Entries |
Document | Title | Date |
20080200371 | THIAZOLE AND THIADIAZOLE INHIBITORS OF TYROSINE PHOSPHATASES - Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B. | 08-21-2008 |
20080207490 | Glucose Uptake Modulator and Method for Treating Diabetes or Diabetic Complications - The present invention relates to an glucose uptake modulator, a pharmaceutical composition comprising the glucose uptake modulator, and a method of treating a diabetes or diabetic complications in a mammal in need thereof, which comprises administering to said mammal an effecting amount of a glucose uptake modulator. | 08-28-2008 |
20080221018 | Crystalline solid and amorphous forms of (-)- halofenate and methods related thereto - The present invention provides crystalline solid and amorphous forms of (−)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (−)-halofenate. | 09-11-2008 |
20080227690 | PARTICLES FOR INHALATION HAVING RAPID RELEASE PROPERTIES - The invention generally relates to formulations having particles comprising phospholipids, bioactive agent and excipients and the pulmonary delivery thereof. Dry powder inhaled insulin formulations are disclosed. Formulations comprising DPPC, insulin and sodium citrate which are useful in the treatment of diabetes are disclosed. Also, the invention relates to a method of for the pulmonary delivery of a bioactive agent comprising administering to the respiratory tract of a patient in need of treatment, or diagnosis an effective amount of particles comprising a bioactive agent or any combination thereof in association, wherein release of the agent from the administered particles occurs in a rapid fashion. | 09-18-2008 |
20080242593 | HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS - The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes. | 10-02-2008 |
20080242594 | Methods for Promoting Stem Cell Proliferation and Survival - It is disclosed herein that STAT3 phosphorylated at serine 727 is a key regulator of proliferation and survival of stem cells and precursor cells. Methods for increasing the survival and proliferation of stem cells and/or precursor are disclosed herein. In one embodiment, the method includes contacting a mammalian stem cell mammalian precursor cell with a JAK inhibitor, a p38 inhibitor, or both. Methods are also disclosed for increasing the survival and proliferation of neuronal precursor cells in a subject. The method includes administering a therapeutically effective amount of a Notch ligand and a growth factor. Methods are also disclosed for identifying an agent that increases the proliferation of stem cells and/or precursor cells. The method includes contacting a stem cell or a precursor cell with an agent of interest, wherein the stem cell or the precursor cell expresses STAT3; and determining the phosphorylation status of serine 727 of STAT3 in the cell. Phosphorylation of serine 727 indicates that the agent increases the survival and/or proliferation of stem cells and/or precursor cells. An isolated population of cells is disclosed, wherein the cells express nestin and STAT3, wherein serine 727 of STAT3 is phosphorylated. | 10-02-2008 |
20080242595 | Conjugate of insulin and vitamin B12 for oral delivery - Compositions containing a therapeutic peptide covalently linked to Vitamin B | 10-02-2008 |
20080255030 | COMPOSITIONS AND METHODS FOR THE MODULATION OF JNK PROTEINS - The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK1 protein. | 10-16-2008 |
20080255031 | METHOD FOR ENHANCING INSULIN SECRETION - 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. | 10-16-2008 |
20080269108 | Crystalline forms of the Di-Sodium Salt of N-(5-Chlorosalicyloyl)-8-Aminocaprylic Acid - The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same. | 10-30-2008 |
20080269109 | SYSTEM AND METHOD OF RESUSCITATION OF A MAMMAL - The present disclosure provides systems and methods of saving people, organs, and cells from the injurious effects of ischemia and the injurious effects of reperfusion by providing artificial circulation while intentionally reducing for a period of rest the normal externally directed functions of the cells. | 10-30-2008 |
20080274946 | Method and composition for restoration of age related tissue loss in the face or selected areas of the body - A treatment method for restoring of age related tissue loss in the face or selected areas of the body is disclosed which includes injecting an injectable composition containing a growth factor and hyaluronic acid as a carrier into the dermis, the hypodermis, or both, in various areas of the face, or selected areas of the body of a person to stimulate collagen, elastin, or fat cell production, thereby restoring age related tissue loss in the face and selected areas of the body. Further disclosed is an injectable composition for restoring of age related tissue loss in the face and selected areas of the body, which contains a growth factor and hyaluronic acid as a carrier for providing time release of the growth factor into tissues. The growth factor can be insulin, insulin-like growth factor, thyroid hormone, fibroblast growth factor, estrogen, retinoic acid, or their combinations. | 11-06-2008 |
