103results about How to "Reduced inhibitory activity" patented technology

It is an object of the present invention to provide a biosensor, which is not significantly affected by the baseline fluctuation and suppresses nonspecific adsorption. The present invention provides a biosensor, which comprises a metal surface or metal film coated with a hydrophobic polymer, and has two or more types of different surfaces in a region coated with a hydrophobic polymer.

The invention provides a microsphere formulation for the sustained delivery of an aptamer, for example, an anti-Vascular Endothelial Growth Factor aptamer, to a preselected locus in a mammal, such as the eye. In addition, the invention provides methods for making such formulations, and methods of using such formulations to deliver an aptamer to a preselected locus in a mammal. In particular, the invention provides a method for delivering the aptamer to an eye for the treatment of an ocular disorder, for example, age-related macular degeneration.

A compound of formula (I),a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atomsThese compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I): wherein R<1 >and R<2 >independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

The present invention relates to methods and compositions designed for the prevention, reduction, treatment or management of ischemia-reperfusion injury. The methods of the invention comprise the administration of an effective amount of a therapeutic formulation containing one or more active compounds in a formulation which specifically decreases or inhibits the activity of and / or eliminates or diminishes the amount of phagocytic cells including, but not limited to, macrophages and / or monocytes. In preferred embodiments, the active compound is a bisphosphonate. The invention also provides pharmaceutical compositions of therapeutic formulations for administration to subjects currently suffering from, having recently suffered, or at risk of suffering from an ischemia-reperfusion injury.

The present invention relates to isolated protein sequences that correspond to cell binding peptides, fragments, neo-structures and / or neo-epitopes of a normally occurring serum protein present in human tissue, wherein the peptide, fragment, neo-structure and / or neo-epitope has an immunoregulatory activity and is the result of either an enhanced proteolytic activity and / or conformational changes in a tissue, or a malignant tumour. In the present patent application, a common structure of several of these peptides, fragments, neo-structures and / or neo-epitopes, having immunoregulatory activity by binding to receptors on immune cells, has been identified. The present invention further also relates to monoclonal and / or polyclonal antibodies directed to a cell binding fragment of a normally occurring serum protein present in human tissue, as described above.

The invention relates to the field of medical chemistry, in particular to derivatives of oseltamivir (I). R1, R2, L and X are explained in the specifications. The invention also discloses a method for preparing the derivatives of oseltamivir and the purpose of the derivatives for treating infectious diseases, particularly the infectious diseases caused by influenza viruses. The oseltamivir is shown in the description.

The invention provides functional white kidney bean polypeptide and a preparation method and an application thereof. With white kidney bean as a raw material, white kidney bean firstly undergoes extraction to obtain white kidney bean albumin; after centrifugation of albumin and ultrafiltration for removal of impurities, acid proteinase is used for enzymolysis; after enzyme deactivation, centrifugation is carried out and a supernatant is taken; after ultrafiltration of the supernatant and concentration, isomaltulose is added according to a certain proportion; and after uniform agitation, vacuum or spray drying is carried out to obtain a polypeptide product. The polypeptide product has high thermostability and an effect of inhibiting alpha-amylase activity, and can be applied to fat-reducing and hypolipemic health food.

The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.

The invention relates to a crizotinib prodrug, as well as a preparation and an application thereof. The invention provides a compound showed as a general formula (II) or a stereoisomer thereof, or a pharmaceutically acceptable salt, or a solvent compound or a hydrate of the compound, wherein X is O or CH2; m is 0 or 1; R1 and R2 are selected from the same or different groups, and are respectively independently hydrogen, halogen, nitryl, cyan, hydroxyl, amino saturated or unsaturated chain hydrocarbyl of C1-C6, and saturated or unsaturated cyclic hydrocarbyl of C1-C6; R1 and R2 also can exist in the same ring and form ternary-hexahydric ring together; the ternary-hexahydric ring can be substituted or un-substituted cyclic hydrocarbon, aromatic ring or hetero-aromatic ring; the substituent group on the ring can be selected from halogen, nitryl, cyan, hydroxyl, amino, C1-C6 alkyl and C1-C6 alkoxy; R3 is selected from hydrogen, substituted or un-substituted C1-C12 saturated or unsaturated alkyl, substituted or un-substituted phenyl or hetero-aryl, substituted or un-substituted alkyl acyloxy, substituted or un-substituted phosphorus acyloxy and substituted or un-substituted aryl acyloxy or hetero-aryl acyloxy; and the substituent groups are selected from halogen, nitryl, cyan, hydroxyl, amino, phenyl or hetero-aryl, C`-C6 alkyl, C1-C6 acyloxy, C1-C6 vinyl and C1-C6 alkynyl.

The present disclosure is directed to methods for reducing the neuronal damage associated with cerebrovascular disease, such as stroke or cerebral edema, by administering R(−)-desmethylselegiline, S(+) desmethylselegiline, or a combination of the two. The cerebrovascular disease may be caused by ischemia or hypoxia.

