Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1995-09-06
1998-02-17
Ivy, C. Warren
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
562 13, C07F 940, C07F 938
Patent
active
057193037
DESCRIPTION:
BRIEF SUMMARY
This is the U.S. National Stage application of PCT/JP94/00354 filed Mar. 4, 1994 published as WO94/20508 Sep. 15, 1994.
1. Field of the Invention
The present invention relates to a novel phosphonic acid derivative and a pharmacologically acceptable salt thereof. More particularly, it relates to a phosphonic acid derivative and a pharmacologically acceptable salt thereof which are useful as a medicine, a use of the phosphonic acid derivative or the pharmacologically acceptable salt thereof and a method for medically treating a disease which comprises administering a therapeutically effective amount of the phosphonic acid derivative or the pharmacologically acceptable salt thereof to a patient.
2. Description of the Related Art
Ischemic heart diseases such as myocardial infarction still account for a high proportion of the death causes of the middle-aged and the elderly. Ischemic heart diseases are known to be induced by hyperlipemia which is a primary factor of atherosclerosis which is one of the adult diseases. Accordingly, the medical treatment of hyperlipemia which is a stage precedent to ischemic heart diseases such as myocardial infarction is essential, so that studies have been made for many years to develop an excellent therapeutic medicine for hyperlipemia.
Recently, an HMG-CoA reductase inhibitor has been developed as a therapeutic medicine for hyperlipemia and has been ascertained to have an excellent cholesterol level lowering activity. However, this inhibitor also hinders the biosynthesis of CoQ.sub.10 or dolichol, so that it is in danger of causing adverse effects such as cardiac hypofunction, muscle ache and infirmity. Meanwhile, a desmosterol reductase inhibitor, which is also a therapeutic medicine for hyperlipemia, also causes a serious adverse effect such as cataract owing to the accumulation of desmosterol.
Under these circumstances, it is still expected to develop a therapeutic medicine for hyperlipemia which is free from the above adverse effects and has an excellent cholesterol level lowering activity.
Under the above circumstances, the present inventors have started the search and studies for a medicine having a squalene synthetase inhibiting action and have found that a specific phosphonic acid derivative can attain the object. The present invention has been accomplished on the basis of this finding.
Although phosphorus-containing hydrocarbon compounds useful as medicines are disclosed in Japanese Patent Publication-A Nos. 56492/1990 and 138288/1990, these compounds are different from those of the present invention in both structure and drug efficacy. Further, phosphorus-containing isoprenoid derivatives useful as medicines are also disclosed in Japanese Patent Publication-A Nos. 101088/1990 and 235821/1990. However, these derivatives are different from those of the present invention in structure.
Constitution of the Invention
The present invention relates to a phosphonic acid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR3## wherein R.sup.1 represents a hydrogen atom, a hydroxyl group, an acyloxyalkyl group, an alkyloxycarbonyl group, a lower alkyl group which may have a substituent or a lower alkoxy group which may have a substituent; represents a hydrogen atom, a lower alkyl group which may have a substituent, an alkali metal or a prodrug ester forming group; ##STR4## (wherein R.sup.4 represents a hydrogen atom, a lower alkyl group, an alkali metal or an acyloxyalkyl group which may have a substituent), a group represented by the formula: ##STR5## (wherein R.sup.4' represents a hydrogen atom, a lower alkyl group or an alkali metal) or a group represented by the formula: ##STR6## wherein R.sup.5 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group; and R.sup.6 represents a lower alkyl group or a group represented by the formula: --OR.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group)!; and represents a
REFERENCES:
CA 108:94778 Abstract & structures pp. 1-9 for Oct. 28, 1987 EP Patent -- 243173.
Abe Shinya
Eguchi Yoshihito
Fukuda Yoshio
Hayashi Kenji
Hiyoshi Hironobu
Eisai Co. Ltd.
Ivy C. Warren
Vollamo Jean F.
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