138 results about "Cytarabine" patented technology

Methods of treating, preventing or managing antecedent hematologic disorders, such as myelodysplastic syndrome, including chronic myelomonocytic leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.

The present invention relates to the use of BI 6727 or a salt thereof or the hydrate thereof for treating patients suffering from acute myeloid leukemia (AML) comprising the administration of a high dose of BI 6727 according to a specific dosage schedule, optionally in combination with cytarabine.

The invention belongs to the technical field of medicines and discloses cytarabine 5'-O-amino-acid ester, pharmaceutically acceptable salts thereof and a preparation method thereof. The preparation method comprises the following steps of: slowly dropping carbobenzoxy chloride into a solution formed by cytarabine, sodium bicarbonate and N,N-dimethylacetylamide, and obtaining a compound A after reacting at room temperature; using the compound A and N-butyloxy formoxyl-amino acid as raw materials; adding a reagent to the solution to carry out an esterification reaction to obtain the cytarabine 5'-O-amino-acid ester; and then adding acid to obtain a finished product. The pharmaceutically acceptable salts comprise hydrochlorides, sulfates, formates, acetates, mesylates, propionates, butyrates, p-toluene sulphonates, phosphates, bisulfates, maleates, lactates, carbonates, bicarbonates, malonates, and salts formed with acidic amino acids, and the like. The invention can obviously improve the membrane permeability of the cytarabine so as to improve the bioavailability of the cytarabine.

The invention discloses a compound of chemical formula I and its preparation method and application. In the compound of chemical formula I: M and V are mutually cis, and MH is cytarabine; the 5' oxygen of the above cytarabine Linked to phosphorus; V is 4-pyridyl; and pharmaceutically acceptable drug precursors and salts thereof.

The present invention provides a new type balloon dilation catheter which includes ballon and medication material coated on stent. Said medication material comes from one or two and more than two mixtures of heparin sodium, fiber degrading enzyme, serine proteinase, batroxobin, aspirin, genistein, hirudin and its recombined product, colchicine, sirolimus, biolimus, zotarolimus, tracrolimus, pimecrolimus, simvastatin, atorvastatin, pravastatin, ciclosporin, Anti-CD34, dexamethasone, bleomycin, plicamycin, daunomycin, mitomycin C, actinomycin D, taxol, celastrol, methopterin, 5-fluorouracil, cytarabine and 6-purinethol. The balloon is made of macromolecule nylon material, and the stimulation to blood vessel is far lower than the stent with metal structure.

The invention discloses a conjugate of fatty aminoacyl alexan, preparation and application in anti-tumor thereof. The invention also discloses a pharmacosome of the conjugate of fatty aminoacyl alexan, preparation thereof, and its applicant in anti-tumor and preparation of target medicine material of microemulsion, lipid medicine carrier. In comparison with alexan, the inventive conjugate of fatty aminoacyl alexan has a strong transmembrane ability, high bioavailability, long halflife, and amphipathic nature. It is demonstrated that the inventive compound and pharmacosome have great anti-tumor activity.

The invention discloses a phosphoryl N-fatty acyl nucleoside analogue for treating viral hepatitis and liver cancer. The phosphoryl N-fatty acyl nucleoside analogue is characterized in that a nucleoside analogue is modified by a cyclophosphoryl group and then is connected to aliphatic chains having different numbers of carbon atoms. The phosphoryl N-fatty acyl nucleoside analogue can be used for convenient preparation of a nanometer transmission system and has obvious hepatocyte and tumor targeting. The nanometer transmission system comprises liposome, nonionic surfactant niosomes, nanoparticles, nano-emulsion and a self-assembled transmission system. The nucleoside analogue is selected from lamivudine, adenine arabinoside, cidofovir, gemcitabine, cytosine arabinoside, azacitidine and fludarabine. After intravenous administration, the nanometer transmission system of the phosphoryl N-fatty acyl nucleoside analogue has effects of targeting treatment on viral hepatitis and liver cancer.

