Novel modulators of melanocortin receptors

a technology of melanocortin and receptors, applied in the field of modulators of melanocortin receptors, can solve the problems of intrinsic challenges in the development of selective ligands of the melanocortin system, and achieve the effect of reducing the amount of side effects

Inactive Publication Date: 2017-01-26
THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent is about a new invention that targets melanocortin receptors specifically, which can be difficult to do with other compounds. The key difference between the new invention and other similar compounds is that it is specific to a specific type of melanocortin receptor, called MC5R. The patent describes a new compound, called N-methylated SHU9 119, which can antagonize MC5R. This may reduce the side effects of treatments involving the new invention.

Problems solved by technology

The melanocortin system remains a challenging target for rational peptide and peptidomimetic design as the 3D-topographical requirements for specific melanocortin receptor subtype recognition have not been fully elucidated.
On the other hand, development of selective ligands to melanocortin system bears intrinsic challenges due to conserved amino acid sequences and their structural similarity contained in the 7 transmembrane GPCR fold.

Method used

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  • Novel modulators of melanocortin receptors
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Embodiment Construction

[0013]Before the present compounds, compositions, articles, devices, and / or methods are disclosed and described, it is to be understood that this invention is not limited to specific synthetic methods or to specific compositions, as such may, of course, vary. It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting.

[0014]Following is a list of abbreviations referred to herein:[0015]Abu 2-aminobutyric acid[0016]Acpc 1-aminocyclopropane carboxylic acid[0017]Aic 2-aminoindane-2-carboxylic acid[0018]Che 1-amino-1-cyclohexane carboxylic acid[0019]Cpe 1-amino-1-cyclopentane carboxylic acid[0020]Dab diaminobutyric acid[0021]Ioc indoline-2-carboxyic acid[0022]Oic octahydroindole-2-carboxylic acid[0023]Orn ornithine[0024]Tic tetrahydro-isoquinoline-3-carboxylic Acid

[0025]As used herein, the term “natural amino acids” refers to the twenty amino acids that are found in nature, i.e. occur natural...

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Abstract

Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1:R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Zaa10]-R2.R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)n—CH3, or −CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COOH, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.

Description

CROSS REFERENCE[0001]This application is a non-provisional and claims benefit of U.S. Provisional Patent Application No. 62 / 242,874, filed Oct. 16, 2015, the specification(s) of which is / are incorporated herein in their entirety by reference.[0002]This application is a continuation-in-part and claims benefit of U.S. Patent Application No. PCT / US15 / 35180, filed Jun. 10, 2015, which claims benefit of U.S. Provisional Patent Application No. 62 / 017,137, filed Jun. 25, 2014, and U.S. patent application Ser. No. 14 / 300,991, filed Jun. 10, 2014, the specification(s) of which is / are incorporated herein in their entirety by reference.FIELD OF THE INVENTION[0003]The present invention relates to modulators of melanocortin receptors (MCR), in particular, to an N-methylated variation of a cyclic peptide and analogues thereof that are modulators for MC5R.BACKGROUND OF THE INVENTION[0004]The melanocortin system remains a challenging target for rational peptide and peptidomimetic design as the 3D-t...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): C07K7/64
CPCC07K7/64A61K9/0014A61K9/107A61K9/7084A61K38/00A61K38/10A61K47/24C07K7/56C07K14/68C07K14/685C07K14/69C07K7/08C07K14/723
InventorHRUBY, VICTOR J.CAI, MINYING
OwnerTHE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA