31 results about "Tamibarotene" patented technology

The present invention provides a practical preparation form of Tamibarotene and dosage form thereof, which exhibit high absorptivity by the body with minimized toxicity, and which are safe and stable without any risk of contamination. It is provided a Tamibarotene capsule preparation which encapsulates a composition comprising an oil component as its base and Tamibarotene as an active ingredient dissolved in the base. It is preferred that the oil component be propylene glycol fatty acid esters or polyethylene glycols. It is also preferred that the Tamibarotene capsule preparation comprise 0.1-50 mg / mL of the Tamibarotene based on the oil component.

The present invention aims to provide a growth inhibitor for cancer stem cells resistant to existing anticancer drug therapies, which growth inhibitor acts on the cells through growth inhibition and apoptosis. The growth inhibitor for cancer stem cells contains a retinoid agonist, preferably tamibarotene, alone or in combination with a rexinoid agonist, preferably bexarotene, as an effective component(s). The growth inhibitor for cancer stem cells enhances the effects of various anticancer drugs when the growth inhibitor is used in combination with the anticancer drugs.

The invention relates to a medicine analyzing method and particularly relates to a method for measuring impurities in tamibarotene and a preparation thereof by using high performance liquid chromatography. Octadecyl silane bonding silica gel is used as a filling agent, a phosphoric acid buffer solution with a volume ratio of water to phosphoric acid being 2000:1-2000:5 is used as a mobile phase A, acetonitrile is used as a mobile phase B, and a gradient elution process is adopted to establish a sensitive, exclusive and comprehensive tamibarotene impurity detecting and analyzing method. The method can be adopted to effectively detect changes of impurities in production and storage processes of the tamibarotene, and has important practical significance to medicine quality control.

The invention provides an orally taken tamibarotene solid preparation. The solid preparation comprises tamibarotene, disintegrating agent, filling agent and lubricating agent, wherein the weight of the tamibarotene is 1%-2% of the weight of the solid preparation, the weight of the filling agent is 70%-90% of the weight of the solid preparation, the weight of the disintegrating agent is 8%-25% of the weight of the solid preparation and the weight of the lubricating agent is 0.5%-0.6% of the weight of the solid preparation. The orally taken tamibarotene solid preparation prepared according to the invention has high dissolution rate, content uniformity and stability, is beneficial to the promotion of the bioavailability of human body and is more suitable for clinical application. The invention also provides a preparation method and an application of the solid preparation.

The invention belongs to the technical field of medicine pharmaceutical synthesis, and particularly relates to a method for catalytically synthesizing tamibarotene through an acenaphthene imidazole n-heterocyclic carbine allyl palladium chloride compound, aiming at providing a novel synthesis method of tamibarotene. The method comprises the following steps of: by taking a novel acenaphthene imidazole n-heterocyclic carbine allyl palladium chloride compound with high catalytic activity as a catalyst; performing amide carbonylation coupled reaction under carbon monoxide in order to directly synthesize a key precursor of tamibarotene by such one step; and then simply hydrolyzing to obtain the target compound, namely, tamibarotene. According to the method, the catalyst adopted has high catalytic performance, so that the catalytic coupling reaction brings high yield; and the catalyst is naturally easily synthesized, the raw materials adopted in the synthetic line are easily available, so that such synthetic line has high competitive advantages and high utility value in industrial production.

The invention discloses a synthesis method for the (I) Linarotene (I), a leukemia treatment drug. The invention mainly proposes a novel synthetic route with the steps as follows: the aniline, and p-chlorocarbonyl benzoic methyl ester are used as the raw materials; the intermediate is the p-chlorocarbonyl benzoic methyl ester and can do the cyclization with the 2,5 - dichloro-2 ,5 - dimethyl hexaneunder the anhydrous condition to get the intermediate 4-[(5,6,7,8-tetrahydrocannabinol-5,5,8,8- tetramethyl-2-naphthalene) carbamoyl] methyl benzoate. After the hydrolysis, the 4-[(5,6,7,8-tetrahydrocannabinol-5,5,8,8- tetramethyl-2-naphthalene) carbamoyl] benzoate (I) can be made, that is, the Linarotene. The synthetic route is simple; the operation is convenient and conducive to the environmental protection; the invention is suitable for the industrial production.

The present invention comprises ternary compositions of tamibarotene and / or ammonium lactate in Pemulen for treatment of effects of aging.

The invention provides a water-soluble prodrug of tamibarotene, and a preparation method and applications thereof and belongs to the technical fields of organic compound synthesis and medical applications. The water-soluble prodrug of tamibarotene has favorable water solubility and suitable drug crystal form, and therefore, is suitable to be used as a raw material for medical preparations and especially suitable for preparing injections. Particularly, the invention provides medical acceptable salts of tamibarotene DMEA ester, which have the general formula (I), wherein HA is HCl, H2SO4, HNO3,H3PO4, HOAc, paratoluenesulfonic acid, maleic acid, succinic acid, citric acid or L(+)-tartaric acid.