1612 results about "Lead compound" patented technology

The present invention is directed to an improved electroplating method, chemistry, and apparatus for selectively depositing tin / lead solder bumps and other structures at a high deposition rate pursuant to manufacturing a microelectronic device from a workpiece, such as a semiconductor wafer. An apparatus for plating solder on a microelectronic workpiece in accordance with one aspect of the present invention comprises a reactor chamber containing an electroplating solution having free ions of tin and lead for plating onto the workpiece. A chemical delivery system is used to deliver the electroplating solution to the reactor chamber at a high flow rate. A workpiece support is used that includes a contact assembly for providing electroplating power to a surface at a side of the workpiece that is to be plated. The contact contacts the workpiece at a large plurality of discrete contact points that isolated from exposure to the electroplating solution. An anode, preferably a consumable anode, is spaced from the workpiece support within the reaction chamber and is in contact with the electroplating solution. In accordance with one embodiment the electroplating solution comprises a concentration of a lead compound, a concentration of a tin compound, water and methane sulfonic acid.

The invention relates to a method of using high mass matrix assisted laser desorption-ionization (MALDI) mass spectrometry for the qualitative and quantitative analysis of the effect of drug candidates on protein complexes such as protein-protein interactions in purified samples or complex biological matrices, as well as to the use of this method for lead compound optimization, drug characterization, drug manufacturing processes, and drug quality control processes, including automated high throughput applications.

The invention belongs to the field of medicinal chemistry, and discloses pyrimidine compounds containing semicarbazide and terminal alkyne structural units, and preparation methods and applications of the pyrimidine compounds in preparation of antitumor drugs by taking lysine specific demethylase 1 (hereafter referred to as LSD1) as a target. A pyrimidine active fragment is built by adopting a three-component one-pot method, and then the target compounds are prepared by substitution, chlorination and ammonification reaction. The general formulas of the compounds are as shown in the formula I in the specification. An in vitro anti-tumor activity experiment and an LSD1 inhibition activity experiment prove that the compounds have obvious inhibiting and killing action on a plurality of tumor cells by inhibiting the activity of the LSD1, can be used as lead compounds for further development, and are applied to preparation of the antitumor drugs.

This invention relates to curcumin analogs and their applications. Curcumin is an excellent precursor compound, and has multiple pharmaceutical activities. The curcumin analogs in this invention have more stable monocarbonyl intermediate connection chain structure. The connection chain can be acetone, cyclopentanone or cyclohexanone. The substituent on benzene ring can be separately selected from H, hydroxyl, halogen, alkoxyl, alkyl, halogenated alkyl, amino, and alkyl amino. This invention also discloses pharmaceutically acceptable salts of the curcumin analogs, preparations containing them, and their pharmaceutical applications. Experiments show that the curcumin analogs can be used to treat inflammation and tumor.

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.

An outstandingly low environmental impact wet process recovers the lead content of an electrode slime and / or of lead minerals in the valuable form of high purity lead oxide or compound convertible to highly pure lead oxide by heat treatment in oven at relatively low temperature, perfectly suited for making active electrode pastes of new batteries or other uses. The process basically comprises the following treatments:a) suspending the impure lead containing material in an aqueous bath containing at least a lead oxide dissolving acid;b) reducing any insoluble lead dioxide to lead oxide by introducing in the suspension either hydrogen peroxide, a sulphite or sulphurous anhydride;c) converting all dissolved lead oxide to lead sulphate in the aqueous bath;d) obtaining a solution of lead sulphate obtained in an aqueous solution containing an acetate salt;e) precipitating and separating a purified lead compound in the form of either carbonate / oxycarbonate or of oxide / or hydroxide by adding to said acetate salt solution a carbonate salt or a hydroxide of the same cation of said acetate salt, respectively.Exemplary flow sheets according to several alternative embodiments and related processing plant diagrams are disclosed.

The present invention provides a medicine composition including icaritin and / or demethylicaritin as active component, medicinal carrier and / or excipient and having plant female hormone action, it can be used in the preparation of medicines for curing various diseases of hormone-dependend type cancers, cardiovascular diseases, after-menopausal osteoporosis, climacteric indisposition, senile dementia, hepatitis, diabetes and others, also can be used as precursor compound of the medicine.

This invention provides principles, methods and compositions for ascertaining the mechanism of action of pharmacologically important compounds in the context of network biology, across the entire scope of the complex pathways of living cells. Importantly, the principles, methods and compositions provided allow a rapid assessment of the on-pathway and off-pathway effects of lead compounds and drug candidates in living cells, and comparisons of lead compounds with well-characterized drugs and toxicants to identify patterns associated with efficacy and toxicity. The invention will be useful in improving the drug discovery process, in particular by identifying drug leads with desired safety and efficacy and in effecting early attrition of compounds with potential adverse effects in man.

