JONATHAN MARTIN, MD
Osteopathic Medicine at Blount Ave, Knoxville, TN

5183818, Feb 2, 1993

Aug 27, 1991

7/750362

Dee W. Brooks - Libertyville IL
Andrew O. Stewart - Wildwood IL
Jonathan G. Martin - Knoxville TN

Abbott Laboratories - Abbott Park IL

A61K 3138, C07D33332

5142315

The present invention provides compounds having the structure Y-Het-[Q. sub. 1 ]-X-[Q. sub. 2 ]-Z which inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B. sub. 4, C. sub. 4, D. sub. 4, and E. sub. 4. In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl. Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR. The group Q. sub. 1 is absent or is divalent alkylene of from one to six carbon atoms, and Q. sub.

5476873, Dec 19, 1995

Apr 19, 1994

8/229860

Dee W. Brooks - Libertyville IL
Andrew O. Stewart - Wildwood IL
Daniel J. Kerkman - Lake Villa IL
Pramila A. Bhatia - Mundelein IL
Anwer Basha - Lake Forest IL
Jonathan G. Martin - Knoxville TN

Abbott Laboratories - Abbott Park IL

C07C25906, C07C27318, C07C27564, A61K 3117

514595

Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR. sup. 1 R. sup. 2, where R. sup. 1 and R. sup. 2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

5559144, Sep 24, 1996

May 5, 1995

8/435399

Dee W. Brooks - Libertyville IL
Andrew O. Stewart - Wildwood IL
Daniel J. Kerkman - Lake Villa IL
Pramila A. Bhatia - Mundelein IL
Anwer Basha - Lake Forest IL
Jonathan G. Martin - Knoxville TN

Abbott Laboratories - Abbott Park IL

A61K 3134, A61K 3138, C07D30746, C07D33322

514445

Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR. sup. 1 R. sup. 2, where R. sup. 1 and R. sup. 2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.