36results about How to "Anti-cancer broad spectrum" patented technology

An anticancer kaurane-type diterpenoid for suppressing esophagus cancer and liver cancer cells is extracted from the stem of soursop through drying in air, pulverizing, extracting in alcohol concentrating, extracting in chloroform, chromatography, eluting, chromatography and eluting. Its advantages are high effect, low toxic by-effect, broad spectrum and high activity.

A microsphere carrying fluoroplex is prepared through dissolving polylactic acid to dichloromethane, dispersing SiO2 in it to become suspension, filling it in the aqueous solution of gelatin while stirring to become oil-in-water O / W emulsion, stirring for volatilizing dichloromethane, solidifying microspheres, centrifugal collecting, washing with secondary distilled water, vacuum drying to obtain SiO2-PLA microspheres, immersing them in the solution of fluoroplex in hydrochloric acid, centrifugal collecting, washing with secondary distilled water and freeze drying. Its advantages are durable acting, slow releasing and targeting function.

The invention relates to new antitumor medicament compounds, namely tetralin amide compounds as shown in a general formula I or pharmaceutically acceptable salts thereof used as an antitumor medicament. The invention also provides a preparation method of the compounds and medicament compositions containing the compounds as well as in vitro and in vivo antitumor effect results and acute toxicity researches thereof. The antitumor medicament, namely tetralin amide compounds obtained by the preparation method, has better antitumor activity and safety, and can be applied to treatment of tumors such as leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer and the like, thus the tetralin amide compounds have wide treatment ranges and also have extremely high application value in the medicine field as antitumor agents.

The invention belongs to the field of pharmacy and tumor diagnosis and treatment, and particularly relates to a compound serving as a cyclin-dependent kinase 7 (CDK7) inhibitor, and application of thecompound in treatment of proliferative diseases such as cancers including breast cancer, ovarian cancer, colon cancer, liver cancer, lung cancer and glioma. The CDK7 small-molecule inhibitor is a compound with the structural general formulas (I)-(X), or a stereoisomer, a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, isotope labeled derivative or prodrug thereof. The small-molecule inhibitor provided by the invention is wide in anticancer spectrum; the compound has a good growth inhibition effect on various cancer cells such as liver cancer, stomach cancer, colorectal cancer, ovarian cancer, glioma, lung cancer and the like, provides an effective drug for preventing or treating proliferative diseases, especially cancers, in the aspects of structure and action mechanism, and has a good application prospect.

The invention provides an anticancer traditional Chinese medicine composition, belonging to the technical field of medicines. The traditional Chinese medicine composition comprises bezoar, sweet wormwood herb, musk, root of China creeper and all-grass of nerved twayblade. The traditional Chinese medicine composition has the beneficial effects that through a reasonable ratio of the five medicinal raw materials, the traditional Chinese medicine composition has synergetic effects and the double effects of directly inhibiting cancer cell growth and proliferation and enhancing the immune function; through clinical research trials, the traditional Chinese medicine composition can selectively inhibit and kill cancer cell proliferation to achieve the anticancer effect, can also promote differentiation of T and B lymphocytes and activate NK cells to enhance the body immunity, has quick treatment effects on cancers, does not have toxic or side effect, has a wide anticancer spectrum, especially has obvious curative effects on lung cancers, liver cancers, gastric cancers, intestinal cancers, lymph cancers, brain tumors, nasopharynx cancers, esophagus cancers, pancreatic cancers and cervical cancers, and does not have any impact on body cells, tissues, organ functions and hemogram in the medication period.

