Abstract: The invention provides a novel adrenomedullin derivative sustainable for a long period which is capable of substantially suppressing unwanted side effects while maintaining pharmacological effects of adrenomedullin. In an exemplary embodiment, the invention relates to a compound represented by formula (I): A-CH2-B (I) [wherein A is a modifying group comprising one or more polyethylene glycol groups, and B is a peptide moiety derived from adrenomedullin or a modified form thereof with adrenomedullin activity, wherein the peptide moiety B is linked to the other moieties through a covalent bond of the nitrogen atom of the N-terminal ?-amino group of the peptide moiety B to the carbon atom of the methylene group] or a salt thereof, or a hydrate thereof.

Abstract: The invention relates to a method for the diagnosis of non-alcoholic steatohepatitis (NASH), for determining the activity, the stage, or the severity of NASH or for classifying a subject as a potential receiver or non receiver of a treatment of NASH using circulating miRNAs and other blood circulating markers of liver damage, e.g. alpha 2 macroglobulin, HbA1c, N-terminal pro-peptide of collagen type III, miR-34 and miR-200. It also relates to a kit for implementing the method of the invention, and the compounds for use in a method for the treatment of NASH, wherein the subject to be treated is identified, evaluated or classified according to the method of the invention.

Abstract: The disclosure relates to a dosage forms and combinations of dosage forms useful for effective oral administration of drugs which are otherwise unsuitable for oral administration, owing to acid- and/or protease-mediated degradation. The dosage forms include a self-microemulsifying drug delivery system (SMEDDS) with which the drug is combined and an antacid. When co-administered to a mammal, the dosage form(s) can prevent drug degradation by the strong acid and digestive enzymes normally present in the gastric environment, and can improve water-soluble drug absorption in gastrointestinal (GI) tract. The dosage forms can be used to effectively administer insulin by an oral route, for example, such as in the form of a powder that can be stored for long periods and reconstituted with water or another fluid shortly before administration.

Abstract: The application relates to an aqueous pharmaceutical formulation for use in the treatment of Type I or Type II Diabetes Mellitus, wherein the treatment reduces the risk of nocturnal hypoglycemia, said formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine, with the proviso that the concentration of said formulation is not 684 U/mL of insulin glargine.

Abstract: Provided herein are liquid pharmaceutical formulations comprising exendin (9-39) or a pharmaceutically acceptable salt thereof and a tonicity modifier in a physiologically acceptable buffer having a pH in the range of about 5 to about 6. In some embodiments, the buffered liquid formulation comprises exendin (9-39) or a pharmaceutically acceptable salt thereof in an acetate buffer or a citrate buffer. Methods of treating or preventing hyperinsulinemic hypoglycemia in a subject comprising administering to the subject the buffered liquid formulation are also provided.

Abstract: Disclosed herein is a method to evaluate the stability of a protein-based formulation including a protein, a peptide and/or a protein derivative and a buffer relative to a lubricant of a lubricated container in which the formulation is intended to be stored, including: a) Evaluating a decrease over time of interfacial tension between the buffer and the lubricant, b) Evaluating a decrease over time of interfacial tension between the protein-based formulation and the lubricant, c) Identifying at least one component of the protein-based formulation interacting with the lubricant by comparing the decrease evaluated in step b) with the decrease evaluated in step a).

Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.

Abstract: A pharmaceutically acceptable insulin premix formulation contains about 0.1-10.0 Unit/mL of insulin for intravenous administration and preferably further contains a tonicity adjuster. The methods for making and using such formulation are also provided. The pharmaceutically acceptable insulin premix formulation may be aseptically filled into a flexible container assembly to form a pharmaceutical insulin premix product. The insulin premix product can be a sterile and ready-to-use aqueous solution for glycemic control in an individual with metabolic disorders through intravenous infusion. The insulin premix product is unexpectedly stable when freshly prepared and also during its shelf-life of storage at refrigeration temperatures of 2° C. to 5° C. for 24 months followed by additional 30 days at room temperatures of 23° C. to 27° C., even without any added preservative, any added zinc, any added surfactant or any other added stabilizing excipient.

Abstract: This invention relates to pharmaceutical formulations comprising 1-(2-thien-2?-yl-2-oxo-ethyl)-3-(methanesulfonyl hydrazine carbonyl) pyridinium, its pharmaceutically acceptable salts, salt-cocrystals and co-crystals, particularly 1-(2-thien-2?-yl-2-oxo-ethyl)-3-5(methanesulfonyl hydrazine carbonyl) pyridinium chloride. The formulations are suitable for oral administration and also comprise a permeability enhancer or a suitable base or a mixture thereof. The formulations of this invention are for treating diseases associated with advanced glycation end products.

