52 results about "Development drugs" patented technology

The present invention relates to methods and materials used to express the HBM protein in animal cells and transgenic animals. The present invention also relates to transgenic animals expressing the high bone mass gene, the corresponding wild-type gene, and mutants thereof. The invention provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in bone development, and methods of diagnosing and treating diseases involved in bone development. In preferred embodiments, the present invention is directed to methods for treating, diagnosing and preventing osteoporosis.

The present invention relates to novel therapeutic uses of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof. Furthermore, the present invention relates to the use of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof, in obtaining methods of screening and of developing drugs. Finally, the present invention relates to the novel therapeutic use of other glutamine synthetase (GS) ligands and to the use of these ligands in obtaining methods for screening and developing drugs.

The invention is related to the field of biotechnology, specifically to the investigation of biomolecular interactions and sensing of biomolecules using a surface plasmon resonance. The biological sensor and a method of its production based on the thin films of graphene, graphene oxide, or single-walled or multi-walled carbon nanotubes are described.The technical results of the invention are a high sensitivity of the biosensor in combination with a high biospecificity; an expansion of the range of device applications; the protection of the metal film from an environmental exposure; the possibility to detect large biological objects.The proposed device and method of its production can be used for monitoring and recording of the concentration of chemical and biochemical substances and for the definition of parameters of biomolecular reactions in different industrial processes using biological materials, the invention can be also used in the pharmaceutical industry for the investigation of pharmacological properties and for the determination of a chemical composition of developing drugs, and also it can be used in processes of quality control of food products.

This invention defines novel research and clinical laboratory methodology and compositions related thereto appropriate for use in (a) determining the presence of a neurodegenerative disease selected from the group limited solely to Charcot-Marie-Tooth disease, familial Alzheimer's disease, familial Parkinson's disease, Huntington's disease, spinal muscular atrophy, Friedreich'a ataxia, giant axon neuropathy, juvenile ceroid-lipofuscinosis, familial motor neuron diseases, juvenile diabetic polyneuropathy and Down's syndrome, (b) monitoring the ongoing status of the physiological expression of said disease and (c) screening candidate therapeutic drug agents for possible effectiveness. The invention is based on the new and novel observation that the presence of a neurodegenerative disease can be characterized in part by the expression in cultured fibroblasts obtained from the patient of one or more proteins which are not the product of a defective disease-inducing gene, but which are stress proteins, one or more other proteins modified by conditions of oxidative stress or one or more other disease-related proteins. The invention depends on living cell material, namely fibroblasts, which are readily and, if necessary, repeatedly available from a patient. When adapted as a method and composition useful for the screening candidate therapeutic drug agents for possible effectiveness, this technology offers advantages in terms of (a) providing research opportunities which, in some cases, never existed before, (b) cost effectiveness when compared to alternative technologies, (c) ability to be used readily on a large scale, (d) ability to generate meaningful data in a comparatively short period of time, and (e) providing an early stage opportunity to obtain information based on direct interaction of a candidate drug and a living tissue disease model. Various aspects of diagnostic methods and compositions are also disclosed.

The invention relates to a pharmaceutical composition containing an FGFR4 inhibitor, in particular to the pharmaceutical composition containing the FGFR4 inhibitor with a structure shown in a formula(I). The pharmaceutical composition developed by the invention has strong inhibition effect on FGFR4 kinase activity, and can be widely used for preparing medicaments for treating cancers, especiallyliver cancer, gastric cancer, prostate cancer, skin cancer, ovarian cancer, lung cancer, breast cancer, colon cancer, pancreatic cancer, esophageal cancer, glioma or rhabdomyosarcoma. (See the instruction for specific formula).

The present invention relates to novel peptide derivatives, which are recognized as ligands to G-coupled protein receptor proteins. The peptide of the present invention can be used in (1) development of a receptor binding assay system using the expression system of the recombinant receptor protein and screening of candidates for pharmaceutical compounds, and (2) development of pharmaceutical preparations such as a neutral nerve function regulator, a circulatory function regulator, a cardiac function regulator, an immune function regulator, a digestive organ function regulator, a metabolic function regulator, a generative organ regulator or the like.

Eukaryotic protein-coding messenger RNAs and non-coding microRNAs are naturally transcribed by type II RNA polymerases (pol-2) but not prokaryotic RNA polymerases. As a result, current eukaryotic RNA and protein production is performed either using eukaryotic pol-2 promoters in hybridomas or mammalian cells or using prokaryotic promoters in bacterial cells. However, because prokaryotic RNA transcription tends to be error-prone, frequent mutation is a big problem. Also, growing hybridomas or mammalian cells is relatively laborious and costly. To overcome these problems, the present invention provides a novel inducible composition and method for producing eukaryotic RNAs and / or their related peptides / proteins directly using eukaryotic pol-2 promoter-driven gene expression in fast growing bacteria, without the need of changing to prokaryotic promoters or growing hybridomas / mammalian cells. The RNAs and peptides / proteins so obtained can be used to develop drugs, cure diseases, treat tumors / cancers, produce pluripotent stem (iPS) cells, enhance wound healing, and make foods.

