32results about How to "Inhibition becomes larger" patented technology

The present invention relates to an orally available galenics formulation of Valproic Acid or derivatives thereof exhibiting a specific bi-phasic pharmacokinetic profile optimized for maximum inhibition of histone deacetylases in a therapeutic setting. This specific galenics formulation is designed for the treatment of malignant diseases and diseases associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect, e.g., by induction of differentiation and / or apoptosis. Due to the bi-phasic release pattern the resulting pharmacokinetic profile is able to inhibit HDAC target enzymes most efficiently and to subsequently induce histone hyperacetylation in a rapid as well as a long-lasting fashion. This profile secures the efficient modulation of a desired target gene expression profile which contributes to the therapeutic benefit.

The present invention is directed to ophthalmic compositions containing protease-inhibiting peptide substrates. In a preferred embodiment, the protease-inhibiting peptide substrate is gelatin. The compositions may also contain a galactomannan. In a particularly preferred embodiment, the compositions contain gelatin, a galactomannan and a borate salt. The present invention also describes methods of use of these compositions to inhibit protease MMP-9, and methods of topical administration of the compositions to the eye, particularly for the treatment of dry eye.

PCT No. PCT / US96 / 00519 Sec. 371 Date Nov. 13, 1997 Sec. 102(e) Date Nov. 13, 1997 PCT Filed Jan. 11, 1996 PCT Pub. No. WO96 / 21435 PCT Pub. Date Jul. 18, 1996Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.

The present invention relates to new polyhydroxylated compounds and, in particular, to its activity as fatty acid synthase (FASN) inhibitors and to their use for the treatment of pathological states for which an inhibitor of this enzyme is indicated. The invention further relate to pharmaceutical compositions containing them and to a process for the preparation of such compounds.

Disclosed are methods for detecting an allergic lung disease that involve assessing the level of one or more microRNAs (miRNAs) in a biological sample, wherein the level of the one or more miRNAs in the biological sample compared to a reference level of the one or more miRNAs is indicative of allergic lung disease. Also disclosed are methods for the treatment or prevention of inflammatory or allergic lung disease that involve administration of a let-7 miRNA inhibitor as set forth herein, as well as biochips and kits that can be applied in the methods of the present invention.

A radio frequency (RF) laterally diffused metal oxide semiconductor (LDMOS) device is disclosed, which includes: a gate structure on a surface of a substrate; and a source region and a drain region beneath the surface of the substrate, the source region and the drain region formed on opposite sides of the gate structure, wherein the gate structure includes a first section proximal to the source region and a second section proximal to the drain region, and wherein the first section of the gate structure has a dopant concentration at least one decimal order higher than a dopant concentration of the second section of the gate structure. A method of forming an RF LDMOS device is also disclosed. With the gate structure including two sections having different dopant concentrations, the present invention is capable of reducing the hot carrier injection effect while possessing a low on-resistance.

The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and / or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and / or prevention of cancer.

The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and / or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and / or prevention of cancer.

The present invention relates to RNAi agents, e.g., double-stranded RNAi agents, targeting the hepatitis B virus (HBV) genome, and methods of using such RNAi agents to inhibit expression of one or more HBV genes and methods of treating subjects having an HBV infection and / or HBV-associated disorder, e.g., chronic hepatitis B infection.

A selective agent comprising a triclosan derivative for use in selective inhibition of non-target cells in a mixed population of target and non-target cells. Preferably the triclosan derivative is a glycoside derivative, more preferably a pyranoside derivative. Suitably a selective medium comprising said selective agent and methods of culturing cells using the selective agent are provided.

A laminated foil manufacturing apparatus includes a transportation unit that transports a lamination target medium onto which foil is to be laminated with intermittent movement and continuous movement, a liquid adhering unit that performs adhering processing of making liquid adhere to the lamination target medium which is transported with the intermittent movement by the transportation unit, and a foil laminating unit that is arranged at a downstream side with respect to a position of the liquid adhering unit in a transportation direction of the lamination target medium which is transported with the intermittent movement, and performs foil laminating processing of laminating the foil onto a surface to which the liquid has been adhered on the lamination target medium which is transported with the continuous movement by the transportation unit after the adhering processing has been performed.

The present invention discloses a process for preparing a dibenzylaminquaternary ammonium salt high-temperature resistant corrosion inhibitor and applications thereof. The preparation process comprises the following steps: (1) Dissolve the amine reagents benzylamine, phenethylamine, morpholine or indole in an organic solvent, slowly add epichlorohydrin dropwise, stir to react at a room temperature for 12-14 hours, and then distill under reduced pressure, and wash to obtain an intermediate I; (2) Dissolve the intermediate I in an organic solvent, add dibenzylamine at a ratio, then add an acid binding agent, warm to 60-80° C. to react for 14 to 16 hours, after cooling to room temperature, perform filtration, extraction and distillation under a reduced pressure to obtain an intermediate II; (3) Dissolve the intermediate II in an organic solvent, add quaternizing reagent at a ratio, then warm to 80-110° C. to react for 12 to 15 hours, after cooling to room temperature, perform filtration, extraction and distillation under a reduced pressure to obtain the dibenzylaminquaternary ammonium salt high-temperature resistant corrosion inhibitor. The process is simple and feasible, and its principle is reliable, and the prepared corrosion inhibitor has good resistance to the acid corrosion of carbon steels in oil-gas wells.

The objective of the present invention is to provide a carbon brush capable of suppressing an increase in temperature and sliding noise caused by excessive generation of coating on a commutator. The present invention is a carbon brush provided with a carbon-block base material having air holes in the surface and interior, the brush sliding in contact with a commutator provided in a motor, wherein the brush is characterized in that a suspension comprising a petroleum solvent with a boiling point higher than the temperature of the carbon brush when the motor is operating, and a fat, are present inside the holes, the ratio of the suspension to the carbon-block base material preferably being 0.5-6 percent by weight.