Abstract: The present invention is in the field of pharmaceutical compositions for the treatment of medical conditions relating to diabetes. More specifically the invention provides pharmaceutical compositions comprising a long-acting acylated derivative of a human insulin analogue, and to the medical use of such compositions for basal insulin administration therapy.

Abstract: The instant disclosure provides a microscale method for providing correctly folded, and assembled biologically active proteins in an efficient and shorted time frame, compared to conventional protein production techniques. Proteins produced from inclusion bodies and other aggregated protein sources are provided. Microscale production of correctly folded and assembled class I MHC protein and complexes thereof are also provided for, as well as for high throughput production for use in epitope discovery protocols. Microscale production of complex proteins from protein aggregates and preparations containing protein aggregates is provided that requires less than 24 hours of processing time.

Abstract: The invention encompasses therapeutic formulations comprising a protein active ingredient and a stabilizing excipient, methods of improving stability in a therapeutic formulation comprising a protein active ingredient by adding a stability-improving amount of a stabilizing excipient to the therapeutic formulation, and methods of reducing adverse infusion-related effects in a patient, comprising administering to a patient in need thereof a therapeutic formulation comprising a protein active ingredient and a stabilizing excipient.

Abstract: The present invention relates to a certain DPP-4 inhibitor for use in combination with metformin in CKD patients.

Abstract: The application relates to an aqueous pharmaceutical formulation for use in the treatment of Type I or Type II Diabetes Mellitus, wherein the treatment reduces the risk of nocturnal hypoglycemia, said formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine, with the proviso that the concentration of said formulation is not 684 U/mL of insulin glargine.

Abstract: A method of reducing hair loss (alopecia) in a patient undergoing or scheduled to undergo chemotherapy is claimed. The method involves administering brimonidine or a pharmaceutically acceptable salt thereof to the site of the hair follicles.

Abstract: Methods useful for reducing or preventing non-alcoholic steatohepatitis or hepatic steatosis are provided herein. Such methods may comprise administering to a subject in need thereof a sirtuin pathway activator and/or PDE5 inhibitor alone or in combination with an amount of a branched amino acid in free amino acid form, or a metabolite thereof. Also provided herein are compositions and kits for practicing any of the methods described herein.

Abstract: A composition, in the form of an aqueous solution, including insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure and at least one polyanionic compound other than the substituted anionic compound.

Abstract: Methods for treating type one diabetes mellitus in a subject in need thereof and pharmaceutical compositions for the treatment of type one diabetes mellitus are disclosed, including combination therapies with insulin. The methods include administering an effective amount of apolipoprotein A-IV to the subject having type I diabetes. The pharmaceutical composition includes apolipoprotein A-IV formulated for administration to a subject for the treatment of type one diabetes mellitus.

Abstract: The invention relates to the compounds and compositions of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprises a salt of metformin and the methods for treating or preventing metabolic syndrome, prediabetes and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.

Abstract: Described herein are compounds comprising modified oligonucleotides that are complementary to miR-103 and/or miR-107 and methods of treating diseases and disorders using the compounds.

Abstract: Methods, compositions, and devices for treating restenosis are described. In accord with the invention, a composition containing CTGF and insulin is applied to blood vessels and restenosis is reduced or prevented.

Abstract: The present invention pertains to novel enaminoketones containing a CF3O-group, novel pyrazole-derivatives containing a CF3O group as well as to a novel process for their preparation comprising aminoformylation of CF3O-ketones and cyclization of the obtained CF3O-enaminoketones with hydrazines to trifluoromethoxy pyrazoles.

Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.

Abstract: The present invention relates to a method or composition for glycemic control in a subject, which is effective for treating diabetes mellitus, comprising administering the subject with a pharmaceutical composition comprising a therapeutically effective amount of an aliphatic alcohol having a general formula of CH3(CH2)nCH2OH, wherein n is an integer from 10 to 40, such as tetracosanol, and a pharmaceutically acceptable carrier.

Abstract: Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time.

