Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Reexamination Certificate
2000-06-30
2001-08-14
Ambrose, Michael G. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
C558S192000
Reexamination Certificate
active
06274571
ABSTRACT:
TECHNICAL FIELD
The present invention relates to an agent for preventing and curing fatty liver and to a method for curing thereof.
BACKGROUND ART
Fatty liver is a diseased state of the liver wherein lipids, mainly neutral fats (triglycerides, TG) are accumulated excessively in the liver, thus fatty vacuoles are observed in about more than a half number of the liver cells. As to the cause of fatty liver, there are reported various pathogenics such as obesity, diabetes mellitus, alcoholic intake, oxygen deficit, endocrinic disorder, exogenic toxins or medicines, endogenic toxins and the like. Particularly, along the recent trend on increasing of obesity, a number of patients with supervenient fatty liver are also increasing. Said fatty liver is necessarily treated at the early stage, because after all this disease may be migrated to severe hepatopathies, such as hepatitis, hepatic cirrhosis and the like, finally such instances are not seldom to court death. However, at the present, an agent effective for curing fatty liver has not been known yet, and dietetic therapy is only known as a general therapy. Thus development of a medicine capable to prevent and cure fatty liver satisfactorily and effectively is earnestly desired.
Heretofore, the present inventors have conducted an extensive research work regarding effective ingredient compounds used for pharmaceuticals. Then in the course of research work, previously the inventors have found the fact that a series of carboxylic acid amide derivatives are effective as antiinflammatory agent and calcium antagonistic agent, then invention relating to said derivatives was completed and patent applications were filed (JP-A-61-151199 and EP-A-273444).
Further, the present inventors have additionally found the fact that other carboxylic acid amide derivatives relating to the above-mentioned carboxylic acid amide derivatives have excellent activity for lowering lipids, and are excellent in low toxicity regarding side-effects etc., thus the latter carboxylic acid amide derivatives are useful agents for curing hyperlipidemia, and also for preventing and curing various diseases (hyperlipidemia), such as hypercholesteremia, hypertriglyceridemia, hyperphospholipidemia, hyper-free fatty acidemia and the like. Then an invention on the basis of such finding was filed as a patent application (Japanese Patent No. 2584336).
Additionally, the present inventors have found the facts that, other than the useful activity for curing hyperlipidemia, the above-mentioned carboxylic acid amide derivatives also have activity for inhibiting excretion of proteinurea, thus these derivatives are effective as agents for curing nephritis, then an invention on the basis of such finding was filed as a patent application (Japanese Patent Application Hei 9-93002).
DISCLOSURE OF THE INVENTION
An object of the present invention is to develop novel pharmaceutical applications of the above-mentioned carboxylic acid amide derivatives by using their excellent properties such as low toxicities. Particularly the present invention is aimed to provide an agent for preventing and curing fatty liver and method for curing thereof.
The present inventors have conducted an extensive research work followed by the above-mentioned object. As the result, regardless of the excellent pharmaceutical applications for curing hyperlipidemia and nephritis performed by the above-mentioned compound, unexpectedly the inventors have found novel knowledges from the above-mentioned pharmacological activities, that the above-mentioned carboxylic acid amide derivatives have activities for lowering neutral fats (triglycerides, TG) and total cholesterols in the liver, also effective for preventing and curing fatty liver. Thus, the present invention was completed on the basis of said novel knowledges.
MEANS FOR SOLVING THE PROBLEM
The present invention relates to an agent for preventing and curing fatty liver containing, as the effective ingredient, a carboxylic acid amide derivative represented by the general formula (1),
(wherein R is a lower alkyl group; and X is a halogen atom), and to a method for curing thereof by administering said agent.
As explained previously, the carboxylic acid amide compound represented by the above-mentioned general formula (1), which is contained as the effective ingredient in the agent for preventing and curing fatty liver and method for curing fatty liver according to the present invention, possesses activity for lowering neutral fats (triglycerides, TG) and cholesterols in the blood. Therefore, said compound is known as effective for curing hyperlipidemia by the present inventors (JP-A-3-68592). However, such activity is understood rather contrary to the activity for inhibiting accumulation of neutral fats in the liver or lowering cholesterols in the liver for preventing and curing fatty liver.
In fact, among compounds having activity for lowering neutral fats and cholesterols in the blood and used as agents for curing hyperlipidemia, for example “clofibrate”, it is known to cause accumulation of neutral fats in the liver as a side-effect and induces hepatomegaly (cf., e.g., JP-A-8-119860).
On the basis of such findings, the present invention was completed surprisingly and contrary to the previous knowledge, although the compound represented by the above-mentioned general formula (1) possesses activity for lowering neutral fats and cholesterols in the blood, said compound also possesses activity for inhibiting both accumulation of fats in the liver and activity for lowering cholesterols in the liver, thus the compound performs desired effects for preventing and curing fatty liver.
REFERENCES:
patent: 4822780 (1989-04-01), Tsuda et al.
patent: 0 402 033 B1 (1995-10-01), None
patent: 61-151199 (1986-07-01), None
patent: 3-68592 (1991-03-01), None
patent: 10-265387 (1998-10-01), None
The Merck Manual of Diagnosis and Therapy. Seventeenth Edition. Merck & Co., Inc., 1999. Mark H. Beers, M.D., and Robert Berkow, M.D., eds; Internet Edition, Section 4, Chapter 39. http://www.merck.com/pubs/mmanual/section4/chapter39/39a.htm.*
JP Patent Abstract, 10265387, Oct. 6, 1998.
Inoue Yasuhide
Tsutsumi Kazuhiko
Ambrose Michael G.
Otsuka Pharmaceutical Factory Inc.
Sughrue Mion Zinn Macpeak & Seas
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