Class / Patent application number | Description | Number of patent applications / Date published |
514600200 | A-chain modified insulin | 39 |
20110059887 | MEAL-TIME INSULIN ANALOGUES OF ENHANCED STABILITY - 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. The fibrillation-resistant insulin may be used to treat a patient by subcutaneous injection or by using an implantable or external insulin pump, due to its fibrillation resistance. | 03-10-2011 |
20110092419 | PROTEASE-STABILIZED INSULIN ANALOGUES - The present invention relates to novel insulin analogues comprising mutations at position A14 in the A chain and at positions B27, B28, B29 and B30 in the B chain and exhibiting resistance towards protease; 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. | 04-21-2011 |
20110144010 | Spontaneously Dispersible Preconcentrates Including a Peptide Drug in a Solid or Semisolid Carrier - The present invention relates to a solid or semi-solid pharmaceutical composition that includes a polypeptide drug, at least one polar organic solvent, at least one surfactant, at least one hydrophilic component and which composition is spontaneously dispersible. | 06-16-2011 |
20110257091 | INSULIN ANALOGS - Full potency analogs of insulin are provided wherein the analog comprises a modification of the tyrosine residue at position 19 of the A chain. | 10-20-2011 |
20110294729 | Novel Insulin Analogues - Insulin analogues wherein the B25 amino acid residue is His or Asn with the proviso that if the B25 amino acid residue is His, then the B27 amino acid residue is Asp or Glu and the A14 amino acid residue is different from Glu, have liver preferential actions. | 12-01-2011 |
20120010134 | SOLUBLE NON-DEPOT INSULIN CONJUGATES AND USES THEREOF - In one aspect, the disclosure provides a conjugate comprising an insulin molecule having an A-chain and a B-chain; an affinity ligand covalently bound to the A-chain; and a monovalent glucose binding agent covalently bound to the B-chain, wherein the affinity ligand competes with glucose for non-covalent binding with the monovalent glucose binding agent. In the absence of glucose, the monovalent glucose binding agent binds the affinity ligand to produce a “closed” inactive form of the insulin molecule. When free glucose is added, it competes with the affinity ligand for binding with the monovalent glucose binding agent to produce an “open” active form of the insulin molecule. The monovalent glucose binding agent and affinity ligand are covalently bound to the insulin molecule. The disclosure also provides methods of using these conjugates and methods of making these conjugates. In another aspect, the disclosure provides exemplary conjugates. The disclosure also provides alternative conjugates that are not necessarily activated by glucose. | 01-12-2012 |
20120021978 | COMBINATION OF AN INSULIN AND A GLP-1-AGONIST - The invention relates to a drug comprising at least one insulin and at least one GLP-1 receptor agonist. | 01-26-2012 |
20120094903 | 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. | 04-19-2012 |
20120122774 | LONG-ACTING FORMULATIONS OF INSULINS - The application relates to an aqueous pharmaceutical formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine. | 05-17-2012 |
20120165251 | Diabetes therapy - The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a DPP-4 inhibitor and a long-acting insulin. The invention further relates to a DPP-4 inhibitor for subcutaneous or transdermal use. | 06-28-2012 |
20120184487 | INSULIN DERIVATIVES - The novel insulin derivates delivers, after administration to humans, insulin as a function of the glucose concentration in the tissue. | 07-19-2012 |
20120184488 | INSULIN ANALOGUES OF ENHANCED RECEPTOR-BINDING SPECIFICITY - A method of treating a patient includes administering a physiologically effective amount of an insulin analogue or a physiologically acceptable salt thereof to the patient. The insulin analogue or physiologically acceptable salt thereof contains an insulin A-chain sequence modified at positions selected from the group consisting of A0, A1, A4, A8, and A21. The insulin analogue may exhibit decreased affinity for the IGF receptor in comparison to wild type insulin of the same species and at least 20% of the affinity of wild-type insulin for the insulin receptor of the same species. Position A0 may be arginine. Position A1 may be D-alanine, D-aspartic acid, or D-leucine. Position A8 may be histidine, lysine, or arginine. Optionally, an insulin B-chain analogue sequence comprises a histidine at position B1. A nucleic acid may encode such an insulin polypeptide. | 07-19-2012 |