20080287343 | METHOD FOR REDUCING CARDIOVASCULAR MORBIDITY AND MORTALITY IN PREDIABETIC PATIENTS AND PATIENTS WITH TYPE 2 DIABETES - This invention relates to a method of reducing cardiovascular morbidity and mortality in a prediabetic or Type 2 Diabetes patient population. The method comprises administering an effective dosage of a long acting insulin, preferably insulin glargine, to a prediabetic or Type 2 Diabetes patient. | 11-20-2008 |
20080287344 | Use of Amino Acids for Making Medicines for Treating Insulin Resistance - The invention concerns the use of monohydroxy or polyhydroxy amino acids, and the lactone forms thereof for making medicines with insulin-analogue and/or insulin-sensitizing effects on peripheral tissues targeted by insulin, and more particularly the use thereof for making medicines for treating and preventing insulin-resistance. | 11-20-2008 |
20080300170 | Compositions and methods for diagnosis and treatment for type 2 diabetes - The present invention relates generally to the identification of biological markers associated with an increased risk of developing Diabetes, as well as methods of using such biological markers in diagnosis and prognosis of Diabetes. The biological markers of the invention may indicate new targets for therapy or constitute new therapeutics for the treatment or prevention of Diabetes. | 12-04-2008 |
20080305989 | Transdermal delivery peptides and method of use thereof - Transdermal delivery peptides for the treatment of skin diseases and/or facilitation or enhancement of transdermal delivery of pharmaceutically active agents are provided. Compositions comprising the transdermal delivery peptides and methods of therapeutic use, including the improvement of transdermal delivery of drugs or other pharmaceutically active agents, are also disclosed. Nucleic acids, expression vectors, and methods of their use, which encode the transdermal delivery peptides are disclosed. Methods are also provided for in vivo phage display for identifying further peptides with enhanced transdermal delivery capability. | 12-11-2008 |
20080312135 | MIXTURES OF DRUG-OLIGOMER CONJUGATES COMPRISING POLYETHYLENE GLYCOL, USES THEREOF, AND METHODS OF MAKING SAME - A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates. | 12-18-2008 |
20090023630 | Methods and Means for Use in Diagnostics and Treatment of Diabetes - The present invention identified novel epitopes from the insulin B chain which is embodied in methods and means for diagnostics and treatment of type 1 diabetes. The epitopes were found in a peptide comprising a fragment of the human insulin B chain. Using HLA-A2 tetramers having the peptide of the invention cytotoxic T-cells were found in peripheral blood cells samples from healthy individuals. The invention demonstrates that these autoreactive CTL directed against insulin B chain are able to destroy insulin producing beta-cells. Moreover, a significant proportion of cytotoxic T-cells from islet transplant recipients with recurrent autoimmunity and loss of insulin production recognized this peptide or analogue thereof. The peptide has a high affinity for the HLA-A2 allele, in particular HLA-A*0201. Based on the novel epitopes according to the invention, diagnostic and therapeutic methods and medicaments for the prevention or treatment of type 1 diabetes are provided. | 01-22-2009 |
20090023631 | Composition and Method of Use for Soft Tissue Augmentation/Drug Delivery - A composition for augmenting soft tissue and drug delivery is provided. The composition includes an active ingredient, a carrier, and a cross-linking agent, wherein the carrier is cross-linked with the cross-linking agent and the active ingredient is combined with the cross-linked carrier into a combination having a therapeutic effect. Techniques are also provided for producing a composition for augmenting soft tissue. Also, techniques are provided for soft tissue augmentation. Additionally, techniques are also provided for delivering a composition. | 01-22-2009 |
20090036353 | Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers - Insulin conjugated with structurally well defined, bifurcated and trifurcated polymers can be use by pulmonary delivery for systemic absorption through the lungs to reduce or eliminate the need for administering other insulins by injection. | 02-05-2009 |
20090036354 | CARRIER COMPRISING ONE OR MORE DI AND/OR MONO-(ELECTRON TRANSFER AGENT) PHOSPHATE DERIVATIVES OR COMPLEXES THEREOF - The invention relates to a carrier for administering biologically active compounds comprising one or more C | 02-05-2009 |
20090048152 | Systems and Methods for Glycemic Control During Pump Disconnection - Techniques and devices are described for allowing a diabetes patient to safely disconnect an insulin infusion system device for a time period. In one aspect, the techniques and devices can be implemented by receiving a maximum glucose amount, a minimum glucose amount, and a contemplated disconnection time; receiving a current glucose amount of the user; determining an expected increase in glucose of the user based on the contemplated disconnection time, an insulin sensitivity of the user and a contemplated basal insulin dose; validating the contemplated disconnection time based on at least one of the expected increase in glucose, the maximum glucose amount, and the minimum glucose amount; and, administering a therapeutic action to the user based on the validation of the contemplated disconnection time. | 02-19-2009 |
