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Details for Patent: 5,112,845

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Details for Patent: 5,112,845

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), Steele; Ronald E. (Long Valley, NJ), Browne; Leslie J. (Morristown, NJ), Ewald; Bruce H. (Long Valley, NJ), Diener; Robert (Chester, NJ)
Assignee: Ciba-Geigy Corporation (Ardsley, NY)
Filing Date:Dec 17, 1990
Application Number:07/628,732
Claims:1. A method of delaying proestrus and estrus and inhibiting proestrus in the anestrus animal which comprises administering to a female animal in need thereof an effective amount of a compound of the formula ##STR16## wherein R and R.sub.o represent hydrogen or lower alkyl; or R and R.sub.o 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 represents hydrogen; R.sub.2 represents hydrogen, lower alkyl, 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, or 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-C.sub.4 -C.sub.6 -straight chain alkylene or ortho phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene to form with the carbon atom attached thereto a corresponding unsubstituted or lower alkyl-substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl or 1-imidazolyl substituted by lower alkyl; aryl within the above definitions represents phenyl or phenyl substituted by one or two substituents selected from lower alkyl, lower alkoxy, hydroxy, lower alkanoyloxy, aroyloxy, nitro, amino, halogen, trifluoromethyl, cyano, carboxy, carboxy functionalized in form of a pharmaceutically acceptable ester or amide, lower alkanoyl, aroyl, lower alkylsulfonyl, sulfamoyl, N-lower alkylsulfamoyl or N,N,-di-lower alkylsulfamoyl; and aryl within the above definitions also represents 2-, 3-, or 4-pyridyl, or a said heterocyclic radical monosubstituted by lower alkyl, lower alkoxy, cyano or halogen; and aroyl within the above definitions represents benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or of a veterinarily acceptable salt thereof; or of a veterinary composition comprising a said compound in combination with one or more veterinarily acceptable carriers

2. A method according to claim 1 wherein proestrus and estrus in a female canine is delayed or wherein proestrus in female canine is inhibited.

3. A method according to claim 1 which comprises administering to female canine in need thereof an effective amount of a compound of the formula ##STR17## wherein R.sub.1 ' represents hydrogen; R.sub.2 ' represents hydrogen, lower alkyl, phenyl, 2-, 3- or 4-pyridyl or benzyl; or R.sub.2 ' represents phenyl or benzyl, each monosubstituted on the phenyl ring by cyano, lower alkyl, lower alkoxy, hydroxy, lower alkanoyloxy, aroyloxy, nitro, halogen, trifluoromethyl, lower alkanoyl, aroyl, lower alkylsulfonyl, carbamoyl, N-mono- or N,N-di-lower alkylcarbamoyl, sulfamoyl, N-mono- or N,N-di-lower alkylsulfamoyl; or R.sub.1 ' and R.sub.2 ' combined represent together lower alkylidene, benzylidene or diphenylmethylidene; or R.sub.1 ' and R.sub.2 ' combined represent together C.sub.4 -C.sub.6 straight chain alkylene; R.sub.3 represents hydrogen or lower alkyl; or a veterinarily acceptable salt thereof; or of a veterinary composition comprising said compound in combination with one or more veterinarily acceptable carriers.

4. A method according to claim 1 which comprises administering to female canine in need thereof an effective amount of a compound of the formula ##STR18## wherein R.sub.2 ' represents 3-pyridinyl, p-cyanobenzyl or p-cyanophenyl; or a veterinarily acceptable salt thereof; or of a veterinary composition comprising said compound in combination with one or more veterinarily acceptable carriers.

5. A method according to claim 1 which comprises administering to female canine in need thereof an effective amount of 4-[alpha-(3-pyridinyl)-1-imidazolylmethyl)]benzonitrile or of a veterinarily acceptable salt thereof; or of a veterinary composition comprising said compound in combination with one or more veterinarily acceptable carriers.

6. A method according to claim 1 which comprises administering to female canine in need thereof an effective amount of 4-[alpha-(4-cyanophenyl)-1-imidaolylmethyl]benzonitrile or of a veterinarily acceptable salt thereof; or of a veterinary composition comprising said compound in combination with one or more veterinarily acceptable carriers.
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