20120220522 | ESTER INSULIN - Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include Glu | 08-30-2012 |
20120225811 | INSULIN ANALOGUES - A dicarba analogue of insulin comprising an A-chain and a B-chain or fragments, salts, solvates, derivatives, isomers or tautomers of the A-chain, the B-chain or both, provided that the dicarba analogue is not [A7,B7-(2,7-diaminosuberoyl]-des-(B26-B30)-insulin B25-amide. | 09-06-2012 |
20120232002 | SLOW-ACTING INSULIN PREPARATIONS - Aqueous pharmaceutical formulations with an insulin analog, comprising
| 09-13-2012 |
20120252724 | INSULIN PREPARATIONS CONTAINING METHIONINE - The invention relates to an aqueous pharmaceutical formulation having insulin, an insulin analog, or an insulin derivative, and methionine; and to the production thereof, to the use thereof for treating diabetes mellitus, and to a medication for treating diabetes mellitus. | 10-04-2012 |
20120277149 | PHARMACEUTICAL COMBINATIONS FOR THE TREATMENT OF METABOLIC DISORDERS - The invention relates to a pharmaceutical composition comprising 1.a and/or 1.b according to claim | 11-01-2012 |
20120316107 | 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. | 12-13-2012 |
20130065826 | Injectable solution at pH 7 Comprising at least one basal insulin whose PI is between 5.8 and 8.5 - A composition in the form of an injectable aqueous solution, the pH of which is between 6.0 and 8.0, includes at least a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and a dextran substituted by radicals carrying carboxylate charges and hydrophobic radicals. Single-dose formulations at a pH of between 7 and 7.8 includes a basal insulin whose isoelectric point is between 5.8 and 8.5 and a prandial insulin. | 03-14-2013 |
20130085101 | LONG-ACTING INSULIN ANALOGUE PREPARATIONS IN SOLUBLE AND CRYSTALLINE FORMS - A pharmaceutical formulation comprises an insulin analogue or a physiologically acceptable salt thereof, wherein the insulin analogue or a physiologically acceptable salt thereof contains an insulin A-chain sequence that contains paired Histidine substitutions at A4 and A8, and optionally a substitution at A21. The formulation further contains a pharmaceutically acceptable buffer containing at least about 4 zinc ions per 6 insulin analogue molecules. The formulation forms a long-acting zinc-dependent subcutaneous depot upon subcutaneous injection. In a zinc-free formulation, the insulin analogue monomer exhibits decreased affinity for the Insulin-like Growth Factor receptor and at least 20% of the affinity for the insulin receptor of the same species, in comparison to an otherwise identical insulin or insulin analogue that does not contain the His | 04-04-2013 |
20130096057 | Chemically and Thermodynamically Stable Insulin Analogues and Improved Methods for their Production - The subject matter of this invention is directed towards chemically and thermodynamically stable single-chain insulin (SCI) analogues that are resistant to deamidation and fibrillation. The invention further discloses improved methods for the recombinant expression, purification and refolding of SCI. | 04-18-2013 |
20130123171 | AMIDE-BASED INSULIN PRODRUGS - Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 05-16-2013 |
20130143802 | FUSION PEPTIDE THERAPEUTIC COMPOSITIONS - Therapeutic compositions containing fusion proteins (FPs) including elastin-like peptides (ELPs) and peptide active therapeutic agents, and methods of making and using such compositions and fusion proteins. Therapeutic compositions of such type enable improved efficacy of the peptide active therapeutic agent to be achieved, in relation to the peptide active therapeutic agent alone. Enhanced efficacy of the peptide active therapeutic agent in the therapeutic composition may include improved solubility, bioavailability, bio-unavailability, half-life. etc., as compared to corresponding compositions containing the same peptide active therapeutic agent without associated ELPs. | 06-06-2013 |
