Substituted imidazo[1,5-A]pyridine derivatives and other substit

Details Substituted imidazo[1,5-A]pyridine derivatives and other substit Substituted imidazo[1,5-A]pyridine derivatives and other substit

1986-02-04

1988-03-01

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514210, 514222, 514233, 514237, 514239, 514227, 514253, 514393, 548324, 546199, 540303, 540476, 540579, 544 61, 544139, 544370, A61K 31415, C07D48704, C07D23502

Patent

active

047286458

ABSTRACT:
Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.g. aromatase inhibition in mammals; processes and intermediates for preparing these compounds.

REFERENCES:
patent: 4444775 (1984-04-01), Ford
patent: 4507481 (1985-03-01), Davidson et al.
patent: 4560758 (1985-04-01), Davidson et al.
patent: 4588732 (1986-10-01), Browne
patent: 4617307 (1986-10-01), Browne
J. Heterocyclic Chem. 13, 111-12 (1976).
Chem. Abstract 55, 7430i (1961).
Tetrahedron, vol. 37, Supple. (1981), 191-200.
Chem. Abstract 95, 7155 (1981).
J. Org. Chem., vol. 38, 284-8 (1973).
Indian J. Chem. 531-2 (1975).

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