Patent application number | Description | Published |
20080207877 | Modified Human Four Helical Bundle Polypeptides and Their Uses - Modified human four helical bundle (4HB) polypeptides and uses thereof are provided. | 08-28-2008 |
20080300163 | Modified Human Four Helical Bundle Polypeptides And Their Uses - Modified human four helical bundle (4HB) polypeptides and uses thereof are provided. | 12-04-2008 |
20090137456 | GLUCAGON ANALOGS EXHIBITING PHYSIOLOGICAL SOLUBILITY AND STABILITY - Modified glucagon peptides are disclosed having improved solubility and stability, wherein the native glucagon peptide has been modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, or both. | 05-28-2009 |
20100160212 | Modified Human Plasma Polypeptide or Fc Scaffolds and Their Uses - Modified human plasma polypeptides or Fc and uses thereof are provided. | 06-24-2010 |
20100190699 | GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY IN PHYSIOLOGICAL pH BUFFERS - Modified glucagon peptides are disclosed having improved solubility while retaining glucagon agonist activity. The glycogen peptides have been modified by substitution of native amino acids with, and/or addition of, charged amino acids to the carboxy terminus of the peptide. The modified glucagon agonists can be further modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 23, or both to further enhance the solubility of the glucagon agonist analogs. | 07-29-2010 |
20100190701 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming lactam bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (K-RNRNNIA) and SEQ ID NO: 28 (KRNR). | 07-29-2010 |
20110065633 | ESTER-BASED PEPTIDE PRODRUGS - Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 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. | 03-17-2011 |
20110098217 | COMPOUNDS EXHIBITING GLUCAGON ANTAGONIST AND GLP-1 AGONIST ACTIVITY - Glucagon analogs are disclosed that exhibit both glucagon antagonist and GLP-1 agonist activity. In one embodiment, the glucagon antagonist/GLP-1 agonist comprises a modified amino acid sequence of native glucagon, in which the first one to five N-terminal amino acids of native glucagon is deleted and in which the alpha helix is stabilized. | 04-28-2011 |
20110166062 | GIP-BASED MIXED AGONISTS FOR TREATMENT OF METABOLIC DISORDERS AND OBESITY - Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-I activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided. | 07-07-2011 |
20110207914 | Modified Human Plasma Polypeptide or Fc Scaffolds and Their Uses - Modified human plasma polypeptides or Fc and uses thereof are provided. | 08-25-2011 |
20110237493 | DIPEPTIDE LINKED MEDICINAL AGENTS - A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration. | 09-29-2011 |
20110245164 | YL-BASED INSULIN-LIKE GROWTH FACTORS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR - Insulin-like growth factor analogs are disclosed wherein substitution of the IGF native amino acids, at positions corresponding to positions B16 and B17 of native insulin, with tyrosine and leucine, respectively, increases potency of the resulting analog at the insulin receptor by tenfold. Also disclosed are prodrug and depot formulations of the IGF analogs, wherein the IGF analog has been modified by the linkage of a dipeptide to the analog through an amide bond linkage. The prodrug and depot formulations disclosed herein have extended half lives of at least 2 hours, 10 hours, and more typically greater than 2 are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 10-06-2011 |
20110257076 | 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. | 10-20-2011 |
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 |
20110257092 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR). | 10-20-2011 |
20110288003 | AMIDE BASED GLUCAGON AND SUPERFAMILY PEPTIDE PRODRUGS - Prodrug formulations of glucagon superfamily peptides are provided wherein the glucagon superfamily peptide has been modified by the linkage of a dipeptide to the glucagon superfamily through an amide bond linkage. The prodrugs disclosed herein have extended half lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 11-24-2011 |
20110294161 | Modified Human Growth Hormone - Modified growth hormone polypeptide and uses thereof are provided. | 12-01-2011 |
20120041180 | Modified Human Plasma Polypeptide or Fc Scaffolds and Their Uses - Modified human plasma polypeptides or Fc and uses thereof are provided. | 02-16-2012 |
20120122783 | GLUCAGON ANTAGONISTS - Glucagon antagonists are provided which comprise amino acid substitutions and/or chemical modifications to glucagon sequence. In one embodiment, the glucagon antagonists comprise a native glucagon peptide that has been modified by the deletion of the first two to five amino acid residues from the N-terminus and (i) an amino acid substitution at position 9 (according to the numbering of native glucagon) or (ii) substitution of the Phe at position 6 (according to the numbering of native glucagon) with phenyl lactic acid (PLA). In another embodiment, the glucagon antagonists comprise the structure A-B-C as described herein, wherein A is PLA, an oxy derivative thereof, or a peptide of 2-6 amino acids in which two consecutive amino acids of the peptide are linked via an ester or ether bond. | 05-17-2012 |