20090054302 | Methods and Preparations For Curing Clinically Ill Patients - This invention relates to a life saving medicament for critically ill patients and a method of treatment. The composition is a pharmaceutically effective amount of a blood glucose regulator which is used to control the blood glucose level. | 02-26-2009 |
20090062180 | Glycogen synthase kinase-3 inhibitors - Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed. | 03-05-2009 |
20090069215 | Acylated Single Chain Insulin - The invention is related to an acylated, single-chain insulin comprising the B- and the A-chain of human insulin or an analogue thereof connected by a connecting peptide, wherein a lysine residue being substituted for the natural amino acid residue in at least one of the positions B20, B21 or B22 in the human insulin B-chain is chemically modified by acylation. | 03-12-2009 |
20090075863 | Periosteal Tissue Grafts - This document relates to methods and materials involved in making and using periosteal tissue grafts in vivo. For example, materials and methods for obtaining grafts comprising periosteal tissue are provided. | 03-19-2009 |
20090082255 | Acidic Insulin Preparations Having Improved Stability - The invention relates to a pharmaceutical formulation comprising a polypeptide selected from the group consisting of insulin, an insulin metabolite, an insulin analog, an insulin derivative and combinations thereof; a surfactant or combinations of two or more surfactants; optionally a preservative or combinations of two or more preservatives; and optionally an isotonicizing agent, buffers or further excipients or combinations thereof, the pharmaceutical formulation having a pH in the acidic range. | 03-26-2009 |
20090088367 | Treatment of Insulin Resistance/Metabolic Syndrome to Alleviate the Risks of Dementia - This invention relates to Applicant's discovery that Metabolic Syndrome, a cluster of disorders stemming from a resistance to insulin, contributes directly to dementia, particularly Alzheimer's disease. Applicant's invention includes a screening method to determine susceptibility and diagnosis of dementia based on the risk factors for Metabolic Syndrome. Applicant's invention further includes methods for the prevention or treatment of dementia and other neurological conditions based on (1) minimizing insulin resistance, thereby preventing excess biosynthesis of insulin; (2) modulating the activity of IDE such that insulin competes less efficiently with β-amyloid protein for the IDE; and (3) blocking the consequences of NMDA receptor activation, such as by minimizing the generation of NO and other harmful free radicals. | 04-02-2009 |
20090099064 | Derivatized insulin oligomers - The present invention provides oligomers of phosphorylated insulin and formulations thereof. The oligomeric derivatives of the invention exhibit pharmacodynamic properties that are significantly improved over native insulin or other intermediate-acting or basal insulins, for example NPH, Lantus or Detemir, in that they demonstrate a 4-fold higher therapeutic index and a 4-fold lower risk of hypoglycemia. The invention provides the advantage of protracted glycemic lowering and combines it with the advantage of reduced hypoglycaemic risk. The above is not a property of any presently-known or available basal or intermediate-acting insulin. In a further embodiment of the invention, formulations of oligomeric phosphorylated insulin are suitable for all routes of administration including inhalation, buccal absorption, subcutaneous injection, infusion or other technically proven routes for insulin administration. The invention additionally provides the advantage of a longer-acting formulation for inhalation between meals and at bedtime. Such longer-acting inhalable formulations are not presently available. | 04-16-2009 |
20090099065 | Acylated Single Chain Insulin - The invention is related to an acylated, single-chain insulin comprising the B- and the A-chain of human insulin or an analogue thereof connected by a connecting peptide, wherein a lysine residue being substituted for the natural amino acid residue in one of the positions A12-A23 in the human insulin A-chain has been chemically modified by acylation. | 04-16-2009 |
20090105121 | Insulin Derivative - The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. | 04-23-2009 |
20090137454 | Insulin Derivatives - The present invention is related to insulin derivatives having a side chain attached to an ε-amino group of a Lys residue present in the A-chain or to an ε-amino group of a Lys residue in the B-chain. | 05-28-2009 |
20090137455 | RAPID ACTING AND LONG ACTING INSULIN COMBINATION FORMULATIONS - An injectable formulation containing a combination of a rapid acting insulin and a long acting insulin has been developed wherein the pH of the rapid acting insulin is adjusted so that the long acting insulin, e.g. insulin glargine, remains soluble when they are mixed together. In the preferred embodiment, this injectable basal bolus insulin is administered before breakfast, provides adequate bolus insulin levels to cover the meal, does not produce hypoglycemia after the meal and provides adequate basal insulin for up to 24 hours. Lunch and dinner can be covered by two bolus injections of a fast acting, or a rapid acting or a very rapid acting insulin. Alternatively, through adjustment of the ratio of rapid acting insulin to long acting insulin, the long acting insulin may be shortened to a 12 hour formulation. This rapid and long acting blend is re-administered to the patient at dinner time, providing a safe and effective basal insulin level until morning. As a result, a patient using intensive insulin therapy should only inject three, rather than four, times a day. | 05-28-2009 |
