36 results about "Translocator protein 2" 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.

An object of the present invention is to provide a monoclonal antibody which is useful for treating or diagnosing a disease relating to system ASC amino acid transporter 2 (hereinafter, referred to as “ASCT2”) or a method using the antibody. The present invention provides a monoclonal antibody which specifically recognizes a native three-dimensional structure of an extracellular region of ASCT2 and binds to the extracellular region, or an antibody fragment thereof; a hybridoma which produces the antibody; a DNA which encodes the antibody; a vector which contains the DNA; a transformant obtainable by introducing the vector; a process for producing an antibody or an antibody fragment thereof using the hybridoma or the transformant; and a therapeutic agent using the antibody or the antibody fragment thereof, and a diagnostic agent using the antibody or the antibody fragment thereof.

An object of the present invention is to provide a monoclonal antibody which is useful for treating or diagnosing a disease relating to system ASC amino acid transporter 2 (ASCT2) or a method using the antibody. The present invention provides a monoclonal antibody which specifically recognizes a native three-dimensional structure of an extracellular region of system ASC amino acid transporter 2 (ASCT2) and binds to the extracellular region, or an antibody fragment thereof; a hybridoma which produces the antibody; a DNA which encodes the antibody; a vector which contains the DNA; a transformant obtainable by introducing the vector; a process for producing an antibody or an antibody fragment thereof using the hybridoma or the transformant; and a therapeutic agent using the antibody or the antibody fragment thereof, and a diagnostic agent using the antibody or the antibody fragment thereof.

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.

The invention belongs to the technical field of organic synthesis route design and medicine and chemical engineering, particularly relates to a synthesis method of a sodium-glucose cotransporter 2(SGLT2) inhibitor, and more particularly relates to a preparation method of empagliflozin. The empagliflozin is synthesized by taking (3S)-3-[4-[(2-chloro-5-iodophenyl) methyl] phenoxy] tetrahydrofuran and glucono delta-lactone as initial raw materials through a series of substep reactions such as protection, addition, substitution, deprotection and reduction. In the synthesis steps disclosed by the invention, a staged target product does not need to be separated and purified after each step of reaction, and the target product is finally obtained by directly subjecting a high-purity reaction intermediate to subsequent steps. The preparation method is simple in process, simple and convenient to operate and good in industrial prospect.

The invention provides glucoside derivatives and pharmaceutical compositions thereof. The invention discloses chemical compounds as shown in general formula (I), pharmaceutically-acceptable salts thereof, easily-hydrolytic lipid prodrug thereof or isomers thereof, and the pharmaceutical compositions containing the chemical compounds which is used as sodium-glucose cotransporter 2 inhibitor used for treating or suspending relative diseases like diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy and insulin resistance.

The present invention relates to a method for diagnosis of a chronic kidney disease in a subject by detecting the expression level of a sodium-glucose linked transporter 2 (SGLT2) protein in urine samples. A method for monitoring progression of a chronic kidney disease in a patient is also provided.

The invention discloses a preparation method of a sodium-glucose cotransporter 2 inhibitor. The preparation method specifically relates to a reaction step for converting a compound of a formula III into a compound of a formula II by a 'one-pot method' in a palladium carbon/acid or 1,2-dichlorobenzene catalytic system, wherein the definition of each substituent in the formula II and the formula IIIare the same as that in the description. The method has simple operation and low cost, and is suitable for large-scale production.

It is to provide an agent for treating and/or ameliorating retinopathy caused by glucose. It is an agent for treating retinopathy caused by glucose comprising sodium/glucose cotransporter2 inhibitor (SGLT2 inhibitor) as an active ingredient, and is used at a normal dosage amount, or at a lower dosage whereby no lowering in blood sugar is observed.

The invention discloses a drug compound containing a sodium-glucose synergic transport protein 2 inhibitor. Specifically, the drug compound contains 1,6-dehydrated-1-C-{4-chlorine-3-[(3-fluorine-4-phenetyl) methyl] phenyl}-5-C-(hydroxymethyl)-beta-L-idose or a compound formed by the same with amino acid, pre-gelled starch and at least one pharmaceutically acceptable excipient. The drug compound disclosed by the invention has the characteristics of strong technical operability and quick and complete dissolution.