31 results about "SGLT2 Inhibitor" patented technology

The invention discloses a preparation method of an SGLT2 inhibitor key intermediate, and belongs to the technical field of medicinal chemistry. The preparation method comprises the following steps: 1) reacting a compound B with trimethylchlorosilane under an alkaline condition to generate a compound C; 2) reacting the compound C with an aldehyde group reagent on an aromatic ring to generate a compound D; 3) reacting the compound E with a bromination reagent to generate a compound F; 4) preparing the compound F into a Grignard reagent to generate a compound G; 5) carrying out addition reaction on the compound D and a compound G to generate a compound H; and 6) carrying out dehydroxylation and trimethylsilyl protection on the compound H to generate a compound A. According to the preparation method, the risk caused by amplification of the Sandmeyer reaction in the original route is avoided, and meanwhile, the preparation cost of the key intermediate is greatly reduced.

One or more SGLT2 inhibitors or pharmaceutically acceptable forms thereof are provided for use in the treatment and / or prevention of a metabolic disorder of an equine animal. For example, the treatment and / or prevention can be for laminitis, vascular dysfunction, hypertension, hepatic lipidosis, atherosclerosis, hyperadrenocorticism, Pituitary Pars Intermedia Dysfunction and / or Equine Metabolic Syndrome in an equine animal.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

The present application relates to a kind of SGLT2 inhibitor in the preparation for treating hormone receptor low reaction type reproductive system disease in the application of drug, in particular, SGLT2 inhibitor and hormone can improve or enhance the sensitivity and / or for reversing the drug resistance of endocrine therapy drug, such as hormone, can enhance the therapeutic effect of such drug, especially in drug-resistant reproductive system disease and tumor treatment has good application prospect.

The present invention consists of a digital, always-online computer system designed to optimize perioperative safety through the automated integration of clinical and laboratory parameters. Unlike conventional medical calculators, this system implements a reactive logic engine that simultaneously calculates glomerular filtration rate (CKD-EPI 2021) and scores multiple risk scales (Goldman, LEE, ASA, CHA2DS2-VASc, HAS-BLED) without duplicate data entry. The system includes a drug reconciliation algorithm that cross-references the bleeding risk of the surgical procedure with the patient's renal function, generating accurate recommendations for discontinuing or continuing high-risk medications (anticoagulants, antiplatelet agents, SGLT2 inhibitors) based on current clinical evidence.

Methods of treating type 1 diabetes, improving cardiovascular health, delaying renal function decline, reducing the risk of cardiovascular death and reducing the risk of heart failure hospitalization, while minimizing adverse events such as diabetic ketoacidosis and severe hypoglycemia, using sodium-glucose cotransporter 2 (SGLT2) inhibitors are disclosed. In a preferred method, the SGLT2 inhibitor is sofogliflozin. Also disclosed are prescriptions for developing sofogliflozin and methods of administering sofogliflozin.

The present invention relates to a pharmaceutical combination, comprising (a) a pharmaceutical formulation comprising (i) lixisenatide or / and a pharmaceutically acceptable salt thereof, and (ii) insulin glargine or / and a pharmaceutically acceptable salt thereof, and (b) an SGLT2 inhibitor, or / and a pharmaceutically acceptable salt thereof.

An object of the present invention is to improve the treatment and / or prevention of cardiovascular and renal diseases compared to already known monotherapies. A further object of the present invention is to provide a combination of pharmaceutical active ingredients for treating cardiovascular diseases, particularly cardiac and renal failure, characterized by chronic sodium retention, which reduces patient mortality and / or morbidity. Another object of the present invention is to improve the treatment and / or prevention of cardiovascular and renal diseases by administering a combination comprising finerenone and an SGLT2 inhibitor. [Solution] The present invention relates to pharmaceutical compositions and combinations comprising finerenone or its hydrate, solvate, or pharmaceutically acceptable salt or polymorph thereof, and an SGLT2 inhibitor or its hydrate, solvate, or pharmaceutically acceptable salt or polymorph thereof. The combinations can be used for the treatment and / or prevention of cardiovascular and / or renal diseases in humans and other mammals.

The invention discloses a pharmaceutical composition of an SGLT2 inhibitor and menthol and application of the pharmaceutical composition in preparation of drugs for preventing, improving and / or treating heart diseases. The pharmaceutical composition has a myocardial cell protection effect, can synergistically reduce intracellular calcium ion concentration and synergistically promote fatty acid metabolism, has advantages compared with single medication, and can be used for preparing drugs for treating, improving and / or preventing heart failure, coronary heart disease, myocardial infarction, hypertensive heart disease and the like.