Galectin 9 exerts various functions depending on its localizations. On the other hand, galectin 9 is expected as participating in various biological functions. Thus, it has been required to clarify the detailed biological activities of galectin 9 and develop galectin 9-related techniques including development of drugs. Human galectin 9 shows a cytotoxic activity and an apoptosis-inducing activity on tumor cells but shows neither cytotoxic activity nor apoptosis-inducing activity on normal cells. Therefore, it is possible to employ galectin 9 proteins, galectin 9 agonists, galectin 9 antagonists, anti-galectin 9 binding protein antibodies, anti-galectin 9 binding sugar chain antibodies, galectin 9-producing, releasing or inducing substances, etc. as antitumor, antiallergic, immunosuppressive agents, drugs for autoimmune diseases, anti-inflammatory agents and active ingredients for adrenocortical steroid hormone alternatives.

Graft copolymer (P) which exhibit pH dependent swelling / dissolution properties comprising a hydrophobic back-bone and graft chains comprising acidic monomer. This Graft copolymer (P) do not swell or dissolve at acidic pH prevalent in the stomach and they swell / dissolve at near neutral pH prevalent in the intestinal region. The graft copolymer (P) is useful for the development of drug delivery formulations particularly for oral drug delivery formulations.

The invention relates to a method for analysing an interaction between a first molecule and a second molecule bonded to a particle, including the following steps: contacting the first molecule with the second molecule bonded to the particle under conditions enabling the interaction thereof; applying a predetermined liquid flow to the particle bonded to the second molecule; observing a movement of the particle bonded to the second molecule caused by the applied flow; analysing the interaction according to the movement observed and the applied flow, the particle having a greater hydrodynamic resistance than the first and / or second molecule, and a mass Péclet number of greater than 1. The invention also relates to a device for analysing an interaction between a first molecule and at least one second molecule, as well as to the use of the method or of the device in screening a candidate molecule for developing a drug.

The present invention relates to methods and materials used to express an HBM-like polypeptide derived from HBM, LRP5 or LRP6 in animal cells and transgenic animals. The present invention also relates to transgenic animals expressing the HBM-like polypeptides. The invention provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in bone development, and methods of diagnosing and treating diseases involved in bone development and lipid modulation. In preferred embodiments, the present invention is directed to methods for treating, diagnosing and preventing osteoporosis.

The present invention relates to methods and materials used to isolate and detect a high bone mass gene and a corresponding wild-type gene, and mutants thereof. The present invention also relates to the high bone mass gene, the corresponding wild-type gene, and mutants thereof. The genes identified in the present invention are implicated in bone development. The invention also provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in bone development, and methods of diagnosing and treating diseases involved in bone development. In preferred embodiments, the present invention is directed to methods for treating, diagnosing and preventing osteoporosis.

A system and a method for linking relevant data relating to clinical supplies needed for the development of a drug. This system makes it possible for a drug developer to (a) plan an extensive series of clinical trials, (b) project the quantities of clinical supplies required for the clinical trials and arrange for the manufacturing of these supplies, (c) trace all lots of clinical supplies during the clinical trials, (d) allocate clinical supplies for a plurality of clinical trials, (e) record data relating to the inventory, and (e provide reports relating to the clinical supplies and clinical trials.

The present invention provides a method of using a physiologically-based pharmacokinetic model to select a prodrug molecule (NO-X) comprising a therapeutic agent X (e.g. nonsteroidal anti- inflammatory drug, (NSAID)) and an appropriate nitric oxide donor NO. The NSAID can be a non- selective or selective cyclooxygenase inhibitor or other biocompatible compound comprising a carboxyl group. The pharmacokinetic model uses in vitro and / or in silico data to estimate an optimal set of parameters that can predict whether a particular NO-X candidate is capable of producing desirable therapeutic effects, e.g. enhanced antiif lammatory activity, reduced intestinal, cardiac and renal toxicity. Accordingly, the present invention can greatly enhance proper selection of an appropriate candidate for drug development, thereby minimizing development time and conserving costs.