A stent having a drug eluting formulation has three components: 1) Anti-neointimal hyperplasia or anti-restenosis agent 2) Main polymer 3) Additive polymer The anti-neointimal hyperplasia or anti-restenosis agent includes, but not limited to, Paclitaxel, Taxol, Rapamycin, Tacrolimus, Actinomycin D, Methotrexate, Doxorubicin, cyclophosphamide, and 5-fluorouracil, 6-mercapatopurine, 6-thioguanine, cytoxan, cyclosporine, cytarabinoside, cis-platin, chlorambucil, busulfan, and any other drug that can inhibit cell proliferation, and combinations thereof. The main polymer includes, but not limited to, polystyrene, parylene and polyurethane. The additive polymer includes, but not limited to, polyethylene glycol capped with diisocyanate moiety (NCO-PEG). TABLERatio between three components without solvent%ComponentformulationAgent1-10%Main polymer80-98% Additive1-19%polymer9.0 g of parylene, 0.6 g of tacrolimus, 0.4 g of NCO-PEG and 0.01 g of triethylene amine were dissolved in 90 g of tetrahydrofuran. The resulting mixture was heated at 40° C. for 30 minutes and cooled to room temperature. To the solution was added 0.1 g of pH 8.0 aqueous solution and mixed thoroughly. The resulting solution is applied to bare metal stents for coating.

The invention provides novel anti-cancer precursor medicaments using NGR(NO2) as a targeting carrier. The novel anti-cancer precursor medicaments are prepared by designing and synthesizing a 5-fluorouracil precursor medicament, a lenalidomide precursor medicament, a cytarabine precursor medicament, an epirubicin precursor medicament and a dasatinib precursor medicament. According to the initial research on the anti-tumor activity of the 5-fluorouracil precursor medicament, the 5-fluorouracil precursor medicament can inhibit the invasion and metastasis of tumor cells and the growth of solid tumors. The 5-fluorouracil precursor medicament is modified in both effectiveness and preparation compared with the 5-fluorouracil serving as a parent medicament and is widely applicable. Concretely, the invention mainly relates to three aspects: (1) design and antiangiogenic effect of a novel tumor-targeted tripeptide NGR(NO2); (2) preparation of anti-cancer precursor medicaments by coupling the tumor-targeted tripeptide NGR(NO2) and 5 anti-cancer medicaments through covalent bonds; and (3) antitumor and antiangiogenic medical use of the novel 5-fluorouracil precursor medicament.

Compounds of Formula I, their preparation and uses are described:wherein:M and V are cis to one another and MH is cytarabine;the 5′ oxygen of said cytarabine is attached to the phosphorus;V is 4-pyridyl;and pharmaceutically acceptable prodrugs and salts thereof.

The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.

The invention relates to novel anti-tumor cytarabine prodrug derivatives through chemically modifying the N4 and O5 positions of cytarabine to prevent N4 amino being metabolized to lose efficacies and result in toxicity and let O5 hydroxy be easily phosphorylated for activation and introducing multifunctional groups of aspirins to the prodrug modules of the cytarabine to increase the drug functions for improving the anti-solid tumor activities. The invention also provides multiple synthesis routes of the cytarabine prodrug derivatives, a cytarabine prodrug derivative preparation and a preparation method thereof in detail and proves the purposes of the cytarabine prodrug derivatives at the aspect of resisting cancers and tumors through a great amount of experimental data. The cytarabine prodrug derivatives have a multi-targeting function and the advantages of increasing bioavailability, reducing multiple drug resistance and increasing solubility and ester dissolution.

The present invention relates to a method of treating patients with solid tumors, leukemias, and other malignancies using a combination of zosuquidar, daunorubicin, and cytarabine. The invention is also directed to pharmaceutical formulations comprising zosuquidar, daunorubicin, and cytarabine. The formulations are particularly effective in treating relapsed Acute Myelogenous Leukemia (AML).

Described are methods and compositions for treating cancer that include a dopamine receptor (DR) antagonist such as thioridazine and a chemotherapeutic agent. Optionally, the chemotherapeutic agent is a DNA synthesis inhibitor such as cytarabine or a microtubule inhibitor such as paclitaxel or docetaxel. The methods and compositions are useful for the treatment of cancers such as acute myeloid leukemia.

Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.

A kit and method for predicting cytarabine sensitivity of patients having acute myeloid leukemia are disclosed.

The present invention relates to a method of treating patients with solid tumors, leukemias, and other malignancies using a combination of zosuquidar, daunorubicin, and cytarabine. The invention is also directed to pharmaceutical formulations comprising zosuquidar, daunorubicin, and cytarabine. The formulations are particularly effective in treating relapsed Acute Myelogenous Leukemia (AML).

