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US 5,688,793 AGranted
Pyridazino4',5':3,4!pyrrolo-2,1-a!-isoquinolines and the use thereof for preparing pharmaceutical preparations
AssigneeBoehringer Ingelheim GmbH
InventorsWalter Losel, Otto Roos, Dietrich Arndts
Life of this patent
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Abstract
The invention relates to new pyridazino4',5':3,4!-pyrrolo2,1-a!isoquinolines of the formula ##STR1## and the physiologically acceptable salts thereof with acids and complex-forming agents, wherein X is O, S or NHO and R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are defined as in the specification, and pharmaceutical preparations containing these compounds.
Claims20
A compound of formula (I) ##STR91## wherein X is O, S or NHO;
- R.sub.1 has one of the following meanings:
- a) C.sub.3-7 -cycloalkyl;
- b) a straight-chained or branched alkyl group having 1 to 10 or an alkenyl or alkynyl group having 2 to 10 carbon atoms, which alkyl, alkenyl or alkynl group may be substituted by hydroxy, C.sub.1-4 -alkoxy, halogen, NH.sub.2, NH-alkyl having 1 to 2 carbon atoms, N,N-di(C.sub.1-2)alkylamino, NH-acyl having 2 to 4 carbon atoms, 1 or 2 C.sub.3-7 -cycloalkyl groups, phenoxy, 1 or 2 phenyl groups (wherein the phenyl ring or rings or phenoxy may in turn be mono- or disubstituted by halogen, CF.sub.3, C.sub.1-4 -alkyl, C.sub.1-2 -alkoxy, NH-alkyl having 1 to 2 carbon atoms, N,N-dialkyl having 1 to 2 carbon atoms, NH.sub.2, N-acyl having 2 to 3 carbon atoms, --OCH.sub.2 O--, (C.sub.1 or C.sub.2) alkylsulphonylamino, phenoxy or benzyloxy), furyl or thienyl;
- R.sub.3, R.sub.4 and R.sub.5, which may be identical or different, are hydrogen or a C.sub.1-4 -alkyl group;
- R.sub.7 and R.sub.8, which may be identical or different, are hydroxy;
- C.sub.1-4 -alkoxy;
- or C.sub.1-4 -alkylthio;
- R.sub.6 and R.sub.9, which may be identical or different, are hydrogen;
- hydroxy;
- C.sub.1-4 -alkoxy;
- C.sub.1-4 -alkylthio;
- or 2 adjacent substituents of the substituents R.sub.6, R.sub.7, R.sub.8 and R.sub.9 together form the group --O--(CH.sub.2).sub.1 or 2 --O-- and the other 2 substituents are as hereinbefore defined,
- or a pharmaceutically acceptable salt thereof,
- with the exception of compounds of formula I as hereinbefore defined wherein XR.sub.1 is the group SR.sub.1 wherein R.sub.1 is C.sub.1-5 alkyl or benzyl.
11 more elements
A compound as recited in claim 10, wherein R.sub.1 is the group ##STR93## wherein R.sub.13 and y are defined as in claim 11.
Dependencies are inferred from the claim text.