The invention discloses application of GL-V9 in preparation of a medicine for preventing and / or treating sepsis. Compared with the prior art, it is found that in an in-vitro experiment, the GL-V9 can be used for remarkably recovering J774A.1 cell viability decline and increased cytotoxic damage caused by two ways of transfecting lipopolysaccharide (LPS) into macrophages by lipidosome 2000 and infecting the macrophages by Escherichia coli to cause pyroptosis, and inhibiting the expression condition of the pyroptosis related protein mediated by the Caspase-11. In in-vivo experiments, the GL-V9 can reduce the death rate of cecum ligation paracentesis (CLP) sepsis model mice, weaken organ function damage and inhibit release of inflammatory factors. The effects show that the GL-V9 can be used for treating sepsis and has a medicine development prospect.

The present invention relates to a composition for preventing, improving or treating a mental disorder, the composition containing a Lactobacillus sp. bacteria-derived vesicle as an active ingredient. The present inventors have confirmed that, when a Lactobacillus sp. bacteria-derived vesicle is administered to a stress and depression animal model, resistance to stress efficiently increases, and an effect of treating chronically persisting long-term depression behavior is exhibited, and thus the Lactobacillus sp. bacteria-derived vesicle, according to the present invention, is expected to be capable of being usefully employed in developing a medicine or a functional health food, etc., for preventing, reducing the symptoms of or treating a mental disorder such as stress, anxiety disorder, post-traumatic stress disorder, panic disorder, depression, autism spectrum disorder, attention deficit hyperactivity disorder and schizophrenia.

The present invention relates to novel peptides that are recognized by G protein-coupled receptor proteins. The peptides of the present invention may be used for 1 &cir& development of receptor binding assay system using the expression system of recombinant receptor proteins and screening of candidate compounds for potent pharmaceutical products and 2 &cir& development of pharmaceuticals such as a central nervous function regulator, a circulatory function regulator, a cardiac function regulator, an immune function regulator, a digestive function regulator, a metabolic function regulator or a reproductive organ function regulator.

The invention relates to a synthesis method of 9-demethyl-(+)-alpha-dihydrotetrabenazine. The synthesis method comprises the following steps: 9-benzyloxy-(+)-alpha-dihydrotetrabenazine serves as a raw material and experiences reactions for at least 10min in a polar protonic solvent at room temperature under the catalysis of hydrobromic acid to obtain the reaction liquid of a crude product of 9-demethyl-(+)-alpha-dihydrotetrabenazine, wherein the polar protonic solvent is at least one of C1-C10 monohydric alcohols. The synthesis method has the advantages of relatively low preparation cost, relatively mild reaction conditions, relatively short reaction time, relatively simple reaction operation and relatively high reaction yield, facilitates the large-scale industrial production of 9-demethyl-(+)-alpha-dihydrotetrabenazine and lays a foundation for the large-scale industrial production of a development drug 11C-(+)-alpha-DTBZ and a development drug 18F-FP-(+)-alpha-DTBZ.

The invention discloses application of isosteviol (ISV) serving as an active ingredient to treatment of sepsis. Compared with the prior art, the ISV has the characteristics of high efficiency and lowtoxicity. The ISV can significantly improve the survival rate of sepsis mice, inhibit the expression of inflammatory factors IL-6, TNF[alpha] and IL-1[beta] in the bodies of the sepsis mice, and improve the damage of the sepsis to the bodies. The effects show that the ISV can be used for treating the sepsis and has medicine development prospects.

This application provides a method for mutagenesis of a gene, which comprises introducing much more point mutations into one strand of double-stranded genomic DNA of cell or organism individual than into another strand. In accordance with such a method, it is now possible to efficiently and effectively construct various useful mutants of microorganisms, cells or organism individuals. It is also now possible by analyzing the mutating conditions of the gene to clarify the mechanism of drug resistance, to estimate the occurrence of a novel insensible microorganism or to develop a drug therefor, to analyze the mutation of an oncogene and the mechanisms of cancer metastasis and increase in malignancy, to develop a therapeutic method using these mechanisms, etc.

The present invention relates to a composition for preventing, improving or treating a mental disorder, the composition containing a Lactobacillus sp. bacteria-derived vesicle as an active ingredient.The present inventors have confirmed that, when a Lactobacillus sp. bacteria-derived vesicle is administered to a stress and depression animal model, resistance to stress efficiently increases, and an effect of treating chronically persisting long-term depression behavior is exhibited, and thus the Lactobacillus sp. bacteria-derived vesicle, according to the present invention, is expected to be capable of being usefully employed in developing a medicine or a functional health food, etc., for preventing, reducing the symptoms of or treating a mental disorder such as stress, anxiety disorder, post-traumatic stress disorder, panic disorder, depression, autism spectrum disorder, attention deficit hyperactivity disorder and schizophrenia.

