141 results about "Sodium dependent" patented technology

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Methods of modifying therapeutic compounds such as drugs to be substrates for active transporters expressed in epithelial cells lining the lumen of the human colon are disclosed. The transporters expressed in the human colon include the sodium dependent multi-vitamin transporter (SMVT), and monocarboxylate transporters 1 and 4 (MCT 1 and MCT 4). The modified compounds can themselves be pharmacologically active, or upon cleavage of a chemical moiety after uptake from the colon, can be metabolized to form a compound that is pharmacologically active (e.g., a prodrug). The modified compounds disclosed herein are suitable for use in extended release oral dosage forms, particularly those that release drug over periods of greater than about 2-4 hours following administration.

The invention relates to the use of cannabidiol (CBD), at a dose of greater than 300 mg / day, in combination with a standard anti-epileptic drug (SAED) which acts via sodium or calcium channels, for use in the treatment of epilepsy. The SAED is preferably one which•modifies low-threshold or transient neuronal calcium currents,or•reduces high-frequency neuronal firing and sodium-dependent action potentials and enhances GABA effects. Preferred SAEDs are ethosuximide and valproate.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Disclosed herein are conjugates comprising a therapeutic agent (e.g., a drug) which is linked to a conjugate moiety that is itself, or itself in combination with the agent, is a good substrate for the sodium dependent multi-vitamin transporter (SMVT). The conjugates have a molecular weight below 1500 daltons and exhibit increased uptake via SMVT through the cells lining the gastrointestinal lumen, and hence higher bioavailability, when administered orally compared to the therapeutic agent itself Also disclosed are methods of delivering agents that, as a result of linkage to a conjugate moiety, are good substrates of the SMVT transporter. Further disclosed are methods of screening conjugates or conjugate moieties, linked or linkable to a therapeutic agent, for capacity to be transported as substrates through the SMVT transporter.

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

The invention relates to compositions comprising three inhibitors, one pancreatic lipase inhibitor, an alpha glucosidase inhibitor, and a sodium dependent glucose transporter inhibitor. The invention also provides methods of using the compositions for controlling glucose and lipid uptake.

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

A compound represented by formula I, or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture thereof, wherein, R1 and R2 are independently hydrogen, -OH, alkyl, -CF3, -OCHF2, -OCF3 or halogen,R3 is cycloalkyl, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or -OCH2CH3,R4 is hydrogen, -OH, -O aryl, -OCH2 aryl, alkyl, cycloalkyl, -CF3, -OCHF2, -OCF3, -OCH2CF3, -OCH2CHF2, -OCH2CH2F or halogen,A is -CX1X2, wherein X1 and X2 are independently H, F and Cl, and when both X1 and X2 are H, R3 is other than -OCH2CH3. The compound has an activity of inhibitors of sodium-dependent glucose transport protein. A method for preparing the compound. A pharmaceutical composition comprising the compound. A use of the compound and pharmaceutical composition thereof in the preparation of medicaments of SGLT2 inhibitors for treating a disease of interest.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

In accordance with the invention, a novel gene translocation, (4p15, 6q22), in human non-small cell lung carcinoma (NSCLC) that results in fusion proteins combining part of Sodium-dependent Phosphate Transporter Isoform NaPi-3b protein (SLC34A2) with Proto-oncogene Tyrosine Protein Kinase ROS Precursor (ROS) kinase has now been identified. The SLC34A2-ROS fusion proteins are anticipated to drive the proliferation and survival of cancer cells, and particularly drive the proliferation and survival of a subgroup of NSCLC tumor cells. The invention therefore provides, in part, isolated polynucleotides and vectors encoding the disclosed mutant ROS kinase polypeptides, probes for detecting it, isolated mutant polypeptides, recombinant polypeptides, and reagents for detecting the fusion and truncated polypeptides. The disclosed identification of the new fusion protein enables new methods for determining the presence of these mutant ROS kinase polypeptides in a biological sample, methods for screening for compounds that inhibit the proteins, and methods for inhibiting the progression of a cancer characterized by the mutant polynucleotides or polypeptides, which are also provided by the invention.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.

The invention relates to compositions comprising at least two inhibitors selected from the group consisting of an alpha amylase inhibitor, an alpha glucosidase inhibitor, and a sodium dependent glucose transporter inhibitor. The invention also provides methods of using the compositions for controlling glucose uptake.

The invention relates to a human idiopathic basal ganglia calcification pathogenic gene and a detection method thereof. Human idiopathic basal ganglia calcification, namely IBGC is a neurodegenerative genetic disease. The invention provides seven mutation forms of four pathogenic genes including SLC20A2 (Sodium-dependent phosphate transporter 2), PDGFRB (Platelet-derived Growth Factor Receptor Beta), PDGFB (Platelet-derived Growth Factor Subunit B) and XPR1 (Xenotropic and Polytropic Retrovirus Receptor 1) and sequences of the seven mutation forms are shown as SEQ ID NO.1 to SEQ ID NO.7. The form of the pathogenic gene provided by the invention is not reported until now and can provide evidence and lay a foundation for analysis and medicine development of a pathogenic mechanism, pathogenic gene screening and detection, formulation of a therapeutic regimen and the like. Meanwhile, the invention constructs a pathogenic gene detection method; the pathogenic gene detection method comprises the following steps: firstly, capturing a pathogenic gene exon region by utilizing multi-PCR (Polymerase Chain Reaction); carrying out next generation sequencing on the pathogenic gene exon region and carrying out information analysis to find out mutation; finally, identifying the mutation by utilizing Sanger sequencing, wherein a PCR captured primer group comprises amplification primer sequences SEQ ID NO.12 to SEQ ID NO.23, and amplification primer sequences of a Sanger sequencing segment are shown as SEQ ID NO.24 to SEQ ID NO.35. The detection method provided by the invention covers all exons of the four pathogenic genes and can be used for efficiently, comprehensively, rapidly and accurately acquiring mutation information.

The invention provides C-aryl glucoside derivatives, a preparation method and an application thereof, relates to the field of medicines relative to diabetes and particularly relates to a sodium-dependent glucose transport protein type-2 (SGLT-2) inhibitor containing a C-aryl glucoside structure, the preparation method of the inhibitor and the application of the inhibitor in preparation of diabetes medicines. Definition of each substituent groups in general formula (I) is same as that in the description.

The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof:wherein ring A, ring B, X and Y have the same meanings as defined in the specification.

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations.

Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

The invention relates to C-aryl glucoside derivatives containing a difluoromethylene group. Specifically, the invention provides novel sodium-dependent glucose transporter (SGLT-2) inhibitors, a preparation method thereof and application thereof in preparing drugs for the treatment of diseases related to SGLT-2, especially diabetes, obesity and diabetic complications. The C-aryl glucoside derivatives provided by the invention have stronger inhibition activity and higher selectivity for sodium-dependent glucose transporter (SGLT-2), and can obviously promote the emission of glucose in urine of animals.