1066 results about "Antineoplastic Drugs" patented technology

A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula I, to inhibit cell proliferation such as that associated with tumor growth and metastasis. A method for inhibiting angiogenesis in an abnormal proliferative cell mass by the administration of an agent of Formula I is also provided.

The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:which relates to morphinan compounds useful as μ, δ, and / or κ receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.

The invention discloses an application of nanometer structure lipid carrier administration system in the antineoplastic drug to reverse the multiple-drug tolerance of tumour cell, which comprises the following parts: solid lipid material, liquid lipid material and antineoplastic drug, wherein the rate of the liquid lipid (such as oleic acid) is 0-30wt%; the solid lipid is selected from monoglyceride; the liquid lipid is oleic acid; the antineoplastic drug is Paclitaxel or adriablastina. The invention has highly effective cell uptaking and cytolymph condensing function with packing molecular target in the antineoplastic drug of cell, which avoids P-glucoprotein in the drug tolerant cytolymph from identifying the antineoplastic drug to reduce exclusion.

The present invention provides oral dosage forms and compositions for administering antineoplastic agents, such as irinotecan, etoposide, paclitaxel, doxorubicin and vincristine, whose oral effectiveness is limited by pre-systemic and systemic deactivation in the GI tract. Gelling of the gastric retention vehicle composition, and in the case of solid forms concomitant expansion of the composition, retains the antineoplastic drug in the patient's stomach, minimizing pre-systemic and / or systemic deactivation of the drug.

The invention discloses polymorphs A, B, C and D of abiraterone acetate. A preparation method of the polymorphs comprises the step of re-crystallizing the abiraterone acetate subjected to the separation and the purification of a chromatographic column in different solvents. Through stable investigation, four polymorphs have favorable stability and flowability, can be used as raw materials for storage and transportation and are suitably applied to antitumor medicinal preparations.

A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula I, to inhibit cell proliferation such as that associated with tumor growth and metastasis. A method for inhibiting angiogenesis in an abnormal proliferative cell mass by the administration of an agent of Formula I is also provided.

The invention discloses pyridylpyrimidyl amine compounds or pyridylpyridyl amine compounds disclosed as Formula I and application thereof in preparing antineoplastic drugs, belonging to the technical field of drugs. The compounds can selectively inhibit CDK4 and CDK6, enable G1-period tumor cells to stop growth and G1-period tumor cells to reduce, can effectively lower the phosphorylation of the tumor inhibiting protein Rb in the Ser780 site, and thus, can be used for various diseases caused by cell cycle control maladjustment participated by CDK4 and CDK6. The compounds are especially suitable for treating malignant tumors, and have the characteristics of high selectivity, high activity and high tumor cell proliferation resistance.

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula:-L1-L2-LP-NH—(CH2)n1-La-Lb-Lc-wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.

Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug.A uracil compound represented by the general formula (I) or a salt thereof:wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.

Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers.

The invention discloses application of nano-selenium in an antineoplastic drug carrier. The nano-selenium is used as a carrier and is used for loading an antineoplastic drug to obtain an antineoplastic drug compound system. The nano-selenium is applied to the antineoplastic drug compound system, so that the prepared antineoplastic drug compound system can bring the synergistic action of an antineoplastic drug and the nano-selenium in resisting tumors into play, and while the penetrability of the antineoplastic drug is enhanced, the toxic or side effect of the antineoplastic drug to human body normal tissues is also reduced. The antineoplastic drug compound system can be preserved in the form of hydrosol in a liquid phase, the preparation process is simple, the condition is mild, the stability is high, and the preservation time is long, so that the antineoplastic drug compound system is suitable for popularization and application.

The invention discloses thiosemicarbazon compounds, their derivatives and their applications for the preparing of antineoplastic drugs. The compound of the invention shows its good inhibitory effect on tumor through the experiments on animals. For example, the inhibition effect on the solid tumor S180 on mouse is up to 81.1%. The compounds can be made into tablet, capsule or injection agent in many forms.

The invention relates to a natural active drug-polysaccharide targeted compound with antitumor activity and targeting property. A natural active drug is introduced onto a polysaccharide framework by chemical grafting, and physically mixed with a ligand distearoylphosphatidyl ethanolamine-polyethyleneglycol-anisoyl amine with targeted transmission capacity to form a natural active drug-polysaccharide targeted compound, and the natural active drug-polysaccharide targeted compound can be self-assembled in water to form a nano micelle. The method is characterized in that the natural active drug-polysaccharide targeted compound has targeted transmission capacity, enhances the tumor transfer efficiency of the preparation, reduces the untoward reaction and enhances the tolerance of the patient; the hydrophobic inner core formed by the hydrophobic group can physically wrap the antineoplastic drug, thereby obviously improving the water solubility of the antineoplastic drug; and the antineoplastic drug which is physically wrapped by the chemically coupled ursolic acid can implement combined treatment of tumors and lower the toxic or side effect. The preparation method is simple and easy to operate, has the advantage of higher yield, and can easily implement industrialization.

