469 results about "Osteosarcoma" patented technology

The invention relates to an image segmentation method based on a multi-supervision full-convolution neural network. According to the invention, further improvement is carried out based on the full convolution neural network, so a novel network structure is provided. The network structure has three edge output layers with supervision which are capable of guiding a network to learn multi-scale features and allowing the network to acquire local features and global features of images. Meanwhile, in order to keep context information in the images, in the upper sampling parts of the network, upper sampling is performed on output feature images by sue of multiple feature channels. Finally, a fusion layer with the weight is used for fusing the classification results of the multiple edge output layers, so the final image segmentation result is obtained. The method is characterized by high segmentation precision and quick segmentation speed. In osteosarcoma CT data segmentation, the DSC coefficient of the acquired segmentation result by use of the provided algorithm reaches 86.88%, which is higher than that of a traditional FCN algorithm.

Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

The present invention relates to compounds of Formula (I),methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury / loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

The invention searches the novel micromolecule inhibitor pyrazolo (1, 5-a) miazines compounds of cyclin-dependent kinase CDK9 (cyclin-dependent kinase) through the virtual screening of a computer, biometrically measures activity thereof, and validates interaction mechanism. The invention specifically comprises the following steps: the three-dimensional crystal conformation of the cyclin-dependent kinase family member CDK9 is obtained in a way of homology modeling; and micromolecule three-dimensional database is screened with DOCK (molecular docking). The invention uses a MTT tumor cell growth inhibition test to biometrically measures the activity of the selected compounds, researches the selected compounds pyrazolo (1, 5-a) miazines with high activety in a way of molecular mechanism, validates the inhibiting effect of the compounds to the activity of CDK9 kinase, and clarifies the interaction mechanism of the compounds for inhibiting the external activity and the molecule of various malignancies such as lung cancer, osteosarcoma, oophoroma, cervical carcinoma, breast cancer, etc.

The invention provides an application of a type of berbamine derivatives and salts thereof in the preparation of drugs for the treatment of tumors, which is mainly applied in the preparation of the drugs for the prevention and treatment of nuclear transcription factor NF-kBp65 activity-related diseases and BCR / ABL transcription activity-related diseases. The drugs are combined and prepared by the compounds of the invention and one or more pharmaceutically acceptable excipients. The preparation forms comprise solid preparations, semi-solid preparations or liquid preparations. The type of berbamine derivatives and the salts thereof provided by the invention have broader and stronger anti-leukemia and anti-solid-tumor activity, the tumors proved to be sensitive are leukemia, multiple myeloma, liver cancer, osteosarcoma and breast cancer; the toxicity and the side effects are lighter. An in vitro cell culture system and animal experiments confirm that the berbamine derivatives and the salts thereof have no significant toxicity or side effects to the growth of normal human hematopoietic cells and experimental animals under the anti-tumor dosage, which are superior to the commonly used chemotherapy drugs.

The invention discloses a long-chain recombination human bone pattern generating protein-2 and preparing method and application, which is characterized by the following: utilizing gene project technique to grow the protein in the expressing system of escherichia coli and bacillus subtilis; adopting human bone sarcoma cell mRNA to do reverse transcription to obtain the cDNA as form; augmenting nucleotide sequence of entire 114 amino acids naturally from carboxyl end; adding a segment of nucleotide in front of the first codon of primer 5' end; increasing a segment of polypeptide at N end corresponding to amino acid sequence; obtaining long-chain rhBMP-2 gene with molecular weight at 30KD and purity over 95%.

A compound of the formula [I]wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like.In addition, an intermediate for the compound is provided.

The invention discloses an application of a WWP1 gene. The WWP1 gene can be used for preparing products for diagnosing osteosarcoma and is used as a specific marker gene for diagnosing osteosarcoma so that the osteosarcoma is more accurately and quickly diagnosed. The products for diagnosing osteosarcoma comprise products for diagnosing osteosarcoma by virtue of RT-PCR, real-time quantitative PCR, immunodetection, in-situ hybridization or gene chips. The WWP1 gene disclosed by the invention can also be used for preparing drugs for treating osteosarcoma which provides novel therapeutic targets and effective novel drugs for prevention and treatment of osteosarcoma.

The invention discloses a carbon nanometer tube decorated by polyethyleneimine and a compound of plasmid DNA thereof. The plasmid DNA adopted in the invention comprises P53DNA, green fluorescent protein expression (JPC) and unmethylated oligomerization deoxynucleotide plasmid DNA. The carbon nanometer tube decorated by the polyethyleneimine and the compound of the plasmid DNA have the advantages of high transfection efficiency and less toxicity to cells; in particular, when the concentration is 30 g / ml, the transfection efficiency is larger than 90 percent, and the validity of the cells is larger than 80 percent. The carbon nanometer tube decorated by the polyethyleneimine and the compound of the plasmid DNA have wide application prospect during the process of preparing medicaments for remedying genes outside transfecting osteosarcoma cell bodies and in animal bodies; and the carbon nanometer tube decorated by the polyethylene imine / the plasmid DNA / an adriacin nanometer compound also have wide application during the process of preparing medicaments for restraining the growth of tumor.