20090156463 | Photokinetic delivery of biologically active substances using pulsed incoherent light - The invention relates generally to transdermal and transmembrane delivery of biologically active substances through the skin, sub-dermal tissues, blood vessels and cellular membranes without causing damage to the cellular surface, tissue or membrane. The invention provides compositions and methods for enhanced transdermal and transmembrane delivery of biologically active substances using pulsed incoherent light. The invention further provides a device for the application of the pulsed incoherent light to cellular surfaces and membranes using those compositions and methods. | 06-18-2009 |
20090156464 | Pharmaceutical Compositions and Methods for Insulin Treatment - Compositions and methods for treating a patient with insulin that combines insulin, a permeation enhancer, and a carrier that maintains an acidic pH, are disclosed. | 06-18-2009 |
20090176691 | Pharmaceutical Compositions Containing at Least One Protein Active Ingredient Protected From Digestive Enzymes - The present invention relates to pharmaceutical compositions containing at least one protein active ingredient protected from digestive enzymes. Said pharmaceutical compositions contain said at least one protein active ingredient, in free form, as well as, for liquids, a system that buffers them to a pH greater than 4 and less than or equal to 8 or, for solids, a system that exerts, when they are placed in a liquid medium, a buffer effect between a pH greater than 4 and a pH less than or equal to 8. | 07-09-2009 |
20090186807 | Zinc-free and low-zinc insulin preparations having improved stability - The invention relates to a formulation comprising a polypeptide selected from at least one of insulin, an insulin metabolite, an insulin analog, and an insulin derivative; at least one surfactant; optionally at least one preservative; and optionally at least one of an isotonicizing agent, a buffer or an excipient, wherein the formulation is free from or low in zinc. The invention also relates to the production of such insulin preparations and their use as pharmaceutical formulations. | 07-23-2009 |
20090192073 | METHOD FOR PRODUCING INSULIN ANALOGS HAVING A DIBASIC B CHAIN TERMINUS - The invention relates to a method for producing a type of insulin by genetically engineering a precursor thereof and converting said precursor to the respective insulin in an enzyme-catalyzed ligation reaction with lysine amide or arginine amide, or by lysine or arginine which is modified by protective groups, and optionally subsequent hydrolysis. | 07-30-2009 |
20090203576 | METHODS AND COMPOSITONS FOR PULMONARY DELIVERY OF INSULIN - Systemic delivery of insulin to a mammalian host is accomplished by inhalation of a dry powder of insulin. It has been found that dry insulin powders are rapidly absorbed through the alveolar regions of the lungs. | 08-13-2009 |
20090239784 | Stablised Insulin Compositions - The present invention relates to human insulin analogues having a fast onset of action. These analogues may have amino acid in position B26 substituted with Phe, or be Des(B30) analogues of human insulin. The invention also relates to compositions comprising such insulin analogues, and to compositions comprising a mixture of an insulin analogue having a fast onset of action and insulin having a protracted action. | 09-24-2009 |
20090258817 | ARYLSULFANYL COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS - Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are also provided. | 10-15-2009 |
20090258818 | Compositions For the Treatment of Diabetes - A supramolecular insulin assembly and supramolecular exendin-4 assembly, which is useful as a protein therapeutic agent for the treatment of metabolic disorders particularly diabetes. The supramolecular assemblies disclosed in the present invention consists of insoluble and aggregated oligomers the protein. The invention also provides pharmaceutical compositions comprising the supramolecular assembly. | 10-15-2009 |
20090264336 | HETEROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES - Compounds of formula (I) | 10-22-2009 |
20090264337 | Cellular GPRS-communication linked glucometer - pedometer - The Cellular GPRS system includes a cellular-based Glucometer (CBG) for blood glucose monitoring, a pedometer for exertion measurement, combined with user-entered dietary or other diabetes-relevant information. Data from all inputs is transmitted over a cellular network, using a GPRS or other wireless link. The data is preferably stored in the device prior to being transmitted wirelessly over the cellular airway to a central computer server. The remote computer server will evaluate the data received and respond with a data packet (making recommendations on further glucose measurement, exercise, diet, insulin requirements or other). | 10-22-2009 |
