Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-11-13
2001-09-25
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S912000
Reexamination Certificate
active
06294544
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a new drug which increases blood flow in the peripheral vessels supplying ocular tissues including the optic disc, choroid, and retina, and thereby shows a therapeutically effective action on visual field defects associated with normal intraocular pressure glaucoma as well as on optic neuropathy, retinopathy, retinal-degeneration diseases, etc.
DESCRIPTION OF THE BACKGROUND
Dihydropyridines are represented by the following general formula (I):
(where R
1
nitrophenyl group and R
2
, R
3
, and R
4
are all lower alkyl groups). Among these dihydropyridines, the compound with a 3-nitrophenyl group as R
1
, an isopropyl group as R
2
, and methyl groups as R
3
and R
4
is called nilvadipine. It is publicly known as a calcium antagonist, and has had wide clinical usage, for example, as a hypotensive drug. Recently, nicardipine (hydrochloride), another calcium antagonist, has been shown to increase peripheral blood flow in the retina of rabbits. In the case of nilvadipine, however, there had been no information about its effects on the peripheral circulation of the retina or its therapeutic actions on ophthalmic diseases.
SUMMARY OF THE INVENTION
These inventors have studied pharmacological effects of nilvadipine on the peripheral ocular circulation to explore new possible ophthalmologic applications for nilvadipine which is already known as a safe drug with few side effects.
Studies on the pharmacological effects of nilvadipine on the peripheral ocular circulation revealed that it is highly effective in increasing blood flow in the optic disc, choroid, and retina. In particular, the effect on the optic disc in increasing its blood flow is one that has not been seen with nicardipine (hydrochloride). Thus, it became apparent that these pharmacological effects of nilvadipine are expected to exert an excellent therapeutic effect in the clinical treatment of visual field defects associated with normal intraocular pressure glaucoma as well as of optic neuropathy, retinopathy, retinal-degeneration-related diseases, etc.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
In a first aspect of the present invention, an optic disc blood flow ameliorant includes dihydropyridines represented by the general formula (I):
(where R
1
is a nitrophenyl group and R
2
, R
3
, and R
4
are all lower alkyl groups), especially 6-cyano-5-methoxycarbonyl-2-methyl-4-(3-nitrophenyl)-1, 4-dihydropyridine-3-carboxylic acid isopropyl ester (generic name: nilvadipine), or their medicinally acceptable salts, in combination with medicinally acceptable vehicles.
In a second aspect of the present invention, a choroidal blood flow ameliorant includes the above-mentioned dihydropyridines, or their medicinally acceptable salts, in combination with medicinally acceptable vehicles.
In a third aspect of the present invention, a retinal blood flow ameliorant includes the above-mentioned dihydropyridines, or their medicinally acceptable salts, in combination with medicinally acceptable vehicles.
More specifically, this invention, as a drug which includes the above-mentioned dihydropyridines including nilvadipine, or their medicinally acceptable salts, in combination with medicinally acceptable vehicles, is intended to provide a therapeutic agent for clinical treatment of visual field defects associated with normal intraocular pressure glaucoma as well as of optic neuropathy, retinopathy, retinal-degeneration-related diseases, etc.
REFERENCES:
patent: 5431907 (1995-07-01), Abelson et al.
patent: WO 93/23082 (1993-11-01), None
Chemical Abstracts 124: 75952. Stone et al., 1995.
Araie Makoto
Tomita Ken
Fay Zohreh
Fujisawa Pharmaceutical Co. Ltd.
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
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