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US 5,350,750 AGranted
.beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives, process for their production and their use in pharmaceutical agents
AssigneeSchering Corporation
InventorsAndreas Huth, Martin Kruger, Dieter Seidelmann, Ralph Schmiechen, Werner Krause, Herbert Schneider, Lechoslaw Turski
Life of this patent
Estimating the term…
Abstract
.beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives of formula I ##STR1## in which R.sup.A, n, R.sup.4 and R.sup.3, have the meaning indicated in the claims, as well as their production and their use in pharmaceutical agents are described.
Claims6
Compounds of formula I ##STR6## in which R.sup.A is halogen, --CHR.sup.1 --R.sup.2 or --OR.sup.5, and
- n is 1 or 2,
- wherein
- R.sup.1 is hydrogen or C.sub.1-4 -alkyl,
- R.sup.2 is hydrogen, C.sub.1-4 -alkyl, O-C.sub.1-4 -alkyl or a phenyl, benzyl or phenoxy radical, optionally substituted 1 to 3 times by halogen, nitro, cyano, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, trifluoromethyl, -SO.sub.2 -C.sub.1-4 -alkyl, amino and C.sub.1-4 -alkoxycarbonyl group(s),
- R.sup.5 is hydrogen, C.sub.1-4 -alkyl, C.sub.3-7 -cycloalkyl or a phenyl, benzyl or hetaryl radical optionally substituted 1 to 3 times by halogen, nitro, cyano, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, trifluoromethyl, -SO.sub.2 -C.sub.1-4 -alkyl, amion and C.sub.1-4 -alkoxycarbonyl group(s), wherein the hetaryl radical is a pyridine, pyrimidine, pyrazine, pyridazine, triazine, furan, thiophene, pyrrole, thiazole, imidazole, quinoline, isoquinoline or quinoxaline radical,
- R.sup.4 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-4 -alkoxy-C.sub.1-2 -alkyl, and
- R.sup.3 is a straight-chain or branched C.sub.1-6 -alkyl, that is substituted one to four times with OR.sup.6,
- wherein
- R.sup.6 is hydrogen, C.sub.1-4 -alkyl or a hydroxy protective group, or isomers or pharmaceutically acceptable acid addition salts thereof.
6 more elements
6-Benzyloxy-4-methoxymethyl-.beta.-carboline-3-carboxylic acid-(2-hydroxy-2-methyl)-propyl ester
- 6-hydroxy-4-methoxymethyl-.beta.-carboline-3-carboxylic acid-(2-hydroxy-2-methyl)-propyl ester
- 4-methoxymethyl-6-(2-pyrazinyloxy)-.beta.-carboline-3-carboxylic acid-(2-hydroxy-2-methyl)-propyl ester
- 6-(5-bromo-2-pyridyloxy)-4-methoxymethyl-.beta.-carboline-3-carboxylic acid-(2-hydroxy-2-methyl)-propyl ester.
Dependencies are inferred from the claim text.