The present invention relates to compounds of Formula (I),methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury / loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

The present invention relates to method for treating bone loss utilizing full length parathyroid hormone. The method dose not increase the risk of osteosarcoma or bone lesions.

The present invention relates to duocarmycin-containing antibody-drug conjugates (ADCs) for use in the treatment of human solid tumors and haematological malignancies expressing HER2, in particular breast cancer, gastric cancer, bladder cancer, ovarian cancer, lung cancer, prostate cancer, pancreatic cancer, colorectal cancer, head and neck squamous cell cancer or osteosarcoma, and acute lymphoblastic leukaemia. In particular, the present invention relates to duocarmycin-containing ADCs for use in the treatment of human solid tumors with HER2 IHC 2+ or 1+ and HER2 FISH negative tissue status. Advantageously, the present invention relates to duocarmycin-containing ADCs for use in the treatment of triple negative breast cancer (TNBC).

The invention relates to an application of chaperonin CCTgamma in preparation of a tumour diagnosis reagent and in particular relates to a new application of the chaperonin CCTgamma in preparation of an osteosarcoma diagnosis reagent. The inventor adopts bioinformatics method analysis for carrying out gene screening based on high-throughput sequencing results, a candidate gene CCTgamma is picked out, and further molecular cell biology experiments prove that CCTgamma has a good correlation with osteosarcoma, can be used for preparing an auxiliary osteosarcoma diagnosis and treatment preparation and has important clinical application value.

The invention discloses an anti-tumor combination and the application thereof; the anti-tumor combination which includes effective dose of platinum-based chemotherapy and AKT inhibitor and / or p70S6K1 inhibitor has the function of inhibiting the drug resistance of the tumor to the platinum-based chemotherapy, improves the effects of anti-tumor drugs, and can be used for preparing drugs that can resist various tumors, such as lung cancer, ovarian cancer, prostate cancer, breast cancer, stomach cancer, nasopharyngeal cancer, esophageal cancer, malignant lymphoma, head and neck squamous cell carcinoma, thyroid cancer, osteosarcoma, etc.

A compound of the formula [I]wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

The present invention relates to compositions and methods for the diagnosis, prognosis, and treatment of cancer. In particular, the present invention provides compositions and methods of using P450 3A4 / 5 expression in the diagnosis, prognosis, and treatment of osteosarcoma. The present invention thus provides improved compositions and methods for providing prognoses to osteosarcoma patients.

Toona sinensis extract for suppressing the proliferation and inducing apoptosis of osteosarcoma, but not normal human osterblasts. The extraction process comprises: extracting Toona sinensis with water to obtain a first extract, and filtering the first extract by a membrane to obtain a filtrate, and the Toona sinensis extract of the invention does not cause biological damages of normal bone cells. In addition, the invention further provides a pharmaceutical composition comprising the Toona sinensis extract.

The invention relates to application of echinacoside in anti-tumor medicaments. The application provided by the invention is as follows: firstly adding MTH1, inorganic pyrophosphatase and dGTP into a reaction solution (100mM pH 8.0 Tris-acetic acid, 40mM NaCl, 10mM magnesium acetate, 0.005% Tween 20 and 1mM DTT), incubating an enzyme and a substrate at room temperature for 1h, then adding 25 mu l of malachite green solution to terminate reaction and performing absorbance detection at 630nm by using an iMark microplate reader, wherein results show that echinacoside has a significant effect of inhibiting enzyme activity of MTH1; and secondly detecting the effects of echinacoside against tumor cells at the cellular level by an MTT experiment, wherein the results show that echinacoside can obviously inhibit the growth of SW480 colon cancer cells and U2OS human osteosarcoma cells. According to the application provided by the invention, echinacoside is used for inhibiting specific enzyme MTH1 for maintaining survival in the tumor cells, and oxidized nucleotide is mixed into DNA, thereby resulting in fatal DNA double-strand break in the cancer cells, producing an anti-tumor effect, finding a new medical use of echinacoside and laying a foundation for future development of the new anti-tumor medicaments.

Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

The invention relates an anticancer active part of fructus terminaliae billericae, and a preparation method of the anticancer active part. The invention comprises extraction of the part containing active components, study of a process for enriching by adopting macroporous absorption resin, identification of the active components in the active part, and use of the active part in in-vivo or in-vitroinhibition of liver cancer HepG2, lung cancer A549, lung adenocarcinoma NCI-H1703, gastric cancer BGC823, osteosarcoma cell MG-63, colorectal cancer HCT116, breast cancer MCF-7, neuroblastoma cells shsy5y, kidney cancer ACHN, normal liver cells L02, human breast ductal carcinoma cells ZR75-1, human colorectal adenocarcinoma cells Colo-205, human breast ductal carcinoma cells BT-474, human breastcancer cells T-47D, human cervical cancer cell line HeLa, liver cancer cells H22, and the like. The enrichment method applying the macroporous absorption resin to the anti-cancer active part of the fructus terminaliae billericae is simple in process, safe, non-toxic and low in production cost, and can be used for industrial production, thus having a great economic benefit and higher generalizationperformance.