The invention relates to a 5-site or 6-site substituent naphthalimide compound and antitumor applications thereof, which belongs to the fine chemical field. The compound is characterized in that various aliphatic amidogen, heterocyclic amidogen, aryl and Ar aryl are respectively introduced into the 5-site or 6-site of the naphthalimide by a nucleophilic substitution reaction to obtain small molecule compound similar to a lead compound amonafide structure. The small molecule compound has obvious inhibiting activity in vitro test on Hela and P388D1, and wherein, some compounds have stronger cytotoxicity than the amonafide under the same test conditions. In addition, the structures of the compounds take on diversity; the compounds without acetylation sites can be prevented from having the side effect similar to the amonafide; the other compounds with the acetylation sites can be prevented from having the side effect by personalized administration, therefore, the compound has medical application prospect in curing diseases related to tumors.

The present invention relates to carbon glycoside compound, and is especially 15-(14-deoxy-11, 12-dehydro)-andrographolide carbon glycoside derivative and its preparation process. The preparation process includes dewatering andrographolide as precursor compound, epoxidation and other reaction to obtain serial andrographolide derivatives; dissolving the derivatives and beta- carbon glycoside ketone in organic solvent and condensation reaction at certain temperature in the presence of catalyst for certain time. The derivative is significant in developing andrographolide.

The invention discloses a small molecule drug virtual screening method based on deep migration learning and application thereof. A source domain is used as an input to be trained, converged and derived to obtain a weight matrix; a target domain is input into an improvement tool to serve as the initialization weight of the target domain; fine adjustment, training and convergence are conducted on the initialization weight and data in the target domain sequentially; a biological activity value of interaction of a lead compound and a drug target in the target domain is predicted, a target domain molecular fingerprint and a predicted value are obtained, and an evaluation index root mean square error and a correlation coefficient of a predicted result are output; the target domain is subjected to fine adjustment by repeating above steps, and the weight matrix of the source domain helps the target domain build a model. According to the small molecule drug virtual screening method and the application thereof, the effective virtual screening model can still be obtained under the condition that the information of a known active ligand sample is insufficient, and does not need to rely on a large number of data samples.

The invention discloses a lead compound nano-powder preparation method for recovery and manufacture of lead-acid battery. The lead compound nano-powder preparation method comprises the following steps that 1, lead, a lead salt or waste lead-acid battery lead paste reacts with one or more organic or inorganic compounds to produce a soluble lead salt solution or a lead hydroxide solution; 2, one or more alkalis or caustic alkalis are added into the soluble lead salt solution, or a part or excess amount of H2CO3 or CO2, sulfuric acid, one or more organic acids or their salts are added into the lead hydroxide solution, and 3, lead oxide or lead hydroxide precipitates obtained by the step 2 are filtered and are subjected to drying and pyrolysis to form the lead compound nano-powder. The lead compound nano-powder preparation method realizes environmentally friendly recovery and production, has low energy consumption, greatly reduces a production cost, and shortens a production period. The lead compound nano-powder obtained by the lead compound nano-powder preparation method is conducive to improvement of technical product performances.

The invention discloses a lead compound virtual screening method and device. The method includes the steps of generation of molecular fingerprints of lead compounds on drug targets and bioactivity prediction of interaction between the lead compounds and the drug targets. The generation of the molecular fingerprints includes a molecular fingerprint part based on a module unit, a weighting molecularfingerprint part and a bioactivity part. During the bioactivity prediction, ligand molecular fingerprints and bioactivity values are utilized to serve as input of a random forest regression model, and a prediction model is constructed. Additionally, the device includes a universal tool for virtual screening on the basis of ligands, a prediction tool for the bioactivity generated when the lead compounds take effects on the drug targets, and a generation tool of the molecular fingerprints of the lead compounds on the drug targets. At present, molecular fingerprints which are excellent in performance and are used for the bioactivity prediction are often greater in length, and however, by adopting a designed deep learning algorithm, molecular fingerprints which are excellent in performance and smaller in length can be generated so that the best bioactivity prediction model of drug target ligands can be obtained.

Methods of screening candidate agents to identify lead compounds for the development of therapeutic agents for the treatment of a neurodegenerative disease, such as Huntington's Disease and Parkinson's Disease and methods for identifying a mutation in, or changes in expression of, a gene associated with neurodegenerative disease, such as Huntington's Disease and Parkinson's Disease, are provided.

A cell-based screen is reported can be used to identify specific receptor-binding compounds in a combinatorial library of peptoids (N-alkylglycine oligomers) displayed on beads. This strategy was applied to the isolation of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2)-binding peptoids, which were optimized to create lead compounds with high affinity for VEGFR2. One of these peptoids was shown to be an antagonist of VEGF-VEGFR2 interaction and receptor function.

