Heterocyclic compounds and their therapeutic use

Details Heterocyclic compounds and their therapeutic use Heterocyclic compounds and their therapeutic use

2001-10-12

2002-09-24

McKane, Joseph K. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S245000, C548S311400, C548S364400

Reexamination Certificate

active

06455561

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to novel heterocyclic compounds and to their formulation and use as pharmaceuticals.
BACKGROUND OF THE INVENTION
The modes of action of phosphodiesterases and also tumour necrosis factor (TNF), and the therapeutic utilities of inhibitors thereof, are described in WO-A-97/4433 7 and U.S. Pat. Nos. 5,925,636 and 5,972,936, the contents of which are incorporated herein by reference. These reference describe benzofurans having such activity.
SUMMARY OF THE INVENTION
This invention provides novel compounds having therapeutic utility, in particular for the treatment of disease states associated with proteins which mediate cellular activity, for example by inhibiting TNF and/or PDE IV. According to the invention, the compounds are of formula (i):
wherein R
1
is C
1-3
alkyl optionally substituted with one or more fluorines;
R
2
is CH
2
OCH
3
or 2 or 3-tetrahydrofuranyl,
R
3
is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C)
R
4
is C
1-3
alkyl and
R
5
and R
6
, which may be the same or different, each represents C,
1-3
alkyl, halogen, CF
3
or CN
or a pharmaceutically-acceptable salt thereof
In summary, the compounds of the invention represent a selection within the scope of WO-A-97/44337. The novel compounds have superior in vivo activity.
This invention provides also a method for mediating or inhibiting the enzymatic activity or catalytic activity of PDE IV in a mammal in need thereof and for inhibiting the production of TNF in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound of Formula (i) or a pharmaceutically-acceptable salt thereof


REFERENCES:
patent: 5925636 (1999-07-01), Dyke et al.
patent: 5972936 (1999-10-01), Dyke et al.
patent: 6121274 (2000-09-01), Ulrich et al.
patent: 9603399 (1996-02-01), None
patent: 9744337 (1997-11-01), None
patent: 9807715 (1998-02-01), None
patent: 9940085 (1999-08-01), None
McGarry, D.G. et al. (1999) “Benzofuran Based PDE4 Inhibitors”Bioorganic & Medicinal Chemistry7:1131-1139.

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