Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-29
1999-12-28
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
540455, C07K 5078, C07K 756, C07K 506, A61K 3805
Patent
active
060082259
DESCRIPTION:
BRIEF SUMMARY
The present invention refers to derivatives of GE2270 factors C.sub.2a, D.sub.2 and E of general formula I ##STR2## wherein W represents a 2-(aminocarbonyl)-pyrrolidinyl moiety of formula ##STR3## or a group of formula ##STR4## wherein R.sup.1 represents hydrogen or (C.sub.1 -C.sub.4)alkyl represent (C.sub.1 -C.sub.4)alkyl or di(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkylene, optionally a further heteroatom selected from nitrogen and oxygen, 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 or di(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkylene, five or six membered heterocycle ring optionally containing a further heteroatom selected from oxygen and nitrogen, 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)alkyl and R.sup.5 represents represent (C.sub.1 -C.sub.4)alkyl or di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkylene heteroatoms selected from nitrogen and oxygen, 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 or di(C.sub.1 -C.sub.4)alkylamino(C.sub.1 -C.sub.4)alkylene; ##STR5## wherein: X.sup.1 is methyl, X.sup.2 is a --CH.sub.2 --W.sup.1 moiety and X.sup.3 is methylamino or amino, or X.sup.3 is methylamino, NR.sup.8 R.sup.9 wherein -C.sub.4)alkylene or six membered heterocycle ring optionally containing a further heteroatom selected from oxygen and nitrogen, 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; 2-(aminocarbonyl)-pyrrolidinyl; then W.sup.1 can not be hydroxy;
The present invention refers also to the processes for preparing the compounds of formula I and to the corresponding precursors of the compounds of formula I, wherein the amidic group of said compounds, i.e. the group of formula: ##STR6## is substituted by the group --COOY, wherein Y represents hydrogen or (C.sub.1 -C.sub.4)alkyl.
Antibiotic GE2270 is prepared by culturing a sample of Planobispora rosea ATCC 53773 or a producing variant or mutant thereof and isolating the desired antibiotic substance from the mycelium and/or the fermentation broth. Planobispora rosea ATCC 53773 was isolated from a soil sample and deposited on Jun. 14, 1988 with the American Type Culture Collection (ATCC), 12301 Parklawn Drive, Rockville, Md. 20852 Maryland, U.S.A., under the provisions of the Budapest Treaty. The strain has been accorded accession number ATCC 53773.
Antibiotic GE2270 factor A is the main component of the antibiotic GE2270 complex. Antibiotic GE2270 factor A and Planobispora rosea ATCC 53773 are described in U.S. Pat. No. 5139778.
At present, a number of minor factors of antibiotic GE2270 have been isolated, namely factors B.sub.1, B.sub.2, C.sub.1, C.sub.2, D.sub.1, D.sub.2, E and T disclosed in European Patent Application Publication no. 451486 which has as its equivalent, U.S. Pat. No. 5,747,295, which is hereby incorporated by reference and factor C.sub.2a disclosed in European Patent Application Publication no. 529410 which has as its equivalent, U.S. Pat. No. 5,514,649, which is hereby incorporated by reference.
Also degradation products of GE2270 factor A are known, namely factors A.sub.1, A.sub.2, A.sub.3 and H disclosed in U.S. Pat. No. 5139778.
Among these compounds, GE2270 factor C.sub.2a, D.sub.2 and E may be employed as suitable starting materials for preparing the compounds of the present invention.
The above factors may be represented by the ollowing formula II ##STR7## wherein: X.sup.1 is hydroxymethylen, X.sup.2 is methoxymethylen and X.sup.3 is methylamino for factor C.sub.2a ; for factor D.sub.2 ; factor E.
It should be noted that this formula does no
REFERENCES:
patent: 5139778 (1992-08-01), Selva et al.
patent: 5202241 (1993-04-01), Selva et al.
patent: 5514649 (1996-05-01), Selva et al.
patent: 5599791 (1997-02-01), Tavecchia et al.
patent: 5747295 (1998-05-01), Selva et al.
patent: 5891869 (1999-04-01), Lociuro et al.
Journal of Antibiotics, vol. 47(12), pp. 1564-1567 (1994).
Journal of Antibiotics, vol. 47(10), pp. 1153-1159 (1994).
Ciabatti Romeo
Lociuro Sergio
Restelli Ermenegildo
Tavecchia Paolo
Biosearch Italia S.p.A.
Kifle Bruck
Shah Mukund J.
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