596 results about "Fluorouracil" patented technology

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

A method of preparing and using a sterile non-toxic pyrogen-free cold extract from the leaves of Nerium oleander as a supplementary medication to cancer chemo-, hormon and / or radiotherapy to restore and / or ameliorate the immune system of the patient and / or to decrease side effects and increase the antitumor effects of radiotherapy and chemotherapeutics, particularly when used in combination with taxol, adriamycin, cisplatin, 5-fluoro-uracil, alimta, cyclophosphamide, mitomycin-C, navelbine, taxotere and topotecan, respectively, and its use in the manufacture of a medicament for the treatment of one or more cancers of bladder, kidney, liver, ovary, pancreas, testicle, uterus, and vagina as well as pleuramesotheliomas and Hodgkin's lymphomas.

The invention relates to biodegradable fluorouracil(Fu) polyester drug-bearing manoparticles with a coating material of polylactic acid, polylactic acid-glycolic acid, polylactic acid-polyethylene glycol block copolymer or polylactic acid-glycolic acid-polyethylene glycol block copolymer and the producing method including: firstly, fully dissolving the copolymer in the dichloromethane, under the ultrasonic shock, injecting the fluorouracil NaOH solution in the dichloromethane solution, dispersing uniformly, forming W / O primary latex, and beating up the primary latex and injecting into the fluorouracil saturated water solution containing 5 wt% of polyvinylalcohol (PVA), and storing in the refrigeratory after freeze-dry. The drug-bearing manoparticle has a drug content which is 10-25% of the microparticle mass, and has a smooth surface, an even diameter distribution, a remarkable slow release function and not adhesive. The micropartical size is 100-1000nm.

The present invention relates to a topically applicable formulation containing Valproic Acid or a derivative thereof which can be used alone or in combination with topically applicable formulations of retinoids or of nuclear receptor ligands, or of chemotherapeutic agents (e.g. 5-Fluorouracil). The formulation is useful for the topical treatment of cancerous skin disorders, such as Basal Cell Carcinoma, Squamous Cell Carcinoma, Keratoakantoma, Bowen Disease, cutaneous T-Cell Lymphoma and also for the topical treatment of pre-malignant lesions, and of inflammations of the skin and / or mucosa. The invention also relates to the use of this topically applicable formulation for the protection from UV light and for the treatment of sun burn. The invention includes the use of VPA for the manufacture of a clinically used medicament for the topical treatment of the human diseases listed above.

The invention relates to a degradable drug loading stent and a preparation method of the degradable drug loading stent. The degradable drug loading stent is characterized by comprising a skeleton structure made of a medical degradable metal or an alloy of the metal, a degradable macromolecular transition layer adhered to the surface of the skeleton structure and a drug loading layer. The degradable metal / macromolecular / drug multilayer composite stent provided by the invention has excellent mechanical property, degradable property and biocompatibility, and such drugs as taxol, taxol derivative, actinomycin D, 5-fluorouracil and sirolimus are loaded to the stent to perform active directional treatment on the focus position, so the stent is a functional degradable stent. The degradable multifunctional drug loading stent provided by the invention is suitable for interventional therapy in the blood vessel field and non-blood vessel fields and is especially suitable for interventional therapy of stenosis, obstruction or tumor of such non-blood vessel cavities as esophagus, bile duct, ductus pancreaticus, intestinal tract, urethral canal, trachea and bronchus, etc.

The present invention provides, for example, methods for treating or preventing colorectal cancer with an anti-IGF1R antibody in association with sunitinib or a combination of leucovorin and 5-fluorouracil.

Described are plant growth regulation compositions and methods utilizing combinations of Class A and Class B gibberellin biosynthesis inhibitors. Preferred methods and compositions involve the combination of trinexapac-ethyl with either or both of flurprimidol and paclobutrazol, in particular to provide a synergistic effect in the regulation of the growth of turfgrass.

The present invention provides a new approach for cancer treatment by utilizing gene therapy combined with radiation therapy to enhance cytotoxicity in malignant cells. Specifically, the present invention demonstrates that molecular chemotherapy with the cytosine deaminase gene and 5-fluorocytosine is an effective radiosensitizing strategy which may lead to substantial improvement in tumor control, with less normal tissue toxicity than conventional systemic administration of 5-fluorouracil, that would translate into improved cure rates and better survival. A noninvasive method is described for continuous in vivo monitoring of 5-fluorouracil production via magnetic resonance spectroscopy. An adenovirus encoding cytosine deaminase gene which selectively replicates in tumor cells with a defective p53 pathway was constructed. Also provided is an adenovirus which encodes a fusion protein of cytosine deaminase and uracil phosphoribosyltransferase.

