1531results about How to "Good antitumor activity" patented technology

By replacing the antigen-binding domain, the present inventors discovered novel polypeptide complexes that retain BiTE's strong anti-tumor activity and excellent safety properties, as well as have long half-life in blood and can damage various different target cells.

The present invention relates to the field of adoptive immunotherapy. The invention provides methods for generating phenotypically defined, functional, and / or expandable T cells from pluripotent stem cells engineered through safe genetic modifications. The engineered cells may provide one or more of: 1) targeting a specific predetermined antigen expressed on the cell surface of a target cell in an HLA independent manner, 2) enhanced survival and functional potential 3) “off-the-shelf” T cells for administration to multiple recipients, eventually across immunogenic barriers, and / or 4) cytotoxic potential and anti-tumor activity.

The present invention relates to a pharmaceutical composition, a kit, a method of treating cancer and / or a method of inhibiting angiogenesis comprising a sulfonamide compound in combination with a platinum complex, a DNA-topoisomerase I inhibitor, an antimetabolite, a microtubule inhibitor or an antibiotic.

The present invention relates to a pharmaceutical composition, a kit and a method for treating cancer, comprising a sulfonamide compound in combination with a substance having an EGF inhibitory activity.

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 present invention relates to pharmaceutical compositions comprising a sulfonamide-including compound in combination with an angiogenesis inhibitor.

An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.

The present invention relates to pyrimidine and triazine compounds represented as a general formula I, geometric isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, wherein substituents R1, R2, R3 and X have the meanings defined in the description. The invention further relates to uses of the compounds represented as the general formula I in preparing medicine for treating and / or preventing cancer and other hyperplasia diseases.

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 present invention relates to a cell division inhibitor comprising various dehydrodiketopiperazines such as dehydrophenylahistin, or analogs thereof as an active ingredient, and a dehydrogenase and a method for producing the same inhibitor.

The invention relates to a penicillium citrinum sourced citrinin compound (penicitrinol O) as well as a preparation method and an application thereof. The compound has an effect on inhibiting tumor cell proliferation and has anti-tumor activity, and the structural formula is shown in the specification. The preparation method comprises the steps: fermenting and culturing penicillium citrinum IBPT-5 to obtain a fermented product; and then separating and purifying the fermented product to obtain the compound. The experiment shows that the compound has high anti-tumor activity for human cervical cancer cell line hela and can be used for preparing cell proliferation inhibition medicines or anti-tumor medicines for the study on anti-tumor.

The invention belongs to the field of drug synthesis and in particular relates to a series of novel peptide boric acids as well as an ester compound or pharmaceutical salt thereof, and a preparation method and application of the peptide boric acids as well as the ester compound or pharmaceutical salt thereof in pharmacodynamics. A structure of the peptide boric acid and the ester compound or pharmaceutical salt thereof is shown in a formula I (described in the specification). The compound provided by the invention can be used for preparing a proteasome inhibitor and can further be used for treating solid tumours and blood tumours, wherein the solid tumours are selected from non-small cell lung cancer, small cell lung cancer, lung adenocarcinoma, lung squamous carcinoma, pancreatic cancer, breast cancer, prostate cancer, liver cancer, skin cancer, epithelial cell cancer, gastrointestinal stromal tumor, nasopharynx cancer and leukemia; and the blood tumours are selected from multiple myeloma, mantle cell lymphoma and histiocytic lymphoma.

The invention discloses a PD-L1 affinity peptide P1 with anti-tumour activity, which is the polypeptide obtained by phage display peptide library screening, wherein the amino acid sequence thereof is FPNWSLRPMNQM, and the molecular weight thereof is1520.7. The affinity peptide P1 with anti-tumour activity and aiming at a PD-L1 target disclosed by the invention has the advantage of being screened with a high flux by utilizing a phage display peptide library screening technology for the first time; and via an in-vivo tumour-bearing experiment for Kunming mice, the affinity peptide P1 disclosed by the invention is proved to have a great anti-tumour activity, can induce the internal tumour cell apoptosis of mice, and have an extremely high killing capacity for tumour cells. Via the affinity peptide P1 disclosed by the invention, new thoughts and theoretical basis are provided for research and development on medicines based on PD-L1.

An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.

The invention discloses a novel glycyrrhetinic acid derivative, and a preparation method and medicinal uses thereof. The glycyrrhetinic acid derivative is a compound prepared by coupling nitric oxide donor of furazan nitrogen oxides and glycyrrhetinic acid through ester bonds or amide bonds. As proved by pharmacological experiments, the glycyrrhetinic acid derivative has superior antitumor effectand can be used for the preparation of antitumor medicines.

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.

