Ciba-geigy Corporation

Other

Robert M Bowman

Leslie J Browne

Ronald E Steele

Heinz W Gschwend

Bruce H Ewald

Leslie Browne

Robert Diener

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.

Alpha-heterocycle substituted tolunitriles

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.

An auto diagnostic apparatus having jawed, needle-toothed clips for connection to variable output wires of engine sensors adjacent to the sensors, and a processor which converts the output voltages to output values in reader friendly units understandable to the auto technician, and which stores and continuously updates the minimum and maximum output values for diagnosing intermittent or periodically interrupted electrical current. The needle-toothed clips establish an electrical connection to the variable output sensor wire without damaging the insulation or integrity of the sensor wire.

Diagnostic apparatus displaying engine operating characteristics in the

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.

Alpha-heterocyclc substituted tolunitriles

Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I ##STR1## wherein X represents oxygen or sulfur; Z represents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-l-yl ring radical; R.sub.1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R.sub.2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylene; or R.sub.1 combined with R.sub.5 located on the Z-carbon atom of the imidazolyl radical represents C.sub.2 -C.sub.4 -alkylene; R.sub.3 and R.sub.4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R.sub.3 and R.sub.4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R.sub.3 and R.sub.4, together when located on the carbon atoms to which attached a benzo-fused or C.sub.5 -C.sub.7 -cycloalka-fused ring, respectively; R.sub.5 located on carbon represents hydrogen, lower alkyl or hydroxy-lower alkyl; R.sub.6 located on carbon represents hydrogen or lower alkyl; or when Z represents carbon, R.sub.5 located on the Z-carbon atom combined with R.sub.6 located on the adjacent carbon atom represents C.sub.3 -C.sub.5 -alkylene; and pharmaceutically acceptable salts thereof; which are active in mammals as anticonvulsant agents.

Certain 1,2-benzisoxazole and 1,2-benzisothiazole derivatives

Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I ##STR1## wherein X represents oxygen or sulfur; Z rep;esents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-1-yl ring radical; R.sub.1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R.sub.2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylene; or R.sub.1 combined with R.sub.5 located on the Z-carbon atom of the imidazolyl radical represents C.sub.2 -C.sub.4 -alkylene; R.sub.3 and R.sub.4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R.sub.3 and R.sub.4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R.sub.3 and R.sub.4, together when located on the carbon atoms to which attached a benzo-fused or C.sub.5 -C.sub.7 -cycloalka-fused ring, respectively; R.sub.5 located on carbon represents hydrogen, lower alkyl or hydroxy-lower alkyl; R.sub.6 located on carbon represents hydrogen or lower alkyl; or when Z represents carbon, R.sub.5 located on the Z-carbon atom combined with R.sub.6 located on the adjacent carbon atom represents C.sub.3 -C.sub.5 -alkylene; and pharmaceutically acceptable salts thereof; which are active in mammals as anticonvulsant agents.

Certain 1,2-benzisoxazole derivatives

The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## where 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.

1-(2-phenyl-3-benzofuryl)-piperazines, e.g. those of the formula ##STR1## R=H, alkyl or halo R', R'=H, alkyl, alkoxy, alkylenedioxy, alkylthio or halo

Benzofurylpiperazines

N-(diphenylmethoxy-mono- or bicyclic-alkyleneiminoalkyl)-dicarboximides, e.g. those of the formula ##STR1## A=aliphatic or cycloaliphatic radical R,R'=H, alkyl, halogen or CF.sub.3

N-alkyleneiminoalkyl-dicarboximides as antiallergics and antiasthmatics

7,7-Diphenyl-hexahydro-1,4-oxazepines, e.g. those of the formula: ##STR1## acyl derivatives, N-oxides and salts thereof are antidepressants.

1,4-Oxazepines

N-(7,7-Diphenyl-hexahydro-1,4-oxazepin-4-yl-alkyl)-dicarboximides, e.g. those of the formula: ##STR1## AND ACID ADDITION SALTS THEREOF ARE ANTIASTHMATICS.

7,7-Diphenyl-1,4-oxazepinoalkyl-dicarboximides

4-Phenyl-9,9a-dihydro-5,6-benzoisoindolines, e.g. those of the formula ##STR1## OR SALTS THEREOF ARE ANTIASTHMATIC AND ANTIALLERGIC AGENTS.

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Summit, NJ, United States of America

Robert M Bowman