The present invention is directed to a screening platform employing a miniaturized three-dimensional cell chip for high-throughput toxicology screening of test and lead compounds, prodrugs, drugs and P-450 generated drug metabolites. To this end, the three-dimensional cell chip, employs human cells encapsulated in a matrix (e.g., collagen or alginate gels) in volumes as small as 10 nL arrayed on a functionalized substrates (e.g., glass microscope slides) for spatially addressable screening against multiple test compounds. With the present platform, over 3,000 cell-matrix islands may be spotted providing for simultaneous screening against multiple compounds at multiple doses and in high replicate.

This invention provides principles, methods and compositions for ascertaining the mechanism of action of pharmacologically important compounds in the context of network biology, across the entire scope of the complex pathways of living cells. Importantly, the principles, methods and compositions provided allow a rapid assessment of the on-pathway and off-pathway effects of lead compounds and drug candidates in living cells, and comparisons of lead compounds with well-characterized drugs and toxicants to identify patterns associated with efficacy and toxicity. The invention will be useful in improving the drug discovery process, in particular by identifying drug leads with desired safety and efficacy and in effecting early attrition of compounds with potential adverse effects in man.

A drug screening method includes the steps: A, screening PPARs (peroxisome proliferator-activated receptors) and building a PPAR action model; B, building a compound database; C, evaluating druggability, LogP, LogS, mutagenicity, tumorigenicity, irritation, reproductive toxicity and water solubility of compounds in the database, and building two-dimensional and three-dimensional compound databases; D, performing structural modification on compounds in the two-dimensional and three-dimensional compound databases; E, performing docking computation on novel molecular structural compounds, and screening; F, verifying the compounds by the aid of a molecular dynamics method, and selecting and determining molecules; and G, obtaining ADMET (absorption, distribution, metabolism, excretion and toxicity) properties of the verified compounds obtained by computation so as to obtain target compounds finally. By the scheme, structures of the compounds are further optimized while structure-function relationship of the compounds is researched, and novel leading compounds with medicinal value are sought.

The present invention provides a quinazoline compound shown in formula (I), or pharmaceutically acceptable salt thereof. R1, R2 and R7 are independently and respectively selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halogenate C1-6 alkyl, halogenate C1-6 alkoxy, hydroxyl C1-6 alkyl, hydroxyl C1-6 alkoxy, C1-6 alkoxy C1-6 alkoxy, C3-8 cycloalkyloxy, optional aryl or heteroaryl substituted by R6, nitryl, amino, C1-6 alkylamino, and di(C1-6 alkyl)amino; it comprises at least one C3-8 heterocycloalkyloxy selected from N, O, S heteroatoms; Z is -NR4-, C(R5)2, S or -O-, R4 being hydrogen or C1-3 alkyl, and R5 being selected from hydrogen or C1-3 alkyl; R3 is selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or halogenate C1-6 alkyl; R6 is selected from hydrogen, C1-3 alkyl, hydroxyl, halogen, C1-3 alkoxy; and n is 0 to 5. The present invention further provides a preparation method of the compound shown in formula (I) or the pharmaceutically acceptable salt and pharmaceutical usage thereof, which can be used as medicines or lead compounds for curing diseases such as tumour and cancer related to protein tyrosine kinase.

The invention discloses a polypeptide for inhibiting aggregation and toxicity of beta amyloid protein (A beta) or a variant of the polypeptide with polypeptide functions. The polypeptide has a strong binding force with the A beta protein, so that the effective content of a beta structure can be greatly reduced when A beta achieves an aggregation balanced state, the secondary structure of A beta in a solution environment can be changed, the content of the beta structure can be greatly reduced, even the beta structure disappears, the toxicity of A beta to SH-SY5Y cells can be remarkably reduced when the concentration of the polypeptide is extremely low, and generation of A beta-induced active oxygen can be greatly inhibited. Therefore, a feasible method is provided to treatment of Alzheimer disease caused by beta amyloid protein, and thought and reference standard can be provided to discovery of polypeptide pilot compounds for treatment of amyloid protein related diseases.

A forward synthetic method is described that utilizes recursive application of established organic chemical reactions to derive more complex synthons from available reagents than are available from the reagent synthons themselves. The product of each reaction serves as the starting point for further reactions thereby permitting the generation of multiple complex molecular structures. This synthon generation procedure typically yields 20 ? 30 new structures within the limits of easily accessible syntheses based upon each starting reagent. More complex syntheses yield even more structures. The generated synthons are characterized with a molecular structural descriptor possessing a neighborhood property and can be further characterized with features. The synthons are searched for three dimensional shape and feature similarity to molecular fragments derived from query molecules, typically pharmacological molecules of interest. Identified synthons can be assembled into molecules possessing the same three dimensional shape and likely activity as the molecule of interest.