20090281020 | Pharmaceutical Compositions Comprising Dextran With A Molecular Weight Of 1.0-100 KDA And Processes For Their Preparation - A solid or semisolid implant obtainable by providing a liquid composition comprising an aqueous solution of dextran with molecular weight of 1.0-100 kDa and introducing the liquid composition into the body of a mammal, whereby the implant is formed in situ in the body of the mammal. A process for preparing a composition useful for biomedical application, comprising the steps of providing a liquid composition comprising an aqueous solution of dextran having a molecular weight of 1-100 kDa; and bringing the liquid composition to solidify; whereby water is gradually eliminated from the liquid composition during the solidification. A biomedical article prepared from the composition. | 11-12-2009 |
20090286715 | Pharmaceutical Composition - A pharmaceutical composition comprising: (A) a continuous liquid phase; (B) liquid droplets dispersed in said continuous phase; (C) a pharmaceutically-active compound; (D) an enhancer as described in U.S. Pat. No. 5,023,252; and (E) a hydrocolloid emulsifying agent; including, for example, a composition in which the liquid phase comprises an aqueous solution of insulin and the liquid droplets comprise a solution of the enhancer and a solvent therefore; and the use of the composition to treat a condition for example diabetes in a patient by applying to the membrane of the patient the composition. | 11-19-2009 |
20090298744 | HETEROCYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST - Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. | 12-03-2009 |
20090312235 | Method for producing insulin in the form of an oral preparation - The invention belongs to pharmacology and medicine, particularly, to endocrinology. | 12-17-2009 |
20090312236 | PEGYLATED INSULIN LISPRO COMPOUNDS - The present invention relates to the field of diabetes. More particularly, the invention relates to PEGylated insulin lispro compounds that are PEGylated with high molecular weight poly(ethylene glycol), are highly soluble at physiological pH, have an extended duration of action, and characterized by pharmacokinetic, pharmacodynamic, and/or activity peak-trough ratios of less than 2. The invention also relates to methods of providing such molecules, to pharmaceutical compositions containing them, and to their therapeutic uses. | 12-17-2009 |
20090325860 | COMPOSITIONS FOR INTRANASAL DELIVERY OF HUMAN INSULIN AND USES THEREOF - What is described is a pharmaceutical formulation for intranasal delivery of insulin to a patient, comprising an aqueous mixture of human insulin, a solubilizing agent, a surface active agent, and a thickening agent, wherein said formulation provides a ultra-rapid acting profile to regular human insulin. | 12-31-2009 |
20100004158 | GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. (I) | 01-07-2010 |
20100009898 | PROTEASE RESISTANT INSULIN ANALOGUES - The present invention relates to novel insulin analogues exhibiting resistance towards protease, wherein at least two amino acids are substituted and/or deleted relative to the parent insulin molecule. A method for the preparation of such insulin analogues, insulin preparations containing the insulin analogues of the invention and a method of treating diabetes mellitus using these insulin analogues is also provided. | 01-14-2010 |
20100009899 | Novel Insulin Derivatives - The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have a side chain attached either to the α-amino group of the N-terminal amino acid residue of the B chain or to the ε-amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula: | 01-14-2010 |
20100022441 | N-TERMINAL POLYSIALYLATION - The present invention relates to a composition comprising a population of polysaccharide derivatives of a protein, wherein the protein is insulin or an insulin-like protein and the polysaccharide is anionic and comprises between 2 and 125 saccharide units, and wherein the population consists of substantially only N-terminal derivatives of the protein. Typically, the polysaccharide is PSA. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds. | 01-28-2010 |
20100029544 | Composition - Novel polyallylamine (PAA) based graft polymers are provided, including groups such as cholesteryl, cetyl, palmitoyl, which are adapted to deliver an entity that is normally of poor solubility in an aqueous medium, said entity being such as a drug, peptide, protein, or polynucleotide that is releasably contained within the said polymer, the resulting complex being of nanoparticle range sizes with a T | 02-04-2010 |
20100029545 | BORONIC ACID-CONTAINING BLOCK COPOLYMERS FOR CONTROLLED DRUG DELIVERY - Polymeric nanoaggregate drug-delivery compositions including boron-containing copolymers are described. The drug-delivery compositions may further include a therapeutic agent comprising a nucleic acid, a polynucletide, a peptide, a polypeptide, a protein, a pharmaceutical or any combinations thereof. Methods for making the polymeric nanoaggregate compositions including at least one therapeutic agent (for example, insulin) as well as methods for administration of these compositions to mammals are also set forth. The disclosure also describes compositions and methods for controlled drug delivery. Further, polymeric nanoaggregate boron-containing compositions including insulin and methods for monitoring and regulating blood glucose levels of a mammal are also described. The disclosure also describes methods for treatment and/or control of diabetes mellitus by administering polymeric nanoaggregate boron-containing compositions including insulin to a mammal in need. | 02-04-2010 |
