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Method and pharmaceutical composition for inhibiting invasion and/or metastasis of ovarian carcinoma

a technology of ovarian cancer and composition, which is applied in the direction of drug compositions, antibacterial agents, biocide, etc., can solve problems such as pathological consequences

Inactive Publication Date: 2003-10-23
HSU LI WEI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011] The compound of formula (I), preferably Compound 1, exhibits an inhibitory effect on matrix metalloproteinases, particularly gelatinase, and more particularly matrix metalloproteinase-2 (gelatinase A) and on the binding of TNF.alpha. to TNF.alpha.-RI, and thus is useful in the prevention or treatment of MMPs-related disorders and TNF.alpha.-related disorders, alone or simultaneously.
[0011] The compound of formula (I), preferably Compound 1, exhibits an inhibitory effect on matrix metalloproteinases, particularly gelatinase, and more particularly matrix metalloproteinase-2 (gelatinase A) and on the binding of TNF.alpha. to TNF.alpha.-RI, and thus is useful in the prevention or treatment of MMPs-related disorders and TNF.alpha.-related disorders, alone or simultaneously.

Problems solved by technology

Even if TNF.alpha. has undoubtedly a beneficial function in the activation of host defense, its unregulated production (mainly on the systematic level) could lead to pathological consequences.

Method used

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  • Method and pharmaceutical composition for inhibiting invasion and/or metastasis of ovarian carcinoma
  • Method and pharmaceutical composition for inhibiting invasion and/or metastasis of ovarian carcinoma
  • Method and pharmaceutical composition for inhibiting invasion and/or metastasis of ovarian carcinoma

Examples

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Embodiment Construction

[0030] The compound of formula I can be administered via a variety of different routes including orally and parenterally. This compound can be combined with, for example, a pharmaceutically acceptable excipient or diluent depending on an administration route thereby to form a medicinal formulation.

[0031] The compound of formula I can be administered in a variety of dosage forms. Examples of dosage forms for oral administration include, but not limited to, tablet, capsule, powder, granule, solution, suspension, syrup and elixir.

[0032] The compound of formula I can be formulated with a binder, a disintegrating agent, a lubricant, a diluent, a buffer, a wetting agent, a preservative and / or a flavor by a known method into tablets, capsules, powders, granules, solutions or suspensions. Examples of the binder include crystalline cellulose, cellulose derivatives, cornstarch and gelatin. Examples of the disintegrating agent include cornstarch, potato starch and sodium carboxymethylcellulose...

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PUM

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Abstract

The invention discloses a compound of the general formula (I) wherein X is selected from the group consisting of -(CH2)nOH, -(CH2)nNH2, -(CH2)nSH, -(CH2)mCOOH, -(CH2)mCOOR, -(CH2)mCONH2, -(CH2)m''CONH-OH, (CH2)m''CONH-R, and -(CH2)n'O(PO3)m''<(m''+1)>, wherein n=2, 3, 4 or 5; n'=2 or 3; m=1, 2, 3 or 4; m'=1, 2, 3, 4, 5 or 6; m''=1, 2 or 3; and R=-Cm'H2m'+1, or an aryl group, especially 1-[3,4-dihydroxy-5-(2-hydroxyethyl)-tetrahydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione, methods for treating or preventing MMP-related disorders and TNFalpha-related disorders alone or simultaneously, methods for the inhibition of the invasion and / or metastasis of ovarian carcinoma, and pharmaceutical compositions containing said compound for said treatments.

Description

[0001] This is a continuation-in-part application claiming the benefit of application Ser. No. 10 / 080,662 filed Feb. 25, 2002.[0002] The present invention relates to novel compounds that are useful in pharmaceutical applications for inhibiting the function of proteins. More specifically, the present invention relates to inhibitors of both of matrix metalloproteinase and tumor necrosis factor. The present invention also relates to methods for treating or preventing MMP-related disorders and TNF.alpha.-related disorders alone or simultaneously; a method for inhibiting invasion and / or metastasis of carcinomas, particularly ovarian carcinoma; and pharmaceutical compositions for the above treatments.[0003] Description of Related Art[0004] Matrix metalloproteinases (MMPs) is constituted of at least 28 zinc-containing proteolytic enzymes that play an integral role in the physiology of the extracellular matrix (ECM). MMPs play a major role in the degradation of basement membrane and the rem...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/70C12N9/99A61K31/7072A61P31/04A61P31/12A61P35/00A61P43/00C07H19/06
CPCY10S930/144A61K31/70A61P19/02A61P29/00A61P31/04A61P31/12A61P35/00A61P43/00
Inventor HSU, LI-WEICHANG, SU-CHEN
Owner HSU LI WEI
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