Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
2000-04-10
2000-12-19
Barts, Samuel
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
564430, A61K 31135
Patent
active
061628328
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to 2-phenoxyaniline derivatives having an inhibitory action on a Na.sup.+ /Ca.sup.2+ exchange system.
BACKGROUND ART
Among prior art compounds which inhibit a Na.sup.+ /Ca.sup.2+ exchange system selectively and prevent overload of Ca.sup.2+ in cells regarded as important in the cell injury mechanism after ischemia or reperfusion, there are known compounds as described in Japanese Patent Kokai 7-41465 and WO97/09306. However, there have not been known any compounds with a phenoxyaniline skeleton which have an inhibitory action on a Na.sup.+ /Ca.sup.2+ exchange system.
DISCLOSURE OF THE INVENTION
As a result of extensive researches on the compounds having an inhibitory action on a Na.sup.+ /Ca.sup.2+ exchange system, the present inventors have found that some kind of compounds having a phenoxyaniline skeleton meet said object, and the present invention has been accomplished based on the finding.
That is, the present invention is directed to a 2-phenoxyaniline derivative represented by Formula (1): ##STR2## wherein R.sup.1 is a hydrogen atom or a lower alkoxy group, R.sup.2 is a halogen atom or a nitro group, and R.sup.3 is a hydrogen atom or a halogen atom, or a pharmaceutically acceptable salt thereof.
Furthermore, the present invention is directed to a pharmaceutical composition containing the above-mentioned compound or the pharmaceutically acceptable salt thereof as an effective component.
Furthermore, the present invention is directed to a pharmaceutical composition for the treatment or prevention of ischemic heart diseases, ischemic cerebral diseases or ischemic renal diseases containing the above-mentioned compound or the pharmaceutically acceptable salt thereof as an effective component.
Furthermore, the present invention is directed to use of the above-mentioned compound or the pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical composition for the treatment or prevention of ischemic heart diseases, ischemic cerebral diseases or ischemic renal diseases.
Furthermore, the present invention is directed to a method for the treatment or prevention of ischemic heart diseases, ischemic cerebral diseases or ischemic renal diseases which includes the step of administering a pharmacologically effective amount of the above-mentioned compound or the pharmaceutically acceptable salt thereof to a human.
Furthermore, the present invention is directed to a pharmaceutical composition for the protection of cells during thrombolytic therapy, angioplasty, bypass operation of coronary artery or organ transplantation containing the above-mentioned compound or the pharmaceutically acceptable salt thereof as an effective component.
Furthermore, the present invention is directed to use of the above-mentioned compound or the pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical composition for the protection of cells during thrombolytic therapy, angioplasty, bypass operation of coronary artery or organ transplantation.
Furthermore, the present invention is directed to a method for the protection of cells during thrombolytic therapy, angioplasty, bypass operation of coronary artery or organ transplantation which includes the step of administering a pharmacologically effective amount of the above-mentioned compound or the pharmaceutically acceptable salt thereof to a human.
In the present invention, the lower alkoxy group refers to a straight or branched C.sub.1-6 alkoxy group, and specific examples thereof are a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group, an isobutoxy group, a sec-butoxy group, a tert-butoxy group, a pentyloxy group, an isopentyloxy group, a neopentyloxy group, a tert-pentyloxy group, a 1-methylbutoxy group, a 2-methylbutoxy group, a 1,2-dimethylpropoxy group, a hexyloxy group and an isohexyloxy group.
The halogen atom refers to a fluorine atom, a chlorine atom, a bromine atom or an iodine atom.
In the present invention, preferred phenoxyaniline derivatives are
REFERENCES:
patent: 5556860 (1996-09-01), Muraoka et al.
Aibe Izumi
Nakanishi Misa
Ota Tomomi
Taguchi Minoru
Tomisawa Kazuyuki
Barts Samuel
Taisho Pharmaceutical Co., Inc.
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