Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-07-25
1991-05-21
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514406, 540470, 540575, 544298, 544322, C07D40312, A61K 31555, A61K 31415
Patent
active
050175734
ABSTRACT:
An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4.
This compound is useful as a potent and selective antagonist of serotonin 3 (5--HT.sub.3) receptor.
REFERENCES:
patent: 4207327 (1980-06-01), Lunsford et al.
patent: 4474964 (1984-10-01), Ibuki
Karasawa Tadahiko
Kato Shiro
Kon Tatsuya
Morie Toshiya
Yoshida Naoyuki
Dainippon Pharmaceutical Co., Ltd.
Gerstl Robert
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