The invention relates to a preparation method and application of 9-bit substituent double-functional group berberine derivatives. In-vitro biological activity assay research shows that the 9-bit substituent double-functional group berberine derivatives provided by the invention has acetylcholinesterase inhibition activity higher than that of berberine serving as a leading compound, and also has higher inhibition activity on butyrylcholine esterase. After being further optimized and screened, the derivatives have favorable foreground of being developed into medicaments for treating diseases such as AD disease, vascular dementia, cognitive dysfunction and the like. The general formula of the derivatives is shown as the following formula, wherein X, Y and Z are defined in specifications.

The invention discloses a myrtle ketone compound and an application thereof in preparation of antibacterial medicines. A compound rhodomyrtosone B (shown in a formula 2) and a compound tomentosone C (shown in a formula 1) are separated from myrtle, and the two compounds have high antibacterial activities, particularly have high inhibitory activity on methicillin-resistant staphylococcus aureus. Therefore, a foundation is laid for developing the compounds into novel drug bacteria resistant lead compounds and launching the compounds on the market. The structural formula is as shown in the specification.

The present invention is a chemical synthesis process of quinolone, which relates to the field of veterinary drug feed additives. The existing synthesis technology is to select from various quinoxaline compound substituted derivatives, but these compounds have relatively large toxic and side effects, and simply change The side chain can no longer meet the needs. The present invention uses heavy ion beams to modify the structure of quinoxaline to produce new compound molecules. Through pharmacodynamic research, the standard sample is separated for chemical synthesis. The present invention designs three synthetic routes. Corresponding to the three chemical synthesis processes, the new compound was identified by spectrum, and it was determined to be quinolone. After further growth-promoting and toxicity tests, it showed obvious improvement and improvement compared with the lead compound quinolone. The invention has the beneficial effects of greatly shortening the development cycle and greatly saving the development cost, and shows that quinolone is a very vital veterinary drug feed additive.

The invention relates to the medicine technical field, in particular to saponin compounds of Siraitic acid IIB and Siraitic acid IIC which are extracted and separated from fructus momordicae roots, a method for preparing the same and application thereof in an anti-tumor medicine. The molecular formulas of the two compounds are C40H60O14 and C41H62O15 respectively. By various modern spectral analysis, particularly the application of advanced two-dimensional nuclear magnetic resonance spectrum to comprehensive analysis, the chemical structures of the two compounds are determined. In vitro anti-tumor tests show that the compound Siraitic acid IIB can obviously inhibit lung cancer cells A-549 and liver cancer cells Hep-G2, and the compound Siraitic acid IIC can also obviously inhibit liver cancer cells Hep-G2. The invention provides lead compound for research on a new anti-tumor medicine, and has essential values in comprehensively developing and utilizing fructus momordicae resources.

The invention provides an ergosterin derivative which is obtained by extraction, separation and purification from traditional Chinese medicine ganoderma lucidum spore powder. In the invention, an anti-aging yeast model, namely a K6001 yeast cell and a mutant strain thereof (delta uth1 and delta skn7) prove that the ergosterin derivative influences the gene expression of the UTH1 by regulating the activity of the Skn7 so as to prolong the duplicability life of yeast. The compound is used as a lead compound to optimize the structure, and can be used for preparing medicaments for delaying aging and preventing or / and treating aging diseases. The general structure formula of the ergosterin derivative is as shown in the specification.

The invention discloses a diterpenoid compound and the preparing method and application thereof. The diterpenoid compound is obtained by using aralia melanocarpa roots as the raw material through extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation. The molecular formula of the diterpenoid compound is C20H30O3. The name of the diterpenoid compound is 14-oxygen-ent-8(9),15-(14-oxo-ent-pimara-8(9),15-diene-19-oic acid). The structural formula is as shown in the specification. According to the preparing method, aralia melanocarpa roots are used as the raw material, and extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation are conducted to generate the diterpenoid compound. The diterpenoid compound can be applied to preparation of anti-inflammatory drugs for prevention and / or treatment. The diterpenoid compound is subjected to in-vitro anti-inflammatory activity testing, and experimental results show a good lipopolysaccharide (LPS) restraining effect and a good effect of inducting pulmonary alveolar macrophages (RAW264.7) to generate NO. A new compound or lead compound with high application value can be provided for the medical industry.

The invention belongs to the field of medicinal chemistry, and discloses a pyrimidine and triazole containing compound and a preparation method and application thereof in preparation of anti-cancer medicine with lysine specific demethylase 1 (LSD1) being a target. The general formula of the compound is shown in the drawing I. In-vitro LSD1 enzyme inhibition activity experiments prove that by inhibiting LSD1 activity, the compound has obvious inhibiting and killing effects on kinds of cancer cells and can be applied to preparation of the anti-cancer medicine as a further developed lead compound.