Hoffmann-la Roche Inc.

Giuseppe Federico Weber

Noal Cohen

Donna Mary Huryn

Urvashi Hooda Dhingra

Dennis D Keith

Nader Fotouhi

Allen John Lovey

Emily Aijun Liu

John Guilfoyle Mullin, Jr

Bruce Lester Banner

June Ke

Disclosed are novel substituted pyrroles having the formula

Substituted pyrroles

Certain substituted pyrroles are antiproliferative agents useful in the treatment of cancer.

Compounds of the formula ##STR1## wherein R is alkyl, alkylthio or hydroxy, as well as, pharmaceutically acceptable salts of compounds of formula I are antiproliferative agents useful in the treatment of cancer.

Compounds of the formula ##STR1## wherein R is hydrogen, alkyl.sub.1-8, geminal alkyl.sub.1-3, unsubstituted or substituted aryl; X is alkylene, --CR.sub.1 .dbd.CR.sub.2 -- (E and/or Z), carbonyl, oxygen or sulfur, wherein one of R.sub.1 and R.sub.2 is alkyl.sub.1-3 and the other is hydrogen; Y is unsubstituted alkyl.sub.1-12 or substituted by one or more alkyl.sub.1-3 groups, or unsubstituted or substituted phenylalkyl .sub.1-3 ; or a salt thereof with a pharmaceutically acceptable base, are described. The compound of formula I are potent inhibitors of phospholipase A.sub.2 (PLA.sub.2) and are therefore useful in the treatment of inflammatory diseases, such as, psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary, myocardial ischemia and trauma induced inflammation, such as, spinal cord injury.

Substituted tetrahydrobenzopyrrolylfuranoic acid derivatives as

The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl; enatiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.

3,4-dihydro-2H-1-benzopyran derivatives

The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl; enantiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.

Methyl derivatives of arachidonic acid and intermediates thereto have been synthesized. These derivatives are inhibitors of SRS-A synthesis and are useful for treating and preventing allergic reactions.

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Cedar Grove, NJ, United States of America

Giuseppe Federico Weber