103 results about "Phosphodiesterase 5 inhibitor" patented technology

Formulations containing a PDE5 inhibitor, a water-soluble diluent, a lubricant, a hydrophilic binder, a disintegrant, and optional microcrystalline cellulose and / or a wetting agent, and their use in treating sexual dysfunction, are disclosed.

This invention relates to oral pharmaceutical compositions suitable for making pharmaceutical formulations for oral administration that provide for the rapid dissolution of the phosphodiesterase 5 inhibitor tadalafil. In particular, the pharmaceutical compositions comprise solid composites of tadalafil exhibiting high solubility and rate of dissolution. The invention further relates to methods of preparing these pharmaceutical formulations and the use of such pharmaceutical formulations for treating diseases associated with PDE5 inhibitors.

The invention features methods and compositions featuring a PDE5 inhibitor for treating or preventing a cardiac indication in a subject.

The invention relates to a preparing method of a phosphodiesterase 5 inhibitor tadalafil. D-methyl tryptophanate hydrochloride is adopted as an initial raw material, and is subjected to cyclization with heliotropin, N-acylation, aminolysis-cyclization, and other reactions to obtain a tadalafil crude product. The tadalafil crude product is recrystallized to obtain a tadalafil finished product. The method has characteristics of mild reaction conditions, short reaction time, high yield, good product stability and convenience for industrial production.

The invention belongs to the field of preparation of chemical raw medicaments, and more in particular relates to an improved preparation method for a phosphodiesterase 5 inhibitor tadalafil. A specific synthesis route is shown in the specification. The method comprises the following steps of performing Pictet-Spengler cyclization reaction and chloroacetyl chloride acylation on starting reactants (D-tryptophan methyl ester hydrochloride and piperonal) to obtain an intermediate product, directly performing subsequent reaction on the intermediate product without purification, preparing an intermediate 1-(1,3-benzodioxol-5-yl)-2-(chloracetyl)-2,3,4,9-tetrahydro-1H-pyridino-[3,4,-B]indol-3-thiophenate methyl by using a one-pot reaction method, performing column chromatography purification to obtain a single cis-isomer, and finally reacting the single cis-isomer with methylamine hydrochloride in the presence of an inorganic base to obtain the tadalafil.

The invention relates to a synthesis method for (6R, 12aR)-6-(1, 3-benzodioxane heterocyclas-5-base)-2-methyl-2, 3, 6, 7, 12, -12a-hexahydro pyrazinyl [1', 2':1, 6] pyridyl [3, 4-b] indole-1, 4-diketone in the technical field of the pharmaceutical engineering. With the D-methyl tryptophan and piperonal as raw materials, the cis-1, 3-disubstituted carboline intermediates are prepared and generated through the Pictet-Spengler cyclization and then the products called tadalafil are obtained through the acylation ammoniation of the 3-secondary amino group and the final MTX substitution and condensation close-loop. By adopting the acidic condition protic solvents in the invention, the trans-1, 3-disubstituted carboline intermediates generated through the Pictet-Spengler cyclization, which is a key step in the existing process, are converted into those with a cis-configuration, thus greatly enhancing the stereospecific configuration yield of the carboline intermediates so as to enhace the overal yield of the tadalafil with reaching the goal of optimizing and improving the synthesis process.

The present invention relates to methods of treating multidrug resistance in cancerous cells with phosphodiesterase (PDE) inhibitors, e.g., PDE5 inhibitors. More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic / antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent.

The present invention is concerned with the use of PDE5 inhibitors in medicine.

Methods useful for sustaining a reduction of non-alcoholic steatohepatitis are provided herein. Such methods may comprise administering to a subject in need thereof a sirtuin pathway activator and / or PDE5 inhibitor alone or in combination with an amount of a branched amino acid in free amino acid form, or a metabolite thereof. Also provided herein are compositions and kits for practicing any of the methods described herein.

The invention features methods and compositions featuring a PDE5 inhibitor for treating or preventing a cardiac indication in a subject.

The present invention encompasses oral formulations of a PDE5 inhibitor which provide rapid disintegration after introduction to the oral cavity, followed by buccal and / or sublingual absorption. The orally disintegrating formulations can be in a variety of dosage forms including lingual strip, sublingual strip, oral mist, rapidly disintegrating tablet, lyophilized wafer, granulated particles and gum. The formulations can include an extended release component that allows the PDE5 inhibitor to be swallowed for gastrointestinal absorption. Combination therapies with a second pharmaceutical agent known to cause a PDE5-treatable condition as a side effect, such as erectile dysfunction, are also described. The PDE5 inhibitor of the following chemical structure is particularly favored for these formulations: