Alpha-heterocycle substituted tolunitriles

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514357, 514278, 546 15, 546264, 546330, A61K 3144, C07D40106

Patent

active

050718614

ABSTRACT:
The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, (1-1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.

REFERENCES:
patent: 2727895 (1955-12-01), Sperber et al.
patent: 3290281 (1966-12-01), Weinstein
patent: 3396224 (1968-08-01), Van Heyningen et al.
patent: 3397273 (1968-08-01), Van Heyningen et al.
patent: 4757076 (1988-07-01), Hirsch et al.
Bradsher et al., CA 85693p, vol. 66, 1967.
Oiji et al., CA 87: 53093k, vol. 87, 1977.
Chem. Abstract 87: 201329j (1977).

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