20100035794 | USE OF ULTRARAPID ACTING INSULIN - Disclosed herein are improved methods of treating hyperglycemia with a combination of an ultrarapid acting insulin and insulin glargine comprising prandial administration of the ultrarapid insulin, and administration of a first dose of insulin glargine within 6 hours of waking for a day. | 02-11-2010 |
20100035795 | USE OF ULTRARAPID ACTING INSULIN - Disclosed herein are improved methods of treating hyperglycemia with a combination of an ultrarapid acting insulin and insulin glargine comprising prandial administration of the ultrarapid insulin, and administration of a first dose of insulin glargine within 6 hours of waking for a day. | 02-11-2010 |
20100048453 | OXAZOLE AND THIAZOLE PPAR MODULATOR - The invention provides compounds (I) pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPARδ. | 02-25-2010 |
20100056425 | Absorption enhancers such as E.G. BHT, BHA or propyl gallate - The invention provides a pharmaceutical composition comprising a mixture of (a) an active macromolecular principle, and (b) an aromatic alcohol absorption enhancer chosen from butylated hydroxy toluene, butylated hydroxy anisole and analogues and derivatives thereof, wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active macromolecular principle, and further comprises a pharmaceutical composition comprising a mixture of (a) an active macromolecular principle, (b) an aromatic alcohol absorption enhancer chosen from propyl gallate, butylated hydroxy toluene, butylated hydroxy anisole and analogues and derivatives thereof, wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active macromolecular principle, and (c) a solubilisation aid capable of increasing the solubility of the aromatic alcohol absorption enhancer in aqueous media. | 03-04-2010 |
20100062970 | SYNTHESIS OF PROPYL PHENOXY ETHERS AND USE AS DELIVERY AGENTS - The present invention provides propyl phenoxy ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same. The delivery agents of the present invention are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals. | 03-11-2010 |
20100069292 | INSULIN WITH A BASAL RELEASE PROFILE - A clear basal insulin formulation composed of insulin (preferably human recombinant insulin), buffering agents, precipitating agents, and/or stabilizing agents for subcutaneous, intradermal or intramuscular administration. The formulation is designed to form a precipitate of insulin following injection, creating a slow releasing “basal insulin” over a period of 12 to 24 hours, which can be varied by compositional changes to tailor the release profile to the needs of the individual diabetic patient | 03-18-2010 |
20100069293 | POLYMERIC CARRIER COMPOSITIONS FOR DELIVERY OF ACTIVE AGENTS, METHODS OF MAKING AND USING THE SAME - In part, the present invention is directed to compositions and methods of making compositions comprising a polymeric backbone, a chelating group, a metal ion, and an active agent with a metal binding domain. The compositions can optionally further comprise protective groups. In part, the present invention is directed to prolonging the blood circulation time of an active agent containing a metal binding domain by using a composition comprising a polymeric backbone with a protective group, a chelator, and a metal ion. | 03-18-2010 |
20100087360 | Heterocycle-substituted benzimidazole derivative - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X | 04-08-2010 |
20100093603 | USE OF ORGANIC COMPOUNDS - The invention relates to the use of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with one or more active ingredient, for the manufacture of a medicament for the treatment of diabetic cardiomyopathy. | 04-15-2010 |
20100099601 | FIBRILLATION-RESISTANT INSULIN AND INSULIN ANALOGUES - A fibrillation-resistant insulin analogue may be a single-chain insulin analogue or a physiologically acceptable salt thereof, containing an insulin A chain sequence or an analogue thereof and an insulin B chain sequence or an analogue thereof connected by a polypeptide of 4-10 amino acids. The fibrillation-resistant insulin analogue preferably displays less than 1 percent fibrillation with incubation at 37° C. for at least 21 days. A single-chain insulin analogue displays greater in vitro insulin receptor binding than normal insulin while displaying less than or equal binding to IGFR than normal insulin. The fibrillation-resistant insulin may be used to treat a patient using an implantable or external insulin pump, due to its greater fibrillation resistance. | 04-22-2010 |
20100105603 | Methods and Preparations For Curing Clinically Ill Patients - This invention relates to a life saving medicament for critically ill patients and a method of treatment. The composition is a pharmaceutically effective amount of a blood glucose regulator which is used to control the blood glucose level. | 04-29-2010 |
20100120660 | HIGHLY CONCENTRATED INSULIN SOLUTIONS AND COMPOSITIONS - Highly concentrated insulin solutions and pharmaceutical compositions are described as are methods of their preparation and uses thereof. | 05-13-2010 |