Belonging to the genetic engineering field in medicine, the invention discloses a construction scheme for artificially modified human adenovirus type 5 (Ad5), and specific application of a tumor-selective replicative adenovirus construct in tumor treatment. With the techniques of PCR (polymerase chain reaction) amplifying fixed point deletion, enzyme cutting, connection, cloning, homologous recombination, transfection, single cloning purification of adenovirus and the like, a recombinant adenovirus construct can be acquired. Acquisition of the construct is characterized in that: 27 bases are deleted in 2(CR2) region of E1A conserved sequence of Ad5 genome; 28530-29360nt in 6.7k / gp19k gene in E3 region are deleted, and meanwhile a fragment of full-length cDNA(1131bp) of HSV-TK (herpes simplex virus thymidine kinase) is inserted into the deletion region. The construct of the invention is a novel oncolytic adenovirus carrier with high tumor-selective replication capability. With the suicide gene of HSV-TK and dissolubility of tumor cells by oncolytic viruses, the dual killing effects have unique utility value in tumor biotherapy.

Disclosed is an anti-cancer medicament ent-kauran-19-al-17-oic acid which is prepared by the steps of, (1) disintegrating the aired round lichee stems, extracting with ethanol, condensing into extract, (2) extracting with chloroform, column chromatography, purging and column chromatography again, and purging to obtain the end product.

The invention relates to substituted-indanyl amide-type compounds as shown in the general formula I, pharmaceutically acceptable salt of the compounds and a preparation method and an application thereof. The invention also provides a pharmaceutical composition of the compounds. Through in vitro and in vivo anti-tumor effect research results and acute toxicity research results, the anti-tumor drug substituted-indanyl amide-type compounds have more excellent antitumor activity and safety, especially resisting imatinib drug-resistant tumors, and can be applied in curing tumors such as leukemia, gastrointestinal stromal tumor, lung cancer, colon cancer, ovarian cancer, kidney cancer and the like. Thus, the compounds have wide therapeutic window and have application value when used as an anti-tumor agent in the field of medicine.

The invention provides a Chinese traditional medicine compound prescription, and a preparation method and the purpose thereof, which mainly provides the Chinese traditional medicine compound prescription consisting of evodia, marsdenia tenacissima, climbing nightshade, oriental biter weed, Chinese fevervine, spatholobus stem, honey-suckle stem, wild grapevine, sargentg loryvine, Radix sophora flavescens, Paris Rhizome, licorice, etc. The preparation method comprisesthe following steps: step one, the alcohol reflux or the warm immersion abstraction of the evodia and the climbing nightshade, step two, the water extract-ethanol precipitation of gruffs and the rest medicinal materials, and step three, the blending of aqueous extract and ethanol extract. The invention provides the purposes of the compound prescription and the extract for the medicines of curing lung cancer, liver cancer, stomach cancer, rectal cancer, oophoroma, cervical carcinoma, prostatic cancer, bone cancer and other cancers, and simultaneously the invention also provides all administration forms including oral administration, rectum administration, intramuscular administration, vena administration, nasal cavity administration, vagina administration, subcutaneous administration, etc., and all preparation forms accepted by pellet, hard capsule, soft capsule, granula, oral liquid, syrup and pharmacy.

The invention relates to a novel compound R1 represented by general formula I. The compound R1 is an S-type or R-type tetrahydro-naphthalene amides compound, or a pharmaceutically acceptable salt or pro-drug of the compound, and is used as an antitumor drug. The invention also provides a preparation method of the compound, and a pharmaceutical composition containing the compound, and an antitumor research in vitro. The antitumor drug R1 obtained by the invention is the S-type or R-type tetrahydronaphthalene amides compound, is better in antitumor activity and safety and can be applied to treating tumors such as leukemia, lung cancer, liver cancer, colon cancer and ovarian cancer, so that the therapeutic window is wide, and the compound as an antitumor agent in the medicine field is very valuable.

The present invention relates to an anticarcinogen prepared through extraction from mistletoe. The extraction process of mistletoe alkaloid includes the steps of: drying and crushing raw material, ethanol reflux extraction, reduced pressure recovering ethanol in extractive liquid, concentration to obtain extract, hydrochloric acid dissolution of alkaloid, still standing, extracting supernatant liquid, sucking filtering, adding dropwise concentrated ammonia water to free alkaloid, chloroform extraction, water washing chloroform liquid, drying with anhydrous sodium sulfate, recovering chloroform, and still standing to separate mistletoe alkaloid crystal. The medicine mistletoe alkaloid has obvious inhibiting effect on liver cancer, stomach cancer oesophagus cancer and mammary cancer, and has high anticancer activity, wide anticancer spectrum and less toxicity.