A pharmaceutical composition comprising: (a) one or more of a first pellet comprising i. a first core, and ii. a first coating on the first core, wherein the first coating comprises a mineralocorticoid receptor (MR) modulator and a first binder; and (b) one or more of a second pellet comprising i. a second core, and ii. a second coating on the second core, wherein the second coating comprises an SGLT2 inhibitor, wherein the SGLT2 inhibitor is about 5% to about 20% by weight of the second pellet, wherein the composition comprises about 20% to about 50% by weight of the mineralocorticoid receptor (MR) modulator; and about 1% to about 10% by weight of the SGLT2 inhibitor. Said compositions for use in the treatment of chronic kidney disease or heart failure.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

A combinational medicine of: esaxerenone or a pharmaceutically acceptable salt thereof; and a SGLT2 inhibitor.

The present invention relates to pharmaceutical compositions of linagliptin, pharmaceutical dosage forms, their preparation, their use and methods for treating metabolic disorders.

Disclosed herein are compositions and methods for transdermal formulations of antidiabetic agents. An example transdermal formulation contains a SGLT2 inhibitor, and is used for the treatment of Type 2 diabetes.

The present invention provides a method for treating a subject with chronic kidney disease (CKD) or CKD and hypertension, the method comprising administering to the subject once daily a certain amount of lorenstat or a pharmaceutically acceptable salt thereof, said amount being effective in treating the subject's CKD or CKD and hypertension.

The present invention describes synergistic compositions and combinations comprising one or more prolyl hydroxylase inhibitors or pharmaceutically acceptable salts thereof and a SGLT2 inhibitors or pharmaceutically acceptable salts thereof for the treatment of diabetes and diabetes induced CKD and the associated symptoms like anemia. Specifically, the present invention provides synergistic composition and combination of compound of formula (Ia) or its pharmaceutically acceptable salts and a SGLT2 inhibitors or pharmaceutically acceptable salts thereof for the treatment of diabetes and diabetes induced CKD and the associated symptoms like anemia. The present invention also describes the preparation of such compositions and combinations.

The present disclosure is directed to methods of treating patients with chronic kidney disease (CKD), with and without Type 2 diabetes, with an SGLT2 inhibitor, such as dapagliflozin.

A pharmaceutical composition containing an SGLT2 inhibitor and menthol is effective for preventing, ameliorating, and / or treating heart diseases. The pharmaceutical composition has a myocardial cell protection effect, synergistically reduces intracellular calcium ion concentration, synergistically promotes fatty acid metabolism, has advantages compared with a single medication. The composition can be used for preparing medicines for treating, ameliorating, and / or preventing heart failure, coronary heart disease, myocardial infarction, hypertension heart disease, etc.

To provide a novel agent having an action of promoting urinary excretion of sugar.SOLUTION: Provided is an agent for promoting urinary excretion of sugar, the agent containing Dai-saiko-to or Bofu-tsusho-san. Also provided is an agent for promoting urinary excretion of sugar, the agent containing Dai-saiko-to and being used so as to be taken before meals. Also provided is an agent for promoting urinary excretion of sugar, the agent containing Bofu-tsusho-san and being used so as to be taken before meals. Further provided is an SGLT2 inhibitor that contains Dai-saiko-to or Bofu-tsusho-san.SELECTED DRAWING: Figure 3

The invention discloses a deep learning and behavior boosting theory-based accurate prediction system for a urogenital system infection risk of SGLT2 inhibitor hypoglycemic drugs. According to the invention, through the innovative structural design of the deep learning risk prediction module, the individualized accurate prediction of the SGLT2 inhibitor hypoglycemic drug related urogenital infection risk is realized. The module adopts a hybrid neural network of a Transform encoder and a gating circulation unit, can process multi-source clinical data of a patient at the same time, not only identifies deep association between static characteristics such as demostatistics and medical history and infection risks, but also captures fluctuation rules of dynamic sequences such as laboratory inspection indexes along with time. The deep mining capability of a high-dimensional complex data mode breaks through the limitation that a traditional scoring tool depends on limited indexes and fixed weights, differentiated risk levels can be output according to the unique clinical trajectory of each patient, and an accurate decision basis is provided for subsequent intervention.

The present invention provides a method for precision anti-obesity therapy, utilizing a proprietary panel of genetic variants to predict individual patient response to weight-loss medications as well as a related companion diagnostic. In particular, the method analyzes variants in genes including GLP-1 R, CNR1, TCF7L2, DPP4 and others, which have established associations with drug efficacy and metabolism in obesity treatment. By genotyping these markers, the method guides selection and dose optimization of specific anti-obesity medications—such as GLP-1 receptor agonists, metformin, SGLT2 inhibitors, and DPP4 inhibitors—tailored to the patient's genetic profile. Notably, GLP-1R polymorphisms (e.g., rs6923761) are leveraged as especially predictive indicators of enhanced weight loss response to GLP-1 receptor agonists. Through this innovative genetic profiling approach, the invention enables personalized treatment strategies that maximize efficacy, minimize trial-and-error in drug choice, and reduce adverse effects, thereby embodying the principles of precision medicine in obesity care.

