Zeneca Limited

Janet Marie Forst

Cyrus J Ohnmacht

Thomas Michael Bare

Diane A Trainor

James Roy Empfield

Richard Bruce Sparks

Mark M Stein

Keith John Herzog

Robert J Harris

Alpha-substituted pyridazino quinoline compounds

The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2' or R2'' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2' is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2'' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.8 is a variety of substituents including hydrogen and (1-12C) alkyl.

Methods of treating asthma are provided which methods comprise administering to a mammal in need of such treatment an effective amount of a compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 have any of the meanings given in the specification.

Heterocyclic derivatives

Compounds of formula I ##STR1## wherein R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

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Wilmington, DE, United States of America

Janet Marie Forst