This invention discloses a new camptothecin derivate of 20-position esterification, its preparation, containing their medicine combination, and its usage of using it as medicine, especially as antitumor drug.

Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug.A uracil compound represented by the general formula (I) or a salt thereof:wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.

The invention discloses a baicalin metal complex of which the molecular formula is (C21H17O11) xM (H2O) y, wherein M in the formula is Cu (II), x is 1 and y is 2; or M is Fe (III), x is 2 and y is 0; or M is La (III) or Y (III), x is 3 and y is 0. The preparation method comprises the following steps: adding aqueous alkali into baicalin until the baicalin and alkali (sodium bicarbonate, potassium bicarbonate, sodium formate, potassium formate, sodium acetate, potassium acetate, disodium hydrogen phosphate, dipotassium hydrogen phosphate, sodium phosphate or potassium phosphate) are just completely reacted, then adding metal salt (copper salt, ferric salt, lanthanum salt or yttrium salt) for reaction to obtain the baicalin metal complex. The baicalin metal complex has obviously stronger antibacterial and antitumor activities than the baicalin, can be used for preparing antibacterial drugs and antitumor drugs, and has good development and application prospects. In the preparation method, an organic solvent is not used, a strong basic condition is not adopted, and the method is simple and feasible, is green and environment-friendly and has the advantages of low cost, high product purity and high yield.

The invention relates to preparation and application of an amphiphilic ursolic acid-polysaccharide coupled substance with antitumor activity. The ursolic acid is chemically modified to substitute C3 site carboxyl group with amino group, the generated aminated ursolic acid is chemically coupled to a polysaccharide framework to form the amphiphilic ursolic acid-polysaccharide coupled substance, and the amphiphilic ursolic acid-polysaccharide coupled substance can be self-assembled into a nano micelle in water. The method is characterized in that the antitumor activity of the chemically modified ursolic acid is obviously enhanced; the hydrophobic inner core formed by the hydrophobic group can physically wrap the antineoplastic drug to obviously improve the solubility of the antineoplastic drug; and the antineoplastic drug which is physically wrapped by the chemically coupled ursolic acid can implement combined chemotherapy, has higher antitumor activity, has the combined synergetic action, and lowers the toxicity. The preparation method is simple and easy to operate, has the advantage of higher yield, and can easily implement industrialization.

Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

A combination for administration to a mammal which combination employs a therapeutically effective amount of a medicinal and / or therapeutic agent to treat a disease or condition and an amount of hyaluronic acid and / or salts thereof and / or homologues, analogues, derivatives, complexes, esters, fragments and subunits of hyaluronic acid sufficient to facilitate the agent's penetration through the tissue (including scar tissue) at the site to be treated, through the cell membranes into the individual cells to be treated.

The invention provides the appraisal and selective method for the antineoplastic drug based on the cell micrograph information, which uses a sort of selection and appraisal hardware system to appraisal and select the antineoplastic drug by different fluorescence dye marking and measuring the multicellular parameter change in cell. The hardware system is made up of the high precision electric hydrous platform, the fluorescence vision system, the image collecting and processing system and working station. The diacetoxyl fluoresceine dyeing measures the active cell number; the double dyeing method of Hoechst33342 and iodized pyridine appraise the drug inducing the cell die; the three dyeing method of FDA, Hoechst33342 and PI analyzes the die mode induced by drug. The invention can measure at least two kinds of single cell or cell subgroup which expresses different drone cell organ. The method is in reason and can be used in study of drug action mechanism and selecting the high hedonic drug and toxicity analyzing, which can be used in selecting drug and appraising the drug toxicity.

The invention relates to celastrol, a celastrol derivative, a method for preparing the celastrol derivative, biogenetic salt prepared from the celastrol derivative serving as a raw material, and application of the celastrol derivative to the preparation of an antitumor medicine. The celastrol derivative has a structure shown as a formula I, wherein R1 is H, C1-C6 straight-chain or branched-chain alkyl, benzyl and benzyl with a substituent group on a benzene ring; and R2 or R3 are independent C5-C6 cyclic hydroxyl, C1-C6 chain alkyl, phenyl and substituted phenyl respectively, or R2 and R3 are cyclized with N, and the cycle is hexahydric cyclic heterocycle containing N or O. The celastrol derivative has high antitumor activity, stability and water solubility. The celastrol derivative can be salified with one of medically acceptable inorganic acids (such as hydrochloric acid, sulfuric acid and phosphoric acid) or organic acids (citric acid, cinnamic acid, succinic acid and the like); and the salt has high water solubility.

