Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-08-12
2001-02-20
Rotman, Alan L. (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S279000, C546S121000, C546S112000, C546S199000
Reexamination Certificate
active
06191141
ABSTRACT:
This invention relates to azaindole compounds having affinity for serotonin receptors, to pharmaceutical and diagnostic compositions containing them and to their medical use, particularly in the diagnosis and treatment of CNS conditions.
According to one aspect of the invention, there are provided compounds of Formula I and a salt, solvate of hydrate thereof:
wherein:
R represents a group of Formula II or Formula III;
one of A, B D or E is a N atom, the remainder being CH groups;
R
1
is selected from the group consisting of SO
2
Ar, C(O)Ar, CH
2
Ar and Ar;
R
2
, R
3
and R
4
are independently selected from the group consisting of H and alkyl;
----- represents a single or double bond, with the proviso that there is only one double bond in the ring at a time;
n is an integer of from 1-3;
Z is selected from the group consisting of C, CH and N, provided that when ----- is a double bond, Z is C and when ----- is a single bond, Z is selected from CH and N;
Ar is an optionally substituted aryl group;
with the proviso that when R is a group of Formula II, R
1
is SO
2
Ar.
It is an aspect of the invention to provide compounds which bind to the 5-HT
6
receptor.
Certain compounds of the invention also bind to the 5-HT
7
receptor, and a further object of the invention provides such compounds having mixed 5-HT
6
and 5-HT
7
activity.
According to another aspect of the invention, there are provided pharmaceutical compositions comprising a compound of Formula I, in an amount effective to antagonize the 5-HT
6
receptor, and a pharmaceutically acceptable carrier.
In another aspect of the invention there are provided compositions containing a compound of Formula I, in amounts for pharmaceutical use, to treat CNS conditions where a 5-HT
6
antagonist is indicated, for example, for the treatment or prevention of central nervous system disturbances such as psychosis, schizophrenia, manic depression, depression, neurological disturbances, memory disturbances, Parkinsonism, amylotrophic lateral sclerosis, Alzheimer's disease and Huntington's disease.
In another aspect of the invention, there are provided compounds useful as intermediates in the preparation of a compound of Formula I, and having a general structure according to Formula IV:
wherein
R represents a group of Formula II or Formula III;
one of A, B D or E is a N atom, the remainder being CH groups;
R
2
, R
3
and R
4
are independently selected from the group consisting of H and alkyl;
----- represents a single or double bond, with the proviso that there is only one double bond in the ring at a time;
n is an integer of from 1-3;
Z is selected from the group consisting of C, CH and N, provided that when ----- is a double bond, Z is C and when ----- is a single bond, Z is selected from CH and N.
These and other aspects of the present invention are described in greater detail hereinbelow.
REFERENCES:
patent: 5874427 (1999-02-01), Filla et al.
Edwards Louise
Slassi Abdelmalik
Tehim Ashok
Xin Tao
Arent Fox Kintner Plotkin & Kahn
Desai Rita
NPS Allelix Corp.
Rotman Alan L.
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