Application of compound in treatment of autoimmune skin diseases caused by inflammation

An autoimmune and compound technology, which is applied in the application field of compounds in the treatment of autoimmune skin diseases caused by inflammation, and can solve problems such as adverse reactions, large toxic and side effects, and poor curative effect

Pending Publication Date: 2020-10-30
GENEROS BIOPHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In order to solve the defects of poor curative effect, more adverse reactions, large toxic and side effects, lack of safety and drug resistance in the prior art for the treatment of diseases such as autoimmune skin diseases caused by inflammation (such as non-specific dermatitis such as psoriasis) , the present invention provides a compound Nib1, its pharmaceutically acceptable salt, its solvate, its pharmaceutically acceptable salt solvate, or its crystal form in the preparation of the treatment of autoimmune skin caused by inflammation disease, improve skin rash, improve skin peeling, reduce skin thickening, reduce epidermal hyperplasia, improve vasodilation and / or reduce immune cell infiltration

Method used

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  • Application of compound in treatment of autoimmune skin diseases caused by inflammation
  • Application of compound in treatment of autoimmune skin diseases caused by inflammation
  • Application of compound in treatment of autoimmune skin diseases caused by inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0175] Embodiment 1 (treatment of psoriasis by oral Nib1):

[0176] 1. Experimental reagents:

[0177] 5% imiquimod ointment, Aldara, 3M Pharmaceuticals; dexamethasone ointment: Shanghai Sanjiu Pharmaceutical; PEG300, Sigma, product number 90878. Nib1(pimozide):Sigma(P1793).

[0178] 2. Experimental plan:

[0179] Female BALB / c mice (purchased from Shanghai Shrek Experimental Animal Company, administered at the age of 6 weeks) were randomly divided into groups after acclimating to the environment. Except for the normal control group, the rest of the animals received imiquimod ointment (5%) External treatment was used to induce the establishment of psoriasis model. The specific method is to shave off the same area of ​​hair on the back of the mice, and apply 62.5 mg of imiquimod ointment daily for seven consecutive days. Animals received different treatment regimens, weighed daily, took orally or externally administered drugs once, and observed disease progression scores. ...

Embodiment 2

[0212] Embodiment 2 (therapeutic effect of Nib1 preparation for external use on animal psoriasis disease model):

[0213] 1. Experimental reagents:

[0214] 5% imiquimod ointment, Aldara, 3M Pharmaceuticals, H20160079; dexamethasone ointment: Shanghai Sanjiu Pharmaceutical. Cetostearyl alcohol was purchased from Hunan Erkang Pharmaceutical, F20170000297.

[0215] 2. Topical preparations:

[0216] There are two formulations designed for external application, and the formulation FLL-15-21-2 is shown in Table 8.

[0217] Table 8: FLL-15-21-2 formulation composition

[0218]

[0219]

[0220] The technical process of the above-mentioned external application formulation FLL-15-21-2:

[0221] 1) Weigh the prescribed amount of API, put it in a beaker, and then add the prescribed amount of acetic acid. When adding, the acetic acid just covers the API powder, and the whole changes from white solid to crystal, which is slightly viscous; then add the prescribed amount of two In ...

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Abstract

The invention discloses application of a compound Nib1, a pharmaceutically acceptable salt, a solvate, a solvate of the pharmaceutically acceptable salt or a crystal form thereof in preparation of a medicine for treating autoimmune skin diseases caused by inflammation, improving skin erythema, improving skin decrustation, reducing skin thickening, reducing epidermal hyperplasia, improving angiectasis and/or reducing immune cell infiltration. The chemical formula of the Nib1 is C28H29F2N3O. The compound provided by the invention is a new treatment mechanism aiming at autoimmune skin diseases (such as psoriasis diseases) caused by inflammation, is small in side effect and convenient in administration route, can achieve the balance of safety and effectiveness, can be used for a long time, andimproves the life quality of patients. The compound can significantly improve clinical symptoms of autoimmune skin diseases caused by inflammation, such as erythema cutanea, skin peeling, skin thickening, epidermal hyperplasia, improve angiectasis and reduce immune cell infiltration and the like.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a compound Nib1, a pharmaceutically acceptable salt thereof, a solvate thereof, a solvate of a pharmaceutically acceptable salt thereof, or its crystal form in the preparation of the treatment of self-infection caused by inflammation Application in drugs for immune skin diseases, improvement of skin rash, improvement of skin peeling, reduction of skin thickening, reduction of epidermal hyperplasia, improvement of vasodilation and / or reduction of immune cell infiltration. Background technique [0002] Pimozide (C 28 h 29 f 2 N 3 O, Pimozide) is a diphenylbutazone antipsychotic. The effect is similar to that of haloperidol, but the effect is weaker and takes a long time, and it only needs to be taken orally once a day. It has good effects on mania, hallucinations, delusions, apathy and withdrawal, and is especially suitable for patients with chronic Tourette's syndrome. This p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61P17/06
CPCA61K31/454A61P17/06A61P17/00A61P37/00A61K9/0014A61K9/06A61K45/06A61K47/10A61K47/14A61K47/20A61K47/26A61K2300/00A61K9/0053A61K9/08C07D235/26
Inventor 傅新元陆费成晨刘新宇周轶
Owner GENEROS BIOPHARMA LTD
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