20100120661 | HETEROCYCLIC BORONIC ACID COMPOUNDS - Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH | 05-13-2010 |
20100130402 | Biomarkers for insulin resistance and beta-cell dysfunction - The invention provides compositions and methods for determining insulin resistance and/or pancreatic β-cell dysfunction in a subject. The invention also provides compositions and methods for treating a subject according to the insulin resistance and/or pancreatic β-cell dysfunction in the subject. | 05-27-2010 |
20100137188 | FORMULATIONS COMPRISING CYCLIC COMPOUNDS - This invention relates to the use of a cyclic compound of formula (I) | 06-03-2010 |
20100144591 | BENZIMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IGT) in a patient. | 06-10-2010 |
20100144592 | Stable Non-Aqueous Pharmaceutical Compositions - The present invention relates to shelf stable non-aqueous pharmaceutical compositions, and to the use thereof in methods of treating diabetes and hyperglycaemia, comprising dehydrated active polypeptide comprising 10-100 amino acids and at least one semi-polar protic organic solvent. | 06-10-2010 |
20100144593 | Pharmaceutical Compositions and Methods for Insulin Treatment - Compositions and methods for treating a patient with insulin that combines insulin, a permeation enhancer, and a carrier that maintains an acidic pH, are disclosed. | 06-10-2010 |
20100160209 | Composition and Method for Increasing Cell Permeability of a Compound - The invention provides for a cell permeable peptide conjugated to an insulin compound for improved cell penetration of the insulin moiety. The composition may be delivered by intravenous, intramuscular, subcutaneous, intranasal, oral inhalation, intrarectal, intravaginal or intraperitoneal means for the treatment, including prophylaxis of Type I, Type II diabetes, prediabetes and/or metabolic syndrome. | 06-24-2010 |
20100167984 | Complex between human insulin and an amphiphilic polymer and use of this complex in the preparation of a fast-acting human insulin formulation - The invention relates to a complex between human insulin and an amphiphilic polymer comprising carboxyl functional groups, said amphiphilic polymer being chosen from functionalized polysaccharides predominantly composed of glycoside monomers bonded via glycoside bonds of (1,6) type which are functionalized by at least one tryptophan derivative. | 07-01-2010 |
20100167985 | ORAL INSULIN COMPOSITION AND METHODS OF MAKING AND USING THEREOF - A method of lowering blood glucose in a mammal includes orally administering a therapeutically effective amount of crystallized dextran microparticles and insulin to the mammal to lower blood glucose of the mammal. The composition may be a one phase or a structured multi-phase composition for controlled release of insulin. | 07-01-2010 |
20100173824 | Azepinoindole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 07-08-2010 |
20100179090 | METHOD FOR DRYING A PROTEIN COMPOSITION, A DRIED PROTEIN COMPOSITION AND A PHARMACEUTICAL COMPOSITION COMPRISING THE DRIED PROTEIN - The present invention relates to a method for spray-drying of protein solutions and the spray-dried protein product. The invention also relates to pharmaceutical compositions containing such spray-dried protein, to methods of treating diabetes and hyperglycaemia using the spray-dried protein of the invention and to the use of such spray-dried protein in the treatment of diabetes and hyperglycaemia. | 07-15-2010 |
20100184640 | DOG DIABETES - A method a method for diagnosing susceptibility to diabetes in a non-human animal, the method comprising: a) identifying whether or not a polymorphism as defined in Table 4 or a polymorphism which is in linkage disequilibrium with such a polymorphism is present in the genome of the animal; and b) thereby diagnosing whether the animal is susceptible to diabetes, wherein optionally the said identifying is carried out on a sample from the animal. | 07-22-2010 |
20100184641 | Novel Plasma Protein Affinity Tags - Method for increasing half-life of therapeutic agents in plasma and novel polypeptide derivatives. | 07-22-2010 |
20100190686 | NOVEL SECRETED PROTEINS OF ADIPOCYTES FOR DIAGNOSTIC PURPOSES - The present invention relates to the discovery of polypeptide biomarkers excreted into the blood stream (serum or plasma) and/or urine from adipocytes and their use to determine the existence of metabolic syndrome (prediabetic) and/or diabetic conditions (including type 2 diabetes) including insulin resistance and/or glucose intolerance, their use to monitor the state of metabolic syndrome or diabetes toward a state of control and/or cure of the disease state or condition and their use to monitor the long-term health of the patient by determining the existence of metabolic syndrome (prediabetic conditions insulin resistance and/or glucose intolerance) or the existence of type 2 diabetes and to identify potential antidiabetes agents. Methods of identifying potential agents to be used in the treatment of metabolic syndrome and/or type2 diabetes and assays for assisting in the diagnosis of metabolic syndrome and/or type 2 diabetes are additional aspects of the invention. Lipoprotein lipase; Quiescin Q6; Cathepsin B; Complement Component 6; Hippocampal Cholinergic Neurostimulating Protein (HCNP); Serine Protease Inhibitor 2C; Adiponectin; Angiotensinogen (angiotensin); Cyclophilin A; Laminin B1 subunit 1; cartilage glycoprotein 39; complement factor MASP-3 (MASP-3); Niemann-Pick disease, type C2, isoform CRA b (NPC2); Tetranectin; tissue inhibitor of metalloproteinase 2 (TIMP2); Superoxide dismutase secreted; and Spondin 1 | 07-29-2010 |