Relating to the medicine field, the invention specifically relates to a glycyrrhetic acid derivative with a 1, 12-diene-3-ketone skeleton or a pharmaceutically acceptable salt thereof, their preparation method and medicinal uses, in particular their application in preparing antitumor drugs. Pharmacological experiment results show that these compounds have good antitumor activity and can be used for preparing antitumor drugs clinically.

The invention relates to the combined use of anti-EGFR antibodies and anti-Her2 antibodies for the treatment of cancer, especially suitable for cancer expressing high levels of the EGFR type and low levels of HER2. The invention refers in particular monoclonal antibody “trastuzumab” (HERCEPTIN®) directed against the HER2 receptors the efficacy of which can be significantly increased in vivo when combined with monoclonal antibody “matuzumab” (hmAB 425, EMD 72000) directed against EGF receptors. The combination treatment is suitable for patients suffering from cancer having said receptor profile, preferably pancreatic cancer.

The invention provides a naphthoyl amine derivative, and a preparation method and an application of the same. The naphthoyl amine derivative is N-(3- trifluoromethyl phenyl)-6-[(7- chloroquinoline-4-oxo) phenolic ether]-2- naphthoyl amine; the N-(3- trifluoromethyl phenyl)-6-[(7- chloroquinoline-4-oxo) phenolic ether]-2- naphthoyl amine can be used as protein kinase inhibitor and histone deacetylase inhibitor, and can be used for treating diseases caused by protein kinase dysregulation. The naphthoyl amine derivative can effectively treat the diseases caused by protein kinase dysregulation, and has the advantages of high bioavailability, obvious antitumor activity and low toxicity; moreover, the naphthoyl amine derivative is low in preparation reaction cost and higher in yield, the reaction process is simple and easy to control, so that the naphthoyl amine derivative is suitable for industrial production.

The invention relates to the technical field of bio-medicines, and particularly relates to a target delivery system based on bio-functionalized nano-silver loaded taxol or analogue thereof. The target delivery system comprises an anti-tumor medicine composition, a target ligand and a bio-degradable high-molecular polymer, wherein the anti-tumor medicine composition is prepared from nano-silver and taxol or analogue thereof. The target delivery system can selectively reach a tumor position to improve the treatment effect and reduce toxic or side effect, and can be used for effectively treating cancers.

The invention relates to the technical field of medicines and in particular relates to oxa- or thio-evodiamine anti-tumor derivatives as well as a preparation method of the derivatives and application of the derivatives in preparation of topoisomerase inhibitors and anti-tumor drugs. The oxa- or thio-evodiamine anti-tumor derivatives are newly discovered topoisomerase I inhibitors with brand-new structures and have remarkable anti-tumor activity, and the structure of a compound is as shown in a general formula I.

The invention discloses a preparation method and application of a sinonovacula constricta enzymolysis polypeptide. The method is characterized by comprising the following steps: shelling sinonovacula constricta, washing, mincing, adding water in the material-liquid mass ratio of 1:(3-5) for homogenizing, and adjusting the pH value to 5.5-6.5; adding protease for performing enzymolysis at the temperature of 60-70 DEG C for 1.5-2.5 hours, wherein the adding amount of the protease is 0.2-0.3 percent based on the total mass of sinonovacula constricta; after enzymolysis, performing enzyme deactivation, and centrifuging to obtain supernatant serving as enzymatic hydrolysate; performing ultrafiltration, G-25 gel chromatography and reversed phase high-performance liquid chromatography elution on the enzymatic hydrolysate to obtain the needed sinonovacula constricta enzymolysis polypeptide. A preparation process is simple, the obtained sinonovacula constricta enzymolysis polypeptide is high in sensitivity and stability and small in side effects, plays a remarkable role in inhibiting the proliferation of DU-145 and PC-3 cells through MTT detection, and can be applied to in-vitro resistance of prostatic cancer. The preparation method plays an important role in further researching and developing functional foods and medicaments based on the sinonovacula constricta enzymolysis polypeptide and increasing the economical value of the sinonovacula constricta.

The invention belongs to the technical field of biopharmacy, particularly relates to a PD-L1 IgV targeted affinity peptide product with antineoplastic activity, and a preparation method and application of the affinity peptide product. According to the invention, the affinity peptide is specifically bonded in the PD-L1 IgV area, the amino acid sequence of the affinity peptide is ANGSRLV (Ala-Asn-Gly-Ser-Arg-Leu-Val), and the molecular weight of the affinity peptide is 715.4; the affinity peptide can be artificially synthesized by adopting the Fomc solid-phase polypeptide synthesis, and can be adopted as the mainly active ingredient in preparing colon cancer (CT26) resistance medicines. Bacteriophages are adopted to display the peptide bank screening technique, the PD-L1 IgV is adopted as the target for high-flux screening, and the affinity peptide with the antineoplastic activity is artificially synthesized; the inventor further proves that the affinity peptide has the better antineoplastic activity, can remarkably inhibit growth of tumors in rats, and provides the novel thinking and theoretical basis for the research and development of PD-L1-based medicines.

