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Melanocyte modulating peptides

A halogen, alkyl technology, used in the field of peptides that regulate melanin production, therapy and cosmetics, can solve the problem of no benefit

Pending Publication Date: 2022-03-25
IDP DISCOVERY PHARMA SL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because post-inflammatory hypopigmentation is often clinically apparent after the inflammatory process has ended, these same topical agents may not be beneficial at this advanced stage

Method used

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  • Melanocyte modulating peptides
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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0159] The preparation method of the peptide according to the first aspect of the present invention comprises:

[0160] (1.a) Coupling the corresponding amino acid of the peptide with a compound of formula (III) and a compound of formula (IV) by condensation corresponding to the compounds designated as "i" and "i+4" or "i+7" amino acid. Compounds (III) and (IV) will undergo a subsequent cyclization step to generate the "L" diradical:

[0161]

[0162] where R 19 As defined above, Z 1 and Z 2 same or different, and represents (C 2 -C 10 ) alkenyl; and (1.b) a cyclization step comprising carrying out Z in solution with a Grubbs (I or II generation) catalyst 1 and Z 2 (see KimYoung-Woo et al., "Synthesis of all-hydrocarbon stapled a-helical peptides byring-closing olefin metathesis", Nature Protocols, 2011, 6(6), pp. 761-771; ScottJ.M. et al. Al, "Application of Ring-Closing Metathesis to the Synthesis of Rigidified Amino Acids and Peptides", J.Am.Chem.Soc., 1996, v.11...

Embodiment

[0220] 1. Materials and Methods

[0221] General procedure for synthesis

[0222] Compound IDP-F

[0223] Materials were purchased as follows: Fmoc-protected α-amino acid (---); Rinkamide MBHA resin (Tianjin Nankai Hecheng Technology Co., Ltd.); HBTU ((2-(1H-benzotriazol-1-yl)-1,1 ,3,3-Tetramethyluronium hexafluorophosphate), GLBiochem); N-methylmorpholine (Sinopharm Chemical Reagent Co., Ltd.); Succinic anhydride (Aladdin); Acetonitrile (Xingke Chemical); Ninhydrin (Sinopharm Chemical Reagent Co., Ltd.); piperidine (Vertellus); dimethylformamide, DMF (Zhejiang Jiangshan Chemical Co., Ltd.); trifluoroacetic acid, TFA (trifluoroacetic acid, Solvay), TIS (thioanisole, Solvay).

[0224] Briefly, linear peptides are artificially synthesized using Fmoc-based SPPS (solid-phase peptide synthesis) using Rink amide MBHA resin as a carrier.

[0225] The following scheme was used:

[0226] 1. Removal of the Fmoc protecting group with 20% piperidine in DMF.

[0227] 2. Wash the r...

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PUM

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Abstract

The peptides of the invention have a sequence having at least 85% identity to the sequence SEQ ID NO: 1 or SEQ ID NO: 2. These peptides modulate melanocyte activity in terms of melanin proliferation and production. Therefore, these peptides can be used in the treatment of melanoma, as well as in the treatment of cosmetic hyperpigmentation or hypopigmentation of the skin.

Description

[0001] This application claims the benefit of European Patent Application EP19382674.0 filed on August 2, 2019. technical field [0002] The present invention relates generally to the field of melanocyte-related disorders. Specifically, the present invention relates to peptides having the ability to regulate melanin production, which promote or reduce the production of melanin, and inhibit the proliferation of malignant melanocytes; to pharmaceutical and cosmetic compositions containing them as active ingredients, and to their therapeutic and Use in cosmetics. Background technique [0003] Through a process called melanogenesis, melanocytes produce melanin, a pigment found in the skin, eyes, hair, nose and inner ear. This melanogenesis results in long-lasting pigmentation, which is in contrast to pigmentation resulting from the oxidation of already existing melanin. [0004] There are both basal and activated levels of melanogenesis; in general, people with lighter skin ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K8/64A61K38/10A61P17/00A61P35/00A61P35/04A61Q19/02A61Q19/04
CPCC07K7/08A61K38/10A61P17/00A61P35/00A61P35/04A61K8/64A61Q19/02A61Q19/04A61K38/00A61Q19/00
Inventor L·内沃拉S·埃斯特班·马丁
Owner IDP DISCOVERY PHARMA SL
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