Patent application number | Description | Published |
20080207507 | Extended Glp-1 Compounds - Protracted GLP-1 compounds and therapeutic uses thereof. | 08-28-2008 |
20080249007 | Protracted Exendin-4 Compounds - Novel protracted exendin-4 compounds and therapeutic uses thereof. | 10-09-2008 |
20080275066 | Condensed Thiophene Derivatives and Their Use as Cyclic Glp-1 Agonists - The invention provides compounds of formula (I) for use as GLP-1 receptor agonists. | 11-06-2008 |
20080319028 | Dicycloalkylcarbamoyl Ureas As Glucokinase Activators - This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. | 12-25-2008 |
20090005312 | NOVEL GLP-1 ANALOGUES LINKED TO ALBUMIN-LIKE AGENTS - Novel GLP-1 agonists which are protracted by coupling to a protraction protein. | 01-01-2009 |
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 |
20090054305 | Mixtures of Amylin and Insulin - The present invention relates to a soluble pharmaceutical composition for parenteral administration, which comprises an amylin peptide, and a meal-related insulin peptide, and to the use of such compositions for treatment of e.g. hyperglycemia. | 02-26-2009 |
20090062192 | Dimeric Peptide Agonists of the Glp-1 Receptor - Dimerization of GLP-1 agonists and therapeutic uses thereof. | 03-05-2009 |
20090099085 | Amylin Derivatives - The present invention relates to novel amylin derivatives having a protracted action profile, to pharmaceutical compositions comprising these derivatives and to the use of the derivatives for the treatment of diseases related to obesity, diabetes and other metabolic disorders. | 04-16-2009 |
20090105482 | Urea Glucokinase Activators - The invention provides a compound of general formula (I) | 04-23-2009 |
20090118501 | Dicycloalkyl Urea Glucokinase Activators - Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. | 05-07-2009 |
20090143592 | Glucagon Antagonists/Inverse Agonists - A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity. | 06-04-2009 |
20090149512 | Use of Ghrelin Antagonists to the Treatment of Certain CNS Diseases - Ghrelin antagonists can be used for the treatment of certain CNS disorders. For example, certain oxadiazoles, preferably such being ghrelin antagonists, can be used to treat obesity, e.g., drug-induced obesity. | 06-11-2009 |
20090156478 | Acylated GLP-1 Compounds - Protracted GLP-1 compounds and therapeutic uses thereof. | 06-18-2009 |
20090176991 | BENZAMIDE GLUCOKINASE ACTIVATORS - The present invention relates to N-heteroaryl-benzamides of the formula (I), pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful as glucokinase activators. | 07-09-2009 |
20090216013 | Heteroaryl-Ureas and Their Use as Glucokinase Activators - This invention relates to compounds of formula (I) | 08-27-2009 |
20090240028 | Synthesis and Application of New Structural Well Defined Branched Polymers as Conjugating Agents for Peptides - The invention provides synthesis and application of new structural well defined branched polymers as protraction agents for peptide and protein. | 09-24-2009 |
20090318353 | Acylated Exendin-4 Compounds - This invention provides new therapeutic peptides, i.e. new protracted Exendin-4 compounds, pharmaceutical compositions and the use of such. | 12-24-2009 |
20100009989 | Urea Glucokinase Activators - This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such. | 01-14-2010 |
20100015146 | TREATING DIABETES USING INHIBITORS OF IL-1 - The present invention describes a method of treating diabetes or metabolic syndrome with a compound that inhibits (a) IL-1, (b) the synthesis of IL-1, or (c) the release of IL-1. | 01-21-2010 |
20100016238 | Peptides for Use in the Treatment of Obesity - The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity. | 01-21-2010 |
20100041711 | Urea Glucokinase Activators - This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such. | 02-18-2010 |
20100173835 | Peptides for Treatment of Obesity - The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity. | 07-08-2010 |
20100204288 | Heteroaryl-Ureas and Their Use as Glucokinase Activators - This invention relates to compounds of formula (I) | 08-12-2010 |
20100222269 | IMPROVED DERIVATIVES OF AMYLIN - The invention relates to derivatives of human amylin or analogues thereof which bind to the amylin receptor and are linked to an albumin binding compound, pharmaceutical compositions comprising these derivatives and methods for obtaining such. | 09-02-2010 |
