68 results about "Co-Transporters" patented technology

Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na⁺—K⁺-2Cl⁻ (NKCC) cotransporter. In certain embodiments, the Na⁺—K⁺-2Cl⁻ co-transporter is NKCC1.

The invention belongs to the field of medical technology, and particularly relates to a glucoside derivate shown as a formula (I), and a medically acceptable salt, an ester easily hydrolyzed, a stereoisomer and an itnemrediate of the glucoside derivate, and a preparation method of the compounds and the intermediate, in particular to a glucoside derivate which is served as a sodium-glucose co-transporter (SGLT) inhibitor, a medically acceptable salt, an ester easily hydrolyzed, a stereoisomer and an itnemrediate of the glucoside derivate, and a preparation method of the compounds and the intermediate. The glucoside derivate provided by the invention can be used for treating diabetes mellitus such as insulin dependent diabetes mellitus (I type diabetes mellitus) and non-insulin dependent diabetes mellitus (II type diabetes mellitus), and also can be applied to treating insulin resistance diseases and various diseases relevant to diabetes mellitus of fat, and preventing such diseases, wherein R1, R2, R3, R4, R5, R6, R7, R7a, R7b, R7c, X, n and A are defined as shown in the specification.

The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcholic fatty liver disease (NAFL), non-alcholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcholic fatty liver disease toxic fatty liver or the like.

The invention discloses an eutectic compound of 1-(beta-D-pyranoglucosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene and L-phenylalanine and a preparation method thereof. Specifically speaking, the invention discloses the eutectic compound shown in a formula (Ia) and formed by L-phenylalanine and a sodium-glucose co-transporter 2 (SGLT-2) inhibitor shown in a formula (I), i.e., 1-(beta-D-pyranoglucosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene. The XRD characteristic peaks of the eutectic compound are shown in a figure 1. The preparation method comprises the following steps: mixing an aqueous solution of L-phenylalanine with an ethanol solution of the compound I; carrying out heating for dissolving of the two substances; then carrying out stirring, cooling and crystallization; and subjecting a filtrate to ethanol water recrystallization so as to obtain the eutectic compound. The formula (I) and the formula (Ia) are described in the specification.

An optical imaging method based on a feedback principle in which the specific scan pattern is adapted according to the shape of the sample. The feedback approach produces nanometer-resolved three dimensional images of very small and moving features in live cells and in a matter of seconds. Images of microvilli in live cultured opossum kidney cells expressing NaPi co-transporter proteins with different GFP constructs and images of cell protrusions in a collagen matrix are produced with a resolution of about 20 nm. Along cell protrusions in three dimensional cellular adhesions could be identified to the extracellular matrix.

The present invention belongs to the field of pharmaceutical technology, more specifically relates to optically pure benzyl-4-chlorophenyl-C-glucoside derivatives represented by formulae (II) and (III), a process for preparing these compounds and intermediates thereof, a pharmaceutical formulation and a pharmaceutical composition containing these compounds, and the use of the optically pure benzyl-4-chlorophenyl-C-glucoside derivative as a sodium glucose co-transporter (SGLT) inhibitor in manufacture of a medicament for treating and/or preventing diabetes mellitus (including insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus) or diabetes-associated diseases (including insulin resistance disease and obesity)

The invention relates to a crystal form of a glucopyranose derivative serving as a sodium-glucose co-transporter (SGLT) inhibitor, a preparation method thereof and a pharmaceutical application thereof, and also relates to a medicine compound containing the crystal form and the application thereof for preparing drugs for treating diabetes and/or diseases related to diabetes.

The invention relates to the field of medicines related to diabetes mellitus and particularly relates to a 2-type sodium-glucose co-transporter (SGLT2) inhibitor with a multi-aryl glucoside structure and shown as the specification, a preparation method thereof, a medicine composition taking the compound as an active components and an application thereof in preparing medicines for resisting diabetes mellitus.

The invention discloses a method for improving drought tolerance of plants by improving photorespiration, which comprises the following steps: inhibiting or knocking out bile acid sodium cotransportergenes in the plants, and simultaneously overexpressing glyoxylate dehydrogenase genes and malate synthase genes. The method creatively discovers that the expression of the BASS6 gene in the plant isinhibited; glycolic acid dehydrogenase genes and malic acid synthase genes are overexpressed in chloroplast, light respiration can be remarkably reduced, the photosynthetic efficiency of plants can beimproved, the biomass or yield of the plants can be increased, more importantly, the drought tolerance of the transgenic plants is remarkably higher than that of plants inhibiting PLGG1 gene expression, and the drought tolerance is improved by 5%-50%.

The present invention relates to the treatment of prevention of tinnitus. More precisely, the present invention relates to a compound modulating chloride co-transporter NKCC1 (chloride co-transporter modulator) for use in the treatment of tinnitus. In addition, the present invention concerns pharmaceutical composition comprising such an NKCC1 chloride co-transporter modulator as an active agent a method for the treatment or prevention of tinnitus by administering such a chloride co-transporter modulator, and a screening method for the identification and characterization of compounds capable of modulation chloride co-transporter NKCC1.

Foods or meals high in available carbohydrate such as sucrose or starch increase postprandial blood glucose concentrations. Repeated high post-prandial plasma glucose “spikes” are associated with an increased risk of developing type II diabetes. Unregulated glycemic excursions are undesirable, and any reduction or “blunting” of the post-prandial glucose concentration in blood is potentially beneficial. This invention relates to an edible composition for delay of intestinal glucose uptake through synergistic inhibition of both active sodium glucose co-transporter 1 (SGLT1) and passive glucose transporter 2 (GLUT2) leading to flattening or blunting of the post-prandial glucose peak. Thus in a first aspect of the invention, an edible composition is provided, the composition comprising at least 5% dry weight at least one flavonoid aglycone and at least 5% dry weight at least one flavonoid glucoside, wherein the flavonoid glucoside is at least 20%, preferably at least 40%, most preferably at least 60% more resistant to hydrolysis by lactase phloridzin hydrolase than quercetin-4-glucoside, and wherein the flavonoid aglycone is a GLUT 2 inhibitor and the flavonoid glucoside is a SGLT 1 inhibitor.

The invention relates to a sulfate of an intestine type 2B sodium phosphate co-transporter inhibitor and its crystal form and particularly relates to N1-methyl-N1-(2-morpholin-ethyl)-N3-(3-(4-phenethylphenylcarbamoyl)-4, 5, 6, 7-tetrahydrobenzo[b]thiophene-2-yl)-m-phthalamide sulfate (compound shown in the formula (I)) and its type I crystal and preparation method. The type I crystal of the compound shown in the formula (I) has good chemical stability and crystal form stability and the used crystallization solvent has low toxicity and low residue content and can be used for clinical treatment.