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US 6,143,886 AGranted
Azepinone compounds useful in the inhibition of ACE and NEP
AssigneeBristol-Myers Squibb Company
InventorJeffrey A. Robl
Life of this patent
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Abstract
Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.
Claims4
An azepinone ester having the following formulae, or a salt thereof:
- ##STR62## where R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, substituted alkyl, cycloalkyl-(CH.sub.2).sub.p -, aryl-(CH.sub.2).sub.p -, substituted aryl-(CH.sub.2).sub.p -, heteroaryl-(CH.sub.2).sub.p -, or R.sup.1 and R.sup.2 may form, together with the carbon to which they are bonded, a 3 to 7 membered carbocyclic ring, where said ring is optionally substituted by alkyl, or by aryl which is fused or bonded by a single bond to said ring;
- R.sup.3 and R.sup.4 are each independently hydrogen, alkyl, aryl, halo, or --C(O)--OR;
- R is hydrogen, alkyl, substituted alkyl, aryl-(CH.sub.2).sub.p -, subsituted aryl-(CH.sub.2).sub.p -, heteroaryl-(CH.sub.2).sub.p -, --CH(R.sup.8)--O--C(O)--R.sup.9, or ##STR63## R.sup.8 is hydrogen, alkyl, substituted alkyl, cycloalkyl-(CH.sub.2).sub.p -, aryl-(CH.sub.2).sub.p -, substituted aryl-(CH.sub.2).sub.p -, or heteraryl-(CH.sub.2).sub.p -;
- R.sup.9 is hydrogen, alkyl, alkoxy, or aryl;
- R.sup.10 is alkyl or aryl-(CH.sub.2).sub.p -;
- PG-N- denotes a protected nitrogen atom;
- R* denotes a group R other than hydrogen, or an acid protecting group other than R;
- and
- p is zero or an integer from 1 to 6.
6 more elements
An amino azepinone ester having the following formulae, or a salt thereof:
- ##STR65## where R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, substituted alkyl, cycloalkyl-(CH.sub.2).sub.p -, aryl-(CH.sub.2).sub.p -, substituted aryl-(CH.sub.2).sub.p -, heteroaryl-(CH.sub.2).sub.p -, or R.sup.1 and R.sup.2 may form, together with the carbon to which they are bonded, a 3 to 7 membered carbocyclic ring, where said ring is optionally substituted by alkyl, or by aryl which is fused or bonded by a single bond to said ring;
- R.sup.3 and R.sup.4 are each independently hydrogen, alkyl, aryl, halo, or --C(O)--OR;
- R is hydrogen, alkyl, substituted alkyl, aryl-(CH.sub.2).sub.p -, subsituted aryl-(CH.sub.2).sub.p -, heteroaryl-(CH.sub.2).sub.p -, --CH(R.sup.8)--O--C(O)--R.sup.9, or ##STR66## R.sup.8 is hydrogen, alkyl, substituted alkyl, cycloalkyl-(CH.sub.2).sub.p -, aryl-(CH.sub.2).sub.p -, substituted aryl-(CH.sub.2).sub.p -, or heteraryl-(CH.sub.2).sub.p -;
- R.sup.9 is hydrogen, alkyl, alkoxy, or aryl;
- R.sup.10 is alkyl or aryl-(CH.sub.2).sub.p -;
- R* denotes a group R other than hydrogen, or an acid protecting group other than R;
- and
- p is zero or an integer from 1 to 6.
5 more elements
Dependencies are inferred from the claim text.