating a patient having pulmonary arterial hypertension includes providing a patient a dry powder inhaler, providing the patient at least one capsule for use in the dry powder inhaler, the capsule including at least 25 micrograms of treprostinil.

The invention provides a synthesis method and application of a treprostinil chiral intermediate and a synthesis method of treprostinil, and relates to the technical field of pharmaceutical chemical synthesis. According to the synthesis method of the treprostinil chiral intermediate, provided by the invention, efficient synthesis of a key intermediate is realized by chemical synthesis methods of constructing a cyclopentanaphthalene skeleton through a Dieckmann reaction catalyzed by LiHMDS and the like in combination with a chiral alcohol preparation technology through asymmetric reduction of carbonyl reductase. The method is efficient, low in cost and environmentally friendly, the total yield is larger than or equal to 75%, the chiral purity ee is larger than or equal to 99%, the method is suitable for large-scale production, and core technical support is provided for large-scale patent medicine of treprostinil.

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

Provided are methods of producing compounds, which are useful in synthesizing prostacyclin derivatives, such as treprostinil.

To provide a dry powder inhalation treatment for pulmonary arterial hypertension, a method of treating a patient suffering from pulmonary arterial hypertension, a dry powder inhalation composition for treatment, and a method of producing particles for delivering a dry powder to the lungs of a patient with pulmonary arterial hypertension.SOLUTION: The dry powder inhalation treatment for pulmonary arterial hypertension includes a dose of dry particles comprising more than 25 micrograms of treprostinil enclosed in a capsule. The dry particles may include treprostinil, a wetting agent, a hydrophobicity modifying agent, a pH modifying agent, and a buffer. A method of treating a patient suffering from pulmonary arterial hypertension comprises the steps of providing the patient with a dry powder inhaler, and providing the patient with at least one capsule for use in the dry powder inhaler, the capsule containing at least 25 micrograms of treprostinil.SELECTED DRAWING: Figure 1

Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

To provide treprostinil derivatives that can act as prodrugs of treprostinil.SOLUTION: The present invention discloses a compound of formula (I), or a pharmaceutically acceptable salt thereof or the like (where R1 and R2 are independently hydrogen, alkylcarbonyl, alkoxyalkylcarbonyl or the like, where, both R1 and R2 are not hydrogen, and neither -OR1 nor -OR2 form acetate, benzoate or the like).SELECTED DRAWING: None