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US 4,233,301 AGranted
Novel imidazoazines and imidazodiazines
AssigneeMerck & Co., Inc.
InventorsJohn J. Baldwin, William C. Lumma, Jr.
Life of this patent
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Abstract
Novel imidazopyridines, -pyrazines, -pyrimidines and -pyridazines having a 3-amino-2-OR-propoxy substituent, are disclosed. The compounds have .beta.-adrenergic blocking activity.
Claims19
Compounds having the formula ##STR19## and pharmaceutically acceptable salts thereof wherein Z is --CH.sub.2 --CHOR.sub.3 --CH.sub.2 --NHR.sub.4 wherein R is H or C.sub.2 -C.sub.12 acyl selected from alkanoyl, benzoyl, naphthoyl, methylbenzoyl and phenylbenzoyl and R.sub.4 is C.sub.1 -C.sub.12 alkyl,
- R is H, --SCF.sub.3, --CN, halogen, C.sub.1-6 alkyl, NH.sub.2, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.12 acyl, of the formula ##STR20## wherein L is H, alkyl or aryl, phenyl, --COOR.sub.5 wherein R.sub.5 is H C.sub.1 -C.sub.6 alkyl or C.sub.6 -C.sub.12 carbocyclic aryl, --CONR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 when separate, are H or C.sub.1 -C.sub.6 alkyl and when joined, are --CH.sub.2 --(CH.sub.2).sub.3 --CH.sub.2, --CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --NH--CH.sub.2 --CH.sub.2 --, or --CH.sub.2 --CH.sub.2 --N(CH.sub.3)--CH.sub.2 --CH.sub.2 --, --C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl or C.sub.1 -C.sub.6 alkylsulfony, and
- R.sub.1 and R.sub.2 when separate are R and when joined are --(CH.sub.2).sub.n -- wherein n is 3, 4 or 5.
Dependencies are inferred from the claim text.