Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1997-10-24
2001-05-15
Spivack, Phyllis G. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S253030, C514S300000, C514S254080
Reexamination Certificate
active
06232324
ABSTRACT:
This case is a 371 of PCT/JP96/01063 filed Apr. 18, 1996.
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition for the prevention and/or the treatment of dialysis-induced hypotension and/or hypotension after dialysis which comprises, as an active ingredient, a pyrazolopyridine compound or a salt thereof, and so is useful in the pharmaceutical field. Here, hypotension after dialysis includes postural hypotension after dialysis.
BACKGROUND ART
Some pyrazolopyridine compounds are known to be useful as diuretic, antihypertensive agent, remedy for renal insufficiency, and the like (e.g. Japanese Laid-Open Nos. 64-45385, 2-243689, 5-112566, etc.).
DISCLOSURE OF INVENTION
A pharmaceutical composition for the prevention and/or the treatment of dialysis-induced hypotension and/or hypotension after dialysis of the present invention is the one which comprises, as an active ingredient, a pyrazolopyridine compound or a salt thereof.
The pyrazolopyridine compound to be used in the present invention is shown by the following formula (I):
wherein
R
1
is lower alkyl, aryl which may have one or more suitable substituent(s) or a heterocyclic group,
R
2
is a group of the formula
(wherein
R
4
is protected amino or hydroxy and
R
5
is hydrogen or lower alkyl); cyano;
a group of the formula:
—A—R
6
(wherein
R
6
is an acyl group, and
A is lower aliphatic hydrocarbon group which may have one or more suitable substitutent(s));
amidated carboxy;
unsaturated heterocyclic group which may have one or more suitable substituent(s); amino or protected amino; and
R
3
is hydrogen, lower alkyl, lower alkoxy or halogen
or a salt thereof.
As for aforesaid pyrazolopyridine compound (I), the known compounds disclosed in Japanese Laid-Open Nos. 64-45385, 2-243689, 4-253978 and 5-112566 are exemplified.
Further, in addition to aforesaid pyrazolopyridine compound (I), the pyrazolopyridine compound disclosed in WO95/18128 (in particular, the compounds of claims
5
and
8
such as 3-[2-(4-carboxy-2-oxocyclohexyl)-3-oxo-2,3-dihydropyridazin-6-yl]-2-phenylpyrazolo[1,5-a]pyridine, 3-[2-(2-carboxymethyl-1-cyclohexenyl)-3-oxo-2,3-dihydropyridazin-6-yl]-2-phenylpyrazolo[1,5-a]pyridine, or the like) can be also used, according to the present invention, as a pharmaceutical composition for the prevention and/or the treatment of dialysis-induced hypotension and/or hypotension after dialysis.
Suitable salts of the pyrazolopyridine compound (I) in the present invention are conventional ones and include a metal salt such as an alkali metal salt (e.g. sodium salt, potassium salt, etc) and an alkaline earth metal salt (e.g. calcium salt, magnesium salt, etc), an ammonium salt, an organic base salt (e.g. trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N′-dibenzylethylenediamine salt, etc), an organic acid salt (e.g. acetate, trifluoroacetate, maleate, tartrate, fumalate, methanesulfonate, benzenesulfonate, formate, toluenesulfonate, etc), an inorganic acid salt (e.g. hydrochloride, hydrobromide, hydriodide, sulfate, phosphate, etc), a salt with an amino acid (e.g. arginine, aspartic acid, glutamic acid, etc), and the like.
REFERENCES:
patent: 0 299 209 (1989-01-01), None
Esumi Kimio
Horiai Haruo
Kajiho Tokuaki
Mizuo Hiroyuki
Motoyama Yukio
Fujisawa Pharmaceutical Co. Ltd.
Oblon, Spivak, McClelland, Maier & Neustadt, Neustadt
Spivack Phyllis G.
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