The present disclosure provides a taxane compound and a preparation method and application thereof. The preparation method includes: protecting two hydroxyl groups in gemcitabine, conducting a condensation reaction between the protected gemcitabine and alkyl chloroformate, and removing of hydroxyl protecting groups to obtain an intermediate G1; protecting a first hydroxyl group of the intermediate G1, and then protecting the other one of the hydroxyl groups, and removing a protecting group of the first hydroxyl group to obtain an intermediate G2; reacting 7,10-di-troc-docetaxel with dianhydride to obtain an intermediate D1; conducting a condensation reaction between the intermediate D1 and the intermediate G2 to obtain an intermediate D2; and subjecting the intermediate D2 to hydroxyl deprotection to obtain a target product comprising the disclosed taxane compound.
C07D 305/14 - Composés hétérocycliques contenant des cycles à quatre chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 405/14 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie
C07H 1/00 - Procédés de préparation des dérivés du sucre
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers. The disclosed compounds are useful for treating a neoplasm in mammalian subjects. The cytidine derivative dimer has the following general formula (I).
n2-Ph-, where n, n1, and n2 are an integer from 0 to 3. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.
The present disclosure provides a new cytidine derivative having the general formula (I), and applications thereof:
As demonstrated by experiments on the growth inhibition effect of the new cytidine derivative of the present invention on HCT-116 colon cancer xenografts in tumor-bearing nude mice, the compound of the present invention has high anti-tumor activity, data of impacts on weight of nude mice bearing human colon cancer HCT-116 and data of mortality rate showed that the toxicity of the compound is comparatively low.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
Provided are a cytidine derivative and an application thereof, having the general formula (I): the cytidine derivative has a growth inhibitory effect, confirmed by testing, on transplanted colon cancer HCT-116 tumors borne by nude mice, thus the cytidine derivative has high antitumor activity, while the impact on the body weight of the colon cancer HCT-116 tumor-bearing mice, as well as mortality rate data, prove the low toxicity of the compound.
C07H 19/04 - Radicaux hétérocycliques contenant uniquement des atomes d'azote comme hétéro-atomes du cycle
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
The present invention provides the cytidine derivative dimer of general formula (I), and an application thereof. The cytidine derivative dimer has a significant inhibitory effect on human colon cancer HCT-116 tumor cells, and has a strong inhibitory effect on transplanted human colon cancer HCT-116 tumors borne by nude mice. The cytidine derivative dimer of the present invention has strong antitumor activity and low toxicity.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
Disclosed are a new type of cytidine derivative dimer, having the general formula (I), and an application thereof. By means of the optimized molecular design of a cytidine compound, the cytidine derivative dimer of the present invention has a significant inhibitory effect on human colon cancer HCT-116 tumor cells, while at the same time having a strong growth inhibitory effect on a transplanted human colon cancer HCT-116 tumor borne by nude mice; the new type of cytidine derivative dimer compound of the present invention has very high antitumor activity, while the toxicity of the compound is low.
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
C07H 1/00 - Procédés de préparation des dérivés du sucre
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
Disclosed are a new type of cytidine derivative, having the general formula (I), and an application thereof. The new type of cytidine derivative of the present invention has a growth inhibitory effect, confirmed by testing, on transplanted colon cancer HCT-116 tumors borne by nude mice; the antitumor activity of the compound of the present invention is high, while the impact on the body weight of the colon cancer HCT-116 tumor-bearing mice, as well as mortality rate data, prove the low toxicity of the compound.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
8.
ENGINEERING BACTERIA PRODUCING GENTAMICIN CLA AND USE THEREOF
Provided is a gntK function-inactivated engineering bacteria producing gentamicin Cla and the use thereof, wherein the engineering bacteria is Micromonospora purpurea GK1101, registered and deposited in the China General Microbiological Culture Collection Centre with deposit number CGMCC No.5245 on 13 September 2011. The engineering bacteria can be used for preparing anti-microbial drugs.
The use of 2'-NH2-3',4'-dideoxy--1-N-acylated derivatives of aminoglycoside antibiotic in the preparation of pharmaceutical composition for treating drug-resistant bacterial infection, the preparation of the derivatives and the formulation thereof.
A61K 31/7036 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine ayant au moins un groupe amino lié directement au carbocycle, p. ex. streptomycine, gentamycine, amikacine, validamycine, fortimicines
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present disclosure provides a new cytidine derivative having the general formula (I), and applications thereof: (see formula I) As demonstrated by experiments on the growth inhibition effect of the new cytidine derivative of the present invention on HCT-116 colon cancer xenografts in tumor-bearing nude mice, the compound of the present invention has high anti- tumor activity, data of impacts on weight of nude mice bearing human colon cancer HCT-116 and data of mortality rate showed that the toxicity of the compound is comparatively low.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers that are useful for treating a neoplasm in mammalian subjects. A cytidine derivative dimer may have the following general formula (I): By molecularly designing such cytidine-based compounds, the disclosed cytidine- based derivative dimers/salts show significant inhibiting effects on HCT-116 human colon cancer cells, and exhibit strong growth inhibiting effects on HCT-116 human colon cancer xenografts grown in nude mice. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers. (see above formula)
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
The present disclosure provides a taxoid compound as shown in formula (I) and preparation method and use thereof, wherein the preparation method comprises the following steps of: firstly protecting the two hydroxyl groups of gemcitabine, then condensing same with alkyl chloroformate, and then removing the hydroxyl protecting group to obtain the intermediate G1; respectively protecting the hydroxyl group of G1 , and then removing the first hydroxyl protecting group to obtain the intermediate G2; reacting 7,10- di(trichloroethoxy carbonyl)docetaxel and dicarboxylic anhydride to obtain the intermediate D1; condensing D1 and G2 to obtain the intermediate D2; and deprotecting the carboxyl group of D2 to obtain the target product. The compound of formula (I) can be used to inhibit solid tumors such as gastrointestinal cancer, lung cancer, breast cancer and leukemia. (see above formula)
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
C07D 305/14 - Composés hétérocycliques contenant des cycles à quatre chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 405/14 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
brevets
