50 results about "Ambrisentan" patented technology

There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis.

There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.

The invention discloses an ambrisentan degradation product and a preparation method thereof. The ambrisentan degradation product is represented by formula I, is one of main impurities of ambrisentan raw materials or preparations thereof and the formula I can be used for analyzing the purity of ambrisentan, and can also be used for controlling the quality of ambrisentan. The preparation method of the product of the formula I is characterized in that a substitution reaction of 2,2-diphenyl acetaldehyde and a compound represented by formula II is carried out under the action of sodium hydride and other alkaline compounds.

The invention relates to a synthetic method of ambrisentan and belongs to the technical field of medicine chemistry. The method comprises the steps of taking a racemoid 1 as a reactant, performing L-proline methyl ester hydrochloride resolution on a compound 1 to obtain a crude product of compound 2, performing nucleophilic reaction on the crude product of the compound 2 and a compound 3 to obtain compound 4. After an enantiomer of the compound 2 of compound 1 is filtered our by resolution, methyl tertiary butyl ether phase obtained by extracting hydrochloric acid free filtrate is used for drying a solvent through distillation to obtain the crude product of the compound 2 which is directly subjected to nucleophilic reaction with the compound 3, a qualified compound 4 is obtained by a subsequent process purifying treatment (comprising decoloration and salifying), the process operation is simplified, process stability is enhanced, loss of the compound 2 caused by crystallization of methylbenzene or crystallization for multiple times is avoided, and cost of process materials is greatly reduced. Lithium amide and sodium-hydrogen are innovatively substituted by lithium hydrate, safety is higher, cost is lower, lithium hydrate is proper in alkalinity, and a reaction system has few impurity points and is suitable for industrialized amplification production.

The invention provides ambrisentan oral tablets and a preparation method thereof. The ambrisentan tablets contain the following ingredients in parts by weight of 1 part of ambrisentan, 8-25 parts of lactose, 3-10 parts of microcrystalline cellulose, 0.3-1.0 part of croscarmellose sodium and 0.05-0.5 part of magnesium stearate. The prepared ambrisentan tablets are smooth in surface, good in contentuniformity, high in dissolution rate, small in dissolution differences between batches, high in in vivo biological availability, simple in preparation technology, easy to operate, low in cost and good in repeatability, and preparation quality and medication safety can be notably elevated.

The invention belongs to the field of chemical synthesis, and discloses an improved method used for preparing ambrisentan. According to the improved method, 2-hydroxy-3-methoxy-3,3-diphenylpropionic ester and 4,6-dimethyl-2-methylsulfonylpyrimidine are subjected to condensation, and one-pot hydrolysis in tetrahydrofuran solvent so as to obtain ambrisentan racemate; and ambrisentan is obtained via resolution with (S)-1-phenylethylamine. The improved method is simple in operation, and high in yield, and is suitable for industrial production.

The present invention relates to a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan. It also relates to the use of a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan, as active ingredient for preventing and/or treating the retinal neurodegeneration induced by diabetes and/or aging.

The invention relates to a purifying method of small-particle-size ambrisentan, and belongs to the technical field of raw material medicine preparation. According to the technical scheme, firstly, anambrisentan crude product is dissolved in ethyl acetate, then temperature is reduced to -5 to 5 DEG C, and under stirring, 50-60% ethanol water with volume 1.5-3 times of that of the solvent in the first step is added in a flowing mode; stirring speed is 230-270 rpm, the speed of adding the ethanol water in a flowing mode is 8-15 ml/min, and after flowing adding is completed, stirring is conductedcontinuously for 4-5 hours; filtering is conducted, 50-60% ethanol water is used for washing filter cake, and drying is conducted. The invention provides a preparation method of the small-particle-size ambrisentan. A raw material medicine which can be used directly is provided for an ambrisentan preparation, environmental pollution is reduced, and a well working environment is provided for preparation workers.

The invention belongs to the field of pharmaceutical analysis, and relates to a method of using isocratic elution high performance liquid chromatography to separate ambrisentan and seven related substances thereof. The main technology characteristics comprise taking a C8 or C18 chromatographic column as a stationary phase, taking an acetonitrile/water/glacial acetic acid mixture as a mobile phase, optimizing the flow velocity and the column temperature, and setting the detection wave length to be 190-230 nm, so as to establish a rapid excellent separation system which is suitable for simultaneously separating ambrisentan and seven related substances thereof. The system employs an isocratic elution method and helps to reduce consumption of separation apparatuses, the experiment separation baseline is stationary, the noise is small, and the separation result reappearance is good. The method is wide in separation object, high in practicality, low in cost, friendly to environment, simple in experiment operation and controllable in separation conditions, is a novel quality control method for ambrisentan, also is a new method for detection analysis on seven related substances of ambrisentan, and has wide application.

The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to a novel intermediate useful in the preparation of ambrisentan and a process for the preparation of the intermediate. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I.

There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.