Pfizer Corporation

Lawrence S Melvin, Jr

Michael Ross Johnson

James F Eggler

Charles A Harbert

Thomas H Althuis

Anthony Marfat

Hiroko Masamune

Kevin Koch

Lawrence Alan Reiter

Frederick J Walker

Sally Gut Ruggeri

Substituted tetralins, chromans and related compounds in the treatment

Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.

Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;

Tetralin and chroman derivatives useful in the treatment of asthma,

Benzopyran and related LTB.sub.4 antagonists

Substituted sulfonamides and related compounds in the treatment of

Substituted chromans and their use in the treatment of asthma, arthritis

Substituted 1-[3-(heteroarylmethoxy)phenyl]alkanols and related

2-Amino and 2-thio-4-substituted-5-(hydroxy or alkoxy)-pyrimidines, which may be 6-substituted, and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are, therefore, useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases. The compounds are also cytoprotective and therefore, useful in the treatment of peptic ulcers.

Derivatives of hydroxyprimidines as leukotriene synthesis inhibitors

Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; and

Pharmacologically active

Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or an ester moiety; Y is --CH(R.sub.2 ')CH(R.sub.2)-- or --CH(R.sub.3)CH.sub.2 --;

Pharmacologically active 2-hydroxy-4-(substituted) phenyl cycloalkanes

1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.

Substituted decahydro-1H-pyrido[1,2-f]phenanthridines and

Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;

Growing community of inventors

Ledyard, CT, United States of America

Lawrence S Melvin, Jr