11519 results about "Inhibitory effect" patented technology

The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.Wherein R1 designates —(CO)h—(NRa)j—(CRb═CRc)k—Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like;Cy designates a 5- or 6-membered heteroaryl; andV each independently designate the formula -L-X—Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The present invention relates to nanosilver-containing antibacterial and antifungal granules ("NAGs"). The NAGs have longlasting inhibitory effect on a broad-spectrum of bacteria and fungi, which include, but are not limited to, Escherichia coli, Methicillin resistant Staphylococcus aureus, Chlamydia trachomatis, Providencia stuartii, Vibrio vulnificus, Pneumobacillus, Nitrate-negative bacillus, Staphylococcus aureus, Candida albicans, Bacillus cloacae, Bacillus allantoides, Morgan's bacillus (Salmonella morgani), Pseudomonas maltophila, Pseudomonas aeruginosa, Neisseria gonorrhoeae, Bacillus subtilis, Bacillus foecalis alkaligenes, Streptococcus hemolyticus B, Citrobacter, and Salmonella paratyphi C. The NAGs contain ground stalk marrow of the plant Juncus effusus L. which has been dispersed with nanosilver particles. The nanosilver particles are about 1-100 nm in diameter. Each of the nanosilver particles contain a metallic silver core which is surrounded by silver oxide. The present invention also provides a process for making the NAGs. The NAGs can be used in a variety of healthcare and industrial products. Examples of the healthcare products include, but are not limited to, ointments or lotions to treat skin trauma, soaking solutions or cleansing solutions for dental or women hygiene, medications for treating gastrointestinal bacteria infections, sexual related diseases, and eye diseases. Examples of industrial products include, but are not limited to, food preservatives, water disinfectants, paper disinfectants, construction filling materials (to prevent mold formation).

The invention relates to an enantiomorphic amine alkyl sesquiterpene alcohol and glucoside and the medicated salt or solvent thereof, as well as the effect and activity of the composed medicine combination, mainly relating to the medical use in reducing HBV-DNA replication activity. And it has considerably strong inhibiting effect on HBsAG screted by HepG2.2.15 and HBV-DNA replication as compared with positive contrast Lamivudine; and it has obvious inhibition activity to HBV-DNA replication at large dosage (100 mug / mL) and medium dosage(20 mug / mL) as contrasted with Lamivudine, and can be expected to apply to preparing medicines for curing HB virus infection disease.

The invention involves A 1- beta-keto-5, 11(13)-diene eudesmane-12-acidum who has the structure as formula (1) shows and its medical salt, or solvate and its drug combinations and its medical usage in reducing hepatitis B surface antgien and inhibiting replication activity of aethyl- hepatovirus HBV-DNA medicinal. The invention compounds has strong inhibitory action in hepatitis B surface antgien (HBsAg) externalized by HepG2.2.15 cells and replication of aethyl- hepatovirus deoxyribonucleotide (HBV-DNA) in vitro, its inhibiting ability against HBsAg surpasses that of positive control Lamivudine in the same dose; it has obvious inhibiting ability against replication of aethyl- hepatovirus HBV-DNA under the concentration of 100 mu g / mL,20 mug / mL and 4 mug / mL DNA, it belongs to anti- aethyl- hepatovirus natural products of superactive non-nucleoside, can be expected for producing drugs for treating aethyl- hepatovirus infected disease.

The present invention relates to an eudesmane type sesquiterpene derivative 1 beta-hydroxyilicic acid, namely 1 beta-hydroxy-5 alpha H-eudesmane-11 (13)-ethylene-12-acid, its medicineal salt or solvent compound and its medicine composition and medicinal application for preparing medicine capable of curing hepatitis B virus infective disease and resisting hepatitis B virus. Said invention also provides its chemical structure formula.

The invention relates to a sesterterpane as formula (1) and relative medical drug or solvent, and relative drug compound, which can reduce hepatitis B surface antigen and restrain hepatitis B HBVDNA copy activity. Wherein, said invention has strong restrain on hepatitis B surface antigen (HBsAg) generated by HepG2.2.15 cell and the copy of hepatitis B deoxyribonucleic acid (HBV-DNA), while it restrain ability is higher than positive contrast difuradin; and the copy restrain activity at large amount (100 mug / mL) and middle amount (20 mug / mL) on the hepatitis B HBV-DNA are both higher then difuradin.

The invention discloses a eudesmane typed sesquiterpene acid compound named 5alphaH-eudesmane-11 (13)-alkylene-12 acid, which is characterized by the following: inhibiting the replication of HBsAg and HBV-DNA; fitting for preparing prevention drug of virus B hepatitis; reducing the application in the hepatitis B surface antigen drug.