The invention discloses streptomyces albidoflavus Actin-1. The streptomyces albidoflavus Actin-1 can grow and propagate with apple tree rot pathogenic bacterium mycelium as nutrition, long-term colonization of biocontrol bacteria on apple tree rot scabs is promoted, a long-term biological prevention and treatment function is achieved, meanwhile, the streptomyces albidoflavus Actin-1 is induced to generate multiple ectoenzyme cell wall hydrolytic enzymes, and pathogenic bacterium cells disintegrate in combination with the enzyme dissolving function; high antibacterial active matter can be generated, the bacteriostasis rate on the apple rot pathogenic bacteria is 89.82%, a good antibacterial effect is achieved on botryosphaeria berengeriana and other pathogenic bacteria, the bacteriostasis rate ranges from 76.08% to 87.10%, and broad spectrum bacteriostasis performance is achieved. The streptomyces albidoflavus Actin-1 is adopted as main biocontrol bacteria for preventing and treating the apple tree rot and other fruit and vegetable pathogenic bacteria, and the advantages of being good in prevention and treatment effect (100%), high in efficiency, low in recurrence rate (0), high in environment adaption capacity, high in stability, not likely to generate resistance to drugs and the like are achieved. Important significance is achieved on improving the prevention and treatment effect on the apple tree rot and other fruit and vegetable pathogenic bacteria, preventing pathogenic bacterium relapse and protecting the environment.

The invention belongs to the technical field of natural herbal medicines and particularly relates to an extract of a plant in blumea as well as a preparation method and application thereof. The extract contains 10-99wt% of total caffeoylquinic acid. The preparation method of the extract comprises the following steps: (S1) pulverizing the plant in blumea wholly or partially, and extracting with an organic solvent, water or the solution of the organic solvent in water to obtain a crude extract; and (S2) extracting the crude extract with n-butanol or purifying with a macroporous adsorption resin column to obtain the extract of the plant in blumea. The extract provided by the invention has a good antiviral effect, can be used for preparing medicines for preventing and treating virus infection and health care products, is definite in effective components, low in toxicity and strong in pharmacologic action and has good application prospect. In addition, the preparation process of the extract is simple and is suitable for large-scale production.

A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).

The invention belongs to a method for preparing inula japonica plant extract and applications of the inula japonica extract. The plant material (root, stem, leaves, inflorescence and whole grass) of the inula japonica (including Inula japonica and Inula britannica) is crushed and extracted by a solvent which comprises 95% of alcohol; and the extract solution is concentrated to have the same weight with the inula japonica crushed matters, thus obtaining inula japonica extract. The inula japonica extract has obvious inhibition effects to cucumber botrytis cinerea, alternaria solani, cladosporium fulvum, colletotrichum lagenarium, sphaerotheca fuliginea, pseudoperonospora cubensis, potato phytophthora infestans, tomato phytophthora infestans and rhizoctonia cerialis; wherein the inflorescence extract has strong antibacterial activity. The inula japonica extract extracted by alcohol can be matched with suitable solvent and pesticide adjuvant to prepare britannica lactone emulsifiable solution and britannica lactione micro-emulsion of botanical fungicide. The inula japonica extract has obvious effects for preventing cucumber downy mildew, sphaerotheca fuliginea, tomato gray mold and tomato leaf mould, is especially suitable for prevention and control on the fungi diseases to economical crops such as vegetables and the like, and is a botanical fungicide with nuisanceless.

A compound of formula (I),a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).

The invention discloses a blocking agent for inhibiting the infection of High Pathogenic Porcine Reproductive and Respiratory Syndrome Virus (HP-PRRSV). According to the blocking agent, a novel HP-PRRSV cell target protein called 14-3-3Epsilon protein and the inhibition targets of the receptor are found. The infection of HP-PRRSV could be significantly reduced by performing interference on the 14-3-3Epsilon gene at these inhibition targets or using inhibitor difopein of the 14-3-3Epsilon protein. These inhibition targets and difopein can be developed into a drug for preventing and curing PRRSVinfection so as to provide a brand-new idea for HP-PRRS research, prevention and cure and expand the scope of research. The invention has great significance in actual production.

An exhaust gas purifying catalyst 1 has a catalyst substrate 3 and catalyst coating layers 5, 7 that are formed on the catalyst substrate 3 and contain (a) Rh, (b) Pt, (c) an alkali metal or alkaline earth element, and (d) an inorganic oxide. The catalyst coating layers 5, 7 has a layered structure including an inside layer 5 where the component (a) is substantially locally existing, and an outside layer 7 where the component (b) is substantially locally existing. The inside layer 5 also contains a zirconia oxide.

The present invention relates to isolated protein sequences that correspond to cell binding peptides, fragments, neo-structures and / or neo-epitopes of a normally occurring serum protein present in human tissue, wherein the peptide, fragment, neo-structure and / or neo-epitope has an immunoregulatory activity and is the result of either an enhanced proteolytic activity and / or conformational changes in a tissue, or a malignant tumour. In the present patent application, a common structure of several of these peptides, fragments, neo-structures and / or neo-epitopes, having immunoregulatory activity by binding to receptors on immune cells, has been identified. The present invention further also relates to monoclonal and / or polyclonal antibodies directed to a cell binding fragment of a normally occurring serum protein present in human tissue, as described above.

This invention provides a compound of the formula (I): wherein R<1 >represents wherein R<5 >represents a hydroxy group or the like; R<6 >and R<7 >independently represents a hydrogen atom or the like: V represents an alkylene or the like: W represents a carbon atom or the like: Z represents a carbon or the like: R<2 >represents a hydrogen atom or the like: R<3 >represents a hydrogen or the like: A represents a cycloalkylene or the like: X represents a covalent bond or the like: R<4 >represents an aryl or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.

The present invention provides a method of selecting an IL-2 production inhibitor and / or an immunocyte proliferation inhibitor having low GATA-1 production inhibitory activity, which comprises measuring the HDAC4 and / or HDAC8 inhibitory activity of a test substance, and a method of selecting an immunosuppressant having low thrombocytopenic activity, which comprises measuring the HDAC4 and / or HDAC8 inhibitory activity of a test HDAC inhibitor.