Abstract: Methods and devices are provided for reducing a diabetic patient's foreign body immune response, including infusion site-loss and/or occlusion. Such foreign body responses are associated with the treatment of the diabetic patient where the treatment requires subcutaneous implantation of a foreign body, such as a cannula or catheter. In certain embodiments of the invention, a response-inhibiting agent is administered to a patient at the site of cannula/catheter insertion, thereby facilitating delivery of insulin to the diabetic patient and mitigating site-loss and/or occlusion over a period of time.

Abstract: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.

Abstract: A transdermal delivery device in the form of a transdermal delivery patch for the delivery of insulin is disclosed. The patch comprises cross-linked amidated low methoxy pectin, insulin and a transdermal transfer enhancing agent.

Abstract: The present disclosure provides a buffered ophthalmic composition for formulation of topically administrable suspensions useful for treating eye disorders by promoting wound healing, delivery of pharmaceutically active agents, and lubricating the eye. In particular the ophthalmic composition includes a buffer solution compatible with application to a mammalian eye, wherein the buffer provides increased mechanism of action of pharmaceutically active agents as well as therapeutic qualities. The ophthalmic composition exhibits dual therapeutic action to alleviate various eye disorders as it concomitantly treats corneal ulcerations and excessive inflammation which results from various eye injuries.

Abstract: A method treating a patient includes administering a physiologically effective amount of a fibrillation-resistant insulin analogue or a physiologically acceptable salt thereof to the patient. The fibrillation-resistant insulin analogue or a physiologically acceptable salt thereof, contains an insulin A-chain sequence modified at position A8 and an insulin B-chain sequence or an analogue thereof. The fibrillation-resistant insulin analogue may exhibit thermodynamic stability similar to or exceeding that of wild-type human insulin and displays a susceptibility to fibrillation similar to or exceeding that of wild-type human insulin. An insulin analogue may display greater in vitro insulin receptor binding than normal insulin while displaying binding to IGFR less than twice that of normal insulin and less than that of fast-acting insulin analogs.

Abstract: Oral non-steroidal anti inflammatory drugs (NSAIDs) are not an effective treatment of Alzheimer's disease, because the brain dose is too low. Nasal delivery of NSAIDs such as ibuprofen, flurbiprofen, indomethacin, diclofenac, or naproxen, which inhibit the enzymes cyclooxygenase-1 (cox-1) and cox-2, are used to prevent and/or treat Alzheimer's disease, a low grade brain inflammation. The large amount of nasal NSAIDs (e.g., ibuprofen, flurbiprofen, indomethacin, diclofenac, or naproxen) that reaches the brain far exceeds that from an oral dose. Low-molecular-weight lipophilic drugs, such as ibuprofen, naproxen, indomethacin, diclofenac, and flurbiprofen, are readily absorbed into the brain by the intranasal route. Alzheimer's starts in the entorhinal cortex, which is closely connected to the olfactory nerves, and spreads anatomically in a defined pattern. Therefore, a nasal NSAID would readily reach the region of the brain where it acts therapeutically.

Abstract: The present invention relates to modified forms of C-peptide, and methods for their use. In one aspect, the modified forms of C-peptide comprise conjugated C-peptide derivatives which exhibit superior pharmacokinetic and biological activity in vivo.

Abstract: Disclosed are methods of modulating the expression of genes linked to adipocytokine signaling, carbohydrate metabolism, fatty acid metabolism, arachidonic acid metabolism, PPAR signaling, insulin signaling, lipid metabolism, extracellular matrix (ECM)-receptor interaction, or combinations thereof, methods of treating hyperlipidemia, obesity, excessive cholesterol, cardiovascular disease, liver disease, diabetes, or combinations thereof, and methods of stimulating glucose uptake in an animal in need thereof, comprising administering a composition comprising at least one isolated glyceollin to said animal.

Abstract: In one embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. In yet another embodiment of the invention, a pharmaceutical composition for intranasal administration comprises insulin, clioquinol, dimethyl sulfoxide and at least one pharmaceutically acceptable excipient. The pharmaceutical compositions of the invention may be used to treat or prevent a neurodegenerative disorder such as Alzheimer's disease, stroke, Parkinson's disease, multiple sclerosis, spinal cord injuries, and/or traumatic brain injuries and the like, in addition to other systemic and local diseases.

Abstract: An individual at risk for necrotizing enterocolitis and related disorders can be identified by measuring the level of at least one secretor antigen in a biological sample from the individual and comparing the measured level of the at least one secretor antigen to a predetermined value or a predetermined range of values. Among the secretor antigens which can be measured are: the H-1, H-2, Lewisb and Lewisy antigens and derivatives thereof (e.g., a sialylated form of Lewis a, Lewis x, Lewis b, Lewis y; H-1, H-2, Lewis a, Lewis x, Lewis b or Lewis y).

