15 results about "Axitinib" patented technology

The present invention relates to a sustained-release biodegradable ophthalmic implant containing axitinib dispersed in a hydrogel for the long-term treatment of retinal diseases.

The present application provides an acesulfame implant which is stable, safe and can achieve at least 6 months of sustained release, can effectively treat various eye diseases including but not limited to glaucoma, cataract, retinal vein obstruction (RVO), uveitis, diabetic macular edema (DME) and age-related macular degeneration (wAMD and nAMD), etc., avoids repeated administration, reduces the formation of side effects, reduces the cost of drug use, and meets the high stability required by drug preparation in production, storage and transportation, has good application prospect, and meets the unmet clinical needs.

The present invention relates to an ocular implant comprising an amorphous solid dispersion (ASD) comprising a tyrosine kinase inhibitor (TKI), such as axitinib, and a polymer excipient. Further, the invention relates to methods of treatment using the ocular implant of the invention comprising the amorphous solid dispersion (ASD) in treating an ocular disease. According to the present invention, ocular diseases are treated by injecting an amorphous solid dispersion (ASD) or an ocular implant comprising the ASD into the eye, wherein the ocular implant releases the TKI. Moreover, the invention relates to processes for preparing an amorphous solid dispersion (ASD) and an ocular implant of the invention comprising an ASD.

The application discloses a preparation method of an intermediate of Axitinib and an intermediate of Axitinib as shown in formula VI. The application provides a preparation method of a compound as shown in formula VII, which comprises the following steps: performing ring formation reaction on a compound of formula VI in the presence of a base and a solvent to obtain the compound of formula VII. The Axitinib synthesis route provided by the application has the advantages of less steps, low cost, high purity of a synthesis product and no introduction of toxic substances.

A composition containing a molecular association in which axitinib is physically bound and a method for preparing the composition are disclosed. The composition contains a molecular association in which axitinib is physically bound, a solubilizer, a stabilizer, and an additive. The additive may include any one or more selected from a buffer, an osmotic pressure regulator, and a pH adjuster.

In a process of making Axitinib, a palladium catalyst is added to a mixture of 2-vinylpyridine and the protected intermediate of formula (III) to form protected-Axitinib of formula (IV).In the formulas, P is a protective group and X is I, Cl, Br, or trifluoromethanesulfonate. The palladium catalyst is prepared separately, before being added to the reaction mixture, and is made from a mixture of a palladium source, a ligand, and a base in a suitable solvent. By adding the palladium catalyst to this protected intermediate, the process can use lower amounts of palladium and can have faster reaction times.

Disclosed herein is an ophthalmic composition of an active ingredient that is poorly soluble in water. The ophthalmic composition comprises cyclodextrin, axitinib, and water, and is a clear solution having a pH of less than about 5.5. In accordance with embodiments of the present disclosure, the ophthalmic composition is a clarified solution that does not contain any water-insoluble precipitates therein.

This invention relates to the field of pharmaceutical intermediate synthesis technology, specifically disclosing a method for preparing 6-iodoinazole. The method uses 6-aminoinazole as a starting material, and in the presence of sodium thiosulfate pentahydrate and nitrate, it reacts with... N The reaction of -iodosuccinimide with 6-iodoindazole yields a highly efficient synthesis of 6-iodoindazole. The preparation method of this invention has the advantages of readily available raw materials, mild reaction conditions, simple operation, high product yield, and good purity. It can be mass-produced industrially, providing an efficient and feasible technical route for the preparation of intermediates for the anticancer drug axitinib, and solving the problems of high cost, complex processes, and poor environmental friendliness in existing 6-iodoindazole preparation methods.

The invention belongs to the technical field of medicines, and discloses a liposome for resisting angiogenesis and down-regulating PD-L1 protein as well as a preparation method and application of the liposome. According to the invention, the active targeting liposome which is modified by NGR and is co-loaded with axitinib and siRNAPD-L1 is prepared by a film dispersion method and a lipid co-extrusion method. The method is simple in preparation process, low in cost, good in stability and high in repeatability. On one hand, Axi / siRNAPD-L1-coated NGR-Lipo inhibits tumor microangiogenesis, reshapes a tumor vascular system, normalizes tumor vessels, inhibits tumor metastasis and improves a tumor immunosuppression microenvironment; on the other hand, PD-L1 protein on the surfaces of tumor cells is silenced, tumor immune escape is relieved, and tumor immunotherapy is enhanced. The Axi / siRNAPD-L1 coated NGR-Lipo realizes an enhanced anti-tumor effect by combining an anti-angiogenesis therapy and an immune checkpoint blocking therapy. The preparation process of the liposome is simple and rapid, is easy for large-scale and industrial production, and also has a better development prospect in the aspect of clinical application transformation.