The invention relates to a furan-azo-[3,2-g] chromene derivative and application thereof, belonging to the technical field of medicine. The furan-azo-[3,2-g] chromene derivative comprises stereoisomers and pharmaceutically applicable salts of a compound of the furan-azo-[3,2-g] chromene derivative and has a structural general formula shown in the specification of the invention. The furan-azo-[3,2-g] chromene derivative and pharmaceutically applicable acid addition salts of the compound can be used as an estrogen receptor regulator singly or by combining with traditional drugs to treat or prevent various diseases related to estrogen functions, such as bone loss, fracture, osteoporosis, hot flash, LDL (Low Density Lipoprotein) cholesterol level rise, angiocardiopathy, cognitive function impairment, brain-wasting diseases, anxiety, depression caused by estrogen shortage, inflammation, inflammatory bowel diseases, sexual dysfunction, hypertension, retinosis and cancer, especially breast cancer, ovarian cancer, osteosarcoma, endometrial cancer and prostatic cancer.

The invention discloses a new use of T-2 toxin, that is, application of T-2 toxin in the preparation of drugs for treating bone cancers and myeloproliferative disorder, wherein the curative dose thereof is 0.1-20 mg / Kg (weight), preferably 0.5-8 mg / Kg (weight), during drug administration, the method comprises oral administration, intravenous injection, hypodermic injection and intramuscular injection. The invention establishes animal or cell models of multiple myeloma, osteosarcoma and myelodysplastic syndrome, and inspects the inhibition of the T-2 toxin on the tumors or tumor cells by injection or cell co-culture. The experiment shows that the T-2 toxin is capable of inhibiting the growth of tumor cells and has good killing effect on the bone cancers and myeloproliferative disorder.

The invention discloses a human osteosarcoma stem-cell related antigenic marker stage-specific embryonic antigen-4 (SSEA-4) and an application thereof in a targeted therapy of osteosarcoma. The SSEA-4 is a specific osteosarcoma stem-cell surface marker which is almost not expressed in each normal adult tissue. The surface marker is easy for antibody labeling without affecting the cell viability, and applicable to the function tests after separation, therefore, a reliable molecular tracer is provided for further researching the function of stem cells in the origin, occurrence and development processes of osteosarcoma, and a foundation for explaining the clinical osteosarcoma drug resistance as well as transferring and looking for cellular and molecular targets for the targeted therapy is laid.

A method for treating cancer by killing selected tumor cells such as human breast, non-small cell lung cancer cells, pancreatic cancer cells, osteosarcoma cancer cells, and glioblastoma cells, includes administering to a patient in need of treatment, an effective amount of at least one mannose analog such as 2-DG or 2-FM or 2-CM. The killing is believed to be due to an interference with glycosylation. A theranostic method includes determining whether a patient. cancer tumor sample comprises cells sensitive to killing to at least one mannose analog due to an interference with glycosylation.

The present invention relates to a novel method for treating a patient that has osteoporosis and the patient may be having administered cyclase activating parathyroid hormone (CAP) or analogues. The patient receives an administration of a cyclase inhibiting parathyroid hormone peptide (CIP) having an amino acid sequence from between (SEQ ID NO:1 [PTH2-84]) and (SEQ ID NO:3 [PTH34-84]) (i.e., a contiguous portion of PTH having an amino acid sequence set forth in SEQ ID NO:5 (PTH1-84), having the N-terminal amino acid residue starting at any position spanning from position 2 through position 34 of the PTH1-84, and the C-terminal amino acid residue ending at position 84 of the PTH1-84), (preferably (SEQ ID NO:2 [PTH3-84]) and (SEQ ID NO:8 [PTH28-84])), or a conservatively substituted variant thereof exhibiting parathyroid hormone (PTH) antagonist activity in a therapeutically effective, but non-toxic amount that reduces the occurrence of hypercalcemia or osteosarcoma in the patient resulting from the administration of CAP, and yet, through a CAP rebound effect, is effective in itself in the treatment of osteoporosis.

Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

The invention relates to a newly identified tumor suppressor gene, designated DOS (for Deleted in Osteosarcoma and alternatively referred to herein as DOCK 3) which has been cloned from human and mouse cells. The DOS nucleic acid and protein molecules and their use in the diagnosing and treating disorders characterized by aberrant DOS molecule expression are described.

The invention relates to a tumor marker LIMK1 and application thereof, in particular to an LIMK1 gene and application of an expression product thereof in diagnosis and treatment of osteosarcoma. A fluorescent quantitative polymerase chain reaction (PCR) technology is used for detecting cells of the osteosarcoma and tissues of patients, so that the overexpression of the LIMK1 gene is shown. Furthermore, a plurality of groups of siRNA are designed so as to silence the expression of the LIMK1 gene. The tumor marker LIMK1 provides a new thought for research of the osteosarcoma on the one hand, and provides a potential new target point for the diagnosis and the treatment of the osteosarcoma in a gene level on the other hand.