Tetracycline derivatives

Details Tetracycline derivatives Tetracycline derivatives

1998-02-23

2000-12-26

Barts, Samuel

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

3,10-dihydroxy-2-naphthacene carboxamide or derivative doai

552203, 552205, C04B 3550

Patent

active

061659991

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

The present invention relates to novel tetracycline derivatives to intermediates used in their preparation, to pharmaceutical compositions containing them and to their medicinal use.
European Patent Publication 618,120, published Oct. 5, 1994, refers to 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines, methods for their production and methods of using the active agents for the prevention, treatment or control of bacterial infections in warm-bloooded animals.
European Patent Publication 536,515, published Apr. 14, 1993, refers to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracyclines, methods for their production and methods of using the active agents for the prevention, treatment or control of bacterial infections in warm-blooded animals.


SUMMARY OF THE INVENTION

The present invention relates to compounds of the formula ##STR1## wherein X is hydrogen; R.sup.1 is methyl; ##STR2## wherein n is an integar from zero to four; R.sup.4 is hydrogen or (C.sub.1 -C.sub.6)alkyl; one or more substitutents, preferably one to three substituents, independently selected from methylthio, (C.sub.1 -C.sub.6)alkoxy, amino, guanidino, amido, carboxamido, ##STR3##
(C.sub.6 -C.sub.10)aryl--(CH.sub.2).sub.h --, wherein h is an integer from zero to three, wherein the (C.sub.6 -C.sub.10)aryl moiety of said (C.sub.6 -C.sub.10)aryl--(CH.sub.2).sub.h group may optionally be substituted with one or more substituents, preferably one to three substituents, independently selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylsulfonyl, trihalo(C.sub.1l -C.sub.6)alkyl, amino, cyano, (C.sub.1 -C.sub.6)alkylamino, di(C.sub.1 -C.sub.6)alkylamino, amido, carboxamido, ##STR4## or (C.sub.3 -C.sub.6)cyloalkyl--(CH.sub.2).sub.j --, wherein j is an integer from zero to three, wherein the (C.sub.3 -C.sub.6)cycloalkyl moeity of said (C.sub.3 -C.sub.6)cycloalkyl--(CH.sub.2).sub.j -- group may optionally be substituted with one or more substituents, preferably one to three subsituents, independentl selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylsulfonyl, trihalo(C.sub.1 -C.sub.6)alkyl, amino, cyano, (C.sub.1 -C.sub.6)alkylamino, di(C.sub.1 -C.sub.6)alkylamino, amido, carboxamido, ##STR5## R.sup.6 is halogen; amino; hydroxylamino; (C.sub.1 -C.sub.12)alkylamino optionally substitued with one or more substituents, preferably one to three substituents, independently selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkysulfony, trihalo(C.sub.1 -C.sub.6)alkyl, amino, cyano, (C.sub.1 -C.sub.6)alkylamino, di(C.sub.1 -C.sub.6)alkylamino, amido, carboxamido, ##STR6## (C.sub.3 -C.sub.18)cycloaklylamino wheein the (C.sub.3 -C.sub.18)cycloalkyl moiety of said (C.sub.3 -C.sub.18)cycloalkyl amino group may optionally be substituted with one or more substituents, preferably one to three substituents, independently selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylsulfonyl, trihalo(C.sub.1 -C.sub.6)alkyl, amino, cyano, (C.sub.1 -C.sub.6)alkylamino, di(C.sub.1 -C.sub.6)alkylamino, amido, carboxamido, (C.sub.1 -C.sub.6)alkyl, ##STR7## amino moiety of said (C.sub.3 -C.sub.18)cycloaklylamino group may optionally be substituted with (C.sub.1 -C.sub.6)alkyl; more substituents, preferably one to three substitutents, independently selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkysulfonyl, trihalo(C.sub.1 -C.sub.6)alkyl, amino, cyano, (C.sub.1 -C.sub.6)alkylamino, di(C.sub.1 -C.sub.6)alkylamino, amido, carboxamido, (C.sub. -C.sub.6)alkyl, ##STR8## (C.sub.6 -C.sub.10)aryl--(CH.sub.2).sub.m --amino, wherein m is an integer from zero to three, wherein the (C.sub.6 -C.sub.10)aryl moiety of said (C.sub.6 -C.sub.10)aryl--(CH.sub.2).sub.m --amino group may optionally be substituted with one or more substituents, preferably one to three substituents, independently selected from halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy

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