Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-09-29
1999-07-06
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544238, 546197, 548126, A61K 3137
Patent
active
059198060
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to the use of pharmaceutically active benzopyran derivatives as a medicine for cardiac insufficiency of mammals including human beings.
BACKGROUND ART
Japanese Patent Application Laid-Opens No. Hei 2-4791, No. Hei 2-49788, No. Hei 2-152974 and No. Hei 5-43432, U.S. Pat. No. 4,900,752, European Patent No. 327,127 and EP-A-492,391 have disclosed the possibility that benzopyran derivatives are usable as a medicine for curing disorders of cardiovascular systems such as hypertension, angina pectoris, arrhythmia, etc. and also as a hair growth stimulants for curing alopecia. However, they do not refer to the possibility that the derivatives might be usable as a medicine for curing diseases associated with cardiac insufficiency.
DISCLOSURE OF INVENTION
The present inventors intensively studied and investigated various benzopyran derivatives so as to obtain those having a low potassium channel opening activity while having no cardio-suppressing activity but rather having an activity of increasing constriction of heart and, as a result, have found that the compounds of the following formula (I) have a strong cardiotonic activity. On the basis of this finding, the present invention has been completed.
Specifically, the present invention is directed to the compounds of the following formula (I), their optical isomers, their stereoisomers and their pharmaceutically acceptable salts when they may form salts. ##STR2## wherein X.sup.1 and X.sup.2 do not exist or represent an oxygen atom; X represents an oxygen atom, a sulfur atom, a nitrogen atom (said nitrogen atom is unsubstituted or substituted by a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group), C(O), C(S), or C(N--CN); A represents a hydrogen atom, a hydroxyl group, or OC(O)R.sup.5 (in which R.sup.5 represents a C.sub.1 -C.sub.4 alkyl group), or may form a single bond together with B; represents hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, or R.sup.1 and R.sup.2 may together form a 1,4-butylene or 1,5-pentylene group which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl group(s); a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group {said alkyl group is unsubstituted or substituted by one or more substituents selected from a halogen atom, a carboxyl group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a hydroxyl group, a C.sub.1 -C.sub.4 alkoxy group, CH(OR).sub.2 (in which R represents a C.sub.1 -C.sub.4 alkyl group), a phenyl group (which is unsubstituted or substituted by one or more substituents selected from a halogen atom, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group), a formyl group, a cyano group and a nitro group}, a C.sub.2 -C.sub.6 alkenyl group {said alkenyl group is unsubstituted or substituted by one or more substituents selected from a halogen atom, a carboxyl group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a hydroxyl group, a C.sub.1 -C.sub.4 alkoxy group, CH(OR).sub.2 (in which R represents a C.sub.1 -C.sub.4 alkyl group), a phenyl group (which is unsubstituted or substituted by one or more substituents selected from a halogen atom, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group), a formyl group, a cyano group and a nitro group}, a C.sub.2 -C.sub.6 alkynyl group {said alkynyl group is unsubstituted or substituted by one or more substituents selected from a halogen atom, a carboxyl group, a C.sub.2 -C.sub.5 alkoxycarbonyl group, a hydroxyl group, a C.sub.1 -C.sub.4 alkoxy group, CH(OR).sub.2 (in which R represents a C.sub.1 -C.sub.4 alkyl group), a phenyl group (which is unsubstituted or substituted by one or more substituents selected from a halogen atom, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group), a formyl group, a cyano group and a nitro group}, a C.sub.3 -C.sub.6 cycloalkyl group {said cycloalkyl group is unsubstituted or substituted by one or more substituents selected from a halogen atom, a carboxyl group, a C.sub.2 -C5 alkoxycarbonyl group, a hydroxyl group, a C.sub.1 -C.sub.4 alkoxy group, CH(OR).sub.2 (in which R represents a C.sub.1 -C.sub.4 alkyl group), a p
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Kamikawaji Yoshimasa
Masuda Yukinori
Matsumoto Hiroo
Ohrai Kazuhiko
Seto Kiyotomo
MacMillan Keith D.
Nissan Chemical Industries Ltd.
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