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WO2007105286A1 - Agent reduisant la lipidemie - Google Patents

Agent reduisant la lipidemie Download PDF

Info

Publication number
WO2007105286A1
WO2007105286A1 PCT/JP2006/304862 JP2006304862W WO2007105286A1 WO 2007105286 A1 WO2007105286 A1 WO 2007105286A1 JP 2006304862 W JP2006304862 W JP 2006304862W WO 2007105286 A1 WO2007105286 A1 WO 2007105286A1
Authority
WO
WIPO (PCT)
Prior art keywords
lowering agent
blood
blood lipid
compound
cholesterol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2006/304862
Other languages
English (en)
Japanese (ja)
Inventor
Kazuhiro Anabuki
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agro Kanesho Co Ltd
Original Assignee
Agro Kanesho Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Agro Kanesho Co Ltd filed Critical Agro Kanesho Co Ltd
Priority to PCT/JP2006/304862 priority Critical patent/WO2007105286A1/fr
Publication of WO2007105286A1 publication Critical patent/WO2007105286A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/02—Halogenated hydrocarbons
    • A61K31/035—Halogenated hydrocarbons having aliphatic unsaturation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the present invention relates to a blood lipid lowering agent containing perchloro 1,1′-bicyclocyclopenter 2,4 gen, particularly a blood cholesterol lowering agent.
  • Perchloro 1,1'-bicyclocyclopenter 2, 4 gen (hereinafter also referred to simply as "the present compound") is a known compound and is called dienochlor. Known as.
  • this compound has a function of lowering blood lipids, particularly blood cholesterol.
  • the present invention provides a blood lipid lowering agent that lowers cholesterol and phospholipid among lipids in blood (particularly cholesterol, neutral lipid and phospholipid) without causing serious side effects.
  • the purpose is to provide.
  • This compound has a function of lowering blood cholesterol particularly in patients with hypercholesterolemia and high cholesterol concentration in blood, and is an excellent blood cholesterol lowering agent.
  • the present inventors have studied the action of the above-mentioned perchloro 1,1'-bicyclocyclopentater 2, 4 gen known as an acaricide, and surprisingly, the present compound is found in animals. It has been found that it has an action of lowering lipids in blood, particularly blood cholesterol. The present inventor has completed the present invention based on this new knowledge.
  • the present invention relates to a blood lipid lowering agent containing perchloro 1,1′-bicyclocyclopenter 2,4 gen as an active ingredient, particularly a blood cholesterol lowering agent (hereinafter referred to as “blood lipid lowering”).
  • a blood lipid lowering agent containing perchloro 1,1′-bicyclocyclopenter 2,4 gen as an active ingredient, particularly a blood cholesterol lowering agent (hereinafter referred to as “blood lipid lowering”).
  • blood lipid lowering a blood cholesterol lowering agent
  • the blood lipid lowering agent of the present invention has an excellent effect of lowering blood lipid in mammals. Therefore, the present invention is excellent in the treatment of hyperlipidemia and is useful for the treatment and prevention of myocardial infarction, cerebral infarction, peripheral artery occlusion, arteriosclerosis and the like caused by hyperlipidemia.
  • perchloro 1,1′-bicyclocyclopenter 2,4 gen is a known compound, and is described in, for example, US Pat. No. 2,908,723 and US Pat. No. 2,934,470. .
  • This compound is, for example, the following reductive dimerization with hydrogen in the presence of a catalyst of the following compound II (hexachlorocyclopentagen), which is readily available in the field. Therefore, it can be easily prepared.
  • examples of the catalyst include noble metals of group VIII of the periodic table, such as
  • the present compound can be easily obtained in the factory as dienochlor. Further, the purification method is obvious to those skilled in the art. For example, dienochlor can be obtained in high purity by purifying it by recrystallization or column chromatography.
  • test substance was filled into gelatin capsules at a weight of 8, 40 and 200 mgZKg body weight and administered orally once daily to 4 male and 4 female beagle dogs.
  • empty gelatin capsules were administered as in the test animals.
  • the cholesterol value was calculated by an enzymatic method.
  • Phospholipids were calculated by an enzymatic method.
  • A1 is an average cholesterol value or phospholipid value in the control group
  • A2 is a corresponding value after elapse of a predetermined period.
  • the rate of cholesterol reduction is as shown in Table 1 below.
  • the amount of blood cholesterol in the control group was 155 to 192 mgZdl.
  • the amount of blood phospholipid in the control group was 324 to 377 mg Zdl.
  • the blood concentration of cholesterol and phospholipids greatly decreases depending on the dose in the number of days after administration.
  • the dose exceeds 3 days at 3 mg / K, the reduction effect is prominent. This effect is also seen in female test animals. It can also be seen that it is not particularly affected by males.
  • this compound acts as a blood lipid lowering agent or blood cholesterol lowering agent on mammals including humans as they are or mixed with excipients.
  • This compound can be administered in the form of tablets, granules, powders, injections, percutaneous absorptions, etc., which are not limited to capsules, either as oral or parenteral dosage forms. it can.
  • the dose of this compound can be appropriately varied depending on the degree of symptoms, age, weight, dosage form and the like. In general, it is 0.1 to 1000 mg / Kg body weight / day, preferably 2 to 500 mg / Kg body weight / day, particularly preferably 3 to 250 mg / Kg body weight / day per day.
  • the administration can be performed once or divided into several times.
  • any additive can be used depending on the dosage form.
  • excipients include lactose, excipients such as mannitol, crystalline cellulose, and dampener, lubricants such as magnesium stearate and talc, hydroxypropylcellulose calcium, low-substituted hydroxypropyl, and the like.
  • a disintegrating agent such as methylcellulose, a coating agent such as hydroxypropylmethylcellulose, macrogol, Eudragit, and silicone resin can be appropriately blended as necessary.
  • Capsule shell (gelatin capsule)
  • the present invention provides an excellent blood lipid lowering agent or blood cholesterol lowering agent that does not cause serious side effects.

