35 results about "Tafluprost" patented technology

The present invention discloses a method of purification of prostaglandins including fluorine atoms by using preparative HPLC. Tafluprost and Travoprost are prostaglandins including fluorine. The chemical structure of the impurities in crude Tafluprost and crude Travoprost also contain fluorine, therefore, the removal of the impurities is difficult. Purification by using preparative high performance liquid chromatography (HPLC) can achieve high-quality liquid bulk drugs.

The invention relates to a tafluprost eye drop and a preparation method thereof. The eye drop takes tafluprost as an active ingredient and also contains a non-ionic solubilizer and a pharmaceutically acceptable carrier, wherein the non-ionic solubilizer is polyethylene glycol-15-hydroxyl stearate. According to the invention, the problem of low solubility of tafluprost in the preparation process can be solved, the stability of tafluprost in an aqueous solution can be increased, and formation of related substances is reduced.

The present invention provides a new pharmaceutical application of a 15,15-difluoroprostaglandin F2α derivative. As a result of intensive studies in order to find a new pharmaceutical application of a 15,15-difluoroprostaglandin F2α derivative, it was found that, in a European Phase III clinical trial for tafluprost, one of the 15,15-difluoroprostaglandin F2α derivatives, with patients with open-angle glaucoma or ocular hypertension, tafluprost has actions of growing eyelashes, making eyelashes thicker, and changing the color thereof, that is, has an effect of promoting the growth of hair (eyelashes). Therefore, a 15,15-difluoroprostaglandin F2α derivative is useful as a hair growth promoting agent, and is expected to be useful as an active ingredient of a preventive or therapeutic agent for a disease associated with hair such as alopecia and a hair care product or a hair cosmetic product for regrowing hair, growing hair, increasing hair density, nourishing hair, or the like.

The invention relates to a novel method of synthesizing tafluprost. The method comprises the following steps: after suitable protection by Corey Lactone, reducing by DIBAL (Diisobutylaluminium hydride); carrying out Wittig reaction, carboxyl protection and Swern oxidization to obtain a universal intermediate compound 1; and by taking the intermediate 1 as a raw material, carrying out reactions to obtain tafluprost (deprotection step is not taken into consideration, and fluorination is the last step) and a plurality of intermediate products. The intermediate 1 is connected with different omega chains to synthesize other various prost analogues such as misoprost, travoprost and latanoprost. 2-4 prost analogues can be further used for synthesizing other 16-phenoxyl prost.

The invention provides a pharmaceutical composition for use in the prevention or therapy of glaucoma, increased intraocular pressure, ocular hypertension and / or a symptom associated therewith, whereinthe composition comprises tafluprost and a semifluorinated alkane.

A composition for preventing or treating glaucoma or ocular hypertension including a combination of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl} pyridin-2-ylamino) acetate and at least one other drug for preventing or treating glaucoma or ocular hypertension, with the proviso that tafluprost is excluded.

The invention discloses a preparation method of Tafluprost. The preparation method comprises the following steps: adopting a compound of formula 1 as a raw material, and carrying out the steps of DIBAL-H reduction, a Wittig reaction and an esterification reaction, wherein alkaline amino acids are adopted for refining after the Wittig reaction. According to the preparation method disclosed by the invention, the total mass yield of the three-step reaction can reach 70%, the technology is stable, a prepared Tafluprost product is colorless or faint yellow thick oily liquid, and the purity reaches up to more than 99%.

The invention discloses a preparation method of a tafluprost raw material drug, which comprises the preparation and separation of a high-efficiency preparation liquid phase, and the beating of C6-C8 alkane; the preparation method of the invention is stable in process and strong in operability, and can obtain other The total purity of the fluprostin is greater than 99.5%, wherein the impurity content of the trans isomer is less than 0.1%, and the content of other simple impurities is less than 0.1%.