Indole derivatives useful in the treatment of osteoporosis

Details Indole derivatives useful in the treatment of osteoporosis Indole derivatives useful in the treatment of osteoporosis

1997-10-09

1999-11-09

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514247, 514255, 514256, 514266, 514258, 514323, 514339, 514397, 514419, 544143, 544238, 544262, 544277, 544333, 544373, 546133, 546146, 546175, 546201, 5462774, C07D20914, C07D20912, C07D40112, C07D41712

Patent

active

059815256

DESCRIPTION:

BRIEF SUMMARY
This invention relates to certain novel compounds, to a process for preparing such compounds, to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in medicine.
It has surprisingly been discovered that certain indole derivatives are indicated to reduce bone resorption by inhibiting osteoclast H.sup.+ -ATPase and are therefore of potential use for the treatment and/or prophylaxis of osteoporosis and related osteopenic diseases. These compounds are also considered to possess anti-tumour activity, antiviral activity (for example against Semliki Forest, Vesicular Stomatitis, Newcastle Disease, Influenza A and B, HIV viruses), antiulcer activity (for example the compounds may be useful for the treatment of chronic gastritis and peptic ulcer induced by Helicobacter pylori), immunosupressant activity, antilipidemic activity, antiatherosclerotic activity and to be useful for the treatment of AIDS and Alzheimer's disease. In a further aspect, these compounds are also considered useful in inhibiting angiogenesis, i.e. the formation of new blood vessels which is observed in various types of pathological conditions (angiogenic diseases) such as rheumatoid arthritis, diabetic retinopathy, psoriasis and solid tumours.
Accordingly, the present invention provides a compound of formula (I): ##STR2## or a salt thereof, or a solvate thereof, wherein either: (i) Ra represents a group R.sub.5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): ##STR3## wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.s Rt wherein R.sub.s and R.sub.t each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or R.sub.s and R.sub.t together may form a heterocyclic group; R.sub.1 represents an alkyl or a substituted or unsubstituted aryl group; and R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl R.sub.b represents the above defined R.sub.5 ;
R.sub.6 and R.sub.7 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R.sub.6 and R.sub.7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and
R.sub.8 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl.
In one aspect, and preferably, Ra represents a group R.sub.5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a).
In a further aspect, R.sub.a represents a moiety of the above defined formula (a) and R.sub.b represents the above defined R5.
In one aspect R.sub.1 represents alkyl or substituted or unsubstituted phenyl.
Suitably, R.sub.1 represents a C.sub.1-4 -alkyl group, for example methyl or ethyl.
Preferably, R.sub.1 represents methyl.
In one aspect, R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl or phenyl.
Examples of R.sub.2 include hydrogen and methyl.
Suitably, R.sub.2 represents hydrogen.
Examples of R.sub.3 include hydrogen and ethyl.
Suitably, R.sub.3 represents hydrogen.
Examples of R.sub.4 include hydrogen, propyl and phenyl.
Suitably, R.sub.4 represents hydrogen.
In one aspect, R.sub.5 is hydrogen, alkyl or substituted or, suitably, unsubstituted phenyl.
Examples of R.sub.5 include hydrogen, ethyl and 4-methoxyphenyl.
Suitably, R.sub.5 is hydrogen.
In one aspect R.sub.6 and R.sub.7 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted phenyloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, nitro, alkyl, carboxy, c

REFERENCES:
patent: 5312928 (1994-05-01), Goldin et al.

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