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Mmp-2 and/or mmp-9 inhibitor

A technology of MMP-9 and MMP-2, applied in the direction of anti-inflammatory agent, anti-toxic agent, anti-viral agent, etc., to achieve the effect of high safety

Inactive Publication Date: 2011-02-09
OTSUKA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, it is not yet known that the thiazole derivatives represented by the above general formula (1) or salts thereof have MMP-2 and / or MMP-9 inhibitory effects that are completely different from the above pharmacological effects.

Method used

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  • Mmp-2 and/or mmp-9 inhibitor
  • Mmp-2 and/or mmp-9 inhibitor
  • Mmp-2 and/or mmp-9 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0050] Compound A 150g

[0051] Avicel (trade name, manufactured by Asahi Kasei Co., Ltd.) 40g

[0052] Cornstarch 30g

[0053] Magnesium Stearate 2g

[0054] Hypromellose 10g

[0055] Macrogol 6000 3g

[0056] Castor oil 40g

[0057] Ethanol 40g

[0058] After compound A, Avicel, cornstarch and magnesium stearate were mixed and ground, the resulting mixture was compressed into tablets with a sugar-coated R10mm punch. The obtained tablet is coated with a coating agent containing hydroxypropylmethylcellulose, polyethylene glycol 6000, castor oil and ethanol to prepare a film-coated tablet.

preparation example 2

[0060] Compound A 150g

[0061] Citric acid 1.0g

[0062] Lactose 33.5g

[0063] Calcium hydrogen phosphate 70.0g

[0064] Pluronic F-68 30.0g

[0065] Sodium Lauryl Sulfate 15.0g

[0066] Polyvinylpyrrolidone 15.0g

[0067] Polyethylene glycol (Carbowax 1500) 4.5g

[0068] Polyethylene glycol (Carbowax 6000) 45.0g

[0069] Cornstarch 30.0g

[0070] Dry sodium stearate 3.0g

[0071] Dry magnesium stearate 3.0g

[0072] Proper amount of ethanol

[0073] Compound A, citric acid, lactose, dibasic calcium phosphate, Pluronic F-68, and sodium lauryl sulfate were mixed.

[0074] The resulting mixture was passed through a No. 60 sieve, and the sieved mixture was subjected to wet granulation with an ethanol solution containing polyvinylpyrrolidone, Carbowax 1500 and Carbowax 6000. Ethanol is added to the resulting wet granulated powder as needed to make the powder a paste-like mass. Next, cornstarch was added to the resulting paste mass and mixing continued until uniform p...

preparation example 3

[0077] Compound A 5g

[0078] Polyethylene glycol (molecular weight: 4000) 0.3g

[0079] Sodium chloride 0.9g

[0080] Polyoxyethylene sorbitan monooleate 0.4g

[0081]Sodium metabisulfite 0.1g

[0082] Methylparaben 0.18g

[0083] Propylparaben 0.02g

[0084] Distilled water for injection 10.0ml

[0085] The parabens, sodium metabisulfite, and sodium chloride were dissolved in about half of the above-mentioned distilled water at 80° C. while stirring. The resulting solution was cooled to 40 °C. Then, Compound A, followed by polyethylene glycol and polyoxyethylene sorbitan monooleate were dissolved in the above solution. Add another half volume of distilled water for injection to the resulting solution to make up the final volume. Using an appropriate filter paper, the resulting solution is sterile-filtered, thereby performing sterilization to prepare an injection.

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Abstract

The present invention provides a highly safe pharmaceutical preparation effective for diseases caused by MMP-2 and / or MMP-9. The pharmaceutical preparation contains, as an active ingredient, at least one member selected from the group consisting of thiazole derivatives represented by Formula (1): wherein R1 represents a phenyl group that may have 1 to 3 lower alkoxy groups as substituents on the phenyl ring, and R2 represents a pyridyl group that may have 1 to 3 carboxyl groups as substituents on the pyridine ring, and salts thereof. Such thiazole derivatives have MMP-2 and / or MMP-9 inhibitory activity.

Description

technical field [0001] The present invention relates to a matrix metalloproteinase (hereinafter referred to as "MMP")-2 and / or MMP-9 inhibitor. Background technique [0002] Matrix metalloprotease (matrix metalloprotease) is a general term for extracellular matrix degrading enzymes containing zinc (II) ions in the active site. Extracellular matrix metabolism is mainly regulated by the balance between MMP and tissue inhibitor of metalloprotease (TIMP) (tissue inhibitor of metalloproteiase) which acts specifically on MMP. [0003] MMP is composed of more than 10 kinds of enzymes, such as collagenase (MMP-1 and MMP-8), stromelysin (MMP-3), gelatinase (MMP-2 and MMP-9), etc. formed in cells. [0004] Among the above-mentioned MMPs, the gelatinase group (MMP-2 and MMP-9) is known not only to have gelatin-degrading activity but also to degrade type IV collagen, fibronectin, vitronectin, and the like. [0005] However, agents capable of inhibiting MMP-2 and / or MMP-9, useful for ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P11/00A61K31/4439
CPCA61K31/4439A61P1/00A61P1/02A61P1/04A61P11/00A61P11/06A61P13/10A61P13/12A61P17/00A61P17/02A61P17/06A61P19/00A61P19/02A61P19/10A61P25/00A61P25/08A61P25/28A61P27/02A61P27/16A61P29/00A61P3/00A61P31/04A61P31/12A61P31/18A61P33/02A61P33/06A61P35/00A61P35/02A61P35/04A61P37/06A61P37/08A61P39/02A61P43/00A61P7/00A61P7/06A61P9/00A61P9/04A61P9/10A61P9/12A61P3/10Y02A50/30
Inventor 凑口信也大野康薮内洋一殊才孝则长本尚
Owner OTSUKA PHARM CO LTD