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Peptides and pharmaceutical compositions for treating eye diseases

A compound, alkyl technology, applied in the field of peptides and pharmaceutical compositions for the treatment of eye diseases

Pending Publication Date: 2021-10-01
株式会社柳柳制药
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term use of these drugs can cause various side effects such as eye congestion and corneal calcification (Bernauer W et al., Br. J. Ophthalmol., 90: 285-8, 2006)

Method used

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  • Peptides and pharmaceutical compositions for treating eye diseases
  • Peptides and pharmaceutical compositions for treating eye diseases
  • Peptides and pharmaceutical compositions for treating eye diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0860] Embodiment 1: the preparation of YDE derivative

[0861] Protein analysis of the extracellular matrix derived from animal chondrocytes was performed in Baek's group of Center of Biomedical Mass Spectrometry (Diatech Korea Co., Ltd., Seoul, Korea). Proline-GQDGLAGPK (P-GQDGLAGPK), which is a part of the amino acid sequence of type II collagen α1 protein, was obtained through the protein analysis described above.

[0862] The following is an exemplary protein synthesis of YDE-011. Other compounds of the invention (e.g., YDE-001-YDE-086) were prepared via similar procedures, e.g., by substituting different amino acid building block reagents at the desired steps.

[0863]

[0864] Exemplary program for YDE-011

[0865] solid phase synthesis

[0866] Fmoc-Pro-Lys(Boc)-Wang Resin(1)

[0867]To a solid phase synthesis reactor equipped with a filter membrane was added Fmoc-Lys(Boc)-Wang resin (1.75 g, 1 mmol) in DCM (30 mL), followed by swelling for 30 min, followed by...

Embodiment 2

[0911] Example 2: Preparation of YDE derivatives with modified C-terminus

[0912] Preparation of YDE peptide

[0913] YDE peptides (YDE-093, YDE-096 and YDE-101 to YDE-107), derivatives of the amino acid sequence of YDE-011 were obtained via C-terminal modification of YDE peptides such as YDE-011.

[0914] To prepare C-terminal modified peptides, Fmoc solid-phase peptide synthesis (SPPS) was performed based on the standard procedure described in WO 2018 / 225961 and further C-terminal amidation reaction was performed.

[0915] Peptides of the invention are prepared via analogous procedures, for example by substituting different amino acid building block reagents at the desired steps.

[0916] Exemplary preparation of YDE-093

[0917] To prepare the C-terminal amidated peptide YDE-093, the synthetic procedure was carried out as depicted in Scheme A below. The Fmoc-protected 10-mer peptide (Fmoc-Hyp-H-Gly-Gln-Leu-Gly-Ala-Leu-Gly-Pro-Lys(Dde)-OH) was prepared according to the p...

Embodiment 3

[0949] Example 3: Evaluation of the eye protection effect of YDE derivatives on dry eye syndrome

[0950] Preparation of rats with dry eye syndrome

[0951] In order to evaluate the eye protection effect of YDE-001 to YDE-028 prepared in Example 1 on dry eye syndrome, a total of 320 Sprague-Dawley-type (Sprague-Dawley-type) male rats (OrientBio, Seungnam, Korea) for 7 days. Thereafter, dry eye syndrome was induced in 264 test rats by extraorbital lacrimal gland excision (hereinafter referred to as ELGE). Eight test rats without ocular abnormalities were sham-operated as a control group.

[0952] By inhalation of 2% to 3% isoflurane (Hana Pharm.Co., Hwasung, Korea), 70% N 2 O and 28.6% O 2 Rats were generally anesthetized using a rodent anesthesia machine (Surgivet, Waukesha, Wis., USA) and a respirator (model 687, Harvard Apparatus, Cambridge, UK). Thereafter, the extraorbital lacrimal gland in the subcutaneous region above the masseter muscle and below the optic nerve wa...

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Abstract

The present invention relates to novel peptides and pharmaceutical compositions comprising the same. The peptide compounds and compositions disclosed herein are useful as therapeutic agents for treating eye diseases. When administered to the eyes, the peptide compounds and compositions disclosed herein increase the amount of tear secretion and promotes recovery of a damaged cornea.

Description

[0001] related application [0002] This application claims the benefit of priority to U.S. Provisional Patent Application Serial No. 62 / 767,180, filed November 14, 2018; the contents of said application are incorporated herein by reference. technical field [0003] The present invention relates to peptides and pharmaceutical compositions for the treatment of eye diseases. Background technique [0004] Dry eye syndrome or keratoconjunctivitis sicca can be broadly defined as damage to the ocular surface due to impaired tear secretion (Joossen C et al., Exp. Eye Res., 146:172-8, 2016). Dry eye syndrome is known to cause disturbance of tear secretion and damage and discomfort to the eyeball due to a combination of various factors. Although the incidence of dry eye syndrome is strongly age-related, the incidence of dry eye syndrome is increasing in younger age groups due to chronic exposure to dry environments, such as contact lenses, computer and smart device use (Stern ME et ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61P27/02A61K38/00A61K9/00
CPCC07K7/06A61K38/00A61P27/02A61K9/0048A61K9/08
Inventor T·白J-Y·蔡G-W·闵C·H·朴
Owner 株式会社柳柳制药
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