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US 4,115,577 AGranted
Pyridopyrrolobenzheterocycles
AssigneeEndo Laboratories, Inc.
InventorParthasarathi Rajagopalan
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Abstract
The compounds are prepared by cyclizing compounds of formula II ##STR2## wherein R.sup.2 is R.sup.1 or acyl. The latter compounds are prepared by reacting 4-piperidones with compoounds of formula III in the presence of a reducing agent ##STR3## or with compounds of formula VI ##STR4##
Claims9
Compound of the formula:
- ##STR22## where X is S, S or SO.sub.2 ;
- m and n are either 0 or 1 and the sum of m and n is at least 1;
- the R's are the same or different and are H or CH.sub.3, and one of them can be C.sub.2 -C.sub.9 alkyl, phenyl, C.sub.7 -C.sub.10 phenylalkyl, furyl, thienyl, pyridyl, phenyl or C.sub.7 -C.sub.10 phenylalkyl substituted on adjacent ring carbon atoms with methylenedioxy, or phenyl or C.sub.7 -C.sub.10 phenylalkyl substituted on the ring with 1, 2 or 3 substituents individually selected from methoxy, ethoxy, bromine, chlorine, fluorine, trifluoromethyl and C.sub.1 -C.sub.4 alkyl;
- when X is S and m is 0 , one R on the group --RCR-- can be --OCH.sub.3 ;
- and when X is S and m is 1, the R on the group (CHR).sub.m can be --OCH.sub.3 ;
- R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.4 alkoxycarbonyl, trifluoroacetyl or substituted C.sub.1 -C.sub.4 alkyl where the substituent is C.sub.3 -C.sub.6 cycloalkyl, phenyl, phenyl substituted on adjacent carbon atoms with methylenedioxy, or phenyl substituted with 1, 2 or 3 substituents individually selected from methoxy, ethoxy, bromine, chlorine, fluorine, trifluoromethyl and C.sub.1 -C.sub.4 alkyl;
- and
- Z is H, Cl or CH.sub.3 ;
- and their pharmaceutically suitable salts.
6 more elements
Dependencies are inferred from the claim text.