The invention discloses a technology for producing cytarabine through a chemical synthesis method, relating to a synthesis technology of an organic compound and aiming to provide a technology for producing the cytarabine through the chemical synthesis method, which has the advantages of cheap and available raw material, simple reaction condition, low cost, environmental protection and high yield. Based on the solving technical scheme, the technology for producing the cytarabine through the chemical synthesis method has a synthetic route which comprises the following synthesis steps of: firstly, reacting the cytarabine (1) used as a starting raw material with hexamethyldisilazane (HMDS) for 10-80h under the pressure of 5-20kg and at the temperature of 70-160 DEG C, cooling, stirring and vacuum concentrating a reaction system, and removing and recovering redundant hexamethyldisilazane to obtain an intermediate (II), wherein the dosage of the hexamethyldisilazane is 2-10 times larger than the weight of the cytarabine; secondly, dissolving the intermediate (II) into a proper solvent, and cooling or stirring to prepare crude cytarabine. The invention is used for preparing an anticancer drug.

The invention discloses application of AZA (Anchoic Acid) in preparation of acute myelogenous leukemia (AML) resistant and chemosensitization drugs. Through demonstration, AZA has a killing effect on multiple AML cell strains (U937, THP-1, KG-1, NB4, and HL-60), and can be used for inhibiting the proliferation of AML cells and simultaneously inducing cell apoptosis, and can be combined with Arac in use to promote the killing effect of Arac on the AML cells. AZA does not have any toxic and side effects, and the price can be accepted by most patients; and AZA can be combined with chemotherapeutics, namely Arac in use to promote the killing effect of Arac on the AML cells, and also to reduce the dosage of Arac to alleviate the toxic and side effects caused by chemotherapy, so that a new approach and method is provided for treatment and curing of the AML.

The invention relates to applications of cytarabine or an analogue of cytarabine and ketorolac or an analogue of ketorolac in treating cachexia, and in particular provides a medicinal composition for treating cachexia. According to the scheme, for the first time, one or more of cytarabine or the analogue of cytarabine and ketorolac or the analogue of ketorolac are creatively adopted as the active ingredients of the composition for treating cachexia, and remarkable treatment effects are obtained in the animal experiment. Based on the severity degree of cachexia, the medicinal composition has the broad clinical application prospect.

The invention belongs to the field of material synthesis and biological medicine, and relates to a dual-drug controlled release system with pH and glutathione dual response and a preparation method thereof.The dual-drug controlled release system is constructed by adopting mesoporous silica, and sodium hyaluronate serves as a gating material to block pore channels of the mesoporous silica; Mesoporous channels of the mesoporous silica are loaded with cytarabine. The mesoporous silica, the chitosan and the sodium carboxymethyl cellulose form a gel system, and methotrexate is loaded in the gel system. The preparation method has the beneficial effects that the prepared pH and glutathione dual-response dual-drug controlled release system can load two anti-cancer drugs at the same time, and realizes the successive release of the two drugs in a subacid tumor environment and a high-concentration glutathione environment. The double-drug controlled release system is simple to prepare and high in biocompatibility, and can be widely applied to the field of biological medicines.

The invention provides a preparation method of cytarabine 5'-O-L-valine ester hydrochloride (structural formula 1) and an intermediate thereof. According to the invention, cytarabine (formula 5) is adopted as a raw material, and a one-step amino protection reaction is carried out, such that a substance represented by a structural formula 3 is obtained; the substance represented by the structural formula 3 and N'-tert-butoxycarbonyl-L-valine are subjected to a reaction with chloroformate or acyl chloride under the existence of alkali, or the substance represented by the structural formula 3 and N'-tert-butoxycarbonyl-L-valine salt are subjected to an esterification reaction under the effect of chloroformate or acyl chloride, such that a substance represented by a structural formula 2 is obtained; and protection group is removed under the effect of hydrogen chloride, such that the substance represented by the structural formula 1 is obtained. The method provided by the invention has the advantages of easy operation, simple post-treatment, no need of column chromatography purification, high selectivity, high reaction yield, and low cost. The method is suitable for industrialized productions.