A method for inhibiting the formation or persistence of brain amyloid deposits in a patient, including administering to the patient a therapeutically effective amount of plant matter from a plant of the genus Hypericum, species perforatum.

The present invention relates to methods and compositions for the treatment, management, or prevention of multiple myeloma and / or renal dysfunction in mammals. The methods of the invention comprise the administration of an effective amount of one or more pituitary adenylate cyclase activating polypeptide (“PACAP”) compounds, which includes PACAP, vasoactive intestinal peptide (“VIP”), their agonists, analogs, fragments, or derivatives, having one or more PACAP activities. The invention also provides pharmaceutical compositions comprising one or more PACAP compounds of the invention either alone or in combination with one or more other prophylactic / therapeutic agents useful in therapy for the treatment, management, or prevention of multiple myeloma and / or renal dysfunction.

The present invention relates to polypeptide modulators of complement activity, including cyclic polypeptide modulators. Included are methods of utilizing such modulators as therapeutics.

The invention discloses a layered anti-aging insulation cover for a solid insulation ring main unit, and belongs to the field of solid insulation ring main units. The insulating cover comprises an insulating sleeve body, and the lower end of the insulating sleeve body is fixedly connected with a bus inlet pipe. A nanometer sterilization layer and a carbon fiber are used, so when the insulating cover is accidentally bumped, fungi or bacteria attached to a wound can be effectively prevented from continuing to spread into the epoxy resin insulating layer, and the wound is prevented from continuously enlarging into the epoxy resin insulating layer, thereby effectively preventing the enlarging of the biological aging range, and decreasing the aging speed of the insulating sleeve body. Meanwhile, the insulating cover is provided with a high heat conduction layer and a heat radiation film, so the heat generated by the switch assembly can be effectively conducted to the outside, the depositionof the heat in the insulation sleeve body is reduced, the benign dissipation of heat inside and outside the insulation sleeve body can be effectively maintained, and the service life of the insulation sleeve body is prolonged.

Sulfonyl derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.

The present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a Type II protein arginine methyltransferase (Type II PRMT) inhibitor. The present invention also provides methods for treating cancer in a human in need thereof, the methods comprising administering to the human a combination of a Type I PRMT inhibitor and a Type II PRMT inhibitor, together with at least one of: a pharmaceutically acceptable carrier and a pharmaceutically acceptable diluent, thereby treating the cancer in the human. The present invention further provide a pharmaceutical composition comprising a therapeutically effective amount of a Type I PRMT inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of a Type II PRMT inhibitor.

The present invention discloses an AKT inhibitor, and specifically relates to a compound represented by formula I or a pharmaceutically acceptable salt thereof. The present invention further provides a preparation method thereof, and the use thereof in prevention and / or treatment of a disease mediated by AKT protein kinase.

The invention relates to a scar-removing microneedle patch, which is characterized in that a microneedle array is arranged at the bottom end of a microneedle base layer and used for being punctured into skin; the top end of the microneedle base layer and the bottom end of a middle layer are integrally formed; the microneedle base layer, the middle layer and the microneedle array are made of degradable gel; sustained-release medicine is added into the degradable gel; the top end of the middle layer is fixedly connected with the bottom end of a top layer, a unidirectional guide layer is arranged in the top layer; the unidirectional guide layer has expansibility in one direction and has no expansibility in the other direction; and the direction without expansibility is perpendicular to the scar direction. The scar-removing microneedle patch in the invention can fix the skin and prevent the scar from becoming larger; and the medicine is slowly released into the skin and is used for avoiding or eliminating scars.

Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

The present invention provides a drug for preventing or treating inflammation-associated diseases in which a periostin isoform having cell adhesion activity is involved, and also provides an inhibitor of a periostin isoform having cell adhesion activity.

The invention discloses a layered anti-aging insulating cover for a solid insulating ring network cabinet, which belongs to the field of solid insulating ring network cabinets. A layered anti-aging insulating cover for a solid insulating ring network cabinet includes an insulating sleeve body, an insulating The lower end of the sleeve body is fixedly connected with the busbar inlet pipe, which can effectively prevent the fungus or bacteria attached to the "wound" from continuing to enter the epoxy resin insulation layer when the insulation cover is accidentally bumped through the use of nano-sterilizing layer and carbon fiber. The effect of spreading, and at the same time inhibiting the "wound" from continuing to grow into the epoxy resin insulation layer, effectively hindering the scope of biological aging, can reduce the aging speed of the insulation sleeve body, and at the same time, the setting of high thermal conductivity layer and heat radiation film can effectively It conducts the heat generated by the switch components to the outside and reduces the heat deposition in the insulating sleeve body, so as to effectively maintain the benign heat distribution inside and outside the insulating sleeve body and improve the service life of the insulating sleeve body.

Methods and compositions for the efficient and accurate determination of susceptibility of a hepatitis C virus (HCV) population to an HCV inhibitor are provided. In certain aspects, the methods involve introducing into a cell a patient derived segment, wherein the cell or the patient derived segment comprises an indicator nucleic acid that produces a detectable signal that is dependent on the HCV; measuring the expression of the indicator gene in the presence of varying concentrations of the HCV inhibitor; determining a standard curve of susceptibility; comparing the IC95 fold change, slope, or maximum inhibition percentage of the HCV population to that of a control HCV population, and determining that the HCV population comprises HCV with a reduced susceptibility to the inhibitor when the IC95 fold change value is increased or the slope and / or maximum inhibition percentage is lower for the HCV population as compared to the control population.