Abstract: The invention relates to a composition for use as a medicament comprising insulin in combination with at least one compound of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof. Another object of the invention concerns a pharmaceutical composition comprising as active ingredients effective amounts of insulin and at least one compound of formula (I), together with pharmaceutically tolerable adjuvants, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with insulin resistance. The invention also relates to a pharmaceutical package comprising insulin in a first dosage unit and at least one compound of formula (I) in a second dosage unit.

Abstract: Disclosed are an aryl glycoside compound as represented by formula I or formula I?, a pharmaceutically acceptable salt thereof, optical isomer thereof or a prodrug thereof. The present invention relates to a method of preparing said aryl glycoside compound and the use thereof. The aryl glycoside compound of the present invention has an excellent ability on inhibit SGLT activity, especially SGLT2 activity, and is diabetes-fighting medicine with great potential.

Abstract: A rapid acting injectable formulation is provided comprising a therapeutic peptide and a vasodilatory agent. The therapeutic peptide has a molecular weight of greater than about 500 Daltons, and the vasodilatory agent is present in an amount effective to increase the absorption of the therapeutic peptide. A method of increasing absorption of a therapeutic peptide by using such a formulation is also provided.

Abstract: The present invention is directed to methods for modulating the Th1 /Th2 cell balance toward anti-inflammatory cytokine producing cells in a subject comprising decreasing the amount, the expression, or the activity of leptin in a subject sufficient to modulate the Th1 /Th2 cell balance toward anti-inflammatory cytokine producing cells. The invention is also directed to methods of treatment of an immune-related disorder in a subject comprising decreasing the amount, the expression, or the activity of leptin in the subject sufficient to treat the immune-related disorder.

Abstract: Disclosed herein are an in situ-forming, bioadhesive hydrogel and the medical uses thereof. Being formed by in situ crosslinking through an enzymatic reaction, the hydrogel has an advantage over conventional bioadhesive hydrogels in terms of biocompatibility. In addition, the in situ-forming bioadhesive hydrogel has excellent biocompatibility and mechanical strength and has excellent tissue adhesiveness thanks to modification with/without dopa derivatives. The hydrogel finds a variety of applications in the biomedical field, including bioadhesives or hemostats, implant substances for tissue regeneration and augmentation, carriers for delivering biologically active materials or drugs, etc.

Abstract: Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time.

Abstract: Human proIslet Peptides (HIP) and HIP analogs and derivatives thereof, derived from or homologous in sequence to the human REG3A protein, chromosome 2p12, are able to induce islet neogenesis from endogenous pancreatic progenitor cells. Human proIslet Peptides are used either alone or in combination with other pharmaceuticals in the treatment of type 1 and type 2 diabetes and other pathologies related to aberrant glucose, carbohydrate, andor lipid metabolism, insulin resistance, overweight, obesity, polycystic ovarian syndrome, eating disorders and the metabolic syndrome.

Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.

Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV(DPP-IV).

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.

Abstract: The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.

Abstract: The disclosure provides for a method for treating a fatty liver disorder in a subject in need thereof, comprising selecting a subject having or suspected of having a fatty liver disease or disorder, wherein the subject is non diabetic, pre-diabetic, mildly diabetic, or has normal or substantially normal biliary tract function; and administering a therapeutically effective amount of a pharmaceutical composition comprising ethyl eicosapentanoate (EPA-E). In some cases EPA-E present may be at least 40% by weight in total of the fatty acids and their derivatives.

Abstract: The present invention is directed to a method of treating a metabolic disorder or key elements of a metabolic disorder such method comprising the use of an agent(s) that increases central dopaminergic activity plus a first-phase insulin secretagouge.

Abstract: The invention relates to peptides of general formula (I): that can reduce or remove bags formed under the eyes, their stereoisomers and racemic or non-racemic mixtures thereof, and the cosmetically or dermopharmaceutically acceptable salts thereof, wherein X is cystenyl, seryl, threonyl or aminobutyryl; R1 is H or alkyl, aryl, aralkyl or acyl group; and R2 is amino, hydroxy or thiol, all of them substituted or non-substituted with aliphatic or cyclic groups. The invention also relates to a method of obtaining, cosmetic or dermopharmaceutical compositions containing them and their use for treating skin, preferably for reducing or removing bags formed under the eyes.