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78 results about "Treprostinil" patented technology

This medication is used to treat a type of high blood pressure in the lungs (pulmonary arterial hypertension).

Use of treprostinil to treat and prevent ischemic lesions

The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and / or prevention of ischemic lesions, such as digital ulcers, in subjects with scleroderma (including systemic sclerosis), Buerger's disease, Raynaud's disease, Raynaud's phenomenon and / or other conditions that cause such lesions. The invention also relates to kits for treatment and / or prevention of ischemic lesions, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
Owner:UNITED THERAPEUTICS CORP

Treprostinil administration using a metered dose inhaler

Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.
Owner:UNITED THERAPEUTICS CORP

Compounds and methods for delivery of prostacyclin analogs

This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:
Owner:UNITED THERAPEUTICS CORP

Combination therapies with cox-2 inhibitors and treprostinil

InactiveUS20120010159A1Less cardiovascular event riskSafe and effectiveBiocideDipeptide ingredientsTreprostinilPain management
The present invention is directed to compositions and methods for pain management, and for treating inflammation or an inflammation-associated disorder in a subject comprising administering to the subject a therapeutically effective amount of a COX-2 inhibitor and a therapeutically effective amount of a prostacyclin analog, such as treprostinil, a pharmaceutically acceptable salt thereof, or a treprostinil derivative described herein.
Owner:UNITED THERAPEUTICS CORP

Treprostinil derivatives and compositions and uses thereof

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.
Owner:CORSAIR PHARMA

Use of treprostinil to treat neuropathic diabetic foot ulcers

The present invention describes novel methods for using 9-deoxy-2′,9-α-methano-3-oxa-4,5,6-trinor-3,7-(1′,3′-interphenylene)-13,14-dihydro-prostaglandin F1 (also known as Treprostinil) or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and / or prevention of foot ulcers in subjects with diabetic neuropathy. The invention also relates to kits for treatment and / or prevention of foot ulcers, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
Owner:UNITED THERAPEUTICS CORP

Process for the preparation of treprostinil and derivatives thereof

A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.
Owner:SCIPHARM SARL

Synthesis Of Treprostinil And Intermediates Useful Therein

Treprostinil is prepared by a process which involves Pauson-Khan cyclization of an an alkene-substituted, alkyne-substituted benzene corresponding to formula: (I) where PMB represents para-methoxy benzyl protecting group and R1 and R2 are alcohol protecting groups. Following cyclization, the resulting compound can be subjected to several chemical trans-formations followed by alkylation, hydrolysis and salt formation to yield treprostinil sodium. The use of para-methoxybenzyl group as the phenolic protecting group confers several process advantages that result in simplified purification of the final product and improved yields.
Owner:EON LABS

Prostacyclin compounds, compositions and methods of use thereof

Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C2-C18 alkyl, branched C3-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, for example, for administration via subcutaneous or intravenous infusion to a patient in need of pulmonary hypertension treatment. 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.
Owner:INSMED INC

Carrier-Linked Treprostinil Prodrugs

The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).
Owner:ASCENDIS PHARM AS

Deep lung pulmonary delivery of treprostinil

Administration of aerosolized Treprostinil formulations may provide a more homogeneous lung deposition of treprostinil, whereby making deep lung delivery possible.
Owner:ARADIGM

Prostacylin compositions and methods for using the same

The present invention relates to pharmaceutical compositions comprising a prostacyclin, a cationic compound, and a surfactant. Particulate compositions, including liposomal, solid nanoparticulate prostacyclin compositions, including treprostinil formulations comprising cationic compound and the surfactant are also described. The present invention also relates to a system comprising the pharmaceutical composition and an inhalation device. Methods for treating pulmonary hypertension and portopulmonary hypertension with the compositions and systems described herein are also provided.
Owner:INSMED INC

Treprostinil treatment for interstitial lung disease and asthma

The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and / or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates to kits for treatment and / or prevention of such condition that include an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
Owner:UNITED THERAPEUTICS CORP

Treprostinil derivatives and compositions and uses thereof

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.
Owner:CORSAIR PHARMA

Protected aldehydes for use as intermediates in chemical syntheses, and processes for their preparation

