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Compound for treating pulmonary fibrosis

A technology of pulmonary fibrosis and compounds, which is applied in the field of compounds for the treatment of pulmonary fibrosis, can solve problems such as no suggestion, no mention of compounds to treat other diseases, etc.

Active Publication Date: 2008-09-17
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the application does not mention that the compound can be used to treat other diseases, and there is no hint in this regard

Method used

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  • Compound for treating pulmonary fibrosis
  • Compound for treating pulmonary fibrosis
  • Compound for treating pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Effect of formula I compound on bleomycin-induced pulmonary fibrosis in mice

[0044] In normal ICR mice, a model of pulmonary fibrosis was established by tracheal instillation of bleomycin. After three days, the drug was administered once a day until 22 days. The lung tissue and body weight were measured to measure the lung index, and the pathological morphology was observed. The results show that the compound of formula I can obviously reduce the increase of lung index caused by modeling. See Table 1. After modeling, the animals developed moderate pulmonary fibrous tissue hyperplasia, accompanied by focal inflammatory cell infiltration. The compound of formula I has a better effect on improving pulmonary fibrosis and inflammatory cell infiltration induced by bleomycin. See figure 1 , figure 2 .

[0045] Table 1. The effect of the compound of formula I on the lung index of mice with pulmonary fibrosis caused by bleomycin

[0046]

[0047] ##P** P...

Embodiment 2

[0048] Example 2: Formula I compound is to bleomycin causing pulmonary fibrosis mouse hydroxyproline, malondialdehyde and glutathione The effect of content

[0049] Normal ICR mice were modeled by tracheal instillation of bleomycin, administered once a day after three days, until 22 days, the lung tissue was taken to measure the content of hydroxyproline (HYP) with a kit, and the content of proline was determined by TBA method. Aldehyde (MDA) content, glutathione (GSH) content was determined with a kit. The results show that the HYP content in the lung tissue increases after modeling, and the compound of formula I can reduce the increased HYP content. See Table 2. After modeling, the MDA content in lung tissue increases, and the compound of formula I can reduce the increased MDA content. See Table 3. After modeling, the content of GSH in the lung tissue is reduced, and the compound of formula I can increase the content of the reduced GSH. See Table 4.

[0050] Table 2...

Embodiment 3

[0059] Example 3: Effect of formula I compound on the content of transforming growth factor β in mice with pulmonary fibrosis induced by bleomycin

[0060] Transforming growth factor β (TGFβ) plays an important role in the pathogenesis of pulmonary fibrosis, so the effect of the compound of formula I on the content of TGFβ in lung tissue was observed. Normal ICR mice were modeled by tracheal instillation of bleomycin. After three days, the drug was administered once a day until day 22. The lung tissue was taken to make a 10% homogenate, and the supernatant was obtained by centrifugation. Determine its content according to the instructions of the TGFβ kit. Compounds of formula I reduce elevated levels of TGF[beta]. See Table 5.

[0061] Table 5. The effect of formula I compound on bleomycin-induced lung tissue TGFβ content in mice with pulmonary fibrosis

[0062]

[0063] #p** p<0.01, vs model group

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PUM

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Abstract

The invention discloses the usage of the compound in a structural formula I in preparing drugs preventing and / or treating lung fibrosis of mammalian. The drugs can be made into orally-taken administration formulation selected from tablet, capsule, powder, granule, crystal, solution, suspension, decoction, syrup, elixirs, tea and masticatory spasm and also can be made into inhale administration or insufflation administration, intranasal administration and transdermal administration or administration formulation selected from spray of nasal cavity, nasal drop, suspension, gel, ointment, cream, emulsion and powder.

Description

technical field [0001] The present invention relates to the compound of structural formula I (5-[(4-ethoxycarbonyl) piperidyl]-1-4-(chlorophenyl)-1-penten-3-one, C 19 h 24 o 3 NCl) in the preparation of medicines for preventing or treating pulmonary fibrosis. Background technique [0002] Compound chemical formula C is disclosed in Chinese patent application No.2004100705282 19 h 24 o 3 NCl, its preparation process, its pharmaceutical composition, and its application in treating or preventing inflammation. The effective dose used in anti-inflammatory animal experiments is 10-100mg.kg -1 . [0003] [0004] Structural Formula I [0005] However, the application does not mention that the compound can be used to treat other diseases, and there is no suggestion in this regard. Contents of the invention [0006] After a lot of experimental research, the inventors found that the compound has great potential in preventing or treating pulmonary fibrosis. [0007] Ther...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61P11/00
Inventor 王文杰彭珊瑛王霖刘洋欧阳雪宇韩文阳朱莉亚黄海洪
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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