20100197564 | DIARYL MORPHOLINES AS CB1 MODULATORS - The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions. | 08-05-2010 |
20100197565 | Dry powder drug delivery system - A pulmonary drug delivery system is disclosed, including a breath-powered, dry powder inhaler, and a cartridge for delivering a dry powder formulation. The inhaler and cartridge can be provided with a drug delivery formulation comprising, for example, a diketopiperazine and an active ingredient, including, peptides and proteins such as insulin and glucagon-like peptide 1 for the treatment of endocrine disease, for example, diabetes and/or obesity. | 08-05-2010 |
20100216690 | Pegylated Single-Chain Insulin - The present invention is related to a single-chain insulin comprising the B- and the A-chain of human insulin or analogues thereof connected by a connecting peptide having from 3-35 amino acid residues, wherein the single-chain insulin comprises at least one PEG group attached to at least one lysine residue in the single-chain insulin molecule and/or to the B1 N terminal amino acid residue. The PEGylated single-chain insulins may comprise up to 4 PEG groups which may be the same or different. | 08-26-2010 |
20100216691 | Protease Stabilized, Pegylated Insulin Analogues - Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K. | 08-26-2010 |
20100216692 | Acidic Insulin Preparations Having Improved Stability - The invention relates to a pharmaceutical formulation comprising a polypeptide selected from the group consisting of insulin, an insulin metabolite, an insulin analog, an insulin derivative and combinations thereof; a surfactant or combinations of two or more surfactants; optionally a preservative or combinations of two or more preservatives; and optionally an isotonicizing agent, buffers or further excipients or combinations thereof, the pharmaceutical formulation having a pH in the acidic range. | 08-26-2010 |
20100227795 | INSULIN FORMULATIONS FOR RAPID UPTAKE - Injectable insulin formulations with improved stability and rapid onset of action are described herein. The formulations may be for subcutaneous, intradermal or intramuscular administration. In the preferred embodiment, the formulations are administered via subcutaneous injection. The formulations contain insulin in combination with a chelator and dissolution agent, and optionally additional excipients. In the preferred embodiment, the formulation contains human insulin, a zinc chelator such as EDTA and a dissolution agent such as citric acid or sodium citrate. These formulations are rapidly absorbed into the blood stream when administered by subcutaneous injection. In the preferred embodiment, the insulin is provided as a clear liquid, neutral pH, in a multi-use sterile vial. In an alternative embodiment, the insulin is provided as a powder in a sterile vial. This is mixed with a diluent containing a pharmaceutically acceptable carrier, such as water, a zinc chelator such as EDTA and a dissolution agent such as citric acid shortly before or at the time of administration. In another embodiment, the insulin is stored as a frozen mixture, ready for use upon thawing. | 09-09-2010 |
20100227796 | Insulin Derivatives - The present invention is related to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of B chain or to an ε-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethylenglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH | 09-09-2010 |
20100234273 | LIGHT-ACTIVATED CATION CHANNEL AND USES THEREOF - The present invention provides compositions and methods for light-activated cation channel proteins and their uses within cell membranes and subcellular regions. The invention provides for proteins, nucleic acids, vectors and methods for genetically targeted expression of light-activated cation channels to specific cells or defined cell populations. In particular the invention provides millisecond-timescale temporal control of cation channels using moderate light intensities in cells, cell lines, transgenic animals, and humans. The invention provides for optically generating electrical spikes in nerve cells and other excitable cells useful for driving neuronal networks, drug screening, and therapy. | 09-16-2010 |
20100249020 | Fast-acting insulin formulation - The invention relates to a complex between an insulin and a polysaccharide comprising carboxyl functional groups, said polysaccharide being chosen from polysaccharides functionalized with at least one phenylalanine derivative, noted Phe, said phenylalanine derivative being chosen from the group consisting of phenylalanine and its alkali metal cation salts, phenylalaninol, phenylalaninamide and ethylbenzylamine or from phenylalanine esters, and said insulin being either a human insulin or an insulin analog. The invention also relates to a pharmaceutical composition comprising at least one complex according to the invention, especially in the form of an injectable solution. | 09-30-2010 |