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Application of pyrazolidinyl compounds in preparation of preparations used for treating dermatitis

A technology of pyrazolidine and compounds, applied in the application field of pyrazolidine compounds in the preparation of preparations for treating dermatitis, which can solve problems such as drug resistance, recurrence of dermatitis symptoms, and reddened skin

Pending Publication Date: 2020-04-17
苏州安康盟医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, despite their proven clinical efficacy, steroid-based formulations (eg, topical corticosteroid formulations) cause many side effects, such as excessive skin thinning, atrophy, so-called "moon face" caused by facial fat deposits, skin Redness, hirsutism and stretch marks etc.
In addition, when patients use steroids for a long period of time, their bodies often develop resistance to these drugs, and dermatitis symptoms may even recur in a more aggressive form
[0004] The literature "Cancer Res 2007; 67:(19).October 1, 2007" and US60738242 disclose that pyrazolidinyl compounds can be used as ubiquitin activating enzyme (E1) inhibitors and applied in the treatment of cancer. Such compounds can Whether there are other new uses, according to the existing public technology is still unknown

Method used

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  • Application of pyrazolidinyl compounds in preparation of preparations used for treating dermatitis
  • Application of pyrazolidinyl compounds in preparation of preparations used for treating dermatitis
  • Application of pyrazolidinyl compounds in preparation of preparations used for treating dermatitis

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Experimental program
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Effect test

preparation example Construction

[0038] The preparation method of above-mentioned emulsifiable paste is as follows:

[0039] A (oil phase): Weigh or measure white vaseline, glyceryl monostearate, stearic acid, ethylparaben, 2,6 tert-butyl p-phenol and liquid paraffin into a No. 1 beaker, and put 1 The beaker was heated to 80°C and stirred to completely dissolve the substances.

[0040] B (water phase): Weigh or measure distilled water, glycerin, triethanolamine, and sodium 12 alkylsulfonate respectively into the No. 2 beaker, heat the No. 2 beaker to 75° C. and stir to completely dissolve each substance.

[0041] C: Dissolve PY-41 in an appropriate amount of ethanol, slowly add A (oil phase) into B (water phase), stir in the same direction while adding, wait until the temperature drops to 60°C, add C, and stir evenly to room temperature to obtain the PY-41 drug cream.

Embodiment 1

[0044]The HaCaT cells cultured in vitro were stimulated with TNF-α for 1 hour, and then treated with PYR-41 for 6 hours, the cells were collected, total RNA was extracted, and the levels of pro-inflammatory cytokines TNF-α and IL-1 were detected by Real-time PCR , and found that: PYR-41 can dose-dependently reduce the expression of TNF-α and IL-1 within the dose range of 0-50uM.

[0045] HaCaT cells cultured in vitro were stimulated with TNF-α for 30 min, and then HaCat cells were treated with PYR-41 (0 μM, 25 μM, 50 μM) in a concentration gradient for 30 min, and Western blot was used to detect the expression of different components in the NF-κB signaling pathway in the cells Condition. Such as figure 1 As shown in C, the results show that PYR-41 can inhibit the phosphorylation of p65 in a concentration gradient and reduce the activation level of IKBA. As the concentration increases, the effect of PYR-41 on reducing the activation level of IKBA is more significant ( figure ...

Embodiment 2

[0047] Induction of dermatitis and eczema: use a hair clipper on the back of the mouse no less than 2×2cm 2 Area shaving. The sensitization was performed one or two days after the skin preparation to reduce the stimulation of the skin preparation on the back of the mice.

[0048] Because MFG (compound dexamethasone acetate cream), hereinafter referred to as MFG, has anti-inflammatory and anti-allergic effects, it is therefore used as the positive drug group in the experiment. On the first day of the experiment (Day 1), the mice were randomly divided into four groups, 5 in each group, namely the normal group (Normal), the model control group (Model), the administration group (PY-41) and the positive drug control group (MGF). The backs of the mice in the model control group, drug treatment group and positive control group were shaved and daubed with 7% DNCB solution 100 μL / mouse for sensitization (50 μL / time), and the normal control group was daubed with the same amount of sol...

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Abstract

The invention relates to application of pyrazolidinyl compounds and pharmaceutically acceptable salts, solvates or hydrates thereof in preparation of preparations used for treating dermatitis. The structural formula of the pyrazolidinyl compounds is as shown in formula (1) which is described in the specification. In the formula (1), each X is independently selected from a group consisting of O, Sand NR<1>; R<1> is selected from the group consisting of H, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aralkyl group, a heteroaralkyl group, -C(O)R,-C(O)OR and -C(O)NR<2>; R<2> is selected from the group consisting of H, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aralkyl group and a heteroaralkyl group; R<2> is selected from the groupconsisting of H, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a nitro group and halogen; Z is H, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, anaralkyl group, a heteroaralkyl group, an aryl group, a heteroaryl group, halogen, -C(O)R<3>, -C(O)OR<3>, -C(O) SR<3>, -C(O)NR<3>R<4>, -C(S)OR<3>, -C(NR1)OR<3> or -C (NR<1>)NR<3>R<4>; and n is any integer in a range of 0 to 5.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of a pyrazolidinyl compound in the preparation of preparations for treating dermatitis. Background technique [0002] As we all know, dermatitis is a common disease in dermatology. The etiology and pathogenesis of dermatitis are not yet clear. The etiology is quite complicated, and most of them are caused by allergies. It is an allergic reaction caused by the interaction of various internal and external factors. But some dermatitis has nothing to do with allergies. [0003] Common current treatment for dermatitis involves identifying and preventing factors that may trigger or exacerbate inflammation, along with good skin care, which is almost always combined with the use of medications appropriate to treat the symptoms of the disease. Among the drugs, steroid preparations are usually used. However, despite their proven clinical efficacy, steroid-based formulations (eg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4155A61P29/00A61P17/00
CPCA61K31/4155A61P29/00A61P17/00
Inventor 杨义力王群
Owner 苏州安康盟医疗科技有限公司
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