Ronald W Steele

US Patent:

47497130, Jun 7, 1988

Filed:

Mar 7, 1986

Appl. No.:

6/837489

Inventors:

Robert M. Bowman - Summit NJ
Ronald E. Steele - Long Valley NJ
Leslie J. Browne - Aesch, CH

Assignee:

Ciba-Geigy Corporation - Ardsley NY

International Classification:

A61K 31415

US Classification:

514341

Abstract:

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.

US Patent:

49786725, Dec 18, 1990

Filed:

Sep 6, 1988

Appl. No.:

7/240862

Inventors:

Robert M. Bowman - Summit NJ
Ronald E. Steele - Long Valley NJ
Leslie Browne - Aesch, CH

Assignee:

Ciba-Geigy Corporation - Ardsley NY

International Classification:

A61K 3141
C07D24908

US Classification:

514383

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.

US Patent:

49372505, Jun 26, 1990

Filed:

Mar 7, 1988

Appl. No.:

7/164696

Inventors:

Robert M. Bowman - Summit NJ
Ronald E. Steele - Long Valley NJ
Leslie J. Browne - Aesch, CH

Assignee:

Ciba-Geigy Corporation - Ardsley NY

International Classification:

A61K 31415
C07D40106

US Classification:

514341

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.

US Patent:

51128454, May 12, 1992

Filed:

Dec 17, 1990

Appl. No.:

7/628732

Inventors:

Robert M. Bowman - Summit NJ
Ronald E. Steele - Long Valley NJ
Leslie J. Browne - Morristown NJ
Bruce H. Ewald - Long Valley NJ
Robert Diener - Chester NJ

Assignee:

Ciba-Geigy Corporation - Ardsley NY

International Classification:

A61A 31415

US Classification:

514399

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.

US Patent:

50718614, Dec 10, 1991

Filed:

Apr 18, 1990

Appl. No.:

7/510501

Inventors:

Robert M. Bowman - Summit NJ
Ronald E. Steele - Long Valley NJ
Leslie J. Browne - Aesch, CH

Assignee:

Ciba-Geigy Corporation - Ardsley NY

International Classification:

A61K 3144
C07D40106

US Classification:

514332

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.