Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1999-09-15
2000-12-05
Ambrose, Michael G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514524, 514535, 514629, 558424, 560 45, 564221, 564430, A61K 31136, A61K 31167, A61K 31277, C07C21790, C07C23740, C07C25558
Patent
active
061568015
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to phenoxyaniline derivatives or pharmaceutically acceptable salts thereof 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 having a quinazoline skeleton as described in Japanese Patent Kokai 7-41465. However, there is no report that the compounds having a phenoxyaniline skeleton as shown in the present invention 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 findings.
That is, the present invention is directed to a 2-phenoxylaniline derivative represented by Formula (1): ##STR2## wherein R.sup.1 is a hydrogen atom, an amino group or an NHCOR.sup.3 group, R.sup.2 is a halogen atom, an amono group, a cyano group, a C.sub.1-6 alkyl group, a C.sub.1-3 perfluoroalkyl group, an NHCOR.sup.3 group, a CH.sub.2 OR.sup.4 group, an OCH.sub.2 R.sup.5 group or a COR.sup.6 group, R.sup.3 is a C.sub.1-6 alkyl group, R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-5 aminoalkyl group, a C.sub.2-7 alkoxy-carbonyl group or a carbamoyl group, and R.sup.6 is a C.sub.1-6 alkyl group or a C.sub.3-8 cycloalkyl group which is unsubstituted or substituted by a halogen atom, an amino group, a cyano group or a C.sub.1-6 alkyl group; 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 ischemia 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 in
REFERENCES:
patent: 5006660 (1991-04-01), Yamakawa
patent: 5556860 (1996-09-01), Muraoka et al.
Coutts, I.G.C. et al. Synthesis of Spiroheterocycles by Oxidative Coupling of Phenolic Sulphonamides. J. Chem. Soc. Chem. Commun. 1980, pp. 949-950.
Nakanishi Misa
Ota Tomomi
Taguchi Minoru
Tomisawa Kazuyuki
Ambrose Michael G.
Taisho Pharmaceutical Co. Ltd.
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