Leslie C Browne

44709862, Sep 11, 1984

Dec 21, 1982

6/451903

Leslie J. Browne - Morris Plains NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3144
C07D47104

424256

Disclosed are e. g. 5-(tetrazolylalkyl, hydroxycarbamoylalkyl)imidazo[1,5-a]-pyridines, and methods of synthesis. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombosis and ischaemic heart disease.

54730783, Dec 5, 1995

Jul 14, 1994

8/275688

Robert M. Bowman - Summit NJ
Leslie J. Browne - Morristown NJ

Ciba-Geigy Corporation - Tarrytown NY

C07D24908

5482622

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.

53527950, Oct 4, 1994

May 11, 1992

7/882188

Robert M. Bowman - Summit NJ
Leslie J. Browne - Morristown NJ

Ciba-Geigy Corporation - Ardsley NY

C07D24908

5482622

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.

45887322, May 13, 1986

Dec 21, 1982

6/451902

Leslie J. Browne - Morris Plains NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3144
C07D47104

514300

Disclosed are compounds of the formula I ##STR1## or a 5,6,7,8-tetrahydro derivative thereof, wherein R. sub. 1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, or aryl-lower alkoxy in which aryl represents phenyl or phenyl substituted by lower alkoxy, lower alkyl, halogen or trifluoromethyl; R. sub. 2 represents hydrogen, halogen, or lower alkyl; C represents carboxy, lower alkoxycarbonyl, unsubstituted or mono- or di-(lower alkyl) substituted carbamoyl, cyano, formyl, hydroxymethyl, 5-tetrazolyl, dihydro-2-oxazolyl, dihydro-2-oxazolyl substituted by lower alkyl, or hydroxycarbamoyl; and (a) A represents ethenylene or ethenylene substituted by lower alkyl; B is straight chain or branched alkylene of 1 to 12 carbon atoms, alkynylene or alkenylene of 2 to 12 carbon atoms, phenylene-lower alkylene, phenylene-lower alkenylene, phenylene, or phenylene-(thio or oxy)-lower alkylene; or (b) A represents a direct bond; B represents lower alkylenephenylene, phenylene lower alkylene, phenylene, lower alkylene-(thio or oxy)-lower alkylene, lower alkylene-(thio or oxy)-phenylene, phenylene-(thio or oxy)-lower alkylene, phenylene-lower alkenylene, lower alkylenephenylene-lower alkenylene, or straight chain or branched alkadienylene of 5 to 12 carbon atoms; or a pharmaceutically acceptable salt thereof; and methods of synthesis thereof. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombosis and ischaemic heart disease.

51128454, May 12, 1992

Dec 17, 1990

7/628732

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

Ciba-Geigy Corporation - Ardsley NY

A61A 31415

514399

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.

47286458, Mar 1, 1988

Feb 4, 1986

6/825830

Leslie J. Browne - Morris Plains NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 31415
C07D48704
C07D23502

514214

Disclosed are compounds of formula I ##STR1## wherein R. sub. 1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C. sub. 2 -C. sub. 20 -acyl, cyano, free or functionally modified carboxy; and R. sub. 2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R. sub. 1 and R. sub. 2 are as defined above under formula I and salts thereof; e. g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e. g.

46173072, Oct 14, 1986

Jun 20, 1984

6/622421

Leslie J. Browne - Morris Plains NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 3144
C07D47104

514300

Compounds of the formula ##STR1## wherein R. sub. 1 represents cyano, nitro or C. sub. 1 -C. sub. 4 -alkyl or the 7,8-dihydro derivative thereof or the 5,6,7,8 tetrahydro derivative of the formula ##STR2## wherein R. sub. 1 is as defined under formula Ia and R. sub. 2 is hydrogen, C. sub. 1 -C. sub. 4 -alkyl, halogen etherified or esterified hydroxy or mercapto, carboxy-C. sub. 1 -C. sub. 4 -alkyl or C. sub. 1 -C. sub. 4 -alkoxycarbonyl-C. sub. 1 -C. sub. 4 -alkyl or C. sub. 1 -C. sub. 4 -alkanoyl, to stereoisomers, mixtures of these stereoisomers and salts of these compounds are disclosed as well as their preparation, pharmaceutical compositions containing the same and the use thereof as inhibitors of aromatase activity.

48898619, Dec 26, 1989

Nov 13, 1987

7/120283

Leslie J. Browne - Morris Plains NJ

Ciba-Geigy Corp. - Ardsley NY

A61K 31395
A61K 31495
C07D47104
C07D41700

514300

Disclosed are compounds of formula I ##STR1## wherein R. sub. 1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidized etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C. sub. 2 --C. sub. 20 -acyl, cyano, free or functionally modified carboxy; and R. sub. 2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidized etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3 or 4, and R. sub. 1 and R. sub. 2 are as defined above under formula I and salts thereof; e. g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e. g.