44 results about "Y2 receptor" patented technology

The invention provides PYY3-36 variants and pegylated derivatives thereof and compositions and methods useful in the treatment of conditions modulated by an NPY Y2 receptor agonist.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

The present invention relates to PYY analogues or derivatives thereof comprising at least one alteration selected from the group consisting of substitutions, insertions, deletions and modifications and optionally a serum albumin binding side chain comprising an alkyl chain with at least 14 carbon atoms. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y2 receptor modulation.

Analogues of the peptide PYY (1-36) are described in which the tertiary structure of the peptide is preserved and stabilised particularly to enhance binding and activation of the Y2 receptor by the use of cross links or rigid bends in the peptide to constrain conformationally the positions of the N-terminal part of the peptide sequence and amino acid 34. The analogues are useful in the control of food intake.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

Y receptor agonists other than PYY 3-36, which are selective for the Y2 receptor over the Y1 and Y4 receptors, and their use in the treatment of conditions responsive to activation of Y2 receptors, are disclosed. Broadly, a Y2-selective agonist is one which (a) is a PP-fold peptide or PP-fold peptide mimic selected from PYY, NPY, PYY mimics and NPY mimics which have a C-terminal Y2 receptor-recognition amino acid sequence and have various modifications relative to the natural peptides or (b) a PP-fold peptide or PP-fold peptide mimic selected from PP and PP-mimics which have a C-terminal Y2 receptor-recognition amino acid sequence and which have various modifications relative to the natural peptide or (c) comprise a C-terminal Y2 receptor-recognition amino acid sequence fused at its N-terminus to an amphiphilic amino acid sequence domain comprising at least one alpha helical turn adjacent the N-terminus of the said Y2 receptor-recognition sequence, said turn being constrained in a helical configuration by a covalent intramolecular link, and (ii), in the case where the agonist has an N-terminal structure analogous to NPY or PYY, having one or more of the modifications listed in (a) above and, in the case where the agonist has an N-terminal structure analogous to PP, having one or more of the modifications listed in (b) above.

The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep / wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY (PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) wherein the formulations have increased resistance to microbial contamination and is comprised of a Y2 receptor-binding peptide, water, a cyclodextrin and sodium benzoate.

A method for treating obesity, inducing weight-loss, or inducing satiety in a mammal comprising administering intranasally to the mammal a therapeutically effective amount of a pharmaceutical composition comprising PYY(3-36), a phosphatidylcholine or diglyceride, and a cyclodextrin, wherein the phosphatidylcholine or diglyceride and the cyclodextrin are present in an amount sufficient to enhance epithelial permeation.

Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

The present invention relates to PYY analogues or derivatives thereof comprising at least one alteration selected from the group consisting of substitutions, insertions, deletions and modifications and optionally a serum albumin binding side chain comprising an alkyl chain with at least 14 carbon atoms. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y2 receptor modulation.

Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

A pharmaceutical device comprising a composition comprising an aqueous solution of PYY(3-36), a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation, and wherein the composition is present in a container; and an actuator fluidly connected to the container, wherein the actuator has a tip which defines a passage through which the solution is ejected to produce a spray of the solution.

The invention relates to PYY compounds with the amino acid modifications 7Lys, 30Trp, and 31Leu, and in addition to these, 22Ile and / or 28Tyr, and derivatives thereof. The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

The invention relates to PYY compounds with the amino acid modifications 7Lys, 30Trp, and 31Leu, and in addition to these, 22Ile and / or 28Tyr, and derivatives thereof. The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

The invention relates to PYY compounds having the amino acid in the position corresponding to position 35 of hPYY(1-36) substituted with beta-homoarginine and derivatives thereof with a modifying group attached to the position corresponding to position 7 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

The invention relates to PYY compounds having the amino acid in the position corresponding to position 30 of hPYY(1-36) substituted with tryptophan and derivatives thereof with a modifying group attached to the position corresponding to position 7 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

The present invention relates to the use of a substance that inhibits the Y2 receptor of neuropeptide Y for the preparation of a pharmaceutical composition for treatment of alcoholism. It also relates to a pharmaceutical composition comprising at least one substance with activity against alcohol consumption.

The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

Y4 receptor agonists which are selective for the Y4 receptor over the Y1 and Y2 receptors, are useful in the prevention and / or treatment of damage to bowel function caused by radiation therapy, radiation exposure, cytotoxic chemotherapy, inflammation, or ischemia-reperfusion of intestinal mucosa.

A monomeric peptide that functions as an agonist for the glucagon receptor (GluR), the glucagon-like peptide 1 receptor (GLP1-R) and neuropeptide Y2 receptor (NPY2-R). The peptide thus targets three of the receptors involved glucoregulation and appetite regulation to more efficiently and completely facilitate weight loss in, among others, type II diabetic patients while also being capable of stimulating a reduction in appetite to complement the weight loss results.

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

This invention provides peptides that act as selective NPY2 receptor agonists in vitro and are efficacious in vivo to reduce food intake. The invention is a peptide selected from a specific group of derivatized NPY-related peptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the peptides to said mammal to reduce food intake and body weight.