7187 results about "Anti-Tumor Drugs" patented technology

Novel polymeric micelles which are used to deliver therapeutic agents, including anti tumor drugs.

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the C ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

The present invention discloses a 3-(2-pyrimidine amino) phenyl acrylic amide compound in the structure of formula (I) or a pharmaceutically acceptable salt or a stereisomer or a prodrug molecule. The 3-(2-pyrimidine amino) phenyl acrylic amide compound or the pharmaceutically acceptable salt can effectively inhibit the growth of various tumor cells, and inhibit EGFR (epidermal growth factor receptor), HER (human epidermal receptor2) family other protease, can be used in the preparation of antitumor drugs, and can overcome the drug resistance induced by gefitinib, erlotinib and the like.

Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.

The invention belongs to the field of medicinal chemistry, and discloses pyrimidine compounds containing semicarbazide and terminal alkyne structural units, and preparation methods and applications of the pyrimidine compounds in preparation of antitumor drugs by taking lysine specific demethylase 1 (hereafter referred to as LSD1) as a target. A pyrimidine active fragment is built by adopting a three-component one-pot method, and then the target compounds are prepared by substitution, chlorination and ammonification reaction. The general formulas of the compounds are as shown in the formula I in the specification. An in vitro anti-tumor activity experiment and an LSD1 inhibition activity experiment prove that the compounds have obvious inhibiting and killing action on a plurality of tumor cells by inhibiting the activity of the LSD1, can be used as lead compounds for further development, and are applied to preparation of the antitumor drugs.

In one aspect, the present invention provides a method of treating uterine cancer, endometrial cancer, or ovarian cancer, comprising administering to a subject at least one PARP inhibitor. In another aspect, the present invention provides a method of treating uterine cancer, endometrial cancer, or ovarian cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one anti-tumor agent.

The invention discloses 20 kinds of 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl, discloses a preparation method of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl, discloses an effect of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl in inhibiting invasion and metastasis of a tumor cell, discloses an activity of the 5-(bi(3-(2-ethoxy)-1H-indol-2)methyl)-2-hydroxy benzoyl-AA-OBzl in inhibiting weight gain of a tumor body of a S180-bearing mouse, and discloses an anti-tumor pulmonary metastasis activity and an anti-inflammatory activity. The compound has an excellent application prospect in preparing an antitumor drug, an anti-tumor metastasis drug and an anti-inflammatory drug.

The invention relates to an injection anticancer long circulating targeting liposome which is characterized in that anti-angiogenic drug is combined with anticancer drug, the liposome modified by polypeptide with tumor targeting function and hydrophilic polyethyleneglycol is adopted for loading and transporting the two drugs to tumor positions, and the tumor curative effect is enhanced through the different releasing rates and action mechanism of the two drugs.

The invention relates to preparation and application of amphiphilic polysaccharide conjugate and medicinal compositions thereof with anti-tumor activity and biodegradability. The conjugate has amphiphilicity by using alkylenediamine as a connecting arm and introducing hydrophobic segmer, namely a carboxyl-containing anti-tumor medicament, on a polysaccharide framework, and are formed into nanometer micelles by self-assembly in water. The invention is characterized in that 1) the anti-tumor medicament is physically coated by a hydrophobic inner core consisting of hydrophobic groups so as to remarkably improve the solubility of the anti-tumor medicament; and 2) the anti-tumor medicament obtained by chemical conjugation and physical coating can jointly achieve treatment effect and improve medicament action. The polysaccharide conjugate and the medicinal compositions thereof can be used for injection, oral administration, external use or mucosa administration. The invention has the advantages of simple preparation method, mature technology, high yield, and suitability for large-scale continuous production.

The present invention relates to a preparation method and an application of a hyaluronic acid-antitumor drug conjugate and composite nanoparticle composition with characteristics of active targeting antitumor effect and biodegradability. The preparation method is characterized by comprising: (1) a synthesis method for conjugating an antitumor drug and a spacer and conjugating a targeting ligand hyaluronic acid or an ammonium salt thereof and the antitumor drug-spacer; and (2) a new technology for assembling the hyaluronic acid-antitumor drug conjugate and amphiphilic polyester block copolymer composite nanoparticles. The composition has effects of substantially increased drug loading, efficacy improving, in vivo long-circulating effect achievement, active tumor targeting property and drug toxic-side effect reduction. The macromolecular conjugate and complex nanoparticle composition can be used for injection administration, oral administration or mucosal administration. In addition, the preparation method has characteristics of mature process and high yield, and is suitable for industrial production.

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.

The invention belongs to the field of medicine, and in particular relates to a medical application of 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl 4-((3-chloro-4-methylphenyl) amino)-4-oxobutanoate in a selective histone lysine-specific demethylase 1 (LSD1) inhibitor, especially the application in anti-tumor medicaments. Pharmacodynamic tests indicate that the 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl 4-((3-chloro-4-methylphenyl) amino)-4-oxobutanoate has a remarkable LSD1 inhibiting effect, and has selectivity to homologous proteins MAO-A (monoamine oxidase-A) and MAO-B.

