1453 results about "Drug development" patented technology

The invention describes a method for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, comprising the steps of: a) compartmentalising the compounds into microcapsules together with the target, such that only a subset of the repertoire is represented in multiple copies in any one microcapsule; and b) identifying the compound which binds to or modulates the activity of the target; wherein at least one step is performed under microfluidic control. The invention enables the screening of large repertoires of molecules which can serve as leads for drug development.

The invention describes a method for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, comprising the steps of: a) compartmentalising the compounds into microcapsules together with the target, such that only a subset of the repertoire is represented in multiple copies in any one microcapsule; and b) identifying the compound which binds to or modulates the activity of the target; wherein at least one step is performed under microfluidic control. The invention enables the screening of large repertoires of molecules which can serve as leads for drug development.

The invention describes a method for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, by compartmentalizing the compounds into microcapsules together with the target, such that only a subset of the repertoire is represented in multiple copies in any one microcapsules; and identifying the compound which binds to or modulates the activity of the target. The invention enables the screening of large repertoires of molecules which can serve as leads for drug development.

X-ray fluorescence (XRF) spectrometry has been used for detecting binding events and measuring binding selectivities between chemicals and receptors. XRF may also be used for estimating the therapeutic index of a chemical, for estimating the binding selectivity of a chemical versus chemical analogs, for measuring post-translational modifications of proteins, and for drug manufacturing.

A system has been constructed that recapitulate the features of a capillary bed through normal human tissue. The system facilitates perfusion of three-dimensional (3D) cell monocultures and heterotypic cell co-cultures at the length scale of the capillary bed. A major feature is that the system can be utilized within a “multiwell plate” format amenable to high-throughput assays compatible with the type of robotics commonly used in pharmaceutical development. The system provides a means to conduct assays for toxicology and metabolism and as a model for human diseases such as hepatic diseases, including hepatitis, exposure-related pathologies, and cancer. Cancer applications include primary liver cancer as well as metastases. The system can also be used as a means of testing gene therapy approaches for treating disease and inborn genetic defects.

Embodiments of the invention relate to omni-tomographic imaging or grand fusion imaging, i.e., large scale fusion of simultaneous data acquisition from multiple imaging modalities such as CT, MRI, PET, SPECT, US, and optical imaging. A preferred omni-tomography system of the invention comprises two or more imaging modalities operably configured for concurrent signal acquisition for performing ROI-targeted reconstruction and contained in a single gantry with a first inner ring as a permanent magnet; a second middle ring containing an x-ray tube, detector array, and a pair of SPECT detectors; and a third outer ring for containing PET crystals and electronics. Omni-tomography offers great synergy in vivo for diagnosis, intervention, and drug development, and can be made versatile and cost-effective, and as such is expected to become an unprecedented imaging platform for development of systems biology and modern medicine.

The present invention provides methods for identifying targets of a drug in a cell by comparing (i) the effects of the drug on a wild-type cell, (ii) the effects on a wild-type cell of modifications to a putative target of the drug, and (iii) the effects of the drug on a wild-type cell which has had the putative target modified of the drug. In various embodiments, the effects on the cell can be determined by measuring gene expression, protein abundances, protein activities, or a combination of such measurements. In various embodiments, modifications to a putative target in the cell can be made by modifications to the genes encoding the target, modification to abundances of RNAs encoding the target, modifications to abundances of target proteins, or modifications to activities of the target proteins. The present invention also provides methods for drug development based on the methods for identifying drug targets.

The invention describes a method for the identification of compounds which bind to a target component of a biochemical system or modulate the activity of the target, by compartmentalizing the compounds into microcapsules together with the target, such that only a subset of the repertoire is represented in multiple copies in any one microcapsules; and identifying the compound which binds to or modulates the activity of the target. The invention enables the screening of large repertoires of molecules which can serve as leads for drug development.

A system has been constructed that recapitulate the features of a capillary bed through normal human tissue. The system facilitates perfusion of three-dimensional (3D) cell monocultures and heterotypic cell co-cultures at the length scale of the capillary bed. A major feature is that the system can be utilized within a “multiwell plate” format amenable to high-throughput assays compatible with the type of robotics commonly used in pharmaceutical development. The system provides a means to conduct assays for toxicology and metabolism and as a model for human diseases such as hepatic diseases, including hepatitis, exposure-related pathologies, and cancer. Cancer applications include primary liver cancer as well as metastases. The system can also be used as a means of testing gene therapy approaches for treating disease and inborn genetic defects.

The present invention generally relates to a combination of the fields of tissue engineering, drug discovery and drug development. It more specifically provides new methods and materials for testing the efficacy and safety of experimental drugs, defining the metabolic pathways of experimental drugs and characterizing the properties (e.g., side effects, new uses) of existing drugs. Preferably, evaluation is carried out in three-dimensional tissue-engineered systems, wherein drug toxicity, metabolism, interaction and / or efficacy can be determined.