20130203665 | SINGLE-CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR - Single chain insulin analogs are provided having high potency and specificity for the insulin receptor. As disclosed herein optimally sized linking moieties can be used to link human insulin A and B chains, or analogs or derivatives thereof, wherein the carboxy terminus of the B25 amino acid of the B chain is linked to the amino terminus of the A1 amino acid of the A chain via the intervening linking moiety. In on embodiment the linking moiety comprises a polyethylene glycol of 6-16 monomer units and in an alternative embodiment the linking moiety comprises a non-native amino acid sequence derived form the IGF-1 C-peptide and comprising at least 8 amino acids and no more than 12 amino acid in length. Also disclosed are prodrug and conjugate derivatives of the single chain insulin analogs. | 08-08-2013 |
20130331320 | FAST-ACTING INSULIN IN COMBINATION WITH LONG-ACTING INSULIN - Insulin preparations comprising a long-acting insulin compound, a fast-acting insulin compound, a nicotinic compound and an amino acid. | 12-12-2013 |
20140107023 | NON-PEPTIDYL POLYMER-INSULIN MULTIMER AND METHOD FOR PRODUCING THE SAME - The present invention relates to a non-peptidyl polymer-insulin multimer comprising two or more of a non-peptidyl polymer-insulin conjugate prepared by linking a non-peptidyl polymer and insulin via a covalent bond, in which the conjugates are complexed with cobalt ion to form a multimer, a method and kit for the preparation of the multimer, a pharmaceutical composition for the prevention or treatment of diabetes comprising the multimer as an active ingredient, and a method for preventing or treating diabetes by administering the composition to a subject. | 04-17-2014 |
20140235537 | N-GLYCOSYLATED INSULIN ANALOGUES - Compositions and formulations comprising N-glycosylated insulin analogues are described. In particular embodiments, the glycosylated insulin analogues are produced in vivo and comprise one or more the N-linked N-glycans selected from high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycans. In other embodiments, the N-glycan comprising the high mannose or fucosylated or non-fucosylated hybrid, paucimannose, or complex N-glycan is attached to the insulin analogue in vitro. Examples of N-glycans include but are not limited to a molecule having a structure selected from N-glycans in the group consisting of Man( | 08-21-2014 |
20140315798 | CHEMICALLY AND THERMODYNAMICALLY STABLE INSULIN ANALOGUES AND IMPROVED METHODS FOR THEIR PRODUCTION - The subject matter of this invention is directed towards chemically and thermodynamically stable single-chain insulin (SCI) analogues that are resistant to deamidation and fibrillation. The invention further discloses improved methods for the recombinant expression, purification and refolding of SCI. | 10-23-2014 |
20140323398 | ULTRA-CONCENTRATED RAPID-ACTING INSULIN ANALOGUE FORMULATIONS - A pharmaceutical formulation comprises insulin having a variant insulin B-chain polypeptide containing an ortho-monofluoro-Phenylalanine substitution at position B24 in combination with a substitution of an amino acid containing an acidic side chain at position B10, allowing the insulin to be present at a concentration of between 0.6 mM and 3.0 mM. The formulation may optionally be devoid of zinc. Amino-acid substitutions at one or more of positions B3, B28, and B29 may additionally be present. The variant B-chain polypeptide may be a portion of a proinsulin analogue or single-chain insulin analogue. The insulin analogue may be an analogue of a mammalian insulin, such as human insulin. A method of lowering the blood sugar of a patient comprises administering a physiologically effective amount of the insulin analogue or a physiologically acceptable salt thereof to the patient. | 10-30-2014 |