The application relates to the technical field of stem cell engineering and regenerative medicine, and specifically discloses a stem cell treatment method for treating type 2 diabetes. The method comprises the following steps: S1, extracting placenta-derived mesenchymal stem cells; S2, performing multi-gene modification on the mesenchymal stem cells to obtain gene-modified mesenchymal stem cells; S3, pretreating the gene-modified mesenchymal stem cells with a culture medium; S4, extracting microvesicles from the mesenchymal stem cells; S5, mixing the microvesicles, baicalin, L-arginine and vitamin D in a buffer to form a composite preparation; S6, introducing the composite preparation into a patient's body through abdominal cavity intervention; and S7, performing synergistic treatment by combining oral administration of an SGLT2 inhibitor after infusion, and regularly monitoring islet function indexes. The stem cell treatment method can be used for treating type 2 diabetes, and has the advantages of being targeted to improve the islet microenvironment, promoting the recovery of beta cell function and being durable in action.

The present disclosure is directed to methods of treating patients with chronic kidney disease (CKD), with and without Type 2 diabetes, with an SGLT2 inhibitor, such as dapagliflozin.

The invention belongs to the technical field of biological medicine, and particularly relates to application of baicalin serving as an SGLT2 inhibitor to treatment of diabetic heart failure. The invention provides the baicalin as a natural SGLT2 inhibitor stimulant for the first time, and the baicalin is used for improving ejection fraction retention heart failure and diabetes related cardiovascular diseases. Molecular docking proves that the binding energy (-9.1 kcal / mol) of the baicalin and the SGLT2 is equivalent to that of phlorizin, and the structural similarity reaches 51.54%. Animal experiments show that 50 mg / kg / day of baicalin can significantly reduce the weight of a classical diabetes model mouse induced by high fat-STZ (Sequence Tagliflozin) by 8.73%, p < t >, 0.01, postprandial blood sugar by 22.7% in 60 min and cardiac hypertrophy indexes by heart weight / weight ratio reduction, p < t >, 0.001, and improve the left ventricular ejection fraction by 21.3%, and has no statistical difference from empagliflozin (EMPA, SGLT-2 inhibitor on the market in China in 2017) in effect. The invention provides a novel natural medicine scheme for HFpEF treatment.

The invention discloses a method for purifying phlorizin of lithocarpus litseifolius and a method for synthesizing an SGLT2 inhibitor T-1095 by using phlorizin, and belongs to the technical field of plant effective component extraction and drug synthesis. The purification method of the lithocarpus litseifolius phlorizin comprises the following steps: digesting lithocarpus litseifolius powder with an ethanol solution, adding polyacrylamide and activated carbon, removing chlorophyll and other flavonoid compounds in a lithocarpus litseifolius extracting solution, and separating and purifying to obtain the lithocarpus litseifolius phlorizin. Phlorizin is used as a raw material to synthesize the SGLT2 inhibitor T-1095. According to the purification method, complex procedures such as resin elution are not needed, purification steps are reduced, and meanwhile the purity and yield of phlorizin are improved; the T-1095 hypoglycemic drug is synthesized by adopting a multi-step synthesis strategy, so that the reaction complexity and difficulty are reduced, the reaction selectivity and controllability are improved, and the whole synthesis process is more efficient and stable.

The invention described herein relates to oral dosage form therapies for treating metabolic disorders using combinations of inhibitors of SGLT1 and SGLT2. In such dosage forms, SGLT1 is effective in the intestinal lumen, and is either not absorbed, or poorly absorbed, while the SGLT2 inhibitor inhibits sugar reabsorption in the kidney by inhibiting SGLT2 activity. Metabolic disorders treated by combined SGLT1 and SGLT2 oral dosage forms include disorders associated with abnormal accumulation of liver lipids, which may also be copresent with hyperglycemia. Combinations of SGLT1 and SGLT2 inhibitors are contemplated herein, particularly combinations.

The pharmacokinetic profile of the SGLT2 inhibitor bexagliflozin can be improved by formulating it as an extended release tablet. Compared with standard immediate-release dosage forms these tablets can permit a lower peak plasma concentration, Cmax, while maintaining plasma concentrations at therapeutic levels for a desired period. This can be used, for instance, to administer lower doses while still providing the same pharmacological effect.

The invention relates to methods for improving glycemic control and for treating erectile dysfunction in a patient diagnosed with prediabetes, type 1 diabetes mellitus, type 2 diabetes mellitus or metabolic syndrome wherein a sodium glucose co-transporter 2 (SGLT2) inhibitor is administered to the patient. Furthermore the invention relates to a method for improving a treatment of erectile dysfunction in a male patient diagnosed with prediabetes, type 1 diabetes mellitus or type 2 diabetes mellitus characterized in that in addition to the treatment of erectile dysfunction a SGLT2 inhibitor is administered to the patient. The invention also relates a pharmaceutical composition comprising a SGLT2 inhibitor and a compounds selected from the group consisting of phosphodiesterase 5 (PDE5) inhibitors or alprostadil.

Disclosed are methods for treating or preventing chronic kidney disease (CKD) or any one of a number of other therapeutic indications, comprising co-administering to a patient in need thereof an effective amount of a SLC6A19 inhibitor and an effective amount of a SGLT2 inhibitor.