The present invention relates to systems and methods for biomedical drug research, addressing major molecular, cell biological and biochemical information management issues within drug discovery and basic biomedical science. The invention allows scientists to enter biological, chemical, and / or molecular data into a central database, analyze the data entries according to entry attributes, and graphically view the results. A group of web-enabled researchers can enter, share and analyze molecular and cellular data and information from the resources using standardized vocabularies and ontologies. This application describes in detail components of the databasing system, including but not limited to annotation modules, reference managers, advanced search algorithms, ontology browsers, molecular network builders, and text processing scripts. Ultimately, the information gathered, viewed, and analyzed by this relational databasing system is relevant to research ranging from basic researchers to advanced research in applied technologies within pharmaceutical development and biotech fields.

The invention provides a system and methods for the determination of the pharmacogenomic phenotype of any individual or group of individuals, ideally classified to a discrete, specific and defined pharmacogenomic population(s) using machine learning and population structure. Specifically, the invention provides a system that integrates several subsystems, including (1) a system to classify an individual as to pharmacogenomic cohort status using properties of underlying structural elements of the human population based on differences in the variations of specific genes that encode proteins and enzymes involved in the absorption, distribution, metabolism and excretion (ADME) of drugs and xenobiotics, (2) the use of a pre-trained learning machine for classification of a set of electronic health records (EHRs) as to pharmacogenomic phenotype in lieu of genotype data contained in the set of EHRs, (3) a system for prediction of pharmacological risk within an inpatient setting using the system of the invention, (4) a method of drug discovery and development using pattern-matching of previous drugs based on pharmacogenomic phenotype population clusters, and (5) a method to build an optimal pharmacogenomics knowledge base through derivatives of private databases contained in pharmaceutical companies, biotechnology companies and academic research centers without the risk of exposing raw data contained in such databases. Embodiments include pharmacogenomic decision support for an individual patient in an inpatient setting, and optimization of clinical cohorts based on pharmacogenomic phenotype for clinical trials in drug development.

This invention relates to computer systems for conducting drug and biomarker discovery, drug development, and personalized medicine, and more generally managing healthcare, and in particular to a system and method for predicting the therapeutic value of a treatment to an individual. The treatment is associated with a function that describes, in a population of individuals, the benefit from a treatment, generally in terms of occurrence of a medical event under treatment, as a function of the risk (e.g., the occurrence of the medical event) without said treatment.

Methods of identifying DNase I Hyper-Resistant Sites (DHRS), or in board sense, highly compact chromatin and characterizing the DNA methylation status of DMRs such as CpG islands and CpG island shores are provided. The methods are particularly useful for analysis of genomic DNA from low quantities of cells, for example, less than 1,000 cells, less than 100 cells, less than 10 cells, or even one cell, and can be used to generate chromatin and methylation profiles. The downstream analyses include in parallel massive sequencing, microarray, PCR and Sanger sequencing, hybridization and other platforms. These methods can be used to generate chromatin and DNA methylation profiles in drug development, diagnostics, and therapeutic applications are also provided.

The activity of multiple proteins in a single living cell, portion of a cell or in a group of cells is simultaneously measured by introducing reporter molecules. The reporter(s) is chemically modified by the enzyme of interest. In some cases the enzyme(s) is affected by the addition of a stimulus or a pharmaceutical compound to the cell. The reactions between the enzymes and the reporters are diminished or terminated, and the reporter and modified reporter are removed. The activity of the enzyme(s) is determined by measuring the amount of reporter remaining, the amount of altered reporter produced, or by comparing the amount of reporter to the amount of altered reporter. A database is compiled of the activities of the different proteins. By performing a series of experiments at different time points, conditions, and varieties of cell types, a database is developed for molecular cellular mechanisms in health and disease states. By exposing cells to a variety of compounds data for drug development and screening is provided.

The invention discloses a method for establishing a fragile X-syndrome non-human primate model on the basis of a CRISPR gene knockout technology. The method comprises the following steps: (1) establishing a FMR1 gene knockout machin model; (2) carrying out identification and related functional analysis on the machin model; (3) carrying out tests on the nerve characteristics and learning and memorizing ability of the machin model. The method utilizes a CRISPR gene knockout technology to establish a fragile X-syndrome non-human primate model. The model fills the blank of non-human primate model, can effectively stimulate the pathological process of human diseases, can be used as an optimum animal model for researching human diseases, can effectively predict the effect of novel vaccine, novel drug or novel diagnostic reagent in clinical applications, and thus greatly reduces the risk of novel drug development.

The invention discloses a water soluble triazole compound and a synthesis method thereof. The water soluble triazole compound has a structure as shown in Formula Ia, Formula Ib, Formula Ic or Formula Id, wherein R1 is a group in Formula II. The compound of the invention is formed by adding a new group on the structural basis of a broad-spectrum, high-efficiency antifungal compound discovered in the present clinical application and new drug development process to increase the water solubility and reduce the toxicity, is a derivate of the triazole antifungal drug, and has the characteristics of broad antifungal spectrum, high antifungal activity, good safety and the like.