20120172295 | GIP RECEPTOR-ACTIVE GLUCAGON COMPOUNDS - Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein. | 07-05-2012 |
20120190827 | Modified Human Plasma Polypeptide or Fc Scaffolds and Their Uses - Modified human plasma polypeptides or Fc and uses thereof are provided. | 07-26-2012 |
20120196804 | GLUCAGON ANALOGS EXHIBITING PHYSIOLOGICAL SOLUBILITY AND STABILITY - Modified glucagon peptides are disclosed having improved solubility and stability, wherein the native glucagon peptide has been modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, or both. | 08-02-2012 |
20120238493 | GLUCAGON ANALOGS EXHIBITING GIP RECEPTOR ACTIVITY - Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. | 09-20-2012 |
20120288511 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are glucagon analogs comprising a modified amino acid sequence of native human glucagon (SEQ ID NO: 2) that exhibit activity at the glucagon receptor, activity at the GLP-I receptor, or activity at each of the glucagon receptor and the GLP-I receptor. In some embodiments, the glucagon analog exhibits at least 100% or more of the activity of native glucagon at the glucagon receptor and/or at least 100% or more of the activity of native GLP-I at the GLP-I receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is within 50-fold or less than the EC50 at the glucagon receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is two- to ten-fold greater than the EC50 at the glucagon receptor. Related conjugates, dimers and multimers, and pharmaceutical compositions, and uses thereof, are further provided. | 11-15-2012 |
20120322725 | GLUCAGON ANTAGONIST-GIP AGONIST CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS AND OBESITY - Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided. | 12-20-2012 |
20120329707 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 12-27-2012 |
20120329708 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 12-27-2012 |
20130116172 | GLUCAGON SUPERFAMILY PEPTIDES EXHBITING G PROTEIN COUPLED RECEPTOR ACTIVITY - Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 05-09-2013 |
20130116173 | Glucagon Analogs Exhibiting GIP Receptor Activity - Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. | 05-09-2013 |
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 |
20130123178 | GLUCAGON SUPERFAMILY PEPTIDES EXHIBITING NUCLEAR HORMONE RECEPTOR ACTIVITY - Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 05-16-2013 |
20130123462 | AMIDE BASED GLUCAGON SUPERFAMILY PEPTIDE PRODRUGS - Prodrug formulations of glucagon superfamily peptides are provided wherein the glucagon superfamily peptide has been modified by the linkage of a dipeptide to the glucagon superfamily through an amide bond linkage. The prodrugs disclosed herein have extended half lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 05-16-2013 |
20130137849 | DIPEPTIDE LINKED MEDICINAL AGENTS - A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration. | 05-30-2013 |
20130157934 | Glucagon Superfamily Peptides Exhibiting Glucocorticoid Receptor Activity - Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention. | 06-20-2013 |
20130203660 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming lactam bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR). | 08-08-2013 |
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 |
20140018291 | METHODS FOR TREATING METABOLIC DISORDERS AND OBESITY WITH GIP AND GLP-1 RECEPTOR-ACTIVE GLUCAGON-BASED PEPTIDES - Methods are provided for administering an extended half-life GLP-1/GIP coagonist peptide to a patient in need thereof for reducing weight gain, inducing weight loss, treating hyperglycemia, reducing blood glucose levels, or normalizing blood glucose levels in said patient. | 01-16-2014 |
20140051834 | Incretin Receptor Ligand Polypeptide Fc-Region Fusion Polypeptides And Conjugates With Altered Fc-Effector Function - Herein is reported an Fc-region fusion polypeptide or Fc-region conjugate comprising one to four incretin receptor ligand polypeptides and a variant human Fc-region with a mutation of the amino acid residue at position 329 and at least one further mutation of at least one amino acid selected from the group comprising amino acid residues at position 228, 233, 234, 235, 236, 237, 297, 318, 320, 322 and 331 to a different residue, wherein the residues in the Fc-region are numbered according to the EU index of Kabat and its use as a medicament. | 02-20-2014 |
20140107021 | GLUCAGON ANTAGONIST-GIP AGONIST CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS AND OBESITY - Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Method of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided. | 04-17-2014 |
20140206607 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 07-24-2014 |
20140212419 | ESTER-BASED INSULIN PRODRUGS - Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 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. | 07-31-2014 |
20140221283 | GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS - Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon. | 08-07-2014 |
20140296487 | Modified Human Plasma Polypeptide or Fc Scaffolds and Their Uses - Modified human plasma polypeptides or Fc and uses thereof are provided. | 10-02-2014 |