102results about How to "Reduced inhibitory activity" patented technology

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.

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 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.

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.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, whereinR1 represents a hydrogen atom or a halogen atom;R2 represents a methyl group or an ethyl group;R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms;with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group.These 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.

The invention relates to azabicyclo derivatives, preparation methods thereof, and pharmaceutical applications thereof. Specifically, the invention discloses compounds represented by a formula (I), or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. The invention also provides preparation methods of the derivatives, and applications of the derivatives in EGFR inhibitors. The definitions of the groups in the formula are defined in the specifications.

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).

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.

The present invention relates to a method for the treatment of fibrosis, in particular cardiac fibrosis, comprising the administration of an inhibitor of insulin-regulated aminopeptidase (IRAP). Preferable the IRAP inhibitor is chosen from the group including HFI-419, HA-08, AL-40, HFI-437, Val-Tyr-Ile-His-Pro-Phe (otherwise known as angiotensin IV or ANG IV), c[Cys-Tyr-Cys]-His-Pro-Phe, and c[Hcy-Tyr-Hcy]-His-Pro-Phe.

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.