7-oxypropylsulfonamido-imidazo[4,5-b]quinolin-2-ones
AssigneeBristol-Meyers Squibb Company
InventorsPiyasena Hewawasam, Nicholas A. Meanwell
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Abstract
A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl; R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ; benzoxazol-2yl, or benzothiazol2-yl; R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl; m is an integer of 1-3; and n is an integer of 1-5; or pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
Claims17
A compound of the formula ##STR32## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;
- R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ;
- benzoxazol-2yl, or benzothiazol-2-yl;
- R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl;
- m is an integer of 1-3;
- and
- n is an integer of 1-5;
- or pharmaceutically acceptable salt thereof.
The intermediate compound which is 4-[[3-[(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolin-7-yl)oxy]propyl]sulfon yl]-1-piperazinecarboxaldehyde.
Dependencies are inferred from the claim text.