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Generated: December 17, 2017

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Title: Alpha-heterocycle substituted tolunitriles
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.
Inventor(s): Bowman; Robert M. (Summit, NJ), Browne; Leslie J. (Morristown, NJ)
Assignee: Ciba-Geigy Corporation (Tarrytown, NY)
Filing Date:Jul 14, 1994
Application Number:08/275,688
Claims:1. A method for preparing a compound of the formula ##STR16## wherein R and R.sub.0 represent hydrogen; R.sub.1 represents hydrogen; R.sub.2 represents 4-cyanophenyl; W represents 1-(1,2,4)-triazolyl; which comprises condensing under basic conditions using an alkali metal alkoxide a compound of the formula XI ##STR17## with cyanobenzene para-substituted by halogen, or lower alkyl- or aryl-sulfonyloxy.
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Serving leading biopharmaceutical companies globally:

US Army
Chinese Patent Office
Boehringer Ingelheim
Johnson and Johnson

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