Patent EP-1468684-A1 (EP)
Inventor: IIMURA YOICHI
IPC: A61P25/00
Filed: 2003-01-22
Abstract: The present invention provides an indanone derivative
and an excellent sigma receptor binding agent comprising an
indanone derivative. More specifically, it provides a
sigma receptor binding agent comprising an indanone
derivative represented by the following formula, a
pharmacologically acceptable salt thereof or a hydrate of
them.
 
In the formula (I), R 1 , R 2 , R 3  and R 4  are the same as or
different from each other and each represents hydrogen atom,
a halogen atom, hydroxyl group, nitrile group, a C 1-6  alkyl
group which may be substituted, a cycloalkyl group having
three to eight carbon atoms which may be substituted, a C 1-6 
alkoxy group which may be substituted, a cycloalkoxy group
having three to eight carbon atoms which may be substituted,
an acyl group having one to six carbon atoms which may be
substituted, a C 1-6  alkoxycarbonyl group which may be
substituted, a C 1-6  alkylaminocarbonyloxy group which may be
substituted, a di(C 1-6  alkyl)aminocarbonyloxy group which
may be substituted, nitro group, an amino group which may
be substituted, an amido group which may be substituted,
mercapto group or a thio-C 1-6  alkoxy group which may be 
substituted, and further R 1  with R 2 , R 2  with R 3 , or R 3  with
R 4  may together form an aliphatic ring, an aromatic ring, a
heterocyclic ring or an alkylenedioxy ring; the partial
structure:
 
represents a group represented by >CH-CH 2 -, >C=CH- or
>C(-R 7 )-CH 2 -; m represents an integer of 0 or 1 to 5; and R 5 
represents hydrogen atom, a C 1-6  alkyl group which may be
substituted, a C 2-6  alkenyl group which may be substituted,
a C 2-6  alkynyl group which may be substituted, a cycloalkyl
group having three to eight carbon atoms which may be
substituted, a 2,2-(alkylenedioxy)ethyl group or a group
represented by the formula:
 
(wherein the ring C represents benzene ring, an aliphatic
ring or a heterocyclic ring; R 6 s are the same as or
different from each other and each represents hydrogen atom,
a halogen atom, hydroxyl group, nitrile group, a C 1-6  alkyl
group which may be substituted, a C 2-6  alkenyl group which
may be substituted, a C 2-6  alkynyl group which may be
substituted, a cycloalkyl group having three to eight
carbon atoms which may be substituted, a C 1-6  alkoxy group
which may be substituted, a C 1-6  alkoxyalkoxy group which 
may be substituted, an aryloxy group which may be
substituted or an aralkyloxy group which may be substituted,
and further two of R 6 s may together form an aliphatic ring,
an aromatic ring, a heterocyclic ring or an alkylenedioxy
ring; R 7  represents a halogen atom, hydroxyl group, a C 1-6 
alkyl group which may be substituted, a C 1-6  alkoxy group,
nitrile group, a halogeno-C 1-6  alkyl group, a hydroxyl-C 1-6 
alkyl group, a cyano-C 1-6  alkyl group, an amino-C 1-6  alkyl
group, nitro group, azide group, an amino group which may
be substituted, a carbamoyl group which may be substituted,
a carboxyl group which may be substituted, mercapto group
or a thio-C 1-6  alkoxy group; and n represents an integer of
1 to 5), provided that 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine,
a pharmacologically
acceptable salt thereof or a hydrate of them are excluded.