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Novel zinc complex, production and use of same

A technology of complexes and uses, applied in the direction of zinc organic compounds, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of ignorance, development and unmet needs for therapeutic uses, etc.

Pending Publication Date: 2021-05-04
OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOSTYU ZET TERAPEVTIKS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] To date, no drug based on zinc complexes of glutaminyl cyclase inhibitors is known for the treatment of atopic dermatitis or other diseases associated with impaired epithelial tissue barrier function and / or abnormal activity of immune cells. Therefore, there is still an unmet need for the development and therapeutic use of new effective drugs based on glutaminyl cyclase inhibitor zinc complexes

Method used

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  • Novel zinc complex, production and use of same
  • Novel zinc complex, production and use of same
  • Novel zinc complex, production and use of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0143] Example 1 (not included in the present invention). Mix Zinc Chloride with Gamma-L-Glutamine Histamine

[0144] This example shows that the zinc complex of γ-L-glutamyl histamine cannot be prepared by simple mixing of ingredients such as zinc salt and γ-L-glutamyl histamine, because under these conditions a Mixture of zinc salts and free gamma-L-glutamyl histamine. For example, an aqueous solution of zinc chloride was mixed with γ-L-glutamyl histamine in a ratio of 1:2 and aqueous ammonia was added (until the medium was slightly basic), followed by precipitation of the product resulting in the formation of a white crystalline substance. Elemental analysis data (see Table 1) showed data values ​​close to those calculated for complexed compounds, but the data could not be considered evidence of complex formation. The underestimated amounts of carbon and nitrogen in the samples suggest possible zinc hydroxide formation, which partially loses water during the analysis, can...

Embodiment 2

[0148] Embodiment 2. prepare zinc complex according to the present invention (method No.1)

[0149] In a further study, the authors developed a method for obtaining complexes of zinc with γ-L-glutamyl histamine, which involved the use of aqueous zinc acetate.

[0150] 2.20g (0.01mol) Zn(CH 3 COO) 2 *2H 2 O was dissolved in 20 ml of methanol and added dropwise to 2.40 g (0.01 mol) of γ-L-glutamyl histamine and 1.08 (0.02 mol) of freshly prepared sodium methoxide in 50 ml of methanol under vigorous stirring at room temperature solution in. After adding about half the volume of the zinc acetate solution, the formation of a white precipitate was observed. After all the zinc acetate solution had been added, stirring was continued for about 4 hours, the product was filtered off, washed with water (4 x 10 ml) and dried in vacuo at 65° C. until its weight remained constant. Yield, 2.67 g (88%).

[0151] Two test runs of this technique of the method embodiment were performed and ...

Embodiment 3

[0160] Embodiment 3. according to the present invention obtains zinc complex compound (method No.2)

[0161] The purpose of the modification of the process according to the invention is to improve the filterability of the product obtained and to ensure the most homogeneous distribution of the zinc hydroxide in the reaction mixture.

[0162] For scaling purposes, the issue of distribution uniformity is extremely important for this technique, since the formation of a complex of zinc with γ-L-glutamyl histamine on the zinc hydroxide surface prevents the reaction from proceeding further. To solve this problem, it was proposed to obtain zinc hydroxide in situ by adding sodium hydroxide and zinc acetate solutions simultaneously.

[0163] Synthesis "A": 12.0 g (0.05 mol) of γ-L-glutamyl histamine and 11.0 (0.05 mol) solution of zinc acetate dihydrate in 80 ml of water. The reaction mixture was stirred at 70°C for 4 hours, cooled to room temperature and left overnight. The precipit...

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Abstract

The invention relates to a novel zinc complex of gamma-L-glutamyl histamine with a metal / ligand ratio of 1 / 1. In particular, the invention relates to a compound of formula (I). The complex according to the invention promotes the recovery of barrier functions of epithelial tissue and suppresses aberrant activity of immune system cells. The invention also relates to the production of the complex and the use of said zinc complex for the treatment of atopic dermatitis and other diseases associated with the disruption of barrier functions of epithelial tissue and the development of an aberrant inflammatory response. The invention also relates to the use of the obtained complex for inhibiting glutaminyl cyclase. The present invention also relates to pharmaceutical compositions containing a therapeutically effective quantity of the compound according to the invention.

Description

technical field [0001] The present invention relates to novel zinc complexes of γ-L-glutamyl histamine, which restore the barrier function of epithelial tissues and suppress abnormal activity of immune cells. The present invention also relates to the preparation of specific zinc complexes and their use in the treatment of atopic dermatitis and other diseases associated with impaired epithelial tissue barrier function and the occurrence of abnormal inflammatory responses. Background technique [0002] Epithelial barriers play crucial roles in human and animal organisms. The epithelial barrier prevents the penetration of various substances, allergens and bacteria into the internal environment of the body. Impaired barrier function of epithelial tissue contributes greatly to several diseases (e.g., oral inflammatory diseases (stomatitis, gingivitis, pharyngitis, etc.), gastrointestinal diseases (colitis, enteritis, intestinal autotoxicity, irritable bowel Irritation syndrome,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/037A61K38/05A61K31/315A61P17/00A61P37/08C07F3/06
CPCA61P37/00A61P17/00C07F3/06C07D233/64A61K33/30A61K31/417A61K2300/00A61K31/4164A61K31/555A61K31/315
Inventor 弗拉迪米尔·叶夫根尼耶维奇·涅博利辛
Owner OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOSTYU ZET TERAPEVTIKS
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