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US 5,684,014 AGranted
Cycloalkano-indole and -azaindole derivatives
AssigneeBayer Aktiengesellschaft
InventorsUlrich Muller, Richard Connell, Siegfried Goldmann, Rudi Grutzmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
Life of this patent
Estimating the term…
Abstract
Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.
Claims11
A cycloalkyl-indole or -azaindole derivative of the formula ##STR347## in which R.sup.1 and R.sup.2 form a pyridyl ring which is optionally substituted 1 to 3 times by identical or different substituents;
- R.sup.3 and R.sup.4, including the double bond connecting them, form a phenyl ring or a 6-membered cycloalkene ring each of which are optionally substituted 1 to 3 times by identical or different substituents,
- wherein said substituents on the pyridyl, phenyl or cycloalkene ring are selected from the group consisting of halogen, trifluoromethyl, carboxyl hydroxyl, straight-chain or branched C.sub.1 -C.sub.6 alkoxy, straight-chain or branched C.sub.1 -C.sub.6 alkoxycarbonyl, or an optionally substituted straight-chain or branched C.sub.1 -C.sub.6 alkyl wherein the substituents on the alkyl group are hydroxyl or straight-chain or branched alkoxy having up to 4 carbon atoms,
- D represents hydrogen, cycloalkyl having 4 to 12 carbon atoms or straight-chain or branched alkyl having up to 12 carbon atoms,
- E represents the --CO-- or --CS group,
- L represents a group of the formula --NR.sup.9
- wherein
- R.sup.9 denotes hydrogen or straight-chain or branched alkyl having up to 6 carbon atoms, which is optionally substituted by hydroxyl or phenyl,
- R.sup.5 represents phenyl which is optionally substituted 1 to 3 times by identical or different substituents selected from the group consisting of nitro, carboxyl, halogen, cyano, straight-chain or branched C.sub.2 -C.sub.6 alkenyl, straight-chain or branched C.sub.1 -C.sub.6 alkoxycarbonyl or optionally substituted C.sub.1 -C.sub.6 straight-chain or branched alkyl wherein the substituents on the alkyl are hydroxyl, carboxyl, straight-chain or branched C.sub.1 -C.sub.6 alkoxy, straight-chain or branched C.sub.1 -C.sub.6 alkoxycarbonyl
- or said phenyl ring is further optionally substituted by a group of the formula --OR.sup. or --NR.sup.11 R.sup.12,
- wherein
- R.sup.10 denotes hydrogen or straight-chain or branched alkyl or alkenyl each having up to 6 carbon atoms,
- R.sup.11 and R.sup.14 are identical or different and denote phenyl, hydrogen or straight-chain or branched alkyl having up to 6 carbon atoms or straight-chain or branched acyl having up to 8 carbon atoms, which is optionally substituted by a group of the formula --NR.sup.-- R.sup.14,
- wherein
- R.sup.13 and R.sup.14 are identical or different and denote hydrogen or straight-chain or branched acyl having up to 8 carbon atoms,
- R.sup.6 represents hydrogen, carboxyl or straight-chain or branched alkoxycarbonyl having up to 5 carbon atoms,
- or represents straight-chain or branched alkyl having up to 6 carbon atoms, which is optionally substituted by hydroxyl or by a group of the formula --O--CO--R.sup.15,
- wherein
- R.sup.15 denotes phenyl which is optionally substituted up to 3 times by identical or different halogen or hydroxyl substituents or by straight-chain or branched alkyl having up to 5 carbon atoms, or straight-chain or branched alkyl or alkenyl each having up to 22 carbon atoms, each of which is optionally substituted by a group of the formula --OR.sup.16,
- wherein
- R.sup.16 is hydrogen, benzyl, triphenylmethyl or straight-chain or branched acyl having up to 6 carbon atoms,
- R.sup.7 represents hydrogen or
- R.sup.6 and R.sup.7 together represent the group of the formula .dbd.O, or its isomeric form or a salt thereof.
19 more elements
Dependencies are inferred from the claim text.