Phosphorus-containing isoprenoid derivatives

Details Phosphorus-containing isoprenoid derivatives Phosphorus-containing isoprenoid derivatives

1994-02-22

1995-09-26

Dees, Jose G.

Gas separation

554 84, 558166, 558179, 558182, 558190, 558155, 558158, 558161, C07F 902

Patent

active

054535247

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP92/01082, filed Aug. 27, 1992.


FIELD OF INDUSTRIAL APPLICATION

The present invention relates to a novel phosphorus-containing isoprenoid derivative. More particularly, it relates to a phosphorus-containing isoprenoid derivative useful as a drug.


BACKGROUND OF THE INVENTION AND PRIOR 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 principal factor of atherosclerosis which is one of the adult diseases. Accordingly, the 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 hyperlipemia remedy.
Recently, an HMG-CoA reductase inhibitor has been developed as a hyperlipemia remedy 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 there is a danger of causing an adverse effect such as cardiac hypofunction, muscle ache or infirmity. Meanwhile, a desmosterol reductase inhibitor has a disadvantage that serious adverse effects such as cataract are caused by the accumulation of desmosterol.
Under these circumstances, it is still eagerly expected to develop a hyperlipemia remedy which is free from the above adverse effects and exhibits an excellent cholesterol level lowering activity.
Under the above circumstances, the inventors of the present invention started studies to find a compound having an inhibitory activity against squalene synthetase, and have found that a phosphorus-containing isoprenoid derivative can attain the object. The present invention has been accomplished on the basis of this finding.
Although some phosphorus-containing hydrocarbon compounds useful as drugs are disclosed in Japanese Patent Laid-Open Nos. 56492/1990 and 188288/1990, they are different from the compounds of the present invention in both structure and efficacy as drugs. Further, some phosphorus-containing isoprenoid derivatives useful as drugs are also disclosed in Japanese Patent Laid-Open Nos. 101088/1990 and 285821/1990. However, these derivatives are different from those of the present invention in structure.


CONSTITUTION OF THE INVENTION

The present invention relates to a phosphorus-containing isoprenoid derivative represented by the following general formula (I) and pharmacologically acceptable salts thereof: ##STR4##
wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group;
R.sup.3 and R.sup.4 may be the same or different from each other and each represent a hydrogen atom, a lower alkyl group or an alkali metal;
Y represents a group represented by the formula: ##STR5## (wherein R.sup.5 and R.sup.6 may be the same or different from each other and each represent a hydrogen atom, a lower alkyl group or an alkali metal), or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal);
Z represents a group represented by the formula: --(CH.sub.2).sub.m -- (wherein m is zero or an integer of 1 to 3), a group represented by the formula: --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.q -- (wherein p is 0 or 1 and q is 1 or 2) or a group represented by the formula: ##STR6## (wherein R.sup.8 represents a hydrogen atom or a lower alkyl group; A represents an alkylene chain whlch has 1 to 5 carbon atoms and which may have a substituent on each carbon atom; and r is zero or an integer of 1 to 5); and
n is zero or an integer of 1 to 5.
In the above definition of the compound (I) according to the present invention, the lower alkyl group defined wit

REFERENCES:
patent: 5157027 (1993-10-01), Biller et al.

Affiliated with

Also associated with

Rating

Phosphorus-containing isoprenoid derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Phosphorus-containing isoprenoid derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phosphorus-containing isoprenoid derivatives will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1552645