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the C ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

The active hypolipemic components in 40 Chinese-medicinal materials and their relative medicines are disclosed. Said active components can suppress the activity of fatty acid synthetase and the differentiation from profat cells to fat cells and activate the activity of acyl-CoA synthetase. Said medicines feature high effect and low toxic by-effect.

The present invention provides one kind of 1, 2, 3-thiobiazole-5-formamide compounds and their synthesis process and pesticide bioactivity screening. The screening system includes the determination of tobacco mosaic disease resisting activity, tobacco mosaic disease virus resistance inducing activity, and pesticidal and fungus-inhibiting activity. The related compounds are 1, 2, 3-thiobiazole-5-formamide derivatives with the general expression as shown, and include 7 hetero cycle containing 1, 2, 3-thiobiazole-5-formamide derivatives, 2 benzene ring containing 1, 2, 3-thiobiazole-5-formamide derivatives, and 2 aliphatic radical containing 1, 2, 3-thiobiazole-5-formamide derivatives.

The invention relates to a compound biological antiseptic and preservation agent for food. The compound biological antiseptic and preservation agent is prepared by evenly mixing pure biological solid preparations or products such as epsilon-polylysine, nisin, natamycin, lysozyme, bacillus subtilis, ascorbic acid, a toona sinensis leaf extract, a water-soluble resveratrol preparation, tea polyphenol and chitosan. The compound biological antiseptic and preservation agent has a strong inhibition effect on spoilage bacteria and pathogenic bacteria in various foods and good inhibition action on oxidative deterioration of the food. Compared with the existing various preservatives, the compound biological antiseptic and preservation agent has the characteristics of broad antibacterial spectrum, high safety, high efficiency and convenience in use.

The invention discloses a pyrimidoheterocyclic compound represented as the formula (I), or a pharmaceutically acceptable salt or a stereisomer thereof, or a prodrug molecule thereof. The pyrimidoheterocyclic compound can effectively inhibit growth of various tumor cells and has an inhibiting effect on EGFR protease. The pyrimidoheterocyclic compound can be used for preparing an anti-tumor drug, and can overcome drug resistance caused by medicines in the prior art, such as gefitinib, erlotinib and the like, has a selectivity on wild non-small cell lung cancer and is excellent in pharmacokinetic property.

A thienotriazolodiazepine compound of the following formula (I)a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound.Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.

There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.

Through screening of a Zymomonas mutant library the himA gene was found to be involved in the inhibitory effect of acetate on Zymomonas performance. Xylose-utilizing Zymomonas strains further engineered to reduce activity of the himA gene were found to have increased ethanol production in comparison to a parental strain, when cultured in mixed-sugars medium comprising xylose, and, in particular, in the presence of acetate.

Antimicrobial compounds from Bacillus subtilis for use against animal and human pathogens. A novel strain of Bacillus subtilis was isolated from the gastrointestinal tract of poultry and was found to produce a factor or factors that have excellent inhibitory effects on Clostridium perfringens, Clostridium difficile, Campylobacter jejuni, Campylobacter coli, and Streptococcus pneumoniae. The factor(s) retain full viability and antimicrobial activity after heat treatment. The invention provides a method of treatment of pathogenic microorganisms including C. perfringens.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

An improved system for screening a multiple of candidate therapeutic or chemotherapeutic agents for efficacy as to a specific patient, in which a tissue sample from the patient is harvested, cultured and separately exposed to a plurality of treatments and / or therapeutic agents for the purpose of objectively identifying the best treatment or agent for the particular patient. Specific method innovations such as tissue sample preparation techniques render this method practically as well as theoretically useful. One particularly important tissue sample preparation technique is the initial preparation of cohesive multicellular particulates of the tissue sample, rather than enzymatically dissociated cell suspensions or preparations, for initial tissue culture monolayer preparation. With respect to the culturing of malignant cells, for example, it is believed (without any intention of being bound by the theory) that by maintaining the malignant cells within a multicellular particulate of the originating tissue, growth of the malignant cells themselves is facilitated versus the overgrowth of fibroblasts or other cells which tends to occur when suspended tumor cells are grown in culture. Practical monolayers of cells may thus be formed to enable meaningful screening of a plurality of treatments and / or agents. Growth of cells is monitored to ascertain the time to initiate the assay and to determine the growth rate of the cultured cells; sequence and timing of drug addition is also monitored and optimized. By subjecting uniform samples of cells to a wide variety of active agents (and concentrations thereof), the most promising agent and concentration for treatment of a particular patient can be determined. For assays concerning cancer treatment, a two-stage evaluation is contemplated in which both acute cytotoxic and longer term inhibitory effect of a given anti-cancer agent are investigated.