The invention relates an amphiphilic polysaccharide-anti-tumor medicament conjugate capable of releasing medicines specifically at a lesion site of a living body, as well as a preparation method and application of a medicinal composition of the amphiphilic polysaccharide-anti-tumor medicament conjugate. In the conjugates, hydrophobic anti-tumor medicaments are introduced into a polysaccharide skeleton through a connecting arm which contains a disulfide bond, so that the polysaccharide-anti-tumor medicament conjugate has amphipathic characteristics and can be self-assembled into nano-micelles; the nano-micelles can load anti-tumor medicaments additionally and also can be directly used as conjugate pre-drug micelles. The amphiphilic polysaccharide-anti-tumor medicament conjugate is mainly characterized in that 1) after the nano-micelles reach the lesion site, the disulfide bond connecting arm of the conjugate can be specifically degraded by high-concentration reducing substances in lesion cells, so that the micelles are depolymerized and the medicament is released quickly, and therefore, the treatment effect is improved; 2) the anti-tumor medicament is chemically conjugated and physically coated to achieve a common treatment effect. The polysaccharide conjugate and the medicinal composition thereof can be used for injection, oral administration or external use administration; the anti-tumor activity can be improved remarkably; new ideas are provided for the development of anti-tumor medicaments.

The invention is directed to novel PDGFRβ-specific antagonists. The antagonists include antibodies, which can be bispecific. The antibodies are used to reduce or inhibit tumor growth and or to treat an angiogenic disease. The invention also includes combinations of PDGFRβ-specific antagonists with VEGFR antagonists for such treatments. The antagonists can further be administered in combination with other anti-angiogenic or anti-neoplastic drugs.

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

The invention relates to modification of a cell penetrating peptide for realizing a low-toxicity administration system with a positive targeting selecting function. A shielding peptide, an enzymolysis substrate peptide and a cell-penetrating peptide are connected in sequence, so that an activatable cell penetrating peptide is formed; and a medicament and / or a tracer and / or a medicament carrier is connected or embedded or adsorbed to the cell penetrating peptide, so that an administration system is constructed. According to a shielding peptide sequence, positive charges carried on the surface of the administration system can be reduced or completely neutralized, the cell penetrating capability of the cell penetrating peptide is shielded, and the toxicity of the administration system on normal cells of an organism is lowered; and an enzymolysis substrate peptide sequence can be identified by enzyme systems secreted specifically by different pathological change tissue cells and fractured by enzyme hydrolysis, so that a cell penetrating peptide is released and is used for carrying a medicament and / or a medicament carrier through a cell membrane, and the medicament enters cells and is brought into play. The invention aims to actively convey an antitumor medicament to tumor tissues in a targeted way and make the antitumor medicament enter tumor cells to a larger extent by using the administration system which can be used for activating a cell penetrating function, so that the toxicity at a non-tumor position is lowered while the antitumor effect of the medicament is enhanced.

The invention relates to the technical field of medicines. The content of DNA topoisomerase I (TopoI) in tumor cells is substantially higher the content of the TopoI in normal tissues, and an inhibitor of the TopoI is listed as one of six types of antitumor drugs which are primarily researched by an American NCI (National Cancer Institute). The invention aims to obtain evodiamine derivatives withstrong antitumor activities by modifying the structure of evodiamine. The evodiamine structure of the evodiamine compounds is represented by general formula (I) in the specification. The invention also provides an application of the evodiamine compounds and medicinal salts thereof in preparing topoisomerase inhibitors and antitumor drugs.

The invention discloses a 3-epi-bufalin 3-O-beta-D-glucoside and derivant, which inhibits cancer cell from growing rather than bufalin to make cardiotonic, local anesthesia, combat shock and tumour-resistant drug.

The invention relates to pentadeuteropyridine compounds represented by the following formula (I) and pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, and a preparation method, pharmaceutical compositions and uses thereof. The compounds can generate an inhibitory effect on variation forms of epidermal growth factor receptor (EGFR) protein kinase, thereby effectively inhibiting the growth of a variety of tumor cells; the compounds can be used for preparation of antitumor drugs, are used for treatment or prevention of a plenty of different cancers, and moreover, can overcome the drug resistance induced by conventional drugs gefitinib, erlotinib and other first-generation EGFR inhibitors. More specifically, the compounds can be used for preparation of drugs for treatment or prevention of diseases, obstacles, disorders or illness conditions mediated by certain variation-form epidermal growth factor receptors (such as L858R activated mutants, Exon19 deletion activated mutants, and T790M resistance mutants).

The invention relates to a common carrier material based on graphene oxide for a targeting anticancer drug and a gene and application and application. Folic acid, lactobionic acid and other tumor cell targeting or liver targeting molecules and part of amino groups of soluble chitosan are connected by amide bonds to prepare a conjugate, the conjugate is then connected with graphene oxide, quaternization is performed by using an epoxy compound with a quaternary ammonium group, and gene molecules are loaded by the quaternizationquaternized part of the chitosan through electrostatic attraction; and then the anticancer drug is loaded by pi-pi conjugates, hydrogen bonds and hydrophobic effects in a non-covalent bond method. By adopting the targeting performance of targeting molecules and effects of graphene oxide of a particular size to enhance penetration and retention in tumor tissues and combining the performance of the graphene oxide for pH response control release of the loaded drug, the drug can be realized released in a tumor cell, an intelligent delivery system for the common carrier of the tumor targeting or liver targeting anticancer drug and the gene is synthesized from the perspective of synergetic medication, and a theoretical basis and a method basis are provided for combined therapy of tumor.