The invention belongs to the field of diagnosis and treatment of tumors, and relates to a hypoxia inducible factor (HIF)-2 alpha small-molecule inhibitor and use thereof in treatment of breast cancer,ovarian cancer and other tumors. The small-molecule inhibitor is a compound shown in a formula (I) or stereoisomers, pharmaceutically acceptable salts, solvates or prodrugs of the compound shown in the formula (I); the proliferation of tumor cells is inhibited mainly by inhibiting HIF-2 alpha protein; furthermore, the HIF-2 alpha small-molecule inhibitor can inhibit the growth of CSCs with high expression of HIF-2 alpha, and can be used as a new anti-tumor drug to completely remove tumors and stem cells, thus having a broad application prospect.

The invention relates to an anti-tumor small-molecule inhibitor with a brand-new skeleton structure and targeting PD1 / PDL1 interaction discovered on the basis of a virtual screening strategy and application of the anti-tumor small-molecule inhibitor. The small-molecule inhibitor N-{4-[(4-chlorobenzyl) oxy] benzyl}-N-(4-pyridinzyl) amine provided by the invention has good affinity and good biological activity with PD-L1, and can activate the immune response of T cells by inhibiting the interaction of PD-1 / PD-L1 at the cell and animal level, so as to effectively target and kill tumor cells and block the immune escape way of tumor cells. In addition, the small molecule inhibitor has no obvious toxic or side effect. Therefore, the small molecule inhibitor can be effectively used for treating cancer diseases, can be used for treating tumors such as melanoma, colon cancer, gastric cancer, breast cancer, liver cancer and lung cancer, has important clinical value and has a wide development prospect.

This invention relates to methylaminopterin derivatives with 4-amino structure modified, which inhibit effect of nitrogen monoxide synthetase and growth of tumors. They have wide anti-cancer spectrum and little toxic side effect so as to be used in preparation of medicines for tumors, cancers, arthritis and intestinal diseases as well as chemicals for birth control.

The invention relates to antitumor drug (hydroxyl morpholine) and derivative thereof as well as preparation method and application thereof. The antitumor drug (hydroxyl morpholine) and the derivative thereof have structures shown in general formula I. In the formula I, R1 represents hydroxyl, carbonyl, amide, low-level alkyl, benzyloxy methyl, arakyl or unsaturated alkyl of C2-5; R2 represents tetrazole, halogen atoms, halohydrocarbon, cyanogen, cyanomethy, low-level alkyl, benzyloxy methyl, arakyl or unsaturated alkyl of C2-5; and R3 represents hydroxyl, carbonyl or amide. The antitumor drug (hydroxyl morpholine) and the derivative thereof have more excellent antitumor activity and safety, and can be applied to treating tumors of liver cancer, lung cancer, breast cancer, leukemia, colon cancer, ovarian cancer, gastric cancer, nerve cancer and the like, thereby having wide treatment range; and the antitumor drug (hydroxyl morpholine) and the derivative thereof as an antitumor agent have application values in the medicine filed.

The invention relates to an anti-tumour small molecule inhibitor targeting PD-1 / PD-L1 interaction, and application of the anti-tumour small molecule inhibitor. According to the small-molecule inhibitor in the invention, N-[2-(aminocarbonyl)phenyl][1,1'-biphenyl]-4-carboxamide can reactivate the immune response of T cells by inhibiting PD-1 / PD-L1 interaction, so as to efficiently kill tumour cellsin a targeted manner. The small molecule inhibitor can be used as a new anti-tumour drug and has important clinical treatment value.