20140364362 | THERAPEUTIC AGENTS COMPRISING INSULIN AMINO ACID SEQUENCES - The present invention relates in part to agents which provide slow absorption from an injection site. In some embodiments, the pharmaceutical compositions comprises an insulin amino acid sequence and an amino acid sequence that provide slow absorption from an injection site, such as, for example, an amino acid sequence that has a substantially repeating pattern of proline residues. | 12-11-2014 |
20140371140 | Insulin derivatives Containing Additional Disulfide bonds - The present invention is related to insulin derivatives containing additional disulfide bonds and methods of making such. | 12-18-2014 |
20150299286 | GLUTAMIC ACID-STABILIZED INSULIN ANALOGUES - An insulin analogue comprises a B-chain polypeptide containing the acidic two-residue extension GluB31-GluB32, and optionally an A-chain polypeptide containing acidic substitution GluA8, and additionally optionally a non-standard modification of PheB24. The analogue may also contain additional B-chain substitutions known in the art to enhance the rate of absorption of an insulin analogue formulation following subcutaneous injection or infusion. The analogue may be an analogue of a mammalian insulin, such as human insulin. A nucleic acid encoding such an insulin analogue is also provided. A method of treating a patient comprises administering a physiologically effective amount of the insulin analogue or a physiologically acceptable salt thereof to a patient. The analogue may be administered at a high concentration while maintaining fast-acting properties. A method of semi-synthesis using an unprotected octapeptide by means of modification of an endogenous tryptic site by non-standard amino-acid substitutions. | 10-22-2015 |
20150374795 | O-GLYCOSYLATED CARBOXY TERMINAL PORTION (CTP) PEPTIDE-BASED INSULIN AND INSULIN ANALOGUES - Compositions and formulations comprising insulin or insulin analogues comprising a carboxy terminal portion (CTP) peptide comprising amino acids 112-188 to 142 of the beta subunit of human chorionic gonadotropin (hCGβ) or a partial variant thereof that includes at least one O-glycosylation site of the CTP peptide, wherein the CTP peptide of the CTP peptide-based insulin or insulin analogue is O-glycosylated are described. In particular embodiments, the O-glycosylated insulin analogues are produced in vivo and in further embodiments, the O-glycosylated CTP-based insulin analogues comprise predominantly mannotriose and mannotetrose O-glycans or predominantly mannose O-glycans. | 12-31-2015 |
20160030521 | THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistance in the body, solubility, and bioavailability. | 02-04-2016 |
20160083448 | SITE 2 INSULIN ANALOGUES - An insulin analogue contains one or more modifications at a distinct protein surface comprising one or more of the residues at position B13, B17, A12, A13, and/or A17. Formulations of the above analogues at successive strengths U-100 to U-1000 in soluble solutions a at least pH value in the range 6.8-8.0 either in the presence of zinc ions at a molar ratio of 2.2-10 zinc ions per six insulin analogue monomers or in the presence of fewer than 1 zinc ions per six insulin analogue monomers. Use of the above formulation in an insulin pump functionally integrated with a continuous glucose monitor and computer-based control algorithm as a closed-loop system. A method of treating a patient with diabetes mellitus comprises administering a physiologically effective amount of the insulin analogue to a patient by means of intravenous, intraperitoneal, or subcutaneous injection. | 03-24-2016 |
20160120952 | THERAPEUTIC AGENTS COMPRISING ELASTIN-LIKE PEPTIDES - The present invention provides therapeutic agents and compositions comprising elastin-like peptides (ELPs) and therapeutic proteins. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist, insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistance in the body, solubility, and bioavailability. | 05-05-2016 |
20160166653 | CHEMICALLY AND THERMODYNAMICALLY STABLE INSULIN ANALOGUES AND IMPROVED METHODS FOR THEIR PRODUCTION | 06-16-2016 |
20160251407 | GLUCOSE-RESPONSIVE INSULIN CONJUGATES | 09-01-2016 |
20220133898 | Derivatisation of Insulin with Polysaccharides - 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. | 05-05-2022 |