31 results about "Melanocortin" patented technology

A medicament for treatment or prevention of interstitial lung disease, and of a disease or symptom accompanied by systemic sclerosis in a subject, the medicament comprising, as an effective ingredient, 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid, or a pharmaceutically acceptable salt or co-crystal thereof.

To provide compounds, pharmaceutical compositions, and uses in the manufacture of a medicament for methods of treating conditions, diseases, or disorders that would benefit from modulation of melanocortin subtype-2 receptor activity.SOLUTION: A compound of formula (I), or a pharmaceutically acceptable salt thereof, is provided. (RA: substituted / unsubstituted phenyl, substituted / unsubstituted monocyclic heteroaryl, etc. L: bond, CO, CONR7, SO2. RB: substituted / unsubstituted carbocycle, substituted / unsubstituted heterocycle, etc. X1: CR6. X2, X3: N, CR6. R1-R7: substituted / unsubstituted C1-C6 alkyl, etc. n: 1, 2.)SELECTED DRAWING: None

The present invention provides methods of using non-naturally occurring melanocortin analogs to increase body weight and / or increase food consumption in a subject having a kidney disease and / or a liver disease (e.g., chronic kidney disease, renal failure, non-alcoholic fatty liver disease (NAFLD)). Also provided are methods of stimulating appetite in a subject via administration of a non-naturally occurring melanocortin analogue. The non-naturally occurring melanocortin analogs may be present in pharmaceutical compositions and delivered via parenteral administration (e.g., subcutaneous injection). The methods improve appetite, increase food consumption, increase body weight, muscle mass, and / or fat mass in the subject.

The description refers to a method for treating a disease or disorder in a subject by using a combination of: (i) a potassium channel activator (e.g., a SURx / Kirx channel activating compound) or a pharmaceutically acceptable salt thereof; and (ii) a melanocortin-4 receptor (MC4R) agonist.

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

A medicament for treatment or prevention of interstitial lung disease, and of a disease or symptom accompanied by systemic sclerosis in a subject includes, as an effective ingredient, 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid, or a pharmaceutically acceptable salt or co-crystal thereof.

Provided herein are methods of treating, preventing, or reducing one or more symptoms or conditions associated with metabolic dysfunction, such as obesity, in a subject in need thereof using a non-naturally occurring melanocortin analog. In some embodiments, the non-naturally occurring melanocortin analog is administered orally. In some embodiments, the method comprises suppressing appetite in a subject in need thereof using a non-naturally occurring melanocortin analog in accordance with the present technology.

The present disclosure relates to novel compounds of Formula (1): or salts thereof: (1) wherein J, X, Z, L1, L2, R1, R2, R3, R3a, R3b, R3c and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling, or reducing the risk of disorders associated with melanocortin subtype 2 receptor (MC2R).

To provide a composition for the treatment of diseases of ACTH excess such as Cushing's disease, ectopic ACTH syndrome, and congenital adrenal hyperplasia.SOLUTION: Provided is a pharmaceutical composition for use in a method of treating congenital adrenal hyperplasia (CAH) in a human comprising a compound having the structure of Compound 1, or a pharmaceutically acceptable salt, or solvate thereof, wherein the method comprises administering the pharmaceutical composition to the human in need thereof.SELECTED DRAWING: Figure 9

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 exhibit (i) full MC4R antagonism and full, partial, or no MC3R agonism; (ii) partial MC4R antagonism and no MC3R activity; or (iii) full MC4R agonism and full MC3R antagonism with sub-micromolar or low-nanomolar binding activity.

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

The disclosure relates to pharmaceutical compositions comprising a melanocortin-1 receptor (MC1R) agonist; a plurality of micrometer or millimeter scale particles; and a pharmaceutically acceptable carrier, and use thereof for the treatment of disease.

Provided herein are methods and compositions for the treatment of diseases of ACTH excess, such as Cushing's disease, ectopic ACTH syndrome, and congenital adrenal hyperplasia.

The present technology comprises non-naturally occurring melanocortin analogs or pharmaceutically acceptable salts, solvates, or stereoisomers thereof and compositions comprising the same. In some embodiments, the non-naturally occurring melanocortin analogs may be agonists of melanocortin 1 which have sub-micromolar or low-nanomolar binding activity. The non-naturally occurring melanocortin analogs may be present in a composition that is formulated for delivery to a subject in need thereof.

The present disclosure relates to the use of a compound of chemical Formula 1 or a pharmaceutically acceptable salt thereof for the purpose of preventing, improving, or treating a genetic obesity disease associated with the melanocortin-4 receptor (MC4R) pathway, particularly a genetic obesity disease associated with SH2B1 deficiency or a LEPR deficiency.

Provided herein are non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs of the present technology may be useful in treating, preventing, reducing, or otherwise ameliorating one or more disorders associated with the melanocortin system. In some embodiments, the non-naturally occurring melanocortin analog is administered orally to a subject in need thereof.

The disclosure herein provides a compound of formula (1): JPEG2026507093000332.jpg3670 or a salt thereof (wherein J, X, Z, L 1 , L 2 , R 1 , R 2 , R 3 , R 3a , R 3b , R 3c and R 4 The present invention relates to their use in the treatment, prevention, amelioration, suppression, or reduction of the risk of disorders associated with the melanocortin subtype-2 receptor (MC2R) (as defined herein) and the melanocortin subtype-2 receptor (MC2R).

The invention relates to an application of tolvaptan as an active ingredient in preparation of a medicine or a medical beauty product for inhibiting melanin synthesis. Cell activity detection and melanin content determination show that the tolvaptan can significantly reduce the melanin content in cells without affecting the cell activity. Tyrosinase activity detection shows that tolvaptan does not affect the catalytic activity of TYR. Protein immunoblotting experiments show that tolvaptan can down-regulate the expression levels of TYR family proteins, ommatidium-associated transcription factors (MITF), cyclic adenylate reaction element binding proteins (CREB) and melanocortin-1 receptors (MC1R).

The present invention relates to compounds of Formula I: (I) and their pharmaceutically acceptable salts that activate the melanocortin-5 receptor (MC5R) and uses thereof in the treatment or prevention of a disease or condition related to MC5R activity.

The disclosures herein relate to compounds of Formula (1) and (2): (1); (2); or a pharmaceutically acceptable salt thereof and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with the melanocortin subtype-2 receptor (MC2R).

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin agonist analogs. The non-naturally occurring melanocortin agonist analog comprises a sequence of Formula (I): Ac-Nle-c[Glu-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

Provided herein are pharmaceutical compositions of non-naturally occurring melanocortin agonist analogs formulated for oral administration. The non-naturally occurring melanocortin agonist analog comprises a sequence of Formula (I): Ac-Nle-c[Glu-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

The disclosures herein relate to pharmaceutically acceptable salts of a compound of Formula (1) and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with the melanocortin subtype-2 receptor (MC2R).

The disclosures herein relate to pharmaceutical compositions comprising a compound of Formula (1): (1); or a pharmaceutically acceptable salt thereof and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with the melanocortin subtype-2 receptor (MC2R).

Provided herein are non-naturally occurring melanocortin analogs. The non-naturally occurring melanocortin analogs of the present technology may be useful in treating, preventing, reducing, or otherwise ameliorating one or more disorders associated with the melanocortin system. In some embodiments, the non-naturally occurring melanocortin analog is administered orally to a subject in need thereof.

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 agonists of melanocortin 1 with sub-micromolar or low-nanomolar binding activity. In some embodiments, the non-naturally occurring melanocortin analogs are formulated for delivery to a subject in need thereof.

Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.