The invention belongs to a biomedical technology field. The invention provides an anti-human ErbB2 antibody and ansamitocin conjugate, comprising: substituting lysine at 30 or / and 65 position in a heavy chain variable region of Trastuzumab with a hydrophilic amino acid, and then coupling with ansamitocin (DM1). On basis of maintaining coupling Pharmaceutical activity, a proportion of ansamitocin in a coupling medicament is reduced, thereby reducing toxic and side effect of the coupling medicament. The invention further provides applications of the anti-human ErbB2 antibody and ansamitocin conjugate for preparing antitumor drugs.

The invention discloses 4-(benzofuran-5-yl)-2-benzal aminothiazole as shown in a chemical structural formula I. The preparation method of the 4-(benzofuran-5-yl)-2-benzal aminothiazole is as follows: 1-(7-hydroxy / alkoxy-2,2-dimethyl-2,3-dihydro-benzofuran-5-yl) butanone is subject to bromination and reacts with thiourea to obtain 4-(7-hydroxy / alkoxy-2,2-dimethyl-2,3-dihydro-benzofuran-5-yl)-2-aminothiazole which reacts with aromatic aldehyde to prepare the 4-(benzofuran-5-yl)-2-benzal aminothiazole. The 4-(benzofuran-5-yl)-2-benzal aminothiazole has good activity inhabiting activity on Hela cells, human liver cancer cells (Bel 7402 cells) and lung carcinoma cells (A549 cells) and can be used for preparing the antineoplastic agent.

The invention provides a preparation method of a mono-dispersed gelatin embolic microsphere with a precisely-controlled particle size. In the provided method, micro water-in-oil liquid drops are formed in a micro channel reactor at first through a micro-fluidic liquid drop control technology, then a crosslinking agent and a gelatin water solution are taken as the dispersing phase and introduced into the water-in-oil system, and then the mixture is directly cured to form microspheres. By adjusting the flowing speeds of the continuous phase and the dispersing phase, and the flowing speeds of two dispersing phases, the particle size and sphericility can be precisely controlled. The preparation technology is simple and rapid, and the process is controllable. The prepared gelatin microsphere can be used as an embolic agent or an antitumor drug carrier, and can also be applied to cell culture.

An application of the pentacyclo-triterpenoid used as the glycogen phosphorylase for preparing the medicines to treat diabetes, ischemic cardiovascular and cerebrovascular diseases, and tumor is disclosed.

An orally-disintegrating tablet of fluterazole for treating tumor contains tegafur, Jimosite and potassium oxyazinate. It has agreeable taste.

The invention belongs to the field of biomedicines, and relates to applications of chrysophanol or a derivative thereof and oncolytic virus in preparation of antitumor drugs. The invention finds that chrysophanol or the derivative thereof can be used for preparing oncolytic virus antitumor synergistic agents for the first time. Meanwhile, the invention also relates to a pharmaceutical composition containing chrysophanol and oncolytic virus, a medicine suit containing chrysophanol and oncolytic virus, and applications of chrysophanol and oncolytic virus in treatment of tumors, particularly tumors insensitive to the oncolytic virus.

The invention relates to a somatostatin receptor-mediated tumor targeted pharmaceutical composition which adopts a targeted somatostatin receptor functional polypeptide and polyethylene glycol for simultaneously modifying a pharmaceutical carrier, and an anti-tumor drug or / and an anti-angiogenic drug is delivered to the tumor part, thereby enhancing the tumor treatment effect.

The invention relates to a novel bufadienolides compound and a preparation method and application thereof, and provides a bufadienolides compound having a general formula (I) or pharmaceutical acceptable salts as well as bufadienolides extract or medication composition containing the compound. The compound and the extract have effect for inhibiting tumour cell activity and application to preparation of anti-tumour drugs. The invention also provides the preparation method applicable for industrial production of the compound and the extract.

The invention provides a rare earth upconversion nano crystal / silver difunctional composite nano material and a preparation method thereof as well as application thereof in preparation of medicine for treating tumour. The composite nano material can inhibit the growth of tumour tissue and can be used with anti-tumour medicine, thus improving medicine effect and achieving the aim of treatment; thecomposite nano material is difficult to decompose and has good light stability; damage to human body is less, the composite nano material can be taken as heat sensitizing agent and can absorb infrared light, the near infrared region (800-1200nm) is a transmission window of organism tissue, and damage of near infrared laser to human body is far less than that of laser in other wavebands, thus reducing damage to human body, being capable of being used as photothermal conversion agent and being superior when used for diagnosis and treatment on malignant tumour.