49 results about "7-ethyl-10-hydroxycamptothecin" patented technology

The present invention relates to methods of treating a HER2 positive cancer in mammals. The present invention includes administering a HER2 antagonist in combination with a polymeric prodrug of 7-ethyl-10-hydroxycamptothecin to the mammals in need thereof.

A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as,is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.

The method of manufacturing of 7-ethyl-10-hydroxycamptothecin of formula I characterized in that 7-ethyl-1,2,6,7-tetrahydrocampotothecin of formula IV is oxidized with an oxidizing agent selected from the group comprising iodosobenzene, an ester of iodosobenzene, sodium periodate, potassium periodate, potassium peroxodisulfate and ammonium peroxodisulfate, in a solvent formed by a saturated aliphatic monocarboxylic acid containing 1 to 3 carbon atoms, and in the presence of water.

The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxy-camptothecin to patients in need thereof.

The invention provides application of a curcumin on preparation of a medicine for preventing or / and treating a late diarrhea caused by an anti-tumor medicine, wherein the anti-tumor medicine is irinotecan or an active metabolite 7-thyl-10-hydroxycamptothecine (SN-38), and the late diarrhea is a severe diarrhea capable of lasting for 7 days appeared after the irinotecan is administrated for 24 hours. The curcumin provided by the invention is definite in efficacy; and with the adoption of the curcumin, the late diarrhea can be effectively relieved and the intestinal mucosa is protected.

The invention discloses a 7-ethyl-10-hydroxycamptothecine drug precursor, a preparation method and an application thereof. A structure formula of the drug precursor is represented as the formula I or II. The drug precursor is prepared through an esterification reaction between a C-10 hydroxyl group or a C-20 hydroxyl group of 7-ethyl-10-hydroxycamptothecine and a hydrophobic molecule. The drug precursor has excellent anti-tumor activity and can directly release active components in vivo in a hydrolysis manner without catalytic hydrolysis of carboxylesterase, thereby achieving a high bioavailability. The drug precursor not only has excellent solubility in water but also has great solubility in amphipathic surfactants, such as tween-80 and the like, wherein the solubility can reach more than 30 mg / ml, and a high stability is achieved even that the drug precursor is diluted in water. The drug precursor can be prepared just through a one-step esterification method, is high in yield and low in preparation cost, is high in stability and good in safety, satisfies requirements in clinical medication and in large-scale industrial production, and has excellent market prospect and clinical application value.

The invention provides a method for synthesizing and purifying irinotecan. The method prepares irinotecan that is an antineoplastic compound with high purity quotient through the purification of 7-ethide-10-hydroxycamptothecine that is an intermediate for synthesizing irinotecan and crystallization for impurity removal of hydrochloric piperidyl piperidine formyl chloride; secondary reaction is reduced, and the purity quotient as well as the yield of products are increased through improving the reaction condition at the same time, especially through cryoconcentration evolution; the purity quotient of the obtained products is more than 99.5 percent, and the single hetero is less than 0.1 percent. In addition, the method overcomes the disadvantages that the cycle is long, the solvent quantity is large, etc. caused by column chromatography that is used for purifying the products, and large scale production is easy to realize.