Labels and methods of producing labels for use in clinical, analytical and pharmaceutical development assays are provided. Labels may comprise shape-encoded particles which may be coupled to ligands such as DNA, RNA and antibodies, where different shapes are used to identify which ligand(s) are present. Labels may also comprise reflectors, including retroreflectors and retroreflectors susceptible to analyte-dependent assembly for efficient homogeneous assays.

Evidence demonstrating that elevated expression of dUTPase protects breast cancer cells from the expansion of the intracellular uracil pool, translating to reduced growth inhibition following treatment with 5-FU is provided. The implementation of in silica drug development techniques to identify and develop small molecule inhibitors of dUTPase are reported. As 5-FU and the oral 5-FU pro-drug capecitabine remain central agents in the treatment of a variety of malignancies, the clinical utility of a small molecule inhibitor to dUTPase represents a viable strategy to improve the clinical efficacy of these mainstay chemotherapeutic agents.

The present invention provides methods and compositions for screening, diagnosis and prognosis of Schizophrenia, for monitoring the effectiveness of Schizophrenia treatment, identifying patients most likely to respond to a particular therapeutic treatment and for drug development. Schizophrenia-Associated Features (SFs), detectable by two-dimensional electrophoresis of cerebrospinal fluid, serum or plasma are described. The invention further provides Schizophrenia-Associated Protein Isoforms (SPIs) detectable in cerebrospinal fluid, serum or plasma, preparations comprising isolated SPIs, antibodies immunospecific for SPIs, and kits comprising the aforesaid.

According to the present invention, capable of safely holding a large amount of undifferentiated embryonic stem cells to culture in the absence of feeder cells or feeder cell-derived components. Cultured embryonic stem cells can be applied to the fields of cell culture, tissue transplantation, drug development, and gene therapy.

The invention discloses a c-di-GMP and analogues thereof which have structures of a general formula I. The invention also discloses a novel preparation method-a kettle phosphoramidite method which can be used for rapidly, simply and conveniently preparing c-di-GMP compounds with high yield and low cost on a large scale and at mild conditions. The c-di-GMP is prevalent in bacteria and is a novel second messenger molecular which takes part in regulating multiple physiological functions. The research shows that the c-di-GMP and the analogues thereof can inhibit the formation of bacterium biological membranes and the multiplication of eukaryotic cells; and thereof the c-di-GMP and the analogues thereof have good medicine development prospect.

Provided are methods for determining concurrently with a simple, minimally invasive test, the adequacy of pancreatic beta-cell compensation and / or the presence of tissue insulin resistance in a subject human or an experimental animal. The methods allow for the determination of a subject's or experimental animal's susceptibility to developing type 2 diabetes mellitus (DM2) or to progression to more advanced forms of DM2. Among other uses, the methods allow for diagnostic classification of subjects for decisions regarding therapeutic interventions, clinical differentiation between type 1 DM and DM2, clinical monitoring of treatments intended to reduce risk of developing DM2 in non-diabetic subjects, clinical monitoring of agents intended to improve existing DM2 and to prevent progression of DM2, clinical development and testing of new compounds, candidate agents, or candidate therapies for preventing progression to DM2 or disease progression in existing DM2, and preclinical screening of candidate agents or candidate therapies in experimental animals to identify and characterize agents having insulin-sensitizing properties, pancreatic stimulatory or regenerative properties or other desirable actions.

Methods for identifying Rheb effectors are provided. The Rheb effectors can be Rheb agonists or antagonists and can be utilized as lead compounds for the development of drugs for the treatment of diabetes or diseases associated with abnormal cell growth. Non-human, transgenic animals over-expressing Rheb protein, and methods of making such transgenic animals, are also provided.

A method of propagating mammalian endodermally derived progenitors such as hepatic progenitors, their progeny, or mixtures thereof is developed which includes culturing mammalian progenitors, their progeny, or mixtures thereof on a layer of embryonic mammalian feeder cells in a culture medium. The culture medium can be supplemented with one or more hormones and other growth agents. These hormones and other growth agents can include insulin, dexamethasone, transferrin, nicotinamide, serum albumin, beta-mercaptoethanol, free fatty acid, glutamine, CUSO4, and H2SeO3. The culture medium can also include antibiotics. Importantly, the culture medium does not include serum. The invention includes means of inducing the differentiation of the progenitors to their adult fates such as the differentiation of hepatic progenitor cells to hepatocytes or biliary cells by adding, or excluding epidermal growth factor, respectively. The method of producing mammalian progenitors is useful in that the progenitors can be used subsequently in one or more of the following processes: identification of growth and differentiation factors, toxicological studies, drug development, antimicrobial studies, or the preparation of an extracorporeal organ such as a bioartificial liver.

The metabolic processes involved in the formation of any glucose-based metabolite of a metabolic network are determined. A precursor molecule is labeled with a stable carbon (13C) isotope at specific positions. The label is allowed to distribute and rearrange in the system. Metabolites are recovered and analyzed against a control system to determine a set of metabolic pathway substrate fluxes caused by changes to the test system relative to the control system such as the addition of compound being tested as a potential drug.