30 results about "MC4 Receptor" patented technology

Provided herein are non-naturally occurring melanocortin analogs that selectively bind at least a portion of a melanocortin receptor The melanocortin receptor may be a melanocortin 3 receptor (MC3R) or a melanocortin 4 receptor (MC4R). The non-naturally occurring melanocortin analogs may have a dissociation constant (Kd) value for a melanocortin receptor or one or more amino acids thereof that is less than that of a conventional melanocortin analog.

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin antagonist analogs. The non-naturally occurring melanocortin antagonist analogs may be antagonists of the melanocortin 3 receptor and / or melanocortin 4 receptor.

To provide anti-obesity agents to overcome defects of currently used anti-obesity agents, that is, as main types of the previously developed anti-obesity drugs, appetite suppressants acting on the central nervous system are drugs that control the action of neurotransmitters (for example, phentermine, mazindol, lorcaserin, fluoxetine and sibutramine) were mostly used, but the neurotransmitter modulators exert a wide range of effects on various physiological actions in addition to appetite suppression by numerous subtype receptors, so that the modulators are lacking in selectivity for each subtype and have a large disadvantage in that various side effects are accompanied in a case of long-term administration.SOLUTION: The present invention relates to uses of a compound of chemical formula 1 or a pharmaceutically acceptable salt thereof for the purpose of preventing or treating rare genetic obesity diseases, particularly rare genetic obesity diseases associated with a damaged melanocortin-4 receptor (MC4R) pathway.SELECTED DRAWING: None

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present technology comprises pharmaceutical compositions of non-naturally occurring melanocortin analogs formulated for oral administration. The non-naturally occurring melanocortin analogs may be agonists or antagonists of the melanocortin 4 receptor (MC4R) and / or the melanocortin 3 receptor (MC3R) with sub-micromolar or low-nanomolar binding activity, or may be agonists of the melanocortin 1 receptor (MC1R) with sub-micromolar or low-nanomolar binding activity.

Provided herein are non-naturally occurring melanocortin analogs that selectively bind at least a portion of a melanocortin receptor The melanocortin receptor may be a melanocortin 3 receptor (MC3R) or a melanocortin 4 receptor (MC4R). The non-naturally occurring melanocortin analogs may have a dissociation constant (Kd) value for a melanocortin receptor or one or more amino acids thereof that is less than that of a conventional melanocortin analog.

The present technology comprises stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin agonist analogs. In some embodiments, the non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor (MC3R) and full or partial agonists of the melanocortin 4 receptor (MC4R) with sub-micromolar and / or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar and / or low-nanomolar binding activity.

The present disclosure relates to methods of treating a disease or disorder comprising administering a combination of an MC4R agonist with a GCHR modulator.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present disclosure features a method for preparing an MC4R agonist and related compositions thereof, such as an MC4R agonist of Formula (I) described herein.

The present disclosure relates to methods of treating a disease or disorder comprising administering a combination of GLP1R agonists and MC4R agonists.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

Provided herein are non-naturally occurring melanocortin analogs that selectively bind at least a portion of a melanocortin receptor The melanocortin receptor may be a melanocortin 3 receptor (MC3R) or a melanocortin 4 receptor (MC4R). The non-naturally occurring melanocortin analogs may have a dissociation constant (Kd) value for a melanocortin receptor or one or more amino acids thereof that is less than that of a conventional melanocortin analog.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

Novel peptides having an extra Arg improve the melanocortin 4 receptor (MC4R) selectivity and potency are described herein. The peptides are used in compositions and methods for treating obesity and / or neurodegenerative diseases. A selective MC4R peptide agonist is administered to a subject in need of such treatment.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may selectively bind the melanocortin 3 receptor and / or the melanocortin 4 receptor over the melanocortin 1, melanocortin 2, and melanocortin 5 receptors. In some embodiments, the non-naturally occurring melanocortin analogs are antagonists of melanocortin 3 and / or 4 receptors with sub-micromolar or low-nanomolar binding activity.

The present disclosure provides, at least in part, a pharmaceutical product comprising: sememartide (also referred to as RM493); sametastide as the sole active pharmaceutical ingredient formulated for injection; as the sole active ingredient, sememartide; as an active pharmaceutical ingredient, sememarin; as an active pharmaceutical ingredient for injection; or another pharmaceutical composition having a major mechanism of action of an MC4 receptor agonist (referred to herein as MC4 RAP), such as a lipid excipient, and / or a pharmaceutically acceptable carrier. The pharmaceutical products described herein provide for sustained release of sememarin or another pharmaceutical composition, which, upon administration, can result in more desirable pharmacokinetic and pharmacodynamic characteristics.

The present disclosure features a method for preparing an MC4R agonist and related compositions thereof, such as an MC4R agonist of Formula (I) described herein.

Provided herein are pharmaceutical compositions of non-naturally occurring melanocortin analogs formulated for oral administration. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs may be agonists or antagonists of the melanocortin 4 receptor (MC4R) and / or the melanocortin 3 receptor (MC3R) with sub-micromolar or low-nanomolar binding activity, or may be agonists of the melanocortin 1 receptor (MC1R) with sub-micromolar or low-nanomolar binding activity.

Provided herein are non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. Some melanocortin analogs are full antagonists of the melanocortin 3 receptor and full agonists of the melanocortin 4 receptor with sub-micromolar or low- nanomolar binding activity. Other melanocortin analogs are full or partial antagonists of the melanocortin 4 receptor with no activity, partial agonist activity or full agonist activity on the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity. Certain non-naturally occurring melanocortin analogs may also be partial agonists or partial antagonists of the melanocortin 3 receptor.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full or partial antagonists of the melanocortin 3 receptor with sub-micromolar or low-nanomolar binding activity. Some of the non-naturally occurring melanocortin analogs may also be full or partial antagonists or partial agonists of the melanocortin 4 receptor with sub-micromolar or low-nanomolar binding activity.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. The non-naturally occurring melanocortin analogs may be full agonists of the melanocortin 3 receptor and full or partial agonists of the melanocortin 4 receptor with sub-micromolar and / or low-nanomolar binding activity.