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Home Vasodialators Pyridopyrrolobenzheterocycles

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 Pyridopyrrolobenzheterocycles

Details
Inventors: Rajagopalan, Parthasarathi;
Assignee: Endo Laboratories, Inc. (Garden City, NY)
Primary Examiner: Brust; Joseph Paul
Assistant Examiner:
Attorney, Agent or Firm:

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 compounds of formula III in the presence of a reducing agent ##STR3## or with compounds of formula VI ##STR4##

DETAILED DESCRIPTION I claim: 1.
Compound of the formula: ##STR23## wherein m and n are 0 or 1 and the sum of m+n is at least 1; the R groups 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; 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 methylene-dioxy, or phenyl substituted with 1, 2 or 3 substituents individually selected from methoxy, ethoxy, bromine, chlorine, fluorine, and trifluoromethyl; and Z is H, Cl or CH.
sub.
3 ; and their pharmaceutically suitable salts.
2.
The compound of claim 1 1,2,8,9,10,11-hexahydro-9-methyl-4H-pyrido[3',4':4,5]pyrrolo[3,2,1-jk][4,1 ]benzoxazepine and its pharmaceutically suitable salts.
3.
The compound of claim 1 (.
+-.
)-1,2,8,9,10,11-hexahydro-4-phenyl-4H-pyrido[3',4':4,5]pyrrolo[3,2,1- jk][4,1]benzoxazepine and its pharmaceutically suitable salts.
4.
A pharmaceutical preparation suitable for use in warm-blooded animals consisting essentially of an effective sedative amount of a compound of claim 1 and a pharmaceutically suitable vehicle.
5.
A method for inducing sedation in a warm-blooded animal which comprises administering to the animal an effective sedative amount of a compound of claim 1.




Description:
BACKGROUND OF THE INVENTION This invention relates to novel pyrido[3',4':4,5]pyrrolo[1,2,3-ef][1,5]benzothiazepines and -benzoxazepines, novel pyrido[3',4':4,5]pyrrolo[1,2,3-de][1,4]benzothiazines and -benzoxazines, novel pyrido[3',4':4,5]pyrrolo[3,2,1-jk][4,1]benzothiazepines and -benzoxazepines, novel pyrido[3',4':4,5]pyrrolo[3,2,1-kl][5,1]benzothiazocines and -benzoxazocines, and novel intermediates therefor



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