The invention relates to novel S-type or R-type tetrahydronaphthalene amide compounds and pharmaceutically acceptable salts thereof, and a preparation method and application thereof. The novel S-typeor R-type tetrahydronaphthalene amide compounds and the pharmaceutically acceptable salts thereof have structures as shown in a general formula (I). The invention also provides the preparation methodfor the compounds, pharmaceutical combinations containing the compounds and antineoplastic action of the compounds. The novel substituted S-type or R-type tetrahydronaphthalene amide compounds have better anti-tumor activity and safety compared with control drugs, and can be used in the treatment of leukemia, gastrointestinal stromal tumors, lung cancer, colon cancer, ovarian cancer, kidney cancerand other tumors, so the therapeutic range of the compounds is wide, and the compounds are very valuable as an anti-tumor agent in the field of medicine.

A medicine for preventing and treating tumor is prepared through preparing the culture liquid of photosynthetic bacteria, preparing the liquid extract of colored mistletoe, proportionally mixing them, culturing for 3-30 days under illuminescence and anaeration condition to obtain the living bacteria preparation, and sterilizing.

The invention provides a flavone derivative represented by a formula I and pharmaceutically acceptable salt, hydrate or solvate thereof. In the formula I, R1 H, is 1-4 alkyl, amino or C1-4 acyl; R2 isisopentenyl or 2-hydroxy isopentyl; R3 is H, methyl or deuterated methyl; R4 represents C1-4 alkyl, amino or C1-4 acyl or R5 represents monosaccharide residue or oligosaccharide residue; and L represents polypeptide, C1-C20 straight chain alkyl or derivative thereof, C1-C20 straight chain or branched chain acyl derivative, C1-C20 ethylene glycol or derivative thereof, wherein Y is an integer of 0to 100, b is an integer of 1 to 100, C is an integer of 1 to 10, d is an integer of 0 to 100, and e is an integer of 0 to 100. The flavone derivative has high-efficiency broad-spectrum anticancer activity.

The invention belongs to the technical field of medicines, and relates to an HIF-2 alpha small-molecule inhibitor as well as a preparation method and an application thereof. The HIF-2alpha small-molecule inhibitor is a compound as shown in a structural general formula I and a stereoisomer, a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug thereof. According to the invention, molecular simulation drug design software MOE is used for screening and molecular docking of pharmacophores, according to a final docking dominant structure and an isosteric principle, a series of compounds are designed and synthesized, and an in-vitro anti-tumor activity screening test shows that the compounds have anti-tumor activity. The HIF-2 alpha small-molecule inhibitor provided by the invention has a relatively good application prospect in the aspect of preventing or treating cancers, particularly glioma.

The present invention relates to antitumor drug (hydroxyl morpholine) and derivative thereof as well as preparation method and application thereof. The antitumor drug (hydroxyl morpholine) and the derivative thereof have structures shown in general formula I. In the formula I, R1 represents hydroxyl, carbonyl, amide, low-level alkyl, benzyloxy methyl, arakyl or unsaturated alkyl of =CH2 or C2-5; R2 represents tetrazole, halogen atoms, halohydrocarbon, cyanogen, cyanomethy, low-level alkyl, benzyloxy methyl, arakyl or unsaturated alkyl of C2-5; and R3 represents hydroxyl, carbonyl or amide. The antitumor drug(hydroxyl morpholine) and the derivative thereof have more excellent antitumor activity and safety, and can be applied to treating tumors of liver cancer, lung cancer, breast cancer, leukemia, colon cancer, ovarian cancer, gastric cancer, nerve cancer and the like, thereby having wide treatment range; and the antitumor drug (hydroxyl morpholine) and the derivative thereof as an antitumor agent have application values in the medicine filed.