The invention relates to field of natural medicine and medicinal chemistry, in particular to novel pentacyclic triterpene and melbine salt I of the derivative thereof. The salt compound can be used for preparing medicaments curing diabetes mellitus and complicating disease thereof, cerebral ischemia, angiocardiopathy, atherosclerosis, hepatitis, fatty liver and metabolic syndrome or tumour, descendens blood fat drugs and anti-obesity drugs. The invention also relates to the preparation method of the salt compound.

The present invention discloses a tumour-related protein and its coding gene. The tumour-related protein is as follows: (a) a protein composed of sequence 4 amino acid residue in sequence list; (b) a protein derived from (a) by substituting and / or deleting and / or adding one or several amino acid residue of sequence 4 amino acid residue in sequence list The recombinant mammal gene expression vector containing tumour-related protein coding gene can be used as antineoplastic drug for preventing and / or treating lung cancer, esophageal carcinoma or cancer of larynx.

The invention discloses a 3,3'-methene-difluoroquinolone derivative of a chiral oxazine quinoline ring as well as a preparation method and application of the 3,3'-methene-difluoroquinolone derivative. The 3,3'-methene-difluoroquinolone derivative has a chemical general structural formula I shown in the specification, wherein R represents cyclopropyl or ethyl or fluoroethyl; R1 represents a hydrogen atom or methyl or ethyl; R2 represents a hydrogen atom or methyl; X represents a nitrogen atom or a hydrocarbon (CH) group or a fluoro-substituted carbon atom (F-C) or a methoxyl-substituted carbon atom (CH3O-C). The 3,3'-methene-difluoroquinolone derivative of the chiral oxazine quinoline ring, disclosed by the invention, can be used for realizing the superposition of a difluoroquinolone framework and alpha, beta-unsaturated ketone pharmacophores, so that the antitumor activity of a new compound is improved, the toxic and side effects on normal cells can be reduced, and the 3,3'-methene-difluoroquinolone derivative can be used as an antitumor active substance for developing an antitumor drug of a totally new structure.

The present invention provides an antineoplastic drug with ferritin as a carrier and a preparation method thereof, the method comprising the following steps: preparing ferritin; performing high pressure treatment on a mixed solution of ferritin and antineoplastic drug at a pressure of 200-800MPa6 ‑20h; the product after high pressure treatment is separated and purified to obtain an anti-tumor drug with ferritin as a carrier. The method of the present invention can not only increase the loading ratio of drugs, the yield of drug-loaded ferritin is close to 100%, but also can completely recover free unloaded anti-tumor drugs, improve production efficiency, reduce production costs, and is suitable for large-scale industrial production .

The invention discloses a preparation method and an application of Maca alkaloid. The method comprises the steps in sequence as follows: (1), Maca is smashed, a certain volume of an acid alcohol solution is added, supersonic extraction is performed for 1-3 times, the mixture is filtered, and an extracting solution is combined and concentrated, so that extractum is obtained; (2), the extractum is dissolved with acid water and filtered, the pH value is adjusted to be 9-12, the mixture is leached with chloroform or ethyl acetate, and an extraction liquid is subjected to pressure reduction concentration and dried, so that a Maca alkaloid crude extract is obtained; and (3), the Maca alkaloid crude extract is subjected to column chromatography with high-speed countercurrent and alkaline alumina, an eluent comprising a target compound is combined, and a solvent is recycled, so that a Maca alkaloid compound is obtained. According to the method, the technological operation is simple, the preparation amount is large, the sample loss is small, the separation effect is good, the energy consumption is low, the pollution is small the method is suitable for large-scale preparation, and a Maca alkaloid monomer obtained through separation is high in purity, has a better antineoplastic activity, is suitable for preparing antineoplastic drugs and neoplasm prevention health-care food, and has a better application and development prospect.

The invention relates to injectable temperature sensitive in situ gel preparation and a preparation method as well as an application thereof. The components of the preparation of the invention comprise 0.01 percent to 10 percent of anticancer drugs, 15 percent to 25 percent of pluronic F127, 0.01 percent to 20 percent tween and 45 percent to 84.98 percent of water or buffer solution.

The invention provides compounds of formula I: wherein Y is F, Cl, Br, methyl or methoxy; and pharmaceutically acceptable salts thereof. The compounds are effective antitumor agents. The invention also provides pharmaceutical compositions comprising a compound of formula I or a salt thereof, intermediates useful for preparing a compound of formula I, and therapeutic methods comprising administering a compound of formula I or a salt thereof to a mammal in need thereof.

The invention belongs to the technical field of natural medicines, in particular to a preparation method of a walnut green husk total tannin and an application of the same in antineoplastic medicines. The walnut green husk total tannin is prepared by using walnut green husk as raw material and extracting, leaching, precipitating, separating and purifying the raw material, has light color and high purity, and the preparation method has the advantages of high yield, low production cost and simple and standard process. The walnut green husk total tannin prepared by the invention can remarkably inhibit the growth of tumor cells and can be used for preparing the antineoplastic medicines.