The invention belongs to the technical field of medicine, and in particular discloses a levo-fluoroquinolone C3 bisazole methyl sulfide, a preparation method and application thereof in the field of pharmacy. The chemical structural formula of the levo-fluoroquinolone C3 bisazole methyl sulfide is shown as a general formula I, wherein in the general formula I, X is selected from any one of O, S and -NH; and Ar is selected from any one of phenyl, substituent-containing phenyl and heterocyclic aromatic hydrocarbon. The levo-fluoroquinolone C3 bisazole methyl sulfide has strong in vitro cytotoxin effect on experimental leukemia cancer cell strains, has strong anti-tumor activity, and can be mixed with a human acceptable acid salt or a medicinal carrier to prepare an anti-tumor medicament.

A method for controlling in vivo heat-inducible gene expression for provision of therapeutic polypeptide. The method includes the steps of: (a) providing a construct comprising a polynucleotide encoding a therapeutic polypeptide, wherein the polynucleotide is operatively linked to a heat-inducible promoter; (b) administering the construct to a warm-blooded vertebrate at a site at or near the tumor; and (c) applying heat to the site at or near the tumor to express the therapeutic polypeptide, whereby anti-tumor activity is observed.

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 discloses a compound as a formula (1), a kalium salt, a sodium salt or an ammonium salt thereof and also discloses a pharmaceutical composition containing the compound as the formula (1), an isoandrographolidume sulfonate E, an andrographolic acid and andrographolidume and a preparation method thereof. The compound and the composition obtained by the method have favorable effects, such as an inflammatory factor resistant effect, an antibacterial effect, an analgesic effect and an antineoplastic effect. The invention also discloses a peroral preparation or an injection preparation prepared by using the compound and the composition.

The invention relates to an industrialized production process of active carboxymethylpachymaran. Firstly, carrying out superfine grinding on the tuckahoe sclerotium to obtain tuckahoe superfine powder; extracting the superfine powder with edible alcohol at normal temperature, filtering to obtain filter cakes; taking the mixture of water and alcohol as a medium, wherein the volume ratio of alcohol to water is 15-10:1; and carrying out reaction between the filter cakes, chloroacetic acid and excessive sodium hydroxide to obtain the carboxymethylpachymaran with anti-tumor activity. The carboxymethylpachymaran obtained by the invention has high purity, favorable water solubility, moderate molecular weight, moderate substitution degree of carboxymethyl and obvious anti-tumor activity. The active carboxymethylpachymaran can be applied to preparing antitumor drugs or health foods. The preparation route of the invention is economic and environment-friendly, and is suitable for large-scale industrialized production.

The invention belongs to the technical field of bio-pharmacy and specifically relates to a PD-L1IgV-targeting D-configuration affinity peptide D1 product with anti-tumor activity, as well as preparation and application thereof. The affinity peptide D1 is specifically bound to a PD-L1IgV region, the amino acid sequence is NYSKPTDRQYHF, and the molecular weight is 1554.7. The affinity peptide D1 is prepared through a Fomc solid-phase polypeptide synthesis method, and plays a role in preparation of anti-colon cancer medicaments as a main active ingredient. The affinity peptide D1 provided by the invention is obtained by utilizing a mirroring bacteriophage display peptide library screening technology and performing high-throughput screening by taking PD-L1IgV as a target point. Through tumor-bearing experiments in mouse bodies, the inventor proves that the affinity peptide D1 has better anti-tumor activity and can obviously inhibit the growth of tumors in the mouse bodies, so that a new idea and theoretical basis are provided for researching and developing PD-L1-based medicaments.

The invention belongs to the technical field of biological pharmacy, and concretely relates to a PD-L1 IgV affinity peptide S10 product with antitumor activity, and preparation and application thereof. The affinity peptide S10 is specifically bond at PD-l1 IgV region, has the amino acid sequence of WSHGGHQHFIRF, and has the molecular weight of 1507.7. The affinity peptide S10 is prepared through a Fomc solid-phase peptide synthesis method, and plays a role as a main active composition for preparing anti-colorectal carcinoma medicines. The provided affinity peptide S10 is obtained by utilizing a phage-display peptide-library screening technology and taking PD-L1 IgV as a target for performing high-flux screening. Experiments of bearing a cancer in a mouse prove that affinity peptide S10 has relatively good antitumor activity, is capable of obviously inhibiting growth of tumor in a mouse, and provides new thinking and theoretical base for research and exploitation of medicines based on PD-L1.