20100261637 | PEPTIDES DERIVATIZED WITH A-B-C-D- AND THEIR THERAPEUTICAL USE - The invention relates to protracted peptide derivatives such as Glucagon-Like Peptide-1 (GLP-1), exendin-4, and analogues thereof, as well as therapeutic uses thereof. The peptide derivative of the invention comprises a peptide wherein at least one amino acid residue is derivatized with A-B-C-, or A-B-C-D-. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, have a low ratio of binding affinity to the GLP-1 receptor in the presence of high/low albumin concentrations, have long half-lives, and have a high affinity of binding to albumin, all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration. | 10-14-2010 |
20100292133 | TRUNCATED GLP-1 DERIVATIES AND THEIR THERAPEUTICAL USE - The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration. | 11-18-2010 |
20100305032 | Novel GLP-1 Derivatives - Novel polypeptide derivatives having protracted profile of action. | 12-02-2010 |
20100317057 | SEMI-RECOMBINANT PREPARATION OF GLP-1 ANALOGUES - A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis. | 12-16-2010 |
20100331379 | BENZAMIDE GLUCOKINASE ACTIVATORS - The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase. | 12-30-2010 |
20110060019 | HETEROARYL-UREAS AND THEIR USE AS GLUCOKINASE ACTIVATORS - This invention relates to compounds of formula (I) | 03-10-2011 |
20110077234 | Urea Glucokinase Activators - The invention provides a compound of general formula (I) | 03-31-2011 |
20110082079 | GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE - The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration. | 04-07-2011 |
20110105394 | Amylin Derivatives - The present invention relates to novel amylin derivatives, pharmaceutical compositions containing such derivatives and to methods of treating diabetes and hyperglycaemia using the amylin derivatives of the invention. | 05-05-2011 |
20110166321 | DOUBLE-ACYLATED GLP-1 DERIVATIVES - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K | 07-07-2011 |
20110230529 | BENZAMIDE GLUCOKINASE ACTIVATORS - The present invention relates to N-heteroaryl-benzamides of the formula (I), pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful as glucokinase activators. | 09-22-2011 |
20110301084 | Protracted Exendin-4 Compounds - Novel protracted exendin-4 compounds and therapeutic uses thereof. | 12-08-2011 |
20110301158 | ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS - This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. | 12-08-2011 |
20120283170 | Acylated Exendin-4 Compounds - This invention provides new therapeutic peptides, i.e. new protracted Exendin-4 compounds, pharmaceutical compositions and the use of such. | 11-08-2012 |
20120289453 | NOVEL GLP-1 COMPOUNDS - Novel GLP-1 compounds and their therapeutic use. | 11-15-2012 |
20120295847 | Acylated GLP-1 Compounds - Protracted GLP-1 compounds and therapeutic uses thereof. | 11-22-2012 |
20130040884 | ALBUMIN-BINDING CONJUGATES COMPRISING FATTY-ACID AND PEG - Novel polypeptide derivatives having protracted profile of action. | 02-14-2013 |
20130053315 | NOVEL GLP-1 DERIVATIVES - Novel polypeptide derivatives having protracted profile of action. | 02-28-2013 |
20130059853 | BIARYL PHOSPHODIESTERASE INHIBITORS - Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z | 03-07-2013 |
20130243770 | TREATING DIABETES USING INHIBITORS OF IL-1 - The present invention describes a method of treating diabetes or metabolic syndrome with a compound that inhibits (a) IL-1, (b) the synthesis of IL-1, or (c) the release of IL-1. | 09-19-2013 |
20130244931 | Novel GLP-1 Derivatives - Novel polypeptide derivatives having protracted profile of action. | 09-19-2013 |
20130288960 | Double-Acylated GLP-1 Derivatives - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH | 10-31-2013 |
20130338068 | DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from | 12-19-2013 |
20140011732 | Peptides Derivatized with A-B-C-D- and their Therapeutical Use - The invention relates to protracted peptide derivatives such as Glucagon-Like Peptide-1 (GLP-1), exendin-4, and analogues thereof, as well as therapeutic uses thereof. The peptide derivative of the invention comprises a peptide wherein at least one amino acid residue is derivatized with A-B—C—, or A-B—C-D-. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, have a low ratio of binding affinity to the GLP-1 receptor in the presence of high/low albumin concentrations, have long half-lives, and have a high affinity of binding to albumin, all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration. | 01-09-2014 |
20140179899 | DOUBLE-ACYLATED GLP-1 DERIVATIVES - The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K | 06-26-2014 |
20140296131 | Truncated GLP-1 Derivatives and Their Therapeutical Use - The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration. | 10-02-2014 |
20140303083 | GLP-1 Derivatives - The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases. | 10-09-2014 |
20150025003 | GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE - The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration. | 01-22-2015 |