N-(3-pyrrolidinyl) benzamide derivative
AssigneeYamanouchi Pharmaceutical Co., Ltd.
InventorsJunya Ohmori, Kyoichi Maeno, Kazuyuki Hidaka, Kazuhiro Nakato, Shuichi Sakamoto, Shin-ichi Tsukamoto
Life of this patent
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Abstract
N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D.sub.3 and/or D.sub.4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof. ##STR1##
Claims12
A novel N-(3-pyrrolidinyl)benzamide compound represented by a general formula (I), or a pharmaceutically acceptable salt thereof, ##STR120## wherein each symbol in the formula has the following meaning, R.sup.1 :
- a hydrogen atom, a lower alkyl group, an aralkyl group or a cycloalkyl or cycloalkyl-lower alkyl group having 3 to 8 ring atoms,
- R.sup.2 :
- a bicyclic or tricyclic bridged hydrocarbon ring group having 4 to 16 ring atoms, which may be substituted by a lower alkyl group(s),
- R.sup.3 :
- a lower alkoxy group, an amino group or a mono- or di-lower alkylamino group,
- R.sup.4 :
- a hydrogen atom, a halogen atom, a lower alkyl group which may be substituted by a hydroxyl group, a lower alkoxy group, a cyano group, a nitro group, an amino group, a mono- or di-lower alkylamino group, an acyl group or a group represented by --S(O).sub.m --R.sup.5,
- R.sup.5 :
- a lower alkyl group, an amino group or a mono- or di-lower alkylamino group,
- m:
- 0, 1 or 2,
- X:
- a bond or a group represented by --O--, --S(O).sub.n --, --NH--or --CONH--, and
- n:
- 0, 1 or 2,
- with the proviso that, when R.sup.1 is a cycloalkyl group, the cases wherein X is a group represented by --CONH--, R.sup.3 is a lower alkoxy group and R.sup.4 is a halogen atom are excluded.
N-1-(Bicyclo 3.3.1!non-9-yl)-3-pyrrolidinyl!-2,4-dimethoxy-5-nitrobenzamide or a pharmaceutically acceptable salt thereof or an optical isomer thereof.
N-1-(Bicyclo3.3.1!non-9-yl)-3-pyrrolidinyl!-2-methoxy-4-methyl-5-n itrobenzamide or a pharmaceutically acceptable salt thereof or an optical isomer thereof.
N-1-(Bicyclo 3.3.1!non-9-yl)-3-pyrrolidinyl!-5-cyano-2,4-dimethoxybenzamide or a pharmaceutically acceptable salt thereof or an optical isomer thereof.
N-1-(Bicyclo3.3.1!non-9-yl)-3-pyrrolidinyl!-2,4-dimethoxy-5-methyl aminobenzamide or a pharmaceutically acceptable salt thereof or an optical isomer thereof.
Dependencies are inferred from the claim text.