The invention discloses a preparation method of a drug intermediate 6-iodoindazole. The method comprises the following steps: by taking 6-nitroindazole as a raw material, in an acetic acid solvent, in the presence of iodized salt and strong acid, firstly heating and stirring for pretreatment, then cooling the system to 0 DEG C, and then adding a sodium nitrite aqueous solution for reaction to obtain the target product 6-iodoindazole. The method provided by the invention has the advantages of easily available raw materials, high reaction selectivity, less three wastes, high total yield (87%) and the like, is safe and simple to operate, effectively overcomes the defects of harsh conditions, serious pollution and high cost of the traditional diazotization method, and provides a technical route with great industrial prospects for large-scale production of the key intermediate of the anti-cancer drug axitinib.

The invention relates to the technical field of organic chemistry, and particularly discloses a benzene ring stereoisosteric modified bicyclo [1.1. 1] pentane compound as well as a preparation method and application thereof, the technical core is that triplet-state carbene is inserted into bicyclo [1.1. 1] butane (BCB) under a photosensitive condition, and a new path for synthesizing C2-substituted BCP is developed. The spanning from a two-dimensional plane to a three-dimensional structure is realized by replacing a disubstituted benzene ring in a drug skeleton (such as Sonidegi and axitinib) with BCP. According to the bioisostere modification, the water solubility and metabolic stability of molecules are improved by utilizing an sp3 skeleton, the limitation that a benzene ring is easily oxidized by P450 enzyme is overcome, the compound is successfully endowed with remarkable cytotoxic activity, and experiments prove that by adjusting charge distribution and spatial conformation, the cytotoxic activity of the compound is remarkably improved. Important guidance is provided for development of active molecules with new purposes, and the project is funded by key support projects of Guangming advanced research institutes of Southern Science and Technology Universities.

The invention relates to a sustained release biodegradable ocular implant containing axitinib dispersed in a hydrogel for the treatment of a retinal disease for an extended period of time.

The present invention relates to a solid oral pharmaceutical for Axitinib, Ibrutinib and / or Palbociclib (API) or any other Kinase Inhibitor API with a novel, well defined method to enhance solubility of active pharmaceutical ingredients (API) with low solubility in aqueous media and use those enhanced API in a new approach of preparing modified and / or sustained release pharmaceutical formulation for API which are regularly not suitable for sustained release formulations because of their low solubility. This invention is applicable for small molecule API (molecular weight < 1000) for which the solubility can be enhanced by formation of a e.g., Cyclodextrin Complex regardless which Cyclodextrin or derivate thereof is employed according to the method described in this invention. Axitinib, Ibrutinib and / or Palbociclib and other Kinase Inhibitors can be found for treatment of malign tumor diseases and others.

The application belongs to the technical field of crystal form drug molecules, and particularly relates to an axitinib oxalate crystal form and a preparation method and application thereof. The axitinib oxalate crystal form provided by the application is composed of one molecule of axitinib, one molecule of oxalic acid and two molecules of water as a basic unit of the crystal form, has high solubility, good stability, a simple preparation method, good reproducibility and is suitable for industrialized production.

The invention relates to the field of pharmaceutical preparations and pharmaceutical crystal forms, in particular to a crystal form alpha of axitinib, a pharmaceutical composition containing the crystal form alpha of axitinib and application of the crystal form alpha of axitinib. The axitinib crystal form alpha provided by the invention has excellent solubility, stability, hygroscopicity and flowability, and both the axitinib crystal form alpha and the pharmaceutical composition containing the axitinib crystal form alpha have remarkably improved bioavailability. The preparation method of the crystal form alpha is simple, good in repeatability, high in yield, easy to operate, green, environmentally friendly, small in needed solvent amount and beneficial to recycling, the reagent cost can be effectively reduced, and large-scale production is easy to achieve.