60 results about "Chlorambucil" patented technology

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).

9.0 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 discloses a light-sensitive targeted anti-tumor predrug for killing tumor cells in response to hydrogen peroxide as well as a preparation method and application of the light-sensitive targeted anti-tumor predrug. A hydrogen peroxide-light stimulated drug and fluorescence double-release system is designed and synthesized by taking hydrogen peroxide as a target molecule released by the drug as well as boric acid ester as a response group. The determination of the fluorescence of the predrug (CM-1) finds that the predrug (CM-1) can well release fluorescence in response to hydrogen peroxide; meanwhile, compared with other light-sensitive drugs, the predrug has relatively good stability and targeting property; a research for determining the anti-tumor activity of the predrug by virtue of an MMT method finds that the compound (CM-1) has the anti-tumor activity higher than that of chlorambucil, namely that the targeting property of the compound (CM-1) is higher than that of chlorambucil; the intake condition of cells to the drug is explored according to the fluorescence characteristic of coumarin, and an experiment result shows that the predrug can be digested by cells. According to the predrug, an effectively research tool is provided for drug release in cell researches.

The invention belongs to the field of compound preparation, and specifically discloses a preparation method of an anti-tumor medicine chlorambucil. The preparation method comprises the steps of performing a Vilsmeier reaction on a raw material N,N-dihydroxyethylaniline and phosphorus oxychloride and DMF so as to prepare 4-[bi(2-chloroethyl)amino]benzaldehyde, then performing a witting reaction on4-[bi(2-chloroethyl)amino]benzaldehyde and methoxymethyl triphenylphosphonium chloride so as to prepare 4-[bi(2-chloroethyl)amino]-BETA-methoxystyrene, reacting under an acid condition so as to obtain4-[bi(2-chloroethyl)amino]phenylacetaldehyde, and finally, reacting with Meldrum's acid in triethylamine and formic acid systems so as to prepare a target product. The raw material N,N-dihydroxyethylaniline is cheap, has a wide source and is easy to obtain; the whole reaction process has high yield, production conditions are mild, the steps are short, and post treatment and purification are easyto operate, so that the preparation method is applicable to commercial large scale production, and meets the rapidly growing market demands.

The invention provides a preparation method and application of oligopeptide hydrogel, and a medicinal composition. The obtained oligopeptide hydrogel has a good targeting tumor suppression effect or in-vivo imaging effect. The preparation method of the oligopeptide hydrogel includes the steps of mixing oligopeptide with an antibody in a water solution, and assembling the oligopeptide and the antibody into the hydrogel under the enzymatic action at the temperature of 2-6 DEG C, wherein the oligopeptide can form the hydrogel under the enzymatic action, and the antibody has a targeting effect ontumor cells. The capping groups of the oligopeptide are groups having an antitumor effect or in-vivo imaging effect; preferably, the antitumor groups are chlorambucil, and the groups with the in-vivoimaging effect are Cy5.5; more preferably, the sequence of the oligopeptide is X-GDFDFpDY, and the X is chlorambucil or Cy5.5; preferably, the antibody is antiHER2.

The invention discloses a chlorambucil derivative with a structure as shown in a formula I, II or III and pharmaceutically acceptable salts thereof, wherein the formula is described in the specification. The invention also relates to a preparation method for the chlorambucil derivative, a preparation of the chlorambucil derivative and application of the chlorambucil derivative.

The invention discloses a preparation method and application of a polypeptide drug conjugate with tumor targeting. The polypeptide drug conjugate with the tumor targeting structurally comprises tumortargeting peptide WA1, a non-splitting connector and a cytotoxicity anti-tumor drug. The preparation method of the polypeptide drug conjugate (PDC-WA1) with the tumor targeting adopts a Fmoc solid-phase synthesis method and comprises the following main synthesis steps of: taking Fmoc-Ala-Wang resin as a raw material, after the tumor targeting peptide is synthesized, connecting the synthesized tumor targeting peptide with Fmoc-Acp-OH and chlorambucil in sequence, and carrying out purification by HPLC to obtain the polypeptide drug conjugate with the tumor targeting and anti-tumor activity. Thepreparation method has the advantages of low production cost, low environment pollution, few reaction by-products and low purification difficulty and is simple in reaction operation.

A library of glycosylated chlorambucil analogs which are useful as anti-tumor and/or anti-metastatic agents is disclosed. The glycosylated chlorambucil analogs have the general formula

wherein

represents a reducing sugar moiety.

The invention relates to a synthesis method of a light controlled-release compound. The above lead compound is composed of a BODIPY parent nucleus and chlorambucil, and light controlled-release drug,photodynamic therapy and chemotherapy are integrated in the same molecular structure. The invention also discloses an application of the compound in tumor treatment. The lead compound is simple in structure and small in molecular weight, has a determined chemical structure, is easy to prepare, purify and further modify, and has the remarkable characteristics of low toxicity to mice and the like, so that the basic requirements of clinical medication are met. Proved by in-vitro and in-vivo experiments, the lead compound has an accurate controlled-release chemotherapeutic drug chlorambucil undervisible light radiation, and the optical radiation time and the drug release amount are in a positive correlation relationship, so that the chemotherapeutic drug and singlet oxygen are accurately released by a single molecule through optical stimulation, and the synergistic treatment of chemotherapy/photodynamic therapy of living tumors is realized. Therefore, the lead compound for photodynamic therapy cooperated with photocontrolled-release chemotherapy has a good application prospect in the aspect of tumor therapy.

The invention belongs to the technical field of artemisinin derivatives, and particularly relates to an artemisinin-chlorambucil ester compound and a preparation method thereof. In order to solve the problems that the tumor effect of artemisinin needs to be improved, the toxic and side effects of chlorambucil are large and the like, artemisinin-chlorambucil ester with a novel structure is designed and synthesized according to a pharmacophore splicing principle, and the structure of the artemisinin-chlorambucil ester compound is represented and determined by 1H NMR, 13C NMR and HRMS-ESI. The compound has good anti-tumor activity, and the toxic and side effects of chlorambucil are reduced. The preparation method is simple, the obtained derivative is high in anti-tumor activity and low in toxic and side effects, a novel medicine is provided for tumor resistance, and the derivative has good application value.

The invention relates to a chlorambucil multi-targeting medicine carrying system and a preparation method and application thereof in the aspect of anti-tumor medicines. The chlorambucil multi-targeted medicine carrying system is prepared by mixing a PEG-HA-CHL (polyethylene glycol-hyaluronic acid-chlorambucil) component with an Fe3O4 magnetofluid component in weigh ratio of 1:(1-5), wherein the PEG-HA-CHL comprises the following components in parts by weight: 20-100 parts of chlorambucil, 500-1500 parts of PEG, 100-500 parts of HA, 10-50 parts of DCC (dicyclohexylcarbodiimide), 1-10 parts of DMAP (dimethylamino pyridine), 100-500 parts of butanedioic anhydride, 10-50 parts of EDC (dichloroethane) and 20-100 parts of sodium hydrogensulfite. The invention has the advantages of intelligent medicine release, multiple targeting and better reverse medicine resistance, controlled medicine release, better blood circulation stability, better invisibility and wide applicability.