A method and composition is provided for organ rescue wherein a specific counter-measure is applied locally to a tissue at risk for or exhibiting an adverse side effect of a cancer treatment. More particularly, the method and composition is directed at controlling Hand-Foot Syndrome, a painful redness and cracking of the skin of the hands and feet which can occur with systemic treatment with 5-fluorouracil or a precursor thereof. Uracil ointment is applied to the skin of the hands and feet to prevent Hand-Foot Syndrome which can occur from systemic administration of 5-fluorouracil (or precursor thereof) as cancer treatment.

Methods of treating a human body for cancer are provided. In one aspect, a therapeutic amount of capecitabine is administered in combination with ET-743 in a dose range between 0.75 and 1.4 mg / m2 for Et-743. In a related aspect, an effective therapeutic amount of ET-743 is administered in combination with capecitabine in a dose range between 1500 to 2500 mg / m / day for capecitabine.

The invention relates to a intraocular lens. At present the Poly-Methyl Methacrylate (PMMA) intraocular lens conventional for clinical treatment of cataract always causes inflammatory treaction after implantation. Posterior capsule opacification is also a major compalication after cataract surgery. The invention selects fluorouracil to solve the above problems. Based on weak penetrating force of chitosan nanoparticles in eyes and the relation between the phagocytosis amount of conjunctival epithelial cells to nanoparticles and the particle size of nanoparticles, the fluorouracil nanoparticles preparation is prepared using chitosan-poly(acrylic acid) as carrier, composite coated on the surface of PMMA intraocular lens. The invantion also provides a preparation method thereof. The said intraocular lens not only increases the biocompatibility of the intraocular lens, but also inhibites posterior capsule opacification pafter cataract surgery. The said intraocular lens can also prevent anterior membrane after implantation of intraocular lens and after-cataract.

The invention discloses a medicinal composition for treating non-small cell lung cancer. The medicinal composition comprises a target medicament, a chemotherapeutic medicament and a traditional Chinese medicament, wherein the target medicament is one or more of bortezomib, imatinib, gefitinib and sunitinib; the chemotherapeutic medicament is one or more of 5-fluorouracil, carboplatin, epirubicin, adriamycin and fludarabine; and the traditional Chinese medicament is one or more of salvia miltiorrhiza, astragalus membranaceus, sappanwood, Chinese pulsatilla root and portulaca oleracea. The medicinal composition has a remarkable synergetic treatment effect when being used for treating the non-small cell lung cancer, and can be used for remarkably strengthening the cancer-inhibition effect compared with treatment of a single medicament, so that the medicament dosage can be reduced, and the toxic and side effects of chemotherapeutic medicaments can be reduced.

The invention belongs to the technical field of medicine, and specifically relates to an industrial tegafur synthesizing method comprising the steps that: under inert gas pressure control and the effects of a Lewis acid catalyst, 5-fluorouracil and 2,3-dihydrofuran are subjected to a substitution reaction in an aprotic polar solvent; and acidification and refining are carried out, such that tegafur is obtained. The method has the advantages of simple reaction process, high yield, less side reactions, mild reaction conditions, and the like. Pharmacopoeia standards can be satisfied with simple refining, and purity is higher than 99.7%.

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

Methods of treating cancer comprising administering a fibroblast growth factor receptor 1 (FGFR1) extracellular domain (ECD) and / or an FGFR1 ECD fusion molecule in combination with at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are provided. Dosage packs comprising an FGFR1 ECD and / or an FGFR1 ECD fusion molecule and / or at least one additional therapeutic agent selected from docetaxel, paclitaxel, vincristine, carboplatin, cisplatin, oxaliplatin, doxorubicin, 5-fluorouracil (5-FU), leucovorin, pemetrexed, and bevacizumab are also provided. In some embodiments, a dosage pack comprises instructions for administering FGFR1 ECD and / or FGFR1 ECD fusion molecule with at least one additional therapeutic agent.

The invention which belongs to the medicine processing field concretely relates to a preparation method of a long-circulating nanoparticle. The preparation method of the long-circulating nanoparticle provided in the invention has the advantages of simple operation, and good targeting and good in vitro release of products. The method comprises the following steps: 1, dissolving 5-Fu (5-fluorouracil), PEG-PHDCA (polyethylene glycol-poly(hexadecyl cyanoacrylate)) and a phosphatide in a mixed organic solvent of tetrahydrofuran and ethanol to form an organic phase; 2, slowly adding the organic phase to a water phase of a surfactant in a dropwise manner under magnetic stirring, and fully diffusing the organic phase by continuously stirring for 1h after finishing the dropwise addition; 3, carrying out reduced pressure evaporation to remove the organic solvent to obtain a nanoparticle colloidal suspension with a blue opalescence; 4, carrying out ultracentrifugation separation deposition on the nanoparticle, and washing; and 5, carrying out ultrasonic dispersion with a 4% mannitol solution, and freeze-drying.