The invention belongs to the field of pharmacy and tumor diagnosis and treatment, and particularly relates to a compound serving as a cyclin-dependent kinase 12 (CDK12) inhibitor and application of the compound to treatment of proliferative diseases such as cancers including rectal cancer, breast cancer, ovarian cancer and the like. The CDK12 small-molecule inhibitor is a compound with the following structural general formulas (I)-(XII), a stereoisomer of the compound, or a pharmaceutically acceptable salt, a solvate, a hydrate, a polymorphic substance, a co-crystal substance, a tautomer, an isotope labeled derivative and a prodrug of the compound. The small-molecule inhibitor provided by the invention is relatively wide in anticancer spectrum, has a good growth inhibition effect on various cancer cells such as rectal cancer, breast cancer and ovarian cancer, provides an effective medicine for preventing or treating proliferative diseases, especially cancers in the aspects of structure and action mechanism, and has a relatively good application prospect.

The invention relates to the technical field of research, development and application of anti-tumor drugs, in particular to application of beta-pentagalloylglucose (PGG) in tumor resistance, and tumors are tumor cells with PALB2-BRCA2 binding characteristics. PGG and PALB2 have high affinity, have good biological activity on cell and animal levels, and can block a DNA homologous recombination repair pathway by inhibiting the interaction of PALB2-BRCA2, thereby enhancing the sensitivity of tumor cells to a PARP (Poly (ADP-ribose) polymerase) inhibitor and radiotherapy. The PGG can penetrate through the blood brain barrier and has no obvious toxic or side effect. The PGG can be effectively used for treating cancers such as breast cancer, lung cancer, liver cancer, brain glioma and the like by being combined with a PARP inhibitor or radiotherapy, and has a wide development prospect as a natural product.

The present invention relates to a novel compound tetrahydronaphthalene amide-group compound as represented by general formula I, or a pharmaceutically acceptable salt thereof, serving as an antineoplastic drug. Also provided are a preparation method of the compound, a pharmaceutical composition comprising the compound, a result of exosomatic and endosomatic antineoplastic effect, and a study on acute toxicity. The antineoplastic drug tetrahydronaphthalene amide-group compound of the present invention has better antineoplastic activity and safety, can be used to treat tumors such as leukemia, lung cancer, colon cancer, ovarian cancer and kidney cancer and the like, thus having a wide therapeutic window and a high application value as an antineoplastic agent in the pharmaceutical field.

A microsphere carrying fluoroplex is prepared through dissolving polylactic acid to dichloromethane, dispersing SiO2 in it to become suspension, filling it in the aqueous solution of gelatin while stirring to become oil-in-water O / W emulsion, stirring for volatilizing dichloromethane, solidifying microspheres, centrifugal collecting, washing with secondary distilled water, vacuum drying to obtain SiO2-PLA microspheres, immersing them in the solution of fluoroplex in hydrochloric acid, centrifugal collecting, washing with secondary distilled water and freeze drying. Its advantages are durable acting, slow releasing and targeting function.

A medicine for preventing and treating tumor is prepared through preparing the culture liquid of photosynthetic bacteria, preparing the liquid extract of colored mistletoe, proportionally mixing them, culturing for 3-30 days under illuminescence and anaeration condition to obtain the living bacteria preparation, and sterilizing.

The invention discloses a malignant tumor treating traditional Chinese medicine composition and a preparation method thereof. The composition is prepared from the ingredients in parts by weight: 3 to5 of borneol, 1 to 3 of musk, 10 to 15 of indigo naturalis, 10 to 15 of radix scrophulariae, 10 to 15 of fructus forsythiae, 10 to 15 of sweet wormwood herb, 10 to 20 of fructus evodiae and 10 to 15 of alumen. The composition disclosed by the invention has the advantages of accurate tumor treating effect, small toxic and side effects and suitability for clinical popularization and application.

This invention relates to methylaminopterin derivatives with 4-amino structure modified, which inhibit effect of nitrogen monoxide synthetase and growth of tumors. They have wide anti-cancer spectrum and little toxic side effect so as to be used in preparation of medicines for tumors, cancers, arthritis and intestinal diseases as well as chemicals for birth control.