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne un agent réduisant la lipidémie ou un agent réduisant la cholestérolémie, doté d'un excellent effet et n'étant associé à aucun effet indésirable grave. Ces agents contiennent en tant que principe actif le perchloro-1,1'-bicyclopenta-2,4-diène.
PCT/JP2006/304862 2006-03-13 2006-03-13 Agent reduisant la lipidemie Ceased WO2007105286A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/JP2006/304862 WO2007105286A1 (fr) 2006-03-13 2006-03-13 Agent reduisant la lipidemie

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/JP2006/304862 WO2007105286A1 (fr) 2006-03-13 2006-03-13 Agent reduisant la lipidemie

Publications (1)

Publication Number Publication Date
WO2007105286A1 true WO2007105286A1 (fr) 2007-09-20

Family

ID=38509137

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2006/304862 Ceased WO2007105286A1 (fr) 2006-03-13 2006-03-13 Agent reduisant la lipidemie

Country Status (1)

Country Link
WO (1) WO2007105286A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2934470A (en) * 1955-06-27 1960-04-26 Hooker Chemical Corp Insecticidal perchlorocarbon
JP2006083074A (ja) * 2004-09-14 2006-03-30 Agro Kanesho Co Ltd 血中脂質低下剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2934470A (en) * 1955-06-27 1960-04-26 Hooker Chemical Corp Insecticidal perchlorocarbon
JP2006083074A (ja) * 2004-09-14 2006-03-30 Agro Kanesho Co Ltd 血中脂質低下剤

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ISHIKAWA T. ET AL.: "Effects of Chlorinated Hydrocarbons on Plasma alpha-Lipoprotein Cholesterol in Rats", METABOLISM, vol. 27, no. 1, 1978, pages 89 - 96, XP026300647, DOI: doi:10.1016/0026-0495(78)90127-0 *
MADHUKAR B.V. ET AL.: "Comparison of Induction Patterns of Rat Hepatic Microsomal Mixed-Function Oxidases by Pesticides and Related Chemicals", PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY, vol. 11, no. 1-3, 1979, pages 301 - 308, XP024867135, DOI: doi:10.1016/0048-3575(79)90070-1 *

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