A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (Formula (1)) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (1a): (Formula (Ia)) to form the m-hydroxy-substituted benzaldehyde of formula (1b): (Formula (Ib)) and then reacting compound (1b) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula (1).
Owner:SANDOZ INC

Treprostinil production

A method is disclosed for preparing a synthetic intermediate for treprostinil via a stereoselective alkyne addition reaction using a chiral inducing agent. Also described are methods of preparing treprostinil or a pharmaceutically acceptable salt thereof comprising the alkyne addition reaction as well as novel intermediates useful for synthesis prostacyclin derivatives. A functional alcohol protecting group protects the alcohol group from participating in reactions that are occurring in other parts of the molecule. The intermediate is later deprotected prior to conversion and hydrolyzing to obtain the final treprostinil product.
Owner:UNITED THERAPEUTICS CORP

Methods of manufacturing treprostinil and treprostinil derivative prodrugs

Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing 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). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.
Owner:INSMED INC

Protected Aldehydes For Use As Intermediates In Chemical Syntheses, And Processes For Their Preparation

ActiveUS20130211145A1High purityAmenable to scale up to industrial levelOrganic compound preparationKetenes preparationChemical synthesisTreprostinil
A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (Formula (1)) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (1a): (Formula (Ia)) to form the m-hydroxy-substituted benzaldehyde of formula (1b): (Formula (Ib)) and then reacting compound (1b) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula (1).
Owner:SANDOZ INC

Methods of manufacturing treprostinil and treprostinil derivative prodrugs

Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing 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). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.
Owner:INSMED INC

Intermediates for synthesizing treprostinil and preparation method thereof as well as the preparation method of treprostinil thereby

The present invention relates to intermediates for preparing treprostinil, a preparation method for same, and a preparation of treprostinil thereby. Specifically, the invention relates to a compound of formula (VI), the preparation thereof and the application of said compound for the synthesis of treprostinil (as represented by formula (I)). The method for the preparation of treprostinil comprises: obtaining the compound of formula (III) by means of reducing the compound of formula (VI) and deprotecting the hydroxy group thereof; reacting said compound of formula (III) with chloroacetonitrile followed by hydrolysis to obtain the treprostinil of formula (I). The present method has simple operation and high synthesis yields, and is suitable for large-scale production.
Owner:JIANGSU HENGRUI MEDICINE CO LTD

Dry powder compositions of treprostinil prodrugs and methods of use thereof

The present disclosure provides a dry powder composition of treprostinil prodrugs and a method of treating pulmonary hypertension (e.g., pulmonary arterial hypertension), portopulmonary hypertension, or pulmonary fibrosis in a patient in need thereof. The dry powder composition includes (a) from about 0.1 wt % to about 3 wt % of a compound of Formula (I):or an enantiomer, diastereomer, or a pharmaceutically acceptable salt thereof, (b) from about 0.01 wt % to about 3 wt % of DSPE-PEG2000, (c) from about 10 wt % to about 50 wt % of leucine, and the balance being (d) a sugar selected from the group consisting of trehalose and mannitol. The entirety of (a), (b), (c), and (d) is 100 wt %, and R1 is tetradecyl, pentadecyl, hexadecyl, heptadecyl, or octadecyl. The method includes administering an effective amount of the dry powder composition to the lungs of the patient by inhalation via a dry powder inhaler. In certain compositions and methods provided herein, R1 is hexadecyl, e.g., linear hexadecyl.
Owner:INSMED INC

Dermal and transdermal administration of treprostinil and salts thereof

The present disclosure provides methods, compositions, devices and systems for dermal and transdermal administration of treprostinil or salts thereof, and optionally an additional therapeutic agent. Treprostinil and salts thereof can be dermally or transdermally administered to treat any medical conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Owner:CORSAIR PHARMA

Sustained release trepostinil-compound microparticle compositions

Provided herein are new compositions comprising novel microparticles that are configured to provide a long acting release of one or more treprostinil compounds when administered to mammalian subjects. The microparticles of the invention are biocompatible and typically injectable through a needle or other injection system. The invention also provides methods of using such compositions, such as in the treatment of pulmonary arterial hypertension.
Owner:LUPIN HLDG BV
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