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US 6,143,739 AGranted
Basic proline-amide derivatives of GE 2270 and GE 2270-like antibiotics
AssigneeBiosearch Italia S.p.A.
InventorsSergio Lociuro, Pierfausto Seneci, Ermenegildo Restelli, Romeo Ciabatti
Life of this patent
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Abstract
The present invention refers to basic amides derivatives of GE 2270 and GE 2270-like antibiotics of general formula (1), wherein the group GE represents the antibiotic core molecule. The amide derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria. ##STR1##
Claims43
Basic amide compounds of GE 2270 and GE 2270-like antibodies of formula I ##STR40## wherein:
- R.sup.1 represents hydrogen, (C.sub.1 -C.sub.4)alkyl or di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkylene, alk represents (C.sub.1 -C.sub.4)alkylene or (C.sub.2 -C.sub.5)alkylene-carbonyl,
- R.sup.2 represents a NR.sup.3 R.sup.4 group wherein
- R.sup.3 represents (C.sub.1 -C.sub.4)alkyl, hydroxy(C.sub.1 -C.sub.4)alkylene, or di(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkylene, and
- R.sup.4 represents (C.sub.1 -C.sub.4)alkyl, di(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkylene or hydroxy(C.sub.1 -C.sub.4)alkylene,
- or a five or six membered heterocycle ring having one or two nitrogen atoms, or one nitrogen atom and one oxygen atom, with the remaining atoms of the heterocycle ring being carbon atoms or oxygen atoms, wherein any nitrogen atom or any carbon atom may be optionally substituted with a group selected from (C.sub.1 -C.sub.4)alkyl, hydroxy(C.sub.1 -C.sub.4)alkylene, di(C.sub.1 -C.sub.4)alkylamino and di(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkylene;
- or R.sup.1 and alk-R.sup.2 together with the adjacent nitrogen atom form a five or six membered heterocycle ring having one or two nitrogen atoms or having one nitrogen atom and one oxygen atom, with the remaining atoms of the heterocycle ring being carbon atoms, wherein any nitrogen atom or any carbon atom may be optionally substituted with a group selected from (C.sub.1 -C.sub.4)alkyl, di(C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkylene, hydroxy(C.sub.1 -C.sub.4)alkylene and a alk.sub.2 -R.sup.5 group wherein
- alk.sub.2 is (C.sub.1 -C.sub.4)alkylene and
- R.sup.5 is a NR.sup.6 R.sup.7 group wherein
- R.sup.6 represents (C.sub.1 -C.sub.4)alkyl or di(C.sub.1 -C.sub.4)alkyl-amino(C.sub.1 -C.sub.4)alkylene and
- R.sup.7 represents (C.sub.1 -C.sub.4)alkyl or di(C.sub.1 -C.sub.4)alkyl-amino(C.sub.1 -C.sub.4)alkylene
- or a five or six membered heterocycle ring having one or two nitrogen atoms, or one nitrogen atom and one oxygen atom, with the remaining atoms of the heterocycle ring being carbon atoms, wherein any nitrogen atom or any carbon atom may be optionally substituted with a group selected from (C.sub.1 -C.sub.4)alkyl, hydroxy(C.sub.1 -C.sub.4)alkylene, di(C.sub.1 -C.sub.4)alkylamino and di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkylene
- and the group of formula ##STR41## represents the antibiotic core portion of the formula ##STR42## wherein:
- W.sup.1 represents phenyl
- W.sup.2 represents hydroxy
- or both W.sup.1 and W.sup.2 represent methyl,
- X.sup.1 represents hydrogen or methyl,
- X.sup.2 represents hydrogen, methyl or methoxymethylene,
- with the proviso that when both W.sup.1 and W.sup.2 are methyl, then X.sup.1 is methyl and X.sup.2 is hydrogen,
- or a pharmaceutical acceptable salt thereof.
16 more elements
Dependencies are inferred from the claim text.