Substituted imidazo[5-a]pyridine derviatives and other substitut

Details Substituted imidazo[5-a]pyridine derviatives and other substitut Substituted imidazo[5-a]pyridine derviatives and other substitut

1990-12-21

1995-06-27

Richter, Johann

Organic compounds -- part of the class 532-570 series

Organic compounds

Chalcogen in the nitrogen containing substituent

544125, 544362, 546121, C07D41704, C07D47104, C07D49104

Patent

active

054281601

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, oxidised 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, oxidised 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: 4228291 (1980-10-01), Durant et al.
patent: 4409226 (1983-10-01), Bristol
patent: 4444775 (1984-08-01), Ford
patent: 4617307 (1986-10-01), Browne
J. of Med. Chem. Vol. 16 (1973) 1272-1276.
Tetrahedron vol. 37 Suppl. 1981 pp. 191-200.

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