Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver

a carbostyril and derivative technology, applied in the direction of biocide, drug composition, metabolic disorder, etc., can solve the problems of insufficient treatment and few medicaments for treating nash, and achieve the effect of inhibiting the initial stage of nash, preventing and/or treating fatty liver, and preventing/treating nash

Inactive Publication Date: 2014-05-01
OTSUKA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The carbostyril derivative effectively reduces lipid droplets in the liver and serum triglyceride levels, demonstrating its potential in preventing and treating fatty liver and inhibiting the initial stages of NASH, as shown in model animal studies.

Problems solved by technology

In addition, there has been no / few medicament for treating NASH because NASH is a newly uprising disease.
Furthermore, the condition of NASH is thought to be composed of a variety of factors which are complicatedly related, and thus it is not enough to treat the disease with a single medicament, and usually plural medicaments must be used for the treatment.

Method used

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  • Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver
  • Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver
  • Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver

Examples

Experimental program
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[0032]Fisher 344 rats were fed only a general diet or a choline-deficiented, L-amino acid-defined (CDAA) diet to prepare a control group and a CDAA group as an animal model for fatty liver, respectively. Three Medicament-treated groups were prepared by administering the following three medicaments to the CDAA groups every day. (Aspirin and ticlopidine are medicaments having the same platelet aggregation inhibitiory action as cilostazol.)

[0033]6 mg / kg of cilostazol

[0034]5 mg / kg of aspirin

[0035]10 mg / kg of ticlopidine

Six weeks after the administration of medicaments started, livers of the rats in each medicament-treated group were taken out and stained with Hematoxylin-eosin staining and Masson staining, in which lipid droplets were observed. The results of the Hematoxylin-eosin staining are shown in FIG. 1-FIG. 5, and the results of the Masson staining are shown in FIG. 6-FIG. 9. According to these results, the lipid droplet of liver in the cilostazol-administration group (i.e. admin...

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Abstract

The invention relates to a medicament for preventing and / or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof.

Description

TECHNICAL FIELD[0001]The invention relates to a medicament for preventing and / or treating fatty liver. More particularly, it relates to a medicament for preventing and / or treating fatty liver which comprises as an active ingredient a carbostyril derivative of formula (1):wherein A is a lower alkylene group, R is a cycloalkyl group, the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond, or a salt thereof.BACKGROUND ART[0002]The carbostyril derivatives of formula (1) or salts thereof and the process for the preparation thereof are disclosed in JP-63-20235-B. And it is known that the carbostyril derivatives (1) have platelet aggregation inhibitiory action, phosphodiesterase (PDE) inhibition action, antiulcer, hypotensive action and antiphlogistic action, and are useful as an antithrombotic agent, a drug for improving cerebral circulation, an antiinflammatory agent, an antiulcer drug, an antihypertensive drug, an antiasthmatic drug, a phosp...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): C07D401/12
CPCC07D401/12A61K31/4709A61P1/16A61P3/06A61K31/41A61K31/4704
InventorNAKAJIMA, ATSUSHIFUJITA, KOJIYONEDA, MASATOMUKEDA, OSAMUICHIMURA, TAKAKO
OwnerOTSUKA PHARM CO LTD