Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
AssigneeAventis Pharmaceuticals Products Inc.
InventorsScott I. Klein, Kevin R. Guertin, Alfred P. Spada
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Abstract
The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
Claims43
A compound of the formula ##STR315## R.sub.1 and R.sub.2 are hydrogen or taken together are .dbd.NR.sub.9 ;
- R.sub.3 is hydrogen, --CO.sub.2 R.sub.6, --C(O)R.sub.6, --CONR.sub.6 R.sub.6, --CH.sub.2 OR.sub.7 or --CH.sub.2 SR.sub.7 ;
- R.sub.4 is hydrogen, alkyl, Q-alkyl, thiocycloalkyl, or cycloalkylalkyl, or a group of formula ##STR316## R.sub.5 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, or optionally substituted aralknyl;
- R.sub.6 is hydrogen or lower alkyl;
- R.sub.7 is hydrogen, lower alkyl, Ar(lower alkyl), lower acyl, aroyl or heteroaroyl;
- R.sub.8 is hydrogen or lower alkyl;
- R.sub.9 is hydrogen, R.sub.10 O.sub.2 C--, R.sub.10 O--, HO--, cyano, R.sub.10 CO--, HCO--, lower alkyl, nitro, or Y.sup.1a Y.sup.2a N--;
- R.sub.10 is optionally substituted alkyl, optionally substituted aralkyl, or optionally substituted heteroaralkyl;
- Y.sup.1a and Y.sup.2a are independently hydrogen or alkyl;
- A and B are hydrogen or taken together are a bond;
- Q is R.sub.7 O-- or R.sub.7 S-- or Y.sup.1 Y.sup.2 N--;
- Ar is optionally substituted aryl or optionally substituted heteroaryl;
- and
- n is 0, 1 or 2;
- or
- a pharmaceutically acceptable salt thereof, an N-oxide thereof, a hydrate thereof, a solvate thereof, or prodrug thereof.
Dependencies are inferred from the claim text.