Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-11-01
1990-07-24
Shen, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514293, 544295, 544361, 546 82, A61K 31495, A61K 31505, A61K 31445, C07D40114, C07D47104
Patent
active
049435736
ABSTRACT:
A novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyloxyalkanoic acid amides having enhanced water solubility is disclosed of the formula ##STR1## wherein n is 3 to 5; R.sub.1 is alkyl of 1 to 4 carbon atoms; R.sub.2 is hydrogen; R.sub.3 is 1-piperidinylethyl, 1-benzylpiperidin-4-yl, 4-(1-piperidinyl)piperidine, (1-alkyl-2-pyrrolidinyl)alkyl where alkyl is 1 to 4 carbon atoms, 3-quinuclidinyl; R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form 4-R.sub.4 -piperazin-1-yl wherein R.sub.4 is alkyl of 1 to 7 carbon atoms, alkoxyethyl of 3 to 7 carbon atoms, pyridinyl, pyrimidinyl, tetrahydropyranylmethyl, thienylmethyl, cycloalkyl-(CH.sub.2).sub.m where m is zero or one and cycloalkyl is 5 to 7 carbon atoms except m is zero when cycloalkyl is 7 carbon atoms, benzyl, 4-fluorobenzyl, 3-trifluoromethylbenzyl, 4-alkoxybenzyl where alkoxy is 1 to 4 carbon atoms.
The compounds are cyclic AMP phosphodiesterase inhibitors and are particularly useful as inhibitors of blood platelet aggregation and/or as cardiotonic agents.
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Bristol--Myers Squibb Company
Shen Cecilia
Uloth Robert H.
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