The invention discloses a vitamin A acyl cytosine arabinoside conjugate with amphipathic and a pharmacome formed by the conjugate. The invention also discloses preparation methods and the application as the antitumor agent of the conjugate and the pharmacome. The invention enables RA and cytosine arabinoside 4'-amido to be coupled so as to obtain the vitamin A acyl cytosine arabinoside conjugate with amphipathic, and the conjugate has the characteristic of self assembly of the pharmacome, thereby not only protecting the cytosine arabinoside 4'-amido from devitalizing, but also enabling the conjugate and prepared pharmacome to have the tumor targeting ability. The invention respectively takes human leukaemia cells HL-60 and S180 ascites carcinoma mousse to value the antineoplastic activity of a compound of formula I and the pharmacome prepared by the compound in vivo and in vitro, and test results show that the compound of formula I and the pharmacome thereof have excellent antineoplastic activity.

The invention relates to application of small RNAs in the field of preparing medicaments for treating and / or preventing lymphoma, in particular to the application of small RNA-15a, small RNA-16-1, precursor of the small RNA-15a and precursor of the small RNA-16-1 or a mixture of more than two of the small RNA-15a, the small RNA-16-1, the precursor of the small RNA-15a and the precursor of the small RNA-16-1 in preparing the medicaments. The over expression of the oligonucleotide array sequences in lymphomatous cells proves that the oligonucleotide array sequences have effects of inhibiting the growth of the lymphomatous cells and promoting the apoptosis of the lymphomatous cells and further discloses that the use of the oligonucleotide array sequences in combination with chemotherapeutics such as cytarabine can strengthen the efficacy of original medicaments, thereby ensuring the application potential of the oligonucleotide array sequences in the field of preparing the medicaments for treating and / or preventing lymphoma. The medicaments can be a single composite containing an oligonucleotide array sequence or mixture of the oligonucleotide array sequences and a pharmaceutically carrier or a chemotherapeutic-containing composite for use in combination.

Provided herein are methods for treating cancer by administering a pharmaceutical composition comprising a fixed, non-antagonistic molar ratio of cytarabine and an anthracycline. Such methods are particularly useful in the treatment of patients with advanced hematologic cancers or proliferative disorders.

Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.

A method of treating a cancer comprising administering to a subject in need thereof an effective amount of a glycylcycline, for example tigecycline in combination with a chemotherapeutic such as daunorubicin or cytarabine.

The present invention relates to a method of treating patients with solid tumors, leukemias, and other malignancies using a combination of zosuquidar, daunorubicin, and cytarabine. The invention is also directed to pharmaceutical formulations comprising zosuquidar, daunorubicin, and cytarabine. The formulations are particularly effective in treating relapsed Acute Myelogenous Leukemia (AML).

The invention discloses a phospholipase A2 sensitive glycerin skeleton anti-tumor prodrug of which a molecular structure is a glycerin skeleton including a long-chain alkyl ether at a 1st position, a conjugated linoleoyl at a 2nd position and a phosphoryl nucleoside at a 3rd position. Because that a tumor tissue can highly express phospholipase A2, the glycerin skeleton anti-tumor prodrug has a tumor environmental specificity and can release a plurality of components which have activities on tumor cells at the position of the tumor. The components work in combination so that a high-efficient anti-tumor effect is achieved. An active compound of a nucleoside-type anti-tumor drug is selected from cytosine arabinoside, gemcitabine, capecitabine, fludarabine and derivatives thereof. The glycerin skeleton anti-tumor prodrug can be prepared into following high-dispersing preparations: a liposome, a nonionic surfactant vesicle, nano particles, a nano emulsion or a self-assembling transmission system.

The invention relates to cytarabine prodrug derivatives which are novel prodrug derivatives designed through chemically modifying N4 and O5 positions and can prevent N4 amino being metabolized to lose efficacies and result in toxicity; and in addition, the cytarabine prodrug derivatives let O5 hydroxy be easily phosphorylated for activation. The cytarabine prodrug derivatives have the advantages of increasing bioavailability, reducing multiple drug resistance (multi-targeting design technique) and increasing solubility and ester dissolution. The invention also provides a synthesis method of the cytarabine prodrug derivatives, a cytarabine prodrug derivative preparation and a preparation method thereof in detail and proves the purposes of the cytarabine prodrug derivatives at the aspect ofresisting cancers and tumors through a great amount of experimental data.