The invention relates to the field of organic synthesis and medicine, and discloses a preparation method for N-substituted methyl-3,5-disubstituted benzylidene base-4-piperidone and biological activity for efficiently inhibiting cell line proliferation such as leukemia, ovarian cancer, breast cancer, liver cancer and esophagus cancer. The method includes: starting from various substituted methylamine and methyl acrylate, sequentially going through Michael addition, Dieckmann condensation, acidolysis and decarboxylation to obtain N-substituted methyl-4-piperidone, and subjecting the N-substituted methyl-4-piperidone to aldol reaction with substituted benzaldehyde to obtain a target compound N-substituted methyl-3,5-disubstituted benzylidene base-4-piperidone. The target compound can selectively and efficiently inhibit cell line proliferation such as leukemia, ovarian cancer, breast cancer, liver cancer and esophagus cancer, and activity of inhibiting carcinoma cell line proliferation is obviously higher than conventional chemotherapeutic 5-fluorouracil.

Hyaluronic Acid (HA) is an essential component of tissue extracellular matrices that contributes to the architecture of stem cell niches, which determine the fate of stem cells. Decreased levels of HA are found in subjects experiencing a variety of pathological conditions, as well as in subjects receiving a variety of therapeutic interventions, for example, chemotherapy or radiotherapy, to treat pathological conditions. The use of HA to reconstitute a tissue extracellular matrix partially or completely depleted of HA is described. More particularly, described herein is the use of exogenous forms of HA as an adjuvant in the restoration of the local tissue specific stem cell microenvironment to enhance stem cell recovery or engraftment and thus tissue recovery and remodeling following stem cell transplantation or other therapies. The effect of HA on hematopoietic stem cells is illustrative of the invention. Mice having severe bone marrow hypoplasia, and pancytopenia resulting from treatment with 5-fluorouracil recovered more rapidly if treated with HA. Similarly, mice transplanted with hematopoietic stem cells following lethal irradiation exhibited enhanced recovery of peripheral blood cell counts when treated with HA as an adjuvant therapy compared to control mice transplanted with hematopoietic stem cells without adjuvant therapy.

The present invention provides novel uses and compositions for 5,10-methylene tetrahydrofolate (“5,10-CH2-THFA”) in the treatment of cancer. The present invention is based on the surprising result that 5,10-CH2-THFA, while increasing the efficacy of 5-fluoruracil (5-FU) in reducing the rate of tumor growth and increasing survivorship, also reduces the toxicity to the patient of 5-FU. The present invention provides methods and compositions for treating cancer patients that include 5-FU, 5,10-CH2-THFA, and one or more additional anticancer drugs. Such methods and compositions can provide increased efficacy and reduced toxicity when compared with current treatment modalities.

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 present invention provides antibiofilm composition comprising two or more agents selected from the group consisting of DispersinB™, 5-Fluorouracil, Deoxyribonuclease I and Proteinase K for preventing growth and proliferation of biofilm-embedded microorganisms in wound care, oral care, and disease-related infections and methods of treatment in mammals. The invention further provides methods for preparing medical devices, and wound care devices using an antibiofilm composition comprising two or more antimicrobial agents selected from the group consisting of DispersinB™, 5-Fluorouracil, Deoxyribonuclease I and Proteinase K.

The invention discloses a 1,3,4-thiadiazole fluorouracil compound as well as a preparation method and application thereof. The compound has a general formula I, wherein R is substituted phenyl, aromatic heterocycle or aryloxy alkyl; the substituent group R1 in tri-substituted phenyl is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl, R2 is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl, and R3 is hydrogen, nitryl, alkoxyl, halogen atom, alkyl, substituted alkyl or phenoxyl; and the aromatic heterocycle is pyridine, thiofuran, furan, indole or isoindole. The invention has less compound consumption, good insecticidal effect, simple process method, low cost and wide market prospect.

The invention provides a pharmaceutical co-crystal of 5-fluorouracil and proline and a preparation method of co-crystal and relates to the pharmaceutical co-crystal field. The co-crystal is [2C4H3FN2O2.C5H9NO2], and a basic structural unit is formed by virtue of two 5-fluorouracil molecules and a proline molecule. The co-crystal is of a monoclinic system, and the space group of the co-crystal is P21 / n. The pharmaceutical co-crystal is prepared from 5-fluorouracil and proline by virtue of a solvent evaporation method and a cooling method. According to the pharmaceutical co-crystal, the solubility of 5-fluorouracil is improved, and a foundation is laid for the increase of bioavailability and the improvement of the pesticide effect of 5-fluorouracil. The preparation method of the pharmaceutical co-crystal is simple, feasible, low in cost and convenient for large-scale popularization in pharmaceutical industry.

The invention discloses a compound being 5-fluorouracil-1-acetyl-Arg-Gly-Asp tetrapeptide, a preparation method, nanostructure, anti-tumor effect and tumor cell adhesion, invasion and migration resisting effect thereof, and application thereof in medical science.