The invention belongs to the field of biomedicine and relates to use of FBP aldolase in preparation of AMPK activating drugs. The present invention also relates to use of the FBP aldolase in preparation of drugs for inhibiting cholesterol synthesis, drugs for reducing fatty acid synthesis, drugs for preventing and / or treating diabetes, drugs for preventing and / or treating tumors, drugs for preventing and / or treating Parkinson's disease, drugs for preventing and / or treating Alzheimer's disease or drugs for prolonging the lifespan of organisms. The FBP aldolase is used as a target to develop theAMPK activating drugs. Difficulties existing in the prior art in direct using of AMPK as a drug target can be overcome, and the FBP aldolase has a good application prospect.

The invention relates to application of an MIIP pS303 blocking agent to preparation of antitumor drugs. According to researches, PKC epsilon (protein kinase C epsilon) phosphorylated MIIP (migration and invasion inhibitory protein) protein serine 303 (S303) is discovered after EGFR (epidermal growth factor receptor) signal activation, the phosphorylated MIIP can be combined with a significant functional molecule RelA in an NF-kB signal pathway, and accordingly a RelA acetylation level is maintained after EGFR signal activation, RelA mediated migration promoting molecule expression is further promoted, and colonic cancer cell migration is promoted finally. Therefore, drugs can be developed by taking the phosphorylated site (MIIP pS303) as a target and clinically used for treating EGFR / PKC epsilon abnormal activation type malignant tumors. In addition, correlation between colorectal cancer migration and poor prognosis and MIIP S303 phosphorylation is verified, so that reagents for detecting MIIP S303 phosphorylation level can be used for diagnosis or prognosis of colorectal cancers.

The invention discloses a nuclear medicine and magnetic resonance bimodal development drug precursor (DOTA-SPIONs-PEG-FA). The drug precursor takes superparamagnetic iron oxide nanoparticles as cores and is coated with a biocompatible material and a double functional chelating agent. Folic acid is connected to the superparamagnetic iron oxide nanoparticles through the biocompatible material. The bimodal development drug precursor is labeled by a radioactive metal nuclide, so that a brand-new nuclear medicine and magnetic resonance bimodal development drug (RM-DOTA-SPIONs-PEG-FA) is obtained for the first time. The drug is good in in-vitro stability, has very high initial uptake, a good tumor / blood ratio and a relatively long residence time in tumor if being applied to folate receptor positive tumor detection, moreover, the nanoparticles have obvious active targeting action on tumor, so that the drug precursor can be effectively suitable for MRI development and EPT or SPECT development.

The present invention relates to methods and materials used to isolate and detect a high bone mass gene and a corresponding wild-type gene, and mutants thereof. The present invention also relates to the high bone mass gene, the corresponding wild-type gene, and mutants thereof. The genes identified in the present invention are implicated in bone development. The invention also provides nucleic acids, including coding sequences, oligonucleotide primers and probes, proteins, cloning vectors, expression vectors, transformed hosts, methods of developing pharmaceutical compositions, methods of identifying molecules involved in bone development, and methods of diagnosing and treating diseases involved in bone development. In preferred embodiments, the present invention is directed to methods for treating, diagnosing and preventing osteoporosis.

The invention discloses an aptamer of methotrexate, an aptamer derivative and application of the aptamer and the aptamer derivative. A nucleotide sequence of the aptamer comprises DNA molecules as shown in sequences 1-5. The aptamer can be a derivative obtained from various similar sequences with high homology or derivatives provided by the invention. A method for detecting the methotrexate is established by utilizing the specific binding effect of the aptamer HMX38 and the methotrexate for the first time. The aptamer and the derivative thereof can be used for preparing methotrexate detection probes and drug carriers or used for drug design and development, drug separation and purification and the like. The aptamer and the derivative thereof have the advantages of being capable of being combined with methotrexate with high specificity and high affinity, free of immunogenicity, capable of being chemically synthesized, good in biocompatibility, small in molecular weight, stable, easy to store and the like.

The invention provides a gene combination for inducing liver cells into liver cancer cells and application of the gene combination. The gene combination comprises a TP53 mutant gene and a c-MYC gene.Specifically, the gene combination is overexpressed in hepatocytes by utilizing lentivirus, so that normal hepatocytes can be induced to form live cancer cells. A primary live cancer humanized mouse model can be obtained by transplanting the human primary hepatocytes subjected to transfer of the gene combination into Fah gene mutation immunodeficient animals such as mice for in-vivo culturing. Liver cancer cells of the model are transformed from normal liver cells, and the model is an in-vivo model in which normal liver cells and liver cancer cells are jointly embedded, so that the human livercancer forming process and the liver cancer microenvironment can be better simulated, researchers can conveniently utilize the model to research occurrence, development and evolution process of livercancer, and a favorable model is provided for development of novel liver cancer drugs, pharmacological toxicology research of the drugs and drug resistance mechanism exploration of liver cancer treatment drugs.