The invention relates to a sulfonamides compound for inhibiting carbonic anhydrase II and a synthesis method and an application thereof. The compound has the structure as shown in the specification. The invention features economical and reasonable synthetic route and high utilization of resources. The synthesis method is simple and easy to carry out and is more suitable for large-scale industrialized production. With human carbonic anhydrase II (Human Carbonic Anhydrase II, hCA II) expressed by procaryotic cell as an enzyme source, the invention establishes an in-vitro carbonic anhydrase inhibitor screening model. In addition, the compound of the invention has inhibitive effect on activity of the human carbonic anhydrase II.

The present invention discloses a 3-(2-pyrimidine amino) phenyl acrylic amide compound in the structure of formula (I) or a pharmaceutically acceptable salt or a stereisomer or a prodrug molecule. The 3-(2-pyrimidine amino) phenyl acrylic amide compound or the pharmaceutically acceptable salt can effectively inhibit the growth of various tumor cells, and inhibit EGFR (epidermal growth factor receptor), HER (human epidermal receptor2) family other protease, can be used in the preparation of antitumor drugs, and can overcome the drug resistance induced by gefitinib, erlotinib and the like.

The invention provides a side wind resistance landing flight track tracking control method based on side direction guide, which belongs to the flight track tracking control technology of airplanes landed under the side wind condition. The flight track tracking control method based on side direction guide is adopted, and comprises the following steps: calculating the inner ring posture control commands through a side direction guide law by the flight track tracking side direction deviation; generating steering engine control commands by an inner ring posture controller for controlling the airplane posture; and calculating the current side direction deviation by the flight line switching logics according to the current state of the airplane for the side direction guide law calculation. A transverse side direction movement model of the airplane is used for simulating the dynamic and kinematic model of the airplane. When being adopted, the side direction flight track control system based on the ground speed guide has better inhabitation effect on the side wind phenomena such as side direction gust wind, air turbulence, side direction wind shear and the like when the airplane is landed. At the same time, the side direction flight line switching logics can also meet the requirement of approach flight of the airplane under the side wind condition.

Endotoxin, also known as lipopolysaccharides (LPS), is the major mediator of septic shock due to Gram-negative bacterial infection. Chemically synthesized S3 peptide, derived from Sushi3 domain of Factor C, which is the endotoxin-sensitive serine protease of the limulus coagulation cascade, binds and neutralizes LPS activity. Fluorescent tagged-S3 is shown to detect LPS-containing bacteria. For large-scale production of S3 and to mimic other pathogen-recognizing molecules, tandem multimers of the S3 gene were constructed and expressed in E. coli. Tetramer of S3 for example is shown to display an enhanced inhibitory effect on LPS-induced activities. An affinity matrix based on tetramer of S3 is also shown to be particularly efficient at removing LPS.

The invention discloses Bacillus subtilis, which is named Bacillus subtilis. The Bacillus subtilis was collected in China General Microbiological Culture Collection Center on January 15th, 2009, with a collection number of CGMCC No.2843. The Bacillus subtilis strain disclosed by the invention is screened from tobacco leaf habitats. Experiments prove that the fermentation liquor of the strain has a strong inhibition effect on fungal pathogens such as Alternaria alternate and pepper anthracnose and demonstrates high prevention effect on Alternaria alternate, tobacco black shank, pepper anthracnose, tomato wilt, phytophthora melonis Katsura, verticillium dahlia and the like and has high growth promoting effects on tobacco, pepper, cucumber, tomato and eggplant. Therefore, the Bacillus subtilis disclosed by the invention can be used for preparing biological bactericides for preventing and controlling fungi in tobacco and vegetables and can be used for preparing growth promoting agents for promoting the growth of tobacco or vegetables.

The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification.The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier.The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.

The invention relates to a preparation method of a biological preservative. As known to all, along with the rapid development of the society, chemical preservatives have been used in food, have strong impact on food safety and endanger the health of consumers, therefore, the use of preservatives causes great concern of government departments and consumers. According to the biological preservative, natural plants and microbial antibiotic substances are used as base materials, for example, the biological preservative is prepared by mixture of carboxymethyl chitosan, xylooligosaccharide, nisin from lactic streptococci, acetic acid, lactobacillus reuteri, pediococcus acidilactici, calcium citrate, ionized calcium, lactic acid, plant essential oil and water. The biological preservative can inhibit growth of harmful microorganisms by antagonistic and competitive inhibition effects among different microorganisms and produce extracted and separated components of antibacterial active ingredients having antifungal and antibacterial functions in normal growth and metabolism processes, thereby achieving antiseptic and fresh-keeping effects.

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.