54 results about "Anti-diabetic Agent" patented technology

The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the invention are described by general formula (1); wherein R¹ is H or CN; R² is selected from CH₂R⁵, CH₂CH₂R⁵ and C(R³)(R⁴)—X²—(CH₂)_aR⁵; R³ and R⁴ are each independently selected from H and Me; R⁵ is selected from CON(R⁶)(R⁷), N(R⁸)C(=0)R⁹, N(R⁸)C(═S)R⁹, N(R⁸)SO₂R¹⁰ and N(R⁸)R¹⁰; R⁶ and R⁷ are each independently R¹¹(CH₂)_b or together they are —(CH₂)₂-Z-(CH₂)₂— or CH₂-o-C₆H₄-Z-CH₂—; R⁸ is H or Me; R⁹ is selected from R¹¹(CH₂)_b, R¹¹(CH₂)_bO and N(R⁶)(R⁷); R¹⁰ is R¹¹(CH₂)_b; R¹¹ is selected from H, alkyl, optionally substituted aryl, optionally substituted aroyl, optionally substituted arylsulphonyl and optionally substituted heteroaryl; R¹² is selected from H₂NCH(R¹³)CO, H₂NCH(R¹⁴)CONHCH(R¹⁵)CO, C(R¹⁶)═C(R¹⁷)COR¹⁸ and R¹⁹OCO; R¹³, R¹⁴ and R¹⁵ are selected from the side chains of the proteinaceous amino acids; R¹⁶ is selected from H, lower alkyl (C₁-C₆) and phenyl; R¹⁷ is selected from H and lower alkyl (C₁-C₆); R¹⁸ is selected from H, lower alkyl (C₁-C₆), OH, O-(lower alkyl (C₁-C₆)) and phenyl; R₁₉ is selected from lower alkyl (C₁-C₆), optionally substituted phenyl and R²⁰C(=0)OC(R²¹)(R²²); R²⁰, R²¹ and R²² are each independently selected from H and lower alkyl (C₁-C₆); Z is selected from a covalent bond, —(CH₂)_c—, —O—, —SO_d— and —N(R¹⁰)—; X¹ is S or CH₂; X² is O, S or CH₂; a is 1, 2 or 3; b is 0-3; c is 1 or 2; and d is 0, 1 or 2.

Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.

The present invention relates to compositions comprising an anti-obesity agent and an anti-diabetic agent useful for the treatment of diabetes, diabetes associated with obesity and diabetes-related disorders. The present invention further relates to methods of treating or preventing obesity, and obesity-related disorders, in a subject in need thereof by administering a composition of the present invention. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods.

Compositions and methods for treating type 2 diabetes and its sequelae by intravenous or subcutaneous administration of formulations of synthesized curcumin (diferuloylmethane) and concomitantly one or more anti-diabetic agents to human subjects are disclosed herein. The composition of the present invention may be used to: (i) treat patients with diabetes in advanced stages with evidence of any or all encephalopathy, retinopathy, nephropathy, pancreatitis or neoplasias; (ii) treat patients with diabetic disease status without symptomatic or pathologic evidence of associated sequelae but requiring better glycemic control than that offered by standard of care anti-diabetic; and (iii) patients with objective signs or symptoms of sequelae from diabetes of anti-diabetic drugs. One three-drug combination of the present invention includes a slow release PLGA-curcumin and an oral gliptin (DPP-4)-inhibitor or any incretin-mimetic and metformin.

The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) or formula (II) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and/or an anti-obesity agent.

Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel b benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and/or an anti-obesity agent.

The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.

The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.

The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

The present invention discloses a novel anti-diabetic composition extracted from fenugreek seeds. The same comprises a furostanolic-saponin-rich fraction (>70%) with approximately 30% protodioscin as one of the bioactive components. Pre-clinical studies in rats indicated significant glucose lowering effect of the fraction (31.5%) as compared to control after two weeks of oral treatment. Clinical studies in human volunteers indicated suitability of a dosage form of 500 mg given once or twice daily as anti-diabetic agent either alone or in combination with standard, synthetic anti-diabetic drugs such as metformin and glipizide in controlling plasma glucose levels.

The present invention describes small molecules that have the activity of directly enhancing insulin sensitivity through epigenetic regulation. These small molecules, therefore, provide a new path for the treatment of type 2 diabetes and insulin resistance in type 1 diabetes or prediabetes and also can be used to treat obesity and chronic liver disease. Methods and compositions including these small molecules or for their administration are described. The methods and compositions can include additional anti-diabetic agents.

The present invention provides compounds of formula (I)

the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R¹, R², R^a, R^b, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.

A complex of glucosamine having a purity of at least about 99 wt. % and a maximum halide content of about 0.01 wt. %, and a therapeutic drug having a pK_a of less than 7. Preferably, the complex is stabilized by coating it with at least one pharmaceutically acceptable polymer comprising a water-soluble, water-immiscible and/or water-swellable homopolymer and/or copolymer. Suitable polymers include carboxypolymethylene homopolymers and copolymers; polyethylene glycol homopolymers and copolymers, povidone homopolymers and copolymers; polyacrylic acid homopolymers and copolymers; polyacrylamide homopolymers and copolymers; polysaccharides; and mixtures of two or more of the foregoing polymers. The resultant coated complex will be stable upon exposure to ambient temperature and/or the atmosphere. Suitable therapeutic drugs fall into the following classes: α- and β-Adrenergic Agonists; Narcotic and Non-Narcotic Analgesics; Anorexics; Antiallergics; Antianginals; Antiarrhythmics; Antiasthmatics; Antibiotics; Anticoagulants; Anticonvulsants; Antidepressants; Antidiabetics; Antihistaminics; Antihypertensives; Nonsteroidal Anti-Inflammatories; Antimigraines; Antineoplastics; Antiparkinsonians; Antipsychotics; Antipyretics; Antispasmodics; Antithrombotics; Antiulceratives; Anxiolytics; Decongestants; Diuretics; Hepatoprotectants; Sedatives; and Vasodilators.

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

A Pdia4 inhibitor for use in preventing, alleviating and/or treating diabetes and/or diabetes-related complications in a subject in need thereof is disclosed, wherein the Pdia4 inhibitor does not comprise cytopiloyene. A Pdia4 inhibitor and one other anti-diabetic agent for use in combination therapy in preventing, alleviating, treating diabetes and diabetes-related complications, and/or reversing diabetes in a subject in need thereof is also disclosed, wherein the Pdia4 inhibitors for use in combination therapy may comprise cytopiloyene. Also disclosed are methods for diagnosing, treating and monitoring diabetes, and methods of screening